Constellation Pharmaceuticals, Inc.

United States of America

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IP Type
        Patent 176
        Trademark 34
Jurisdiction
        World 90
        United States 79
        Canada 32
        Europe 9
Date
2025 January 2
2024 November 3
2025 (YTD) 2
2024 16
2023 24
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IPC Class
A61P 35/00 - Antineoplastic agents 95
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole 35
C07D 471/04 - Ortho-condensed systems 33
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links 32
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings 27
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NICE Class
05 - Pharmaceutical, veterinary and sanitary products 34
42 - Scientific, technological and industrial services, research and design 6
01 - Chemical and biological materials for industrial, scientific and agricultural use 5
Status
Pending 52
Registered / In Force 158
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1.

PELLMOFY

      
Application Number 1834620
Status Registered
Filing Date 2024-09-30
Registration Date 2024-09-30
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

2.

PELLMOFI

      
Application Number 1834619
Status Registered
Filing Date 2024-09-30
Registration Date 2024-09-30
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

3.

Miscellaneous Design

      
Serial Number 98840863
Status Pending
Filing Date 2024-11-06
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceutical preparations comprising small molecules for treating cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; small molecule pharmaceuticals for the treatment of diseases and conditions, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies sold as a component ingredient of pharmaceuticals for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; diagnostic preparations for medical purposes; clinical medical reagents; biological preparations for medical purposes, namely for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceutical and veterinary preparations and agents for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways

4.

Miscellaneous Design

      
Serial Number 98840878
Status Pending
Filing Date 2024-11-06
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceutical preparations comprising small molecules for treating cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; small molecule pharmaceuticals for the treatment of diseases and conditions, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies sold as a component ingredient of pharmaceuticals for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; diagnostic preparations for medical purposes; clinical medical reagents; biological preparations for medical purposes, namely for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceutical and veterinary preparations and agents for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways

5.

Miscellaneous Design

      
Serial Number 98840849
Status Pending
Filing Date 2024-11-06
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceutical preparations comprising small molecules for treating cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; small molecule pharmaceuticals for the treatment of diseases and conditions, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies sold as a component ingredient of pharmaceuticals for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; diagnostic preparations for medical purposes; clinical medical reagents; biological preparations for medical purposes, namely for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceutical and veterinary preparations and agents for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, thrombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways

6.

PELLMOFY

      
Application Number 237570000
Status Pending
Filing Date 2024-09-30
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

7.

PELLMOFI

      
Application Number 237569900
Status Pending
Filing Date 2024-09-30
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

8.

USE OF PELABRESIB FOR TREATING ANEMIAS

      
Application Number 18290181
Status Pending
Filing Date 2022-05-10
First Publication Date 2024-08-15
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor Colak, Gözde

Abstract

The present disclosure relates to the use of pelabresib, and pharmaceutically acceptable salts thereof, for treating conditions associated with low reticulocyte counts.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 7/06 - Antianaemics

9.

MODULATORS OF TREX1

      
Application Number 18289467
Status Pending
Filing Date 2022-05-04
First Publication Date 2024-08-08
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Levell, Julian R.
  • Coffin, Aaron
  • Khanna, Avinash
  • Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1. Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine

10.

MODULATORS OF TREX1

      
Application Number 18288455
Status Pending
Filing Date 2022-04-25
First Publication Date 2024-07-25
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Levell, Julian R.
  • Coffin, Aaron
  • Zablocki, Mary-Margaret
  • Wilson, Jonathan E.
  • Khanna, Avinash
  • Guerin, David J.
  • Mcelroy, William T.
  • Rocnik, Jennifer L.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1. Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine

11.

METHODS FOR TREATING LOWER RISK MYELODYSPLASTIC SYNDROME

      
Application Number US2023084959
Publication Number 2024/137713
Status In Force
Filing Date 2023-12-19
Publication Date 2024-06-27
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Luptakova, Katarina

Abstract

The present disclosure relates to the use of pelabresib, and pharmaceutically acceptable salts and hydrates thereof, for treating lower risk myelodysplastic syndrome (LR-MDS) and conditions associated therewith.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

12.

PELLMOFI

      
Application Number 019012072
Status Registered
Filing Date 2024-04-11
Registration Date 2024-08-31
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

13.

EZH2 INHIBITION THERAPIES FOR THE TREATMENT OF BRCA1-ASSOCIATED PROTEIN (BAP1) MUTATED CANCERS

      
Application Number US2023034522
Publication Number 2024/076663
Status In Force
Filing Date 2023-10-05
Publication Date 2024-04-11
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Reddy, Archana, Bommi
  • Keller, Patricia, Joyce
  • Trojer, Patrick

Abstract

Provided herein is (R)-7-chloro-2-((lr,4R)-4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, or a pharmaceutically acceptable salt thereof for use in methods of treating certain cancers having at least one BAP1 mutation.

IPC Classes  ?

  • A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61P 35/00 - Antineoplastic agents

14.

PELLMOFY

      
Application Number 019012205
Status Registered
Filing Date 2024-04-11
Registration Date 2024-08-31
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

15.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

      
Application Number 18140730
Status Pending
Filing Date 2023-04-28
First Publication Date 2024-04-11
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Côté, Alexandre
  • Gehling, Victor S.
  • Khanna, Avinash
  • Moine, Ludivine
  • Stuckey, Jacob I.

Abstract

Provided are novel compounds of Formula (I): Provided are novel compounds of Formula (I): Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • A61P 35/00 - Antineoplastic agents
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

16.

PELLMOFI

      
Serial Number 98479628
Status Pending
Filing Date 2024-04-02
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances

17.

PELLMOFY

      
Serial Number 98479643
Status Pending
Filing Date 2024-04-02
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances

18.

EZH2 INHIBITION THERAPIES FOR THE TREATMENT OF AT-RICH INTERACTIVE DOMAIN-CONTAINING PROTEIN 1A (ARID1A) MUTATED CANCERS

      
Application Number US2023027761
Publication Number 2024/015566
Status In Force
Filing Date 2023-07-14
Publication Date 2024-01-18
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Whicher, Elizabeth, Adams
  • Yu, Ziyang
  • Sun, Kaiming
  • Keller, Patricia, Joyce
  • Trojer, Patrick

Abstract

Provided herein are methods of treating cancers having at least one ARID 1 A mutation with (R)-7-chloro-2-((1r,4R)-4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61P 35/00 - Antineoplastic agents

19.

EZH2 INHIBITION THERAPIES FOR THE TREATMENT OF ANDROGEN RECEPTOR MUTATED PROSTATE CANCERS

      
Application Number 18037120
Status Pending
Filing Date 2021-11-18
First Publication Date 2023-12-28
Owner Constellation Pharmaceuticals, Inc (USA)
Inventor
  • Bradley, William D.
  • Cui, Jike
  • Sun, Kaiming
  • Trojer, Patrick
  • Wang, Jing
  • Wu, Rentian

Abstract

Provided herein are methods of treating prostate cancer having at least one pathogenic AR mutation using 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3- yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, or a pharmaceutically acceptable salt thereof, alone or in combination with a therapeutically effective amount of an androgen receptor signaling inhibitor (ARSI) such as enzalutamide.

IPC Classes  ?

  • A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61P 35/00 - Antineoplastic agents

20.

PELMOFY

      
Application Number 1757750
Status Registered
Filing Date 2023-08-02
Registration Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, bromodomain and extra-terminal (BET) protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

21.

BETPELMY

      
Application Number 1758006
Status Registered
Filing Date 2023-08-02
Registration Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

22.

PELAMOFY

      
Application Number 1757751
Status Registered
Filing Date 2023-08-02
Registration Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, bromodomain and extra-terminal (BET) protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

23.

BETFIRSO

      
Application Number 1758004
Status Registered
Filing Date 2023-08-02
Registration Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

24.

2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4,5-E]AZEPIN-4-YL)ACETAMIDE FOR TREATING THROMBOCYTHEMIA

      
Application Number 18019634
Status Pending
Filing Date 2021-08-03
First Publication Date 2023-09-28
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor Senderowicz, Adrian

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating thrombocythemia.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

25.

ANHYDROUS CRYSTALLINE FORMS OF 2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4,5-E]AZEPIN-4-YL)ACETAMIDE

      
Application Number US2023011919
Publication Number 2023/147149
Status In Force
Filing Date 2023-01-31
Publication Date 2023-08-03
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Plamondon, Louis

Abstract

Provided is an anhydrous crystalline form of Pelabresib as well as its use for treating conditions associated with BET proteins.

IPC Classes  ?

  • C07D 491/04 - Ortho-condensed systems
  • A61P 35/00 - Antineoplastic agents
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

26.

PELMOFY

      
Application Number 228912500
Status Pending
Filing Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, bromodomain and extra-terminal (BET) protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

27.

BETPELMY

      
Application Number 228912700
Status Pending
Filing Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

28.

BETFIRSO

      
Application Number 228912800
Status Pending
Filing Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

29.

PELAMOFY

      
Application Number 228912600
Status Pending
Filing Date 2023-08-02
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, bromodomain and extra-terminal (BET) protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; antibodies sold as a component ingredient of pharmaceuticals; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

30.

SUBSTITUTED BENZAMIDES AS MODULATORS OF TREX1

      
Application Number 17926849
Status Pending
Filing Date 2021-05-27
First Publication Date 2023-07-27
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Zablocki, Mary-Margaret
  • Taveras, Kennedy
  • Wilson, Jonathan E.
  • Coffin, Aaron
  • Levell, Julian R.
  • Medikonda, Aravind Prasad

Abstract

Provided are compounds of Formula (I): (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1. Provided are compounds of Formula (I): (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/4245 - Oxadiazoles
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
  • A61P 35/00 - Antineoplastic agents

31.

MODULATORS OF TREX1

      
Application Number US2023010541
Publication Number 2023/137030
Status In Force
Filing Date 2023-01-11
Publication Date 2023-07-20
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Coffin, Aaron

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 239/557 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61P 35/00 - Antineoplastic agents
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

32.

MODULATORS OF TREX1

      
Application Number 17922388
Status Pending
Filing Date 2021-04-30
First Publication Date 2023-06-01
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Levell, Julian R.
  • Wilson, Jonathan E.
  • Coffin, Aaron
  • Taveras, Kennedy

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1. Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 239/14 - Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
  • A61P 35/00 - Antineoplastic agents

33.

Methods of treating myeloproliferative disorders

      
Application Number 17711872
Grant Number 12070464
Status In Force
Filing Date 2022-04-01
First Publication Date 2023-02-23
Grant Date 2024-08-27
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Senderowicz, Adrian
  • Cooper, Michael

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 35/00 - Antineoplastic agents

34.

BETFIRSO

      
Application Number 018836370
Status Registered
Filing Date 2023-02-15
Registration Date 2023-09-28
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 01 - Chemical and biological materials for industrial, scientific and agricultural use
  • 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines. Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

35.

BETPELMY

      
Application Number 018836408
Status Registered
Filing Date 2023-02-15
Registration Date 2023-08-22
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 01 - Chemical and biological materials for industrial, scientific and agricultural use
  • 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines. Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

36.

BETMOFY

      
Application Number 018836422
Status Registered
Filing Date 2023-02-15
Registration Date 2023-08-22
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 01 - Chemical and biological materials for industrial, scientific and agricultural use
  • 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines. Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

37.

PELAMOFY

      
Application Number 018836402
Status Registered
Filing Date 2023-02-15
Registration Date 2023-08-22
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 01 - Chemical and biological materials for industrial, scientific and agricultural use
  • 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines. Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

38.

PELMOFY

      
Application Number 018836425
Status Registered
Filing Date 2023-02-15
Registration Date 2023-08-22
Owner Constellation Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 01 - Chemical and biological materials for industrial, scientific and agricultural use
  • 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Antibodies sold as a component ingredient of pharmaceuticals; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines. Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceuticals comprising small molecules; small molecule compounds for medical use and drug delivery; small molecule pharmaceuticals for the treatment of diseases and conditions; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders; diagnostic preparations for medical purposes; biological substances for human medical diagnostics and analysis; clinical medical reagents; biological preparations for medical purposes; pharmaceutical and veterinary preparations, agents and substances.

39.

PELAMOFY

      
Serial Number 97786656
Status Pending
Filing Date 2023-02-08
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceutical preparations comprising small molecules for treating cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; small molecule pharmaceuticals for the treatment of diseases and conditions, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies sold as a component ingredient of pharmaceuticals for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; diagnostic preparations for medical purposes; clinical medical reagents; biological preparations for medical purposes, namely for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceutical and veterinary preparations and agents for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways

40.

BETMOFY

      
Serial Number 97786664
Status Pending
Filing Date 2023-02-08
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceutical preparations comprising small molecules for treating cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; small molecule pharmaceuticals for the treatment of diseases and conditions, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies sold as a component ingredient of pharmaceuticals for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; diagnostic preparations for medical purposes; clinical medical reagents; biological preparations for medical purposes, namely for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceutical and veterinary preparations and agents for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways

41.

BETFIRSO

      
Serial Number 97786648
Status Pending
Filing Date 2023-02-08
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceutical preparations comprising small molecules for treating cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; small molecule pharmaceuticals for the treatment of diseases and conditions, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies sold as a component ingredient of pharmaceuticals for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; diagnostic preparations for medical purposes; clinical medical reagents; biological preparations for medical purposes, namely for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceutical and veterinary preparations and agents for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways

42.

PELMOFY

      
Serial Number 97786669
Status Pending
Filing Date 2023-02-08
Owner Constellation Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of blood diseases; pharmaceutical preparations for the treatment of diseases of the bone marrow; pharmaceutical preparations for the treatment of cancer, namely, BET protein inhibitors; pharmaceutical preparations for the treatment of myelofibrosis; pharmaceutical preparation for the treatment of myelodysplastic syndrome (MDS); pharmaceutical preparations for the treatment of myeloproliferative neoplasm; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment of thrombocythemia; pharmaceutical preparations for the treatment of diseases that involve dysregulation of epigenetic pathways; pharmaceutical preparations for epigenetic modulators as therapeutics; pharmaceutical preparations comprising small molecules for treating cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; small molecule pharmaceuticals for the treatment of diseases and conditions, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceuticals and pharmaceutical preparations for human use for the treatment and prevention of diseases and disorders, namely cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies sold as a component ingredient of pharmaceuticals for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; antibodies for use in the manufacture of active ingredients of pharmaceuticals and vaccines for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; diagnostic preparations for medical purposes; clinical medical reagents; biological preparations for medical purposes, namely for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways; pharmaceutical and veterinary preparations and agents for the treatment of cancer, myelofibrosis, myelodysplasic syndrome (MDS), myeloproliferative neoplasm, trombocythemia, anemia, low-risk myelodysplasic syndrome (MDS), essential thrombocythemia (ET) and diseases that involve dysregulation of epigenetic pathways

43.

USE OF PELABRESIB FOR TREATING ANEMIAS

      
Document Number 03218297
Status Pending
Filing Date 2022-05-10
Open to Public Date 2022-11-17
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Colak, Gozde

Abstract

The present disclosure relates to the use of pelabresib, and pharmaceutically acceptable salts thereof, for treating conditions associated with low reticulocyte counts.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 7/06 - Antianaemics

44.

USE OF PELABRESIB FOR TREATING ANEMIAS

      
Application Number US2022028457
Publication Number 2022/240800
Status In Force
Filing Date 2022-05-10
Publication Date 2022-11-17
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Colak, Gözde

Abstract

The present disclosure relates to the use of pelabresib, and pharmaceutically acceptable salts thereof, for treating conditions associated with low reticulocyte counts.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 7/06 - Antianaemics

45.

MODULATORS OF TREX1

      
Application Number US2022027571
Publication Number 2022/235725
Status In Force
Filing Date 2022-05-04
Publication Date 2022-11-10
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Levell, Julian, R.
  • Coffin, Aaron
  • Khanna, Avinash
  • Wilson, Jonathan, E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • A61P 35/00 - Antineoplastic agents
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine

46.

MODULATORS OF TREX1

      
Document Number 03217421
Status Pending
Filing Date 2022-05-04
Open to Public Date 2022-11-10
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Levell, Julian R.
  • Coffin, Aaron
  • Khanna, Avinash
  • Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61P 35/00 - Antineoplastic agents

47.

MODULATORS OF TREX1

      
Document Number 03216752
Status Pending
Filing Date 2022-04-25
Open to Public Date 2022-11-03
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Levell, Julian R.
  • Coffin, Aaron
  • Zablocki, Mary-Margaret
  • Wilson, Jonathan E.
  • Khanna, Avinash
  • Guerin, David J.
  • Mcelroy, William T.
  • Rocnik, Jennifer L.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

48.

MODULATORS OF TREX1

      
Application Number US2022026103
Publication Number 2022/232004
Status In Force
Filing Date 2022-04-25
Publication Date 2022-11-03
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Levell, Julian, R.
  • Coffin, Aaron
  • Zablocki, Mary-Margaret
  • Wilson, Jonathan, E.
  • Khanna, Avinash
  • Guerin, David, J.
  • Mcelroy, William, T.
  • Rocnik, Jennifer, L.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • A61P 35/00 - Antineoplastic agents
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine

49.

COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS

      
Application Number 17631010
Status Pending
Filing Date 2020-07-29
First Publication Date 2022-10-20
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Brucelle, Francois
  • Levell, Julian R.
  • Wilson, Jonathan E.

Abstract

Provided are methods for treating neurological disorders using compounds of Formula (I), and pharmaceutically acceptable salts and compositions thereof. Provided are methods for treating neurological disorders using compounds of Formula (I), and pharmaceutically acceptable salts and compositions thereof.

IPC Classes  ?

  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/415 - 1,2-Diazoles
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/4164 - 1,3-Diazoles
  • A61K 31/50 - PyridazinesHydrogenated pyridazines
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
  • A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
  • A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin

50.

MODULATORS OF TREX1

      
Application Number 17607940
Status Pending
Filing Date 2020-05-01
First Publication Date 2022-10-06
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Khanna, Avinash
  • Wilson, Jonathan E.
  • Zablocki, Mary-Margaret

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compostions thereof, which are useful for treating a variety of conditions associated with TREX1. Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compostions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61P 35/00 - Antineoplastic agents

51.

MODULATORS OF TREX1

      
Application Number 17628946
Status Pending
Filing Date 2020-07-22
First Publication Date 2022-09-15
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Khanna, Avinash
  • Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1. Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

52.

EZH2 INHIBITION IN COMBINATION THERAPIES FOR THE TREATMENT OF CANCERS

      
Application Number 17628948
Status Pending
Filing Date 2020-07-23
First Publication Date 2022-08-18
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor Bradley, William D.

Abstract

Provided herein are methods for treating advanced relapsed solid tumors using 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2, 4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide; or a pharmaceutically acceptable salt thereof. Also provided herein are methods of treating cancers (e.g., solid tumors) using 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide; or a pharmaceutically acceptable salt thereof; and a second agent selected from a topoisomerase inhibitor, a DNA alkylating agent, and an androgen receptor signaling inhibitor.

IPC Classes  ?

  • A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 33/243 - PlatinumCompounds thereof
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
  • A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
  • A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
  • A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
  • A61K 31/282 - Platinum compounds
  • A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
  • A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin

53.

CRYSTALLINE FORMS OF 7-CHLORO-2-(4-(3-METHOXYAZETIDIN-1-YL)CYCLOHEXYL)-2,4-DIMETHYL-N-((6-METHYL-4-(METHYLTHIO)-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)BENZO[D][1,3]DIOXOLE-5-CARBOXAMIDE

      
Application Number 17628947
Status Pending
Filing Date 2020-07-23
First Publication Date 2022-08-11
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Banda, Alamelu
  • Gehling, Victor S.

Abstract

The present disclosure relates to a crystalline Form 1 of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-di -methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d] [1,3]dioxole-5-carboxamide, which is useful as modulators the activity of histone methyl modifying enzymes. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline form and methods of using said compositions in the treatment of various disorders.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

54.

EZH2 INHIBITION THERAPIES FOR THE TREATMENT OF ANDROGEN RECEPTOR MUTATED PROSTATE CANCERS

      
Application Number US2021059847
Publication Number 2022/109106
Status In Force
Filing Date 2021-11-18
Publication Date 2022-05-27
Owner CONSTELLATION PHARMACEUTICALS, INC (USA)
Inventor
  • Bradley, William, D.
  • Cui, Jike
  • Sun, Kaiming
  • Trojer, Patrick
  • Wang, Jing
  • Wu, Rentian

Abstract

Provided herein are methods of treating prostate cancer having at least one pathogenic AR mutation using 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6- methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5- carboxamide, or a pharmaceutically acceptable salt thereof, alone or in combination with a therapeutically effective amount of an androgen receptor signaling inhibitor (ARSI) such as enzalutamide.

IPC Classes  ?

  • A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/04 - Antineoplastic agents specific for metastasis

55.

EZH2 INHIBITION THERAPIES FOR THE TREATMENT OF ANDROGEN RECEPTOR MUTATED PROSTATE CANCERS

      
Document Number 03199421
Status Pending
Filing Date 2021-11-18
Open to Public Date 2022-05-27
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Bradley, William D.
  • Cui, Jike
  • Sun, Kaiming
  • Trojer, Patrick
  • Wang, Jing
  • Wu, Rentian

Abstract

Provided herein are methods of treating prostate cancer having at least one pathogenic AR mutation using 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6- methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5- carboxamide, or a pharmaceutically acceptable salt thereof, alone or in combination with a therapeutically effective amount of an androgen receptor signaling inhibitor (ARSI) such as enzalutamide.

IPC Classes  ?

  • A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 35/04 - Antineoplastic agents specific for metastasis

56.

P300/CBP HAT INHIBITORS AND METHODS FOR THEIR USE

      
Application Number 17434102
Status Pending
Filing Date 2020-02-26
First Publication Date 2022-05-05
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT). Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

57.

THERAPEUTIC COMPOUNDS AND USES THEREOF

      
Application Number 17570139
Status Pending
Filing Date 2022-01-06
First Publication Date 2022-04-28
Owner
  • GENENTECH, INC. (USA)
  • CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Cyr, Patrick
  • Bronner, Sarah
  • Romero, F. Anthony
  • Magnuson, Steven
  • Tsui, Vickie Hsiao-Wei
  • Murray, Jeremy M.
  • Wai, John
  • Lai, Kwong Wah
  • Wang, Fei
  • Chen, Kevin X.

Abstract

The present invention relates to a compound formula (I): The present invention relates to a compound formula (I): The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2 X, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

58.

LSD1 inhibitors and medical uses thereof

      
Application Number 17241315
Grant Number 11547695
Status In Force
Filing Date 2021-04-27
First Publication Date 2022-03-17
Grant Date 2023-01-10
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Brucelle, Francois
  • Gehling, Victor S.
  • Khanna, Avinash

Abstract

Provided are novel compounds of Formula (I or Ia′): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I or Ia′), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.

IPC Classes  ?

  • C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
  • C07D 221/20 - Spiro-condensed ring systems
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61P 31/22 - Antivirals for DNA viruses for herpes viruses
  • A61P 31/18 - Antivirals for RNA viruses for HIV
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
  • A61P 35/00 - Antineoplastic agents

59.

2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4,5-E]AZEPIN-4-YL)ACETAMIDE FOR TREATING THROMBOCYTHEMIA

      
Document Number 03188245
Status Pending
Filing Date 2021-08-03
Open to Public Date 2022-02-10
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Senderowicz, Adrian

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-l-methyl-4H- benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating thrombocythemia.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
  • A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

60.

2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4,5-E]AZEPIN-4-YL)ACETAMIDE FOR TREATING THROMBOCYTHEMIA

      
Application Number US2021044318
Publication Number 2022/031686
Status In Force
Filing Date 2021-08-03
Publication Date 2022-02-10
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Senderowicz, Adrian

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-l-methyl-4H- benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating thrombocythemia.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
  • A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

61.

Modulators of TREX1

      
Application Number 17311526
Grant Number 12172990
Status In Force
Filing Date 2019-12-06
First Publication Date 2022-01-20
Grant Date 2024-12-24
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Gardberg, Anna
  • Gehling, Victor S.
  • Khanna, Avinash
  • Levell, Julian R.
  • Wilson, Jonathan E.
  • Taveras, Kennedy

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61P 35/00 - Antineoplastic agents
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

62.

SUBSTITUTED BENZAMIDES AS MODULATORS OF TREX1

      
Application Number US2021034488
Publication Number 2021/243001
Status In Force
Filing Date 2021-05-27
Publication Date 2021-12-02
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Zablocki, Mary-Margaret
  • Taveras, Kennedy
  • Wilson, Jonathan, E.

Abstract

Provided are compounds of Formula (I): (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 213/40 - Acylated substituent nitrogen atom
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P 35/00 - Antineoplastic agents
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof

63.

SUBSTITUTED BENZAMIDES AS MODULATORS OF TREX1

      
Document Number 03179627
Status Pending
Filing Date 2021-05-27
Open to Public Date 2021-12-02
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Coffin, Aaron
  • Levell, Julian R.
  • Medikonda, Aravind Prasad
  • Zablocki, Mary-Margaret
  • Taveras, Kennedy
  • Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I): (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 213/40 - Acylated substituent nitrogen atom
  • C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 471/04 - Ortho-condensed systems

64.

MODULATORS OF TREX1

      
Application Number US2021030189
Publication Number 2021/222761
Status In Force
Filing Date 2021-04-30
Publication Date 2021-11-04
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Levell, Julian R.
  • Wilson, Jonathan E.
  • Coffin, Aaron
  • Taveras, Kennedy

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 233/96 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 35/00 - Antineoplastic agents

65.

MODULATORS OF TREX1

      
Document Number 03177376
Status Pending
Filing Date 2021-04-30
Open to Public Date 2021-11-04
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Levell, Julian R.
  • Wilson, Jonathan E.
  • Coffin, Aaron
  • Taveras, Kennedy

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 233/96 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

66.

Modulators of methyl modifying enzymes, compositions and uses thereof

      
Application Number 16762600
Grant Number 11459315
Status In Force
Filing Date 2018-11-08
First Publication Date 2021-07-29
Grant Date 2022-10-04
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Brenneman, Jehrod B.
  • Côté, Alexandre
  • Gehling, Victor S.
  • Khanna, Avinash
  • Levell, Julian R.
  • Moine, Ludivine

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compostions thereof, which are useful for treating a variety of conditions associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

67.

Modulators of methyl modifying enzymes, compositions and uses thereof

      
Application Number 17057225
Grant Number 11919912
Status In Force
Filing Date 2019-05-17
First Publication Date 2021-07-08
Grant Date 2024-03-05
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Côté, Alexandre
  • Khanna, Avinash
  • Moine, Ludivine

Abstract

Provided are novel compounds of Formula (I): Formula (I); and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61P 35/00 - Antineoplastic agents

68.

METHODS OF TREATING MYELOPROLIFERATIVE DISORDERS

      
Application Number US2019059784
Publication Number 2021/091532
Status In Force
Filing Date 2019-11-05
Publication Date 2021-05-14
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Cooper, Michael
  • Senderowicz, Adrian

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 7/06 - Antianaemics
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

69.

TREATING MYELOPROLIFERATIVE DISORDERS WITH CPI-0610 AND A JAK INHIBITOR

      
Application Number US2019059813
Publication Number 2021/091535
Status In Force
Filing Date 2019-11-05
Publication Date 2021-05-14
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Cooper, Michael
  • Senderowicz, Adrian

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide in combination with JAK inhibitors for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

70.

P300/CBP HAT inhibitors

      
Application Number 16970169
Grant Number 11274090
Status In Force
Filing Date 2019-02-15
First Publication Date 2021-04-22
Grant Date 2022-03-15
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Wilson, Jonathan E.
  • Brucelle, Francois
  • Levell, Julian R.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • C07D 215/08 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
  • C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 231/40 - Acylated on said nitrogen atom
  • C07D 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 487/04 - Ortho-condensed systems
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

71.

P300/CBP hat inhibitors

      
Application Number 16970046
Grant Number 11414384
Status In Force
Filing Date 2019-02-15
First Publication Date 2021-03-04
Grant Date 2022-08-16
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Wilson, Jonathan E.
  • Levell, Julian R.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

IPC Classes  ?

  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 471/04 - Ortho-condensed systems

72.

COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS

      
Application Number US2020044014
Publication Number 2021/021893
Status In Force
Filing Date 2020-07-29
Publication Date 2021-02-04
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Brucelle, Francois
  • Levell, Julian R.
  • Wilson, Jonathan E.

Abstract

Provided are methods for treating neurological disorders using compounds of Formula (I), and pharmaceutically acceptable salts and compositions thereof.

IPC Classes  ?

  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

73.

ALPHA-AMINO AMIDE COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS

      
Document Number 03149095
Status Pending
Filing Date 2020-07-29
Open to Public Date 2021-02-04
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Brucelle, Francois
  • Levell, Julian R.
  • Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I):and pharmaceutically acceptable salts and compositions thereof for use in treating a neurological disorder or in the manufacture of a medicament for treating a neurological disorder, wherein Ring B and R1 are each an optionally substituted phenyl, and R7 is an optionally substituted phenyl, pyridyl, pyrimidinyl, or quinolinyl.

IPC Classes  ?

  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/415 - 1,2-Diazoles
  • A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
  • A61K 31/4164 - 1,3-Diazoles
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
  • A61K 31/50 - PyridazinesHydrogenated pyridazines
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

74.

Methods of treating myeloproliferative disorders

      
Application Number 17065316
Grant Number 10918646
Status In Force
Filing Date 2020-10-07
First Publication Date 2021-02-04
Grant Date 2021-02-16
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Senderowicz, Adrian
  • Cooper, Michael

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 35/00 - Antineoplastic agents

75.

MODULATORS OF TREX1

      
Document Number 03147419
Status Pending
Filing Date 2020-07-22
Open to Public Date 2021-01-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Khanna, Avinash
  • Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 35/00 - Antineoplastic agents
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

76.

EZH2 INHIBITION THERAPIES FOR THE TREATMENT OF CANCERS

      
Document Number 03148444
Status Pending
Filing Date 2020-07-23
Open to Public Date 2021-01-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Bradley, William D.

Abstract

Provided herein are methods for treating advanced relapsed solid tumors using 7- chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2, 4-dimethyl -N-((6-methyl-4-(methylthio)- 2-oxo-l,2-dihydropyridin-3-yl)methyl)benzo[d][l,3]dioxole-5-carboxamide; or a pharmaceutically acceptable salt thereof. Also provided herein are methods of treating cancers (e.g., solid tumors) using 7-chloro-2-(4-(3-methoxyazetidin-l-yl)cyclohexyl)-2,4- dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-l,2-dihydropyri din-3- yl)methyl)benzo[d][1,3]dioxole-5-carboxamide; or a pharmaceutically acceptable salt thereof; and a second agent selected from a topoisomerase inhibitor, a DNA alkylating agent, and an androgen receptor signaling inhibitor.

IPC Classes  ?

  • A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 33/243 - PlatinumCompounds thereof
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61P 35/00 - Antineoplastic agents

77.

MODULATORS OF TREX1

      
Application Number US2020043012
Publication Number 2021/016317
Status In Force
Filing Date 2020-07-22
Publication Date 2021-01-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Khanna, Avinash
  • Wilson, Jonathan, E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 35/00 - Antineoplastic agents

78.

EZH2 INHIBITION IN COMBINATION THERAPIES FOR THE TREATMENT OF CANCERS

      
Application Number US2020043163
Publication Number 2021/016409
Status In Force
Filing Date 2020-07-23
Publication Date 2021-01-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Bradley, William, D.

Abstract

Provided herein are methods for treating advanced relapsed solid tumors using 7- chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2, 4-dimethyl -N-((6-methyl-4-(methylthio)- 2-oxo-l,2-dihydropyridin-3-yl)methyl)benzo[d][l,3]dioxole-5-carboxamide; or a pharmaceutically acceptable salt thereof. Also provided herein are methods of treating cancers (e.g., solid tumors) using 7-chloro-2-(4-(3-methoxyazetidin-l-yl)cyclohexyl)-2,4- dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-l,2-dihydropyri din-3- yl)methyl)benzo[d][1,3]dioxole-5-carboxamide; or a pharmaceutically acceptable salt thereof; and a second agent selected from a topoisomerase inhibitor, a DNA alkylating agent, and an androgen receptor signaling inhibitor.

IPC Classes  ?

  • A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61K 33/243 - PlatinumCompounds thereof
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 35/00 - Antineoplastic agents

79.

CRYSTALLINE FORMS OF 7-CHLORO-2-(4-(3-METHOXYAZETIDIN-1-YL)CYCLOHEXYL)-2,4-DIMETHYL-N-((6-METHYL-4-(METHYLTHIO)-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)BENZO[D][1,3]DIOXOLE-5-CARBOXA MIDE

      
Document Number 03148447
Status Pending
Filing Date 2020-07-23
Open to Public Date 2021-01-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Banda, Alamelu
  • Gehling, Victor S.

Abstract

The present disclosure relates to a crystalline Form 1 of 7-chloro-2-(4-(3- methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2- dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, which is useful as modulators the activity of histone methyl modifying enzymes. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline form and methods of using said compositions in the treatment of various disorders.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61P 35/00 - Antineoplastic agents

80.

CRYSTALLINE FORMS OF 7-CHLORO-2-(4-(3-METHOXYAZETIDIN-1-YL)CYCLOHEXYL)-2,4-DIMETHYL-N-((6-METHYL-4-(METHYLTHIO)-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)BENZO[D][1,3]DIOXOLE-5-CARBOXAMIDE

      
Application Number US2020043178
Publication Number 2021/016414
Status In Force
Filing Date 2020-07-23
Publication Date 2021-01-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Banda, Alamelu
  • Gehling, Victor, S.

Abstract

The present disclosure relates to a crystalline Form 1 of 7-chloro-2-(4-(3- methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2- dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, which is useful as modulators the activity of histone methyl modifying enzymes. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline form and methods of using said compositions in the treatment of various disorders.

IPC Classes  ?

  • A61P 35/00 - Antineoplastic agents
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom

81.

Therapeutic compounds and uses thereof

      
Application Number 16886541
Grant Number 11168070
Status In Force
Filing Date 2020-05-28
First Publication Date 2020-12-24
Grant Date 2021-11-09
Owner
  • GENENTECH, INC. (USA)
  • CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Cyr, Patrick
  • Bronner, Sarah
  • Romero, F. Anthony
  • Magnuson, Steven
  • Tsui, Vickie Hsiao-Wei
  • Wai, John
  • Lai, Kwong Wah
  • Wang, Fei

Abstract

The present invention relates to compounds of formula (I) and formula (II): 6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/47 - QuinolinesIsoquinolines
  • A61P 25/00 - Drugs for disorders of the nervous system
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 243/14 - 1,4-BenzodiazepinesHydrogenated 1,4-benzodiazepines
  • C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 267/14 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
  • C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
  • A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/5513 - 1,4-Benzodiazepines, e.g. diazepam
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings

82.

METHODS OF TREATING MYELOPROLIFERATIVE DISORDERS

      
Application Number US2020038727
Publication Number 2020/257644
Status In Force
Filing Date 2020-06-19
Publication Date 2020-12-24
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Senderowicz, Adrian
  • Cooper, Michael

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-l-methyl-4H- benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide in combination with JAK inhibitors for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

83.

METHODS OF TREATING MYELOPROLIFERATIVE DISORDERS

      
Application Number US2019038506
Publication Number 2020/256739
Status In Force
Filing Date 2019-06-21
Publication Date 2020-12-24
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Senderowicz, Adrian
  • Cooper, Michael

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H- benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide in combination with JAK inhibitors for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

84.

MODULATORS OF TREX1

      
Application Number US2020030921
Publication Number 2020/223590
Status In Force
Filing Date 2020-05-01
Publication Date 2020-11-05
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Khanna, Avinash
  • Wilson, Jonathan, E.
  • Zablocki, Mary-Margaret

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

85.

MODULATORS OF TREX1

      
Document Number 03138859
Status Pending
Filing Date 2020-05-01
Open to Public Date 2020-11-05
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Khanna, Avinash
  • Wilson, Jonathan E.
  • Zablocki, Mary-Margaret

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

86.

Modulators of methyl modifying enzymes, compositions and uses thereof

      
Application Number 16856454
Grant Number 11274095
Status In Force
Filing Date 2020-04-23
First Publication Date 2020-10-08
Grant Date 2022-03-15
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Côté, Alexandre
  • Gehling, Victor S.
  • Khanna, Avinash
  • Moine, Ludivine
  • Stuckey, Jacob I.

Abstract

Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61P 35/00 - Antineoplastic agents

87.

LSD1 inhibitors and medical uses thereof

      
Application Number 16671559
Grant Number 11013718
Status In Force
Filing Date 2019-11-01
First Publication Date 2020-10-01
Grant Date 2021-05-25
Owner Constellation Pharmaceuticals, Inc. (USA)
Inventor
  • Brucelle, Francois
  • Gehling, Victor S.
  • Khanna, Avinash

Abstract

Provided are novel compounds of Formula (I or Ia′): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I or Ia′), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.

IPC Classes  ?

  • C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61P 31/22 - Antivirals for DNA viruses for herpes viruses
  • A61P 31/18 - Antivirals for RNA viruses for HIV
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
  • C07D 221/20 - Spiro-condensed ring systems
  • A61P 35/00 - Antineoplastic agents

88.

P300/CBP HAT INHIBITORS AND METHODS FOR THEIR USE

      
Document Number 03131383
Status Pending
Filing Date 2020-02-26
Open to Public Date 2020-09-03
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Wilson, Jonathan E.

Abstract

Provided are compounds of Formula (I) : and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

89.

P300/CBP HAT INHIBITORS AND METHODS FOR THEIR USE

      
Application Number US2020019786
Publication Number 2020/176558
Status In Force
Filing Date 2020-02-26
Publication Date 2020-09-03
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor Wilson, Jonathan, E.

Abstract

Provided are compounds of Formula (I) : and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

IPC Classes  ?

  • A61P 3/00 - Drugs for disorders of the metabolism
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P 35/00 - Antineoplastic agents
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine

90.

EZH2 AND ANDROGEN RECEPTOR SIGNALING INHIBITORS AS TOOLS FOR TARGETING PROSTATE CANCER

      
Application Number US2018067646
Publication Number 2020/139339
Status In Force
Filing Date 2018-12-27
Publication Date 2020-07-02
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Mcgrath, John
  • Senderowicz, Adrian
  • Trojer, Patrick
  • Bradley, William, D.

Abstract

Provided herein are methods of using (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide, or a pharmaceutically acceptable salt thereof and an androgen receptor signaling inhibitor for treating prostate cancer. Also provided are pharmaceutical compositions comprising (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1 H-indole-3-carboxamide, or a pharmaceutically acceptable salt thereof and an androgen receptor signaling inhibitor.

IPC Classes  ?

  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
  • A61P 35/00 - Antineoplastic agents
  • A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone

91.

EZH2 AND ANDROGEN RECEPTOR SIGNALING INHIBITORS AS TOOLS FOR TARGETING PROSTATE CANCER

      
Application Number US2019068575
Publication Number 2020/139943
Status In Force
Filing Date 2019-12-26
Publication Date 2020-07-02
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Mcgrath, John
  • Senderowicz, Adrian
  • Trojer, Patrick
  • Bradley, William, D.

Abstract

Provided herein are methods of using (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide, or a pharmaceutically acceptable salt thereof and an androgen receptor signaling inhibitor for treating prostate cancer. Also provided are pharmaceutical compositions comprising (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2- methyl- 1-( 1-( 1-(2, 2, 2-trifluoroethyl)piperidin-4-yl)ethyl)-1H- indole-3-carboxamide, or a pharmaceutically acceptable salt thereof and an androgen receptor signaling inhibitor.

IPC Classes  ?

  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
  • A61P 35/00 - Antineoplastic agents
  • A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone

92.

MODULATORS OF TREX1

      
Application Number US2019064825
Publication Number 2020/118133
Status In Force
Filing Date 2019-12-06
Publication Date 2020-06-11
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Gardberg, Anna
  • Gehling, Victor, S.
  • Khanna, Avinash
  • Levell, Julian, R.
  • Wilson, Jonathan, E.

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
  • A61P 35/00 - Antineoplastic agents

93.

MODULATORS OF TREX1

      
Document Number 03122093
Status Pending
Filing Date 2019-12-06
Open to Public Date 2020-06-11
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Gardberg, Anna
  • Gehling, Victor S.
  • Khanna, Avinash
  • Levell, Julian R.
  • Wilson, Jonathan E.
  • Taveras, Kennedy

Abstract

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.

IPC Classes  ?

  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
  • A61P 35/00 - Antineoplastic agents
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

94.

METHODS OF TREATING MYELOPROLIFERATIVE DISORDERS

      
Document Number 03120973
Status Pending
Filing Date 2018-11-27
Open to Public Date 2020-06-04
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Senderowicz, Adrian
  • Cooper, Michael

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 7/06 - Antianaemics
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

95.

METHODS OF TREATING MYELOPROLIFERATIVE DISORDERS

      
Application Number US2018062534
Publication Number 2020/112086
Status In Force
Filing Date 2018-11-27
Publication Date 2020-06-04
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Senderowicz, Adrian
  • Cooper, Michael

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 7/06 - Antianaemics
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

96.

METHODS OF TREATING MYELOPROLIFERATIVE DISORDERS

      
Application Number US2019063515
Publication Number 2020/112939
Status In Force
Filing Date 2019-11-27
Publication Date 2020-06-04
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Senderowicz, Adrian
  • Cooper, Michael

Abstract

The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-l-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.

IPC Classes  ?

  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 7/06 - Antianaemics
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

97.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

      
Document Number 03100977
Status Pending
Filing Date 2019-05-17
Open to Public Date 2019-11-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Cote, Alexandre
  • Khanna, Avinash
  • Moine, Ludivine

Abstract

Provided are novel compounds of Formula (I): Formula (I); and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
  • A61P 35/00 - Antineoplastic agents

98.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

      
Application Number US2019032926
Publication Number 2019/226491
Status In Force
Filing Date 2019-05-17
Publication Date 2019-11-28
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Côté, Alexandre
  • Khanna, Avinash
  • Moine, Ludivine

Abstract

Provided are novel compounds of Formula (I): Formula (I); and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
  • A61P 35/00 - Antineoplastic agents

99.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

      
Document Number 03098428
Status Pending
Filing Date 2019-04-17
Open to Public Date 2019-10-24
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Cote, Alexandre
  • Gehling, Victor S.
  • Khanna, Avinash
  • Moine, Ludivine
  • Stuckey, Jacob I.

Abstract

Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61P 35/00 - Antineoplastic agents
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

100.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

      
Application Number US2019027932
Publication Number 2019/204490
Status In Force
Filing Date 2019-04-17
Publication Date 2019-10-24
Owner CONSTELLATION PHARMACEUTICALS, INC. (USA)
Inventor
  • Côté, Alexandre
  • Gehling, Victor, S.
  • Khanna, Avinash
  • Moine, Ludivine
  • Stuckey, Jacob, I.

Abstract

Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61P 35/00 - Antineoplastic agents
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