Abstract

Reanalysis of the SIMPLIFY 1 and 2 trials data indicates MMB is effective in JAKi-naïve patients and in second line therapy to RUX, providing benefits of reducing enlarged spleens, improving myelofibrosis-related symptoms, and increasing transfusion independence in patient at risk for thrombocytopenia from the underlying disease and RUX therapy. Accordingly, methods of treating myeloproliferative neoplasms (MPN) such as myelofibrosis are described. The methods can include administering a therapeutically effective amount of momelotinib or a pharmaceutically acceptable salt thereof to a subject identified as having (i) myelofibrosis and (ii) a platelet count of less than 150×109/L. Also described are methods including administering to a subject with myelofibrosis a therapeutically effective stable dose of momelotinib or a pharmaceutically acceptable salt thereof, for a period of a plurality of weeks, where the subject is assessed as maintaining a platelet count above a predetermined threshold platelet count during the period.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure relates to methods of treating an inflammatory disease or disorder, the method comprising: administering to a subject in need thereof a therapeutically effective amount of momelotinib (MMB) or a pharmaceutically acceptable salt thereof; and administering to the subject one or more anti-inflammatory agents, and combinations for use in treating an inflammatory disease or disorder.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present disclosure relates to combination therapies for use in treating an inflammatory disease or disorder, for example methods of treating an inflammatory disease or disorder, the method comprising: administering to a subject in need thereof a therapeutically effective amount of N-(cyanomethyl)-4-(2-((4-(morpholino-3,3,5,5- d4)phenyl)amino)pyrimidin-4-yl)benzamide or a pharmaceutically acceptable salt thereof; and administering to the subject one or more anti-inflammatory agents.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Goods & Services

Antibiotic preparations

Abstract

The disclosure provides methods of treating joint inflammation, including rheumatoid arthritis, in a subject using mo-melotinib (MMB).

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

Abstract

The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 265/30 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings

Abstract

The present disclosure relates to methods of treating an inflammatory disease or disorder, the method comprising: administering to a subject in need thereof a therapeutically effective amount of momelotinib (MMB) or a pharmaceutically acceptable salt thereof; and administering to the subject one or more anti-inflammatory agents, and combinations for use in treating an inflammatory disease or disorder.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Transfusion independence in, and overall survival of, myelofibrosis patients can be improved by selecting a patient specific treatment method. A patient's baseline ferritin level can be used as a biomarker to select a first line treatment. The patient's ferritin levels during treatment can inform decisions about terminating treatment, or changing treatments to maintain transfusion dependence and/or convert a patient to transfusion independent from transfusion requiring or transfusion dependent.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• C07D 295/02 - 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
• C07D 295/12 - 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
• 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 403/12 - 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 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
• A61P 35/00 - Antineoplastic agents
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/02 - Antineoplastic agents specific for leukemia
• 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

Goods & Services

(1) Pharmaceutical preparations and drugs for the treatment of cancer, namely, Myelofibrosis (MF); pharmaceutical preparations and drugs for the treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and disorders; Biological preparations made from living tissues for the treatment of cancer; chemical preparations for medical purposes for the treatment of cancer; Pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and disorders; Pharmaceutical preparations and substance for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; Diagnostic reagents for medical purposes; Medical diagnostic reagents, assays, and test kits for testing of body fluids; Cells protein molecules and molecular compounds, namely, drug delivery agents consisting of compounds that facilitate delivery of a wide range of pharmaceuticals to treat cancer; DNA damage response assets, namely, pharmaceutical preparations for the treatment of conditions associated with DNA damage, namely cancer, for medical use (1) Pharmaceutical research and development; development of pharmaceutical preparations and drugs; development of pharmaceutical preparations and drugs for the treatment of blood diseases, bone and bone marrow diseases, and cancers; Scientific research and development in the field of cancer treatment and diagnosis, medical research services; Scientific research laboratories for conducting research in the field of cancer, cancer prevention and cancer diagnosis; Medical research laboratory services; conducting clinical trials for others; conducting clinical trial for others regarding pharmaceutical preparations and drugs in the field of blood diseases, bone and bone marrow diseases, and cancers; DNA screening and analysis services for scientific research purposes (2) Medical diagnostic services, medical examination services, medical analysis services for cancer diagnosis and prognosis, medical care and analysis services relating to patient treatment, providing medical information in the field of cancer treatment; medical testing services; DNA screening and analysis services for medical purposes

Goods & Services

Pharmaceutical preparations and drugs for the treatment of cancer, namely, Myelofibrosis (MF); pharmaceutical preparations and drugs for the treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Biological and chemical preparations for the treatment of cancer; Pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Pharmaceutical preparations and substance for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; medical reagents; Medical diagnostic reagents, assays, and test kits for testing of body fluids; cells, protein molecules, and molecular compounds in the nature of drug delivery agents consisting of compounds that facilitate delivery of a wide range of pharmaceuticals for medical purposes; DNA damage response assets, namely, pharmaceutical preparations for the treatment of conditions associated with DNA damage, namely cancer, for medical use. Pharmaceutical research and development; development of pharmaceutical preparations and drugs; development of pharmaceutical preparations and drugs for the treatment of blood diseases, bone and bone marrow diseases, and cancers; scientific research and development; scientific laboratory services; medical laboratory services; conducting clinical trials for others; conducting clinical trial for others regarding pharmaceutical preparations and drugs in the field of blood diseases, bone and bone marrow diseases, and cancers; DNA screening and analysis services for scientific research purposes. Medical services; medical testing services; DNA screening and analysis services for medical purposes.

Goods & Services

(1) Pharmaceutical preparations and drugs for the treatment of cancer, namely, Myelofibrosis (MF); pharmaceutical preparations and drugs for the treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Biological and chemical preparations for the treatment of cancer; Pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Pharmaceutical preparations and substance for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; medical reagents; Medical diagnostic reagents, assays, and test kits for testing of body fluids; cells, protein molecules, and molecular compounds in the nature of drug delivery agents consisting of compounds that facilitate delivery of a wide range of pharmaceuticals for medical purposes; DNA damage response assets, namely, pharmaceutical preparations for the treatment of conditions associated with DNA damage, namely cancer, for medical use (1) Pharmaceutical research and development; development of pharmaceutical preparations and drugs; development of pharmaceutical preparations and drugs for the treatment of blood diseases, bone and bone marrow diseases, and cancers; scientific research and development; scientific laboratory services; medical laboratory services; conducting clinical trials for others; conducting clinical trial for others regarding pharmaceutical preparations and drugs in the field of blood diseases, bone and bone marrow diseases, and cancers; DNA screening and analysis services for scientific research purposes (2) Medical services; medical testing services; DNA screening and analysis services for medical purposes

Abstract

Herein disclosed are methods of treatment administering SRA141 as a monotherapy or in a combination therapy useful for inhibiting the growth of tumors such as those in patients with cancer.

IPC Classes  ?

• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/519 - Pyrimidines; Hydrogenated 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 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 35/04 - Antineoplastic agents specific for metastasis
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 239/60 - Three or more oxygen or sulfur atoms
• A61K 31/515 - Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
• C07D 239/62 - Barbituric acids
• 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 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 405/10 - 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 carbon chain containing aromatic rings
• C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 409/10 - 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 carbon chain containing aromatic rings
• C07D 413/06 - 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 only aliphatic carbon atoms
• 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
• C07D 417/10 - 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 carbon chain containing aromatic rings
• C07D 239/22 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms

Abstract

9/L. Also described are methods including administering to a subject with myelofibrosis a therapeutically effective stable dose of momelotinib or a pharmaceutically acceptable salt thereof, for a period of a plurality of weeks, where the subject is assessed as maintaining a platelet count above a predetermined threshold platelet count during the period.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 35/00 - Antineoplastic agents

Goods & Services

(1) Pharmaceuticals preparations and drugs; pharmaceutical preparations and drugs for the treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Biological and chemical preparations for the treatment of cancer; Pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Pharmaceutical preparations and substance for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; medical reagents; Medical diagnostic reagents, assays, and test kits; cells, proteins, and molecular compounds for medical purposes; DNA damage response assets for medical use (1) Pharmaceutical research and development; development of pharmaceutical preparations and drugs; development of pharmaceutical preparations and drugs for the treatment of blood diseases, bone and bone marrow diseases, and cancers; scientific research and development; scientific laboratory services; medical laboratory services; conducting clinical trials; conducting clinical trial regarding pharmaceutical preparations and drugs in the field of blood diseases, bone and bone marrow diseases, and cancers; DNA screening and analysis services for scientific research purposes (2) Medical services; medical testing services; DNA screening and analysis services for medical purposes

Goods & Services

Pharmaceutical preparations and drugs; pharmaceutical preparations and drugs for the treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; biological and chemical preparations for the treatment of cancer; pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; pharmaceutical preparations and substance for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; medical reagents; medical diagnostic reagents and assays for testing of body fluids; cells, proteins, and molecular compounds for medical purposes; DNA damage response assets for medical use. Pharmaceutical research and development; development of pharmaceutical preparations and drugs; development of pharmaceutical preparations and drugs for the treatment of blood diseases, bone and bone marrow diseases, and cancers; scientific research and development; scientific laboratory services; medical laboratory services; conducting clinical trials; conducting clinical trial regarding pharmaceutical preparations and drugs in the field of blood diseases, bone and bone marrow diseases, and cancers; DNA screening and analysis services for scientific research purposes. Medical services; medical testing services; DNA screening and analysis services for medical purposes.

Goods & Services

(1) Pharmaceuticals preparations and drugs; pharmaceutical preparations and drugs for the treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Biological and chemical preparations for the treatment of cancer; Pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; Pharmaceutical preparations and substance for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; medical reagents; Medical diagnostic reagents, assays, and test kits; cells, proteins, and molecular compounds for medical purposes; DNA damage response assets for medical use (1) Pharmaceutical research and development; development of pharmaceutical preparations and drugs; development of pharmaceutical preparations and drugs for the treatment of blood diseases, bone and bone marrow diseases, and cancers; scientific research and development; scientific laboratory services; medical laboratory services; conducting clinical trials; conducting clinical trial regarding pharmaceutical preparations and drugs in the field of blood diseases, bone and bone marrow diseases, and cancers; DNA screening and analysis services for scientific research purposes (2) Medical services; medical testing services; DNA screening and analysis services for medical purposes

Abstract

The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 265/30 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings

Abstract

Methods of manufacturing squalene and alpha-tocopherol-containing oil-in-water emulsions having small oil droplet particle sizes. Such emulsions being of use as vaccine adjuvants.

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants

Goods & Services

Pharmaceutical preparations and drugs for the treatment of cancer, namely, myelofibrosis (mf); pharmaceutical preparations and drugs for the treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders; biological and chemical preparations for the treatment of cancer; pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors, treatment of blood diseases or disorders, bone and bone marrow diseases, and cancers associated with blood diseases and/or disorders

Goods & Services

Pharmaceutical research and development; development of pharmaceutical preparations and drugs; development of pharmaceutical preparations and drugs for the treatment of blood diseases, bone and bone marrow diseases, and cancers; scientific research and development; scientific laboratory services; medical laboratory services; conducting clinical trials; conducting clinical trial regarding pharmaceutical preparations and drugs in the field of blood diseases, bone and bone marrow diseases, and cancers; DNA screening and analysis services for scientific research purposes; all the above services related to the field of blood diseases, bone and bone marrow diseases, and cancers.

Abstract

Herein disclosed are methods of treatment administering SRA141 as a monotherapy or in a combination therapy useful for inhibiting the growth of tumors such as those in patients with cancer.

IPC Classes  ?

• 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
• A61P 35/00 - Antineoplastic agents
• G01N 33/48 - Biological material, e.g. blood, urine; Haemocytometers

Abstract

The present invention relates generally to the methods for the treatment and diagnosis of conditions mediated by IL-5 and excess eosinophil production, and more specifically to mAbs, Fabs, chimeric and humanized antibodies. More particularly, the present invention relates generally to the treatment of eosinophilic bronchitis with an anti-IL-5 antibody or fragment thereof.

IPC Classes  ?

• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
• A61P 11/00 - Drugs for disorders of the respiratory system
• C07K 14/54 - Interleukins (IL)

Abstract

Reanalysis of the SIMPLIFY 1 and 2 trials data indicates MMB is effective in JAKi- naïve patients and in second line therapy to RUX, providing benefits of reducing enlarged spleens, improving myelofibrosis-related symptoms, and increasing transfusion independence in patient at risk for thrombocytopenia from the underlying disease and RUX therapy. Accordingly, methods of treating myeloproliferative neoplasms (MPN) such as myelofibrosis are described. The methods can include administering a therapeutically effective amount of momelotinib or a pharmaceutically acceptable salt thereof to a subject identified as having (i) myelofibrosis and (ii) a platelet count of less than 150 x l09/L. Also described are methods including administering to a subject with myelofibrosis a therapeutically effective stable dose of momelotinib or a pharmaceutically acceptable salt thereof, for a period of a plurality of weeks, where the subject is assessed as maintaining a platelet count above a predetermined threshold platelet count during the period.

IPC Classes  ?

• A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• C07D 235/10 - Radicals substituted by halogen atoms or nitro radicals
• C07D 235/24 - Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
• 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 235/08 - Radicals containing only hydrogen and carbon atoms
• C07D 401/10 - 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 carbon chain containing aromatic rings
• C07D 403/10 - 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 aromatic rings
• C07D 405/10 - 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 carbon chain containing aromatic rings
• C07D 409/10 - 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 carbon chain containing aromatic rings
• 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
• C07D 417/10 - 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 carbon chain containing aromatic rings

Abstract

A cap (100) for a container (300) having a pair of side walls each with an inner wall surface (120). Each inner wall surface having two ribs (240) distributed thereon for retention of a liner. Each of the two ribs has a concave arc with a concave radius of curvature forming a curved portion of the inner wall, and a convex arc. Each of the two ribs has a different overall configuration that facilitates removal, and securing onto, of the cap from/to the container without damage of the ribs and the retention of the liner in the cap.

IPC Classes  ?

• B65D 41/48 - Snap-on caps or cap-like covers non-metallic, e.g. made of paper or plastics
• B65D 51/18 - Arrangements of closures with protective outer cap-like covers or of two or more co-operating closures
• B65D 53/04 - Discs

Abstract

The present disclosure relates to compositions, for treating interleukin 5 (IL-5) mediated diseases in pediatric subjects, and related methods.

IPC Classes  ?

• A61K 38/20 - Interleukins
• A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
• A61P 37/02 - Immunomodulators
• C07K 14/54 - Interleukins (IL)
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• C07K 19/00 - Hybrid peptides

Abstract

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 239/60 - Three or more oxygen or sulfur atoms
• A61K 31/515 - Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
• C07D 239/62 - Barbituric acids
• 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 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 405/10 - 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 carbon chain containing aromatic rings
• C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 409/10 - 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 carbon chain containing aromatic rings
• C07D 413/06 - 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 only aliphatic carbon atoms
• 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
• C07D 417/10 - 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 carbon chain containing aromatic rings
• C07D 239/22 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms

Abstract

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 235/08 - Radicals containing only hydrogen and carbon atoms
• C07D 235/10 - Radicals substituted by halogen atoms or nitro radicals
• C07D 235/24 - Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
• 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 401/10 - 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 carbon chain containing aromatic rings
• C07D 403/10 - 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 aromatic rings
• C07D 405/10 - 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 carbon chain containing aromatic rings
• C07D 409/10 - 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 carbon chain containing aromatic rings
• 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
• C07D 417/10 - 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 carbon chain containing aromatic rings
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol

Abstract

This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.

IPC Classes  ?

• A61K 31/4412 - Non-condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• C07D 213/64 - One oxygen atom attached in position 2 or 6
• C07D 211/86 - Oxygen atoms
• 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 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
• A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4433 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated 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 pyridines; Hydrogenated 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
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene

Abstract

A new oral solid dosage form of dutasteride, including fixed dose combinatins with tamsulosin, are provided. A process for preparation, and uses, particularly for BPH and other androgen mediated diseases or conditions, are also disclosed.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/473 - Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines

Abstract

Provided herein are methods, compositions, and kits for treating ACVR-1-mediated diseases using N-(cyanomethyl)-4-[2-4-morpholinoanilino)pyrimidin-4-yl]benzamide.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines

Abstract

This invention relates to important intermediates in the preparation of a compound which is an inhibitor of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1).

IPC Classes  ?

• C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
• C07D 498/04 - 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

Abstract

Compounds of formula (I) and salts thereof: 1-3alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.

IPC Classes  ?

• A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
• A61K 31/225 - Polycarboxylic acids
• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• 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 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
• 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
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
• C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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 243/08 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
• C07D 265/32 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
• C07C 219/24 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups or amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
• C07C 225/14 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated
• A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• C07D 239/48 - Two nitrogen atoms
• C07D 498/14 - Ortho-condensed 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
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• C07D 213/40 - Acylated substituent nitrogen atom
• C07D 265/30 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
• C07D 413/06 - 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 only aliphatic carbon atoms
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• C07J 53/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by condensation with carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms

Goods & Services

Biological and chemical preparations for the treatment of cancer; Pharmaceutical products, preparations, and compounds for the prevention and treatment of cancer and tumors; Pharmaceutical preparations and substances for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders but specifically excluding biological eye tissue, corneas, and other ocular or eye-related human tissue intended for subsequent tissue and organ implantation; Pharmaceutical preparations for use in dermatology, oncology, hematology and for gastroenterological disorders but specifically excluding biological eye tissue, corneas, and other ocular or eye-related human tissue intended for subsequent tissue and organ implantation. Providing links to the websites of others featuring information about the diagnosis and treatment of cancer; providing links to the websites of others. Development of pharmaceutical preparations and medicines; drug discovery services; pharmaceutical drug development services; research relating to medicines; medical research; pharmaceutical research and development services; medical research services in the field of cancer; research and development of biological and chemical preparations for the treatment of cancer; research and development of pharmaceutical products, preparations and compounds for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; research and development of pharmaceutical preparations for use in dermatology, oncology, hematology, and for gastroenterological disorders; information, consultancy and advisory services relating to all of the aforesaid. Medical services; medical services for the treatment of cancer; medical analysis services; medical analysis services for the diagnosis of cancer; providing cancer screening services; providing a website via a global computer network featuring information in the fields of health, cancer, cancer treatment, recovery and survival; medical evaluation services; medical evaluation and diagnosis of cancer; RNA or DNA analysis for cancer diagnosis and prognosis; medical services for the diagnosis of conditions of the human body; providing a website via a global computer network featuring information in the fields of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; providing a website via a global computer network featuring information in the fields of dermatology, oncology, hematology, and for gastroenterological disorders; information, consultancy and advisory services relating to all of the aforesaid.

Abstract

Novel uses of selective class Ila HDAC inhibitors are described.

IPC Classes  ?

• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A61K 31/33 - Heterocyclic compounds
• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• 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 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim

Abstract

Disclosed in this invention are human IgG Fc variants sequences that demonstrate low and no binding activities to Fc gamma receptor. The disclosed Fc variants are useful for making Fc fusion proteins and/or IgGs where low or no Fc effector function of the mentioned molecules are desirable.

IPC Classes  ?

• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• C07K 16/42 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against immunoglobulins (anti-idiotypic antibodies)

Abstract

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.

IPC Classes  ?

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

Abstract

This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.

IPC Classes  ?

• A61K 31/4412 - Non-condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
• A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated 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 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4433 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom

Abstract

This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.

IPC Classes  ?

• C07D 498/04 - 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

Abstract

Compounds of formula (I) and salts thereof: 1-3alkyl; m is an integer having a value of 2 to 4; n is an integer having a value of 0 to 3; and p is an integer having a value of 0 to 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• C07D 487/04 - Ortho-condensed systems

Goods & Services

(1) Biological, chemical and pharmaceutical products, preparations and compounds for the treatment of cancer, namely blood cancers and solid tumors; Biological, chemical and pharmaceutical products, preparations and compounds for the treatment of cancer related diseases, namely anemia, thrombocytopenia, neutropenia, fatigue; Biological, chemical and pharmaceutical products, preparations and compounds for the treatment of disorders and infections of the endocrine system, namely growth and thyroid disorders; Biological, chemical and pharmaceutical products, preparations and compounds for the treatment of immunologic diseases, namely, autoimmune diseases, immunologic deficiency syndromes; Biological, chemical and pharmaceutical products, preparations and compounds for the treatment of metabolic diseases and disorders, namely diabetes, hypoglycaemia, gout, osteoarthritis, muscular dystrophy, anemia; Biological, chemical and pharmaceutical products, preparations and compounds for the treatment of genito-urinary and pelvic diseases, disorders and infections, namely infertility, sexually transmitted diseases, incontinence and sexual dysfunction but specifically excluding biological eye tissue, corneas, and other ocular or eye-related human tissue intended for subsequent tissue or organ implantation.

Abstract

The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

IPC Classes  ?

• A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 239/42 - One nitrogen atom
• C07D 265/30 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings

Abstract

The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

IPC Classes  ?

• C07D 239/86 - Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
• 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 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical

Abstract

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

IPC Classes  ?

• C07D 239/60 - Three or more oxygen or sulfur atoms
• A61K 31/515 - Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 239/62 - Barbituric acids
• 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 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 405/10 - 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 carbon chain containing aromatic rings
• C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 409/10 - 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 carbon chain containing aromatic rings
• C07D 413/06 - 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 only aliphatic carbon atoms
• 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
• C07D 417/10 - 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 carbon chain containing aromatic rings
• C07D 239/22 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms

Abstract

Thienopyridone compounds of formula (I): or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
• A61K 31/4427 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• 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
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine

Abstract

a) form a hydrogen bonding interaction in which the compound accepts a hydrogen bond from the sidechain NH2 group of the asparagine residue found at: b) accept a water-mediated hydrogen bond in which the compound accepts a hydrogen bond from a water that is itself hydrogen-bonded to the sidechain hydroxyl of the tyrosine residue found at c) which are also able to form a Van der Waals interaction with a lipophilic binding region of a binding pocket such that one or more heavy atoms of the said compounds lie within a 5 Å range of any of the heavy atoms of the following bromodomain residues which define the binding pocket: pharmaceutical compositions containing such compounds, and their use in therapy.

IPC Classes  ?

• G01N 21/64 - Fluorescence; Phosphorescence
• G01N 33/566 - Immunoassay; Biospecific binding assay; Materials therefor using specific carrier or receptor proteins as ligand binding reagent
• C12N 9/12 - Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids

Abstract

Compounds of formula (I): 3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• 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
• A61K 9/00 - Medicinal preparations characterised by special physical form
• C07D 473/16 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
• C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine

Abstract

The present invention is based on the finding that enrichment of D3-creatinine in a urine sample following oral administration of a single defined dose of D3-creatine can be used to calculate total-body creatine pool size and total body skeletal muscle mass in a subject. The invention further encompasses methods for detecting creatinine and D3-creatinine in a single sample. The methods of the invention find use, inter alia, in diagnosing disorders related to skeletal muscle mass, and in screening potential therapeutic agents to determine their effects on muscle mass.

IPC Classes  ?

• G01N 33/70 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving creatine or creatinine
• G01N 33/48 - Biological material, e.g. blood, urine; Haemocytometers
• A61B 10/00 - Other methods or instruments for diagnosis, e.g. for vaccination diagnosis; Sex determination; Ovulation-period determination; Throat striking implements
• A61B 5/00 - Measuring for diagnostic purposes ; Identification of persons
• H01J 49/00 - Particle spectrometers or separator tubes
• A61B 5/107 - Measuring physical dimensions, e.g. size of the entire body or parts thereof
• G01N 30/72 - Mass spectrometers
• A61B 5/15 - Devices for taking samples of blood
• G01N 33/493 - Physical analysis of biological material of liquid biological material urine

Abstract

The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 513/18 - Bridged systems

Abstract

The invention relates to denture adhesives and methods for making denture adhesives.

IPC Classes  ?

• A61K 6/00 - Preparations for dentistry

Abstract

The present invention relates to a compound of formula (I): 13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.

IPC Classes  ?

• A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• 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

Abstract

Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

IPC Classes  ?

• A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
• C07D 487/18 - Bridged systems
• C07D 471/18 - Bridged systems
• A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
• A61K 31/506 - Pyrimidines; Hydrogenated 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
• C07D 487/04 - Ortho-condensed systems
• C07D 513/18 - Bridged 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
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Aspects of the present invention are directed to a heat sealed packaging wherein the heat seal is along a curved surface. Additional aspects of the present invention are directed to a device for heat sealing a package on a surface that is curved along the direction of force.

IPC Classes  ?

• B65D 53/06 - Sealings formed by liquid or plastic material
• B29C 65/02 - Joining of preformed parts; Apparatus therefor by heating, with or without pressure
• B29C 65/00 - Joining of preformed parts; Apparatus therefor

Abstract

The present invention relates to genetically modified host cells, in particular yeast cells, comprising at least one isolated polynucleotide encoding a Killer Expression protease (Kex2p) or a fragment and/or variant thereof which has at least one Kex2p functional activity and at least one isolated polynucleotide encoding a Protein Disulfide-Isomerase (Pdi1) or a fragment and/or variant thereof which has at least one Pdi functional activity. Also provided herein are genetically modified host cells comprising at least one isolated polynucleotide encoding a Killer Expression protease (Kex2p) or a fragment and/or variant thereof which has at least one Kex2p functional activity, at least one isolated polynucleotide encoding a Protein Disulfide-Isomerase (Pdi1) or a fragment and/or variant thereof which has at least one Pdi1 functional activity and at least one isolated polynucleotide encoding a Endoplasmic Reticulum Oxidoreductin (Ero1) or a fragment and/or variant thereof which has at least one Ero1 functional activity.

IPC Classes  ?

• C12N 15/81 - Vectors or expression systems specially adapted for eukaryotic hosts for fungi for yeasts
• C12N 1/16 - Yeasts; Culture media therefor
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• C12N 9/90 - Isomerases (5.)
• C12N 9/02 - Oxidoreductases (1.), e.g. luciferase
• C12N 9/60 - Proteinases derived from fungi from yeast

Abstract

The present invention provides liquid compositions comprising albiglutide or a variant thereof, a buffering agent, at least one saccharide and/or at least one polyol, at least one stabilizing agent and optionally a surfactant wherein said albiglutide remains stable in said liquid composition. Albiglutide or a variant thereof can be considered to remain stable in liquid if at least about ≥96% of said albiglutide or a variant thereof remains as a monomer in the liquid composition over a period of at least one week.

IPC Classes  ?

• A61K 38/26 - Glucagons
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• C07K 14/00 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof

Abstract

The disclosure includes a method to treat glucose intolerance and/or insulin resistance and associated symptoms by administering a calcilytic drug to a subject in need thereof.

IPC Classes  ?

• C07D 213/00 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members

Abstract

The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4- morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

IPC Classes  ?

• A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• C07D 265/30 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
• C07D 239/42 - One nitrogen atom
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
• C07D 471/04 - Ortho-condensed systems
• 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 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines

Abstract

The present invention relates to long acting pharmaceutical compositions of betulin derivatives or pharmaceutically acceptable salts thereof, useful in the treatment or prevention of Human Immunodeficiency Virus (HIV) infections.

IPC Classes  ?

• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone

Abstract

The present invention relates to compounds of formula (I) and salts thereof: 1-6alkyl, and m is an integer having a value of 1 to 4; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

Benzodiazepine compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.

IPC Classes  ?

• 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
• C07D 487/04 - Ortho-condensed systems

Abstract

Compounds of formula (I) and salts thereof: 1-3alkyl; m is an integer having a value of 2 to 4; n is an integer having a value of 0 to 3; and p is an integer having a value of 0 to 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• C07D 487/04 - Ortho-condensed systems
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The present invention relates to Compounds of formula (I) and salts thereof: 1-6alkyl, and m is an integer having a value of 0 to 3; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• C07D 487/04 - Ortho-condensed systems

Abstract

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.

IPC Classes  ?

• 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 413/10 - 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
• C07D 235/08 - Radicals containing only hydrogen and carbon atoms

Abstract

Compounds of formula (I) and salts thereof: 1-3alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 11/06 - Antiasthmatics
• A61P 37/08 - Antiallergic agents
• A61K 31/52 - Purines, e.g. adenine
• 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 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants

Abstract

The present disclosure provides a device for preventing the fouling of a liquid dispensing nozzle. The end of the dispensing nozzle is placed in a hollow interior of a band carrying the same solvent that is dispensed by the nozzle. The solvent on the band evaporates into a gap between the band and the dispensing nozzle, thus providing a vapor sheath, or environment in the gap, that helps to prevent the fouling of the dispensing nozzle.

IPC Classes  ?

• B05B 15/50 - Arrangements for cleaning; Arrangements for preventing deposits, drying-out or blockage; Arrangements for detecting improper discharge caused by the presence of foreign matter
• B05B 15/55 - Arrangements for cleaning; Arrangements for preventing deposits, drying-out or blockage; Arrangements for detecting improper discharge caused by the presence of foreign matter using cleaning fluids
• B05D 1/02 - Processes for applying liquids or other fluent materials performed by spraying
• A61M 11/00 - Sprayers or atomisers specially adapted for therapeutic purposes

Abstract

Aspects of the present invention are directed to a metered dose container. The container may comprise a body; a first barrier in contact with a base of the container and extending partially along the vertical axis of the body; a second barrier in contact with a top of the container and extending partially along with vertical axis of the body. The space between the first barrier and the second barrier defines a loading chamber, the space between the second barrier and a front wall of the container defines a dispensing chamber, and the space between a rear wall of the container and the first barrier defines a storage chamber. The base also comprises a depressible portion that can convert the container from a transit mode to a dispensing mode.

IPC Classes  ?

• G01F 11/12 - Apparatus requiring external operation adapted at each repeated and identical operation to measure and separate a predetermined volume of fluid or fluent solid material from a supply or container, without regard to weight, and to deliver it with measuring chambers moved during operation of the valve type, i.e. the separating being effected by fluid-tight or powder-tight movements

Abstract

The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and VEGFR inhibitor, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express PD-L1.

IPC Classes  ?

• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

Abstract

This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.

IPC Classes  ?

• C07D 211/86 - Oxygen atoms
• 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 213/64 - One oxygen atom attached in position 2 or 6
• 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

Abstract

The present invention is directed to crystalline forms of a compound which has retinoid-related orphan receptor gamma (RORy) modulator activity, processes for their preparation, pharmaceutical compositions containing the same and their use in therapy.

IPC Classes  ?

• C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• C07D 257/04 - Five-membered rings

Abstract

A novel combination comprising the androgen receptor inhibitor, 4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide or a pharmaceutically acceptable salt or solvate thereof, with a PI3Kß inhibitor, 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of androgen receptor and/or PI3Kß is beneficial, e.g., cancer.

IPC Classes  ?

• A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
• A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin
• 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

Abstract

A novel combination comprising the17 α-hydroxylase/C17,20 lyase inhibitor, (3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-ol or a pharmaceutically acceptable salt or solvate thereof, with a PI3Kβ inhibitor, 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of 17 α-hydroxylase/C17,20 lyase and/or PI3Kβ is beneficial, e.g., cancer.

IPC Classes  ?

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

Abstract

A continuous dosage form coating apparatus uses vibrational impulses to maintain a dosage forms in a fluid state to expose them to a coating material atomized by spraying.

IPC Classes  ?

• A61K 9/50 - Microcapsules
• B05C 3/05 - Apparatus in which the work is brought into contact with a bulk quantity of liquid or other fluent material the work being immersed in the liquid or other fluent material with special provision for agitating the work or the liquid or other fluent material by applying vibrations thereto
• B05C 19/02 - Apparatus specially adapted for applying particulate materials to surfaces using fluidised-bed technique
• B05C 5/02 - Apparatus in which liquid or other fluent material is projected, poured or allowed to flow on to the surface of the work from an outlet device in contact, or almost in contact, with the work
• B05C 9/08 - Apparatus or plant for applying liquid or other fluent material to surfaces by means not covered by groups , or in which the means of applying the liquid or other fluent material is not important for applying liquid or other fluent material and performing an auxiliary operation
• B05C 13/00 - Means for manipulating or holding work, e.g. for separate articles
• B01J 2/00 - Processes or devices for granulating materials, in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
• B05B 13/02 - Means for supporting work; Arrangement or mounting of spray heads; Adaptation or arrangement of means for feeding work
• B05D 1/02 - Processes for applying liquids or other fluent materials performed by spraying
• B01J 2/18 - Processes or devices for granulating materials, in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic using a vibrating apparatus
• A61J 3/00 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
• A01C 1/06 - Coating or dressing seed
• A23G 3/26 - Apparatus for coating by tumbling
• B05D 1/22 - Processes for applying liquids or other fluent materials performed by dipping using fluidised-bed technique
• B05D 3/12 - Pretreatment of surfaces to which liquids or other fluent materials are to be applied; After-treatment of applied coatings, e.g. intermediate treating of an applied coating preparatory to subsequent applications of liquids or other fluent materials by mechanical means

Abstract

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 235/08 - Radicals containing only hydrogen and carbon atoms
• C07D 235/10 - Radicals substituted by halogen atoms or nitro radicals
• C07D 235/24 - Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
• 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 401/10 - 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 carbon chain containing aromatic rings
• C07D 403/10 - 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 aromatic rings
• C07D 405/10 - 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 carbon chain containing aromatic rings
• C07D 409/10 - 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 carbon chain containing aromatic rings
• 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
• C07D 417/10 - 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 carbon chain containing aromatic rings
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol

Abstract

A novel combination comprising a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and a PD-1 antagonist; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf and/or immune modulation through PD-1 is beneficial, e.g., cancer.

IPC Classes  ?

• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• 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 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems

Abstract

Aspects of the present invention are directed to a nicotine lozenge for oral administration comprising: a nicotine active; at least one high viscosity, water soluble, synthetic or semi-synthetic, non-ionic polymer; and at least one low viscosity, water soluble, synthetic or semi-synthetic, non-ionic polymer. Lozenges of the present invention are more stable and less expensive than traditional lozenges.

IPC Classes  ?

• A61K 31/465 - Nicotine; Derivatives thereof
• A61K 9/20 - Pills, lozenges or tablets

Abstract

Aspects of the present invention are directed to a nicotine lozenge for oral administration comprising: a nicotine active; at least one high viscosity, water soluble, synthetic or semi-synthetic, non-ionic polymer; and at least one low viscosity, water soluble, synthetic or semi-synthetic, non-ionic polymer. Lozenges of the present invention are more stable and less expensive than traditional lozenges.

IPC Classes  ?

• A61K 31/465 - Nicotine; Derivatives thereof
• A61K 9/20 - Pills, lozenges or tablets

Abstract

A novel combination comprising the PI3K-β inhibitor 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of PI3K-β and/or B-Raf is beneficial, eg. cancer.

IPC Classes  ?

• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

Abstract

Provided herein are novel substituted thieno[3,2-d]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Abstract

The present invention relates to genetically modified host cells, in particular yeast cells, comprising at least one isolated polynucleotide encoding a Killer Expression protease (Kex2p) or a fragment and/or variant thereof which has at least one Kex2p functional activity and at least one isolated polynucleotide encoding a Protein Disulfide- Isomerase (Pdil) or a fragment and/or variant thereof which has at least one Pdi functional activity. Also provided herein are genetically modified host cells comprising at least one isolated polynucleotide encoding a Killer Expression protease (Kex2p) or a fragment and/or variant thereof which has at least one Kex2p functional activity, at least one isolated polynucleotide encoding a Protein Disulfide -Isomerase (Pdil) or a fragment and/or variant thereof which has at least one Pdil functional activity and at least one isolated polynucleotide encoding a Endoplasmic Reticulum Oxidoreductin (Erol) or a fragment and/or variant thereof which has at least one Erol functional activity.

IPC Classes  ?

• C07K 14/395 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from fungi from yeasts from Saccharomyces

Abstract

This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. Epigenetic modifications play an important role in the regulation of many cellular processes including cell proliferation, differentiation, and cell survival. Global epigenetic modifications are common in cancer, and include global changes in DNA and/or histone methylation, dysregulation of non-coding RNAs and nucleosome remodeling leading to aberrant activation or inactivation of oncogenes, tumor suppressors and signaling pathways.

IPC Classes  ?

• C07D 213/56 - Amides

Abstract

The present invention relates to a method of treating cancer and pre-cancerous syndromes in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering: (i) an EZH2 inhibitor selected from: N-[4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-[(1 S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide, or a pharmaceutically acceptable salt thereof; 1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pryidinyl)methyl]-6-[2- (4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide, or a pharmaceutically acceptable salt thereof; and N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetahydro-2H-pyran-4-yl)amino)-4-mehtyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide, or a pharmaceutically acceptable salt thereof; and (ii) a Bcl-2 inhibitor, to a human in need thereof.

IPC Classes  ?

• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene

Abstract

The present Invention relates to long acting pharmaceutical compositions of betulin defivatives or pharmaceutically acceptabnle salts thereof, useful in the treatment or prevention of Human Immunodeficiency Virus (HIV) infections.

IPC Classes  ?

• A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
• A61P 31/18 - Antivirals for RNA viruses for HIV
• C07C 69/74 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms

Abstract

Disclosed are compounds of Formula I, Formula II, and Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.

IPC Classes  ?

• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• C07D 233/54 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group 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 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

Abstract

The present invention relates to the administration of a multikinase inhibitor and its effect on patients with particular genetic variant cancers. More specifically, this present invention is directed to methods of administering foretinib or pharmaceutically acceptable salts or solvates thereof to patients with a ros1 variant cancer including non-small cell lung cancer.

IPC Classes  ?

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

Abstract

The present invention relates to a method of treating cancer and pre-cancerous syndromes in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5 - [[4- [(2,3 -dimethyl-2H-indazol-6-yl)methy lamino] -2-pyrimidinyl] amino]-2-methylbenze nesulfonamide, or a pharmaceutically acceptable salt thereof, and 3'-[(2Z)-[l-(3,4-dimethylphenyl)-l,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydra zino]-2'-hydroxy-[l,l'-biphenyl]-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to a human in need thereof.

IPC Classes  ?

• C07D 231/38 - Nitrogen atoms
• A61K 9/20 - Pills, lozenges or tablets
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are novel pharmaceutical formulations containing N-{3-[3-cyclopropyl-5- (2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H- pyrido[4,3-d]pyrimidin-1 -yl]phenyl}acetamide dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same.

IPC Classes  ?

• A61K 9/14 - Particulate form, e.g. powders
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Compounds of formula (I) and salts thereof wherein R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl, and m is an integer having a value of 1 to 4; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1 ), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit.

IPC Classes  ?

• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine

Abstract

Compounds of formula (I) and salts thereof: wherein R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl, and m is an integer having a value of 0 to 3; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

Compounds of formula (I) and salts thereof: wherein R1 is n-C4-6alkyl or C1-2alkoxyC1-2alkyl-; R2 is hydrogen or methyl; each R3 is hydroxy, halo or n-C1-3alkyl; m is an integer having a value of 2 to 4; n is an integer having a value of 0 to 3; and p is an integer having a value of 0 to 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

IPC Classes  ?

• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit.

IPC Classes  ?

• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1 ), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGA T-1 activity may have therapeutic benefit.

IPC Classes  ?

• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.

IPC Classes  ?

• C07D 498/04 - 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