Abstract

A novel quinazoline compound having SOS1 inhibitory activity and uses of the quinazoline compound are disclosed. More particularly, the present invention relates to a novel quinazoline derivative compound having inhibitory activity on SOS1 binding to RAS family proteins and/or RAC1, to pharmacologically acceptable salts thereof, and to pharmaceutical compositions containing the quinazoline compound. The novel quinazoline compound has the following chemical formula 1: A novel quinazoline compound having SOS1 inhibitory activity and uses of the quinazoline compound are disclosed. More particularly, the present invention relates to a novel quinazoline derivative compound having inhibitory activity on SOS1 binding to RAS family proteins and/or RAC1, to pharmacologically acceptable salts thereof, and to pharmaceutical compositions containing the quinazoline compound. The novel quinazoline compound has the following chemical formula 1: wherein all the variables have meaning as defined in the specification.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/06 - 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 only aliphatic carbon atoms
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Abstract

Disclosed are novel dioxoisoquinolinone derivative compounds, pharmaceutically acceptable salts thereof, optical isomers, hydrates, and solvates thereof as well as uses thereof. More specifically, the novel dioxoisoquinolinone derivative compounds, pharmaceutically acceptable salts, optical isomers, hydrates, solvates show inhibition activity of EZH1 (Enhancer of zeste homolog 1) and/or EZH2 (Enhancer of zeste homolog 2) activity. Pharmaceutical compositions containing the compound is also disclosed.

IPC Classes  ?

• C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a novel quinazoline derivative compound that serves as an SOS1 inhibitor, and a use thereof, and more specifically to: a novel quinazoline derivative compound having inhibitory activity against SOS1 binding to RAS family proteins and/or RAC1; a pharmacologically acceptable salt thereof; or a pharmaceutical composition containing the compound.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• 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 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

The present invention relates to a novel quinazoline derivative compound that serves as an SOS1 inhibitor, and a use thereof, and more specifically to: a novel quinazoline derivative compound having inhibitory activity against SOS1 binding to RAS family proteins and/or RAC1; a pharmacologically acceptable salt thereof; or a pharmaceutical composition containing the compound.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents
• 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 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

A novel heterotricyclic compounds of Formula 1 or pharmaceutically acceptable salts thereof, and uses thereof are disclosed. The novel heterotricyclic compounds exhibit an inhibitory activity against EZH1 (enhancer of zeste homolog 1) and/or EZH2 (enhancer of zeste homolog 2) activity. Pharmaceutical compositions containing these compounds as active ingredient is also disclosed. The heterotricyclic compound, pharmaceutically acceptable salts thereof, or compositions containing the compound or salt are useful in treating tumor or cancer in a subject. A novel heterotricyclic compounds of Formula 1 or pharmaceutically acceptable salts thereof, and uses thereof are disclosed. The novel heterotricyclic compounds exhibit an inhibitory activity against EZH1 (enhancer of zeste homolog 1) and/or EZH2 (enhancer of zeste homolog 2) activity. Pharmaceutical compositions containing these compounds as active ingredient is also disclosed. The heterotricyclic compound, pharmaceutically acceptable salts thereof, or compositions containing the compound or salt are useful in treating tumor or cancer in a subject.

IPC Classes  ?

• C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Abstract

This patent document relates to the crystalline forms of a quinazoline compound and the hydrochloride salts thereof. More particularly, this patent document relates to a preparation method of the crystalline forms of 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one and its hydrochloride salts.

IPC Classes  ?

• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 33/243 - PlatinumCompounds thereof
• A61K 31/282 - Platinum compounds
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/52 - Purines, e.g. adenine
• A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
• A61K 31/7068 - 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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61K 31/7072 - 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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
• A61K 31/7076 - 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 containing purines, e.g. adenosine, adenylic acid
• A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• 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 relates to novel dioxoisoquinolinone derivative compounds and use thereof. More specifically, the present invention relates to novel dioxoisoquinolinone derivative compounds with inhibition activity of EZH1(Enhancer of zeste homolog 1) and/or EZH2(Enhancer of zeste homolog 2) activity, a pharmaceutically acceptable salt thereof, and/or pharmaceutical compositions comprising the same.

IPC Classes  ?

• C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Abstract

The present invention relates to novel dioxoisoquinolinone derivative compounds and use thereof. More specifically, the present invention relates to novel dioxoisoquinolinone derivative compounds with inhibition activity of EZH1(Enhancer of zeste homolog 1) and/or EZH2(Enhancer of zeste homolog 2) activity, a pharmaceutically acceptable salt thereof, and/or pharmaceutical compositions comprising the same.

IPC Classes  ?

• C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
• A61K 31/4738 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are combinations of poziotinib and an anti-HER1, anti-HER2 or anti-HER4 antibody, optionally with other agents, and use of the combinations for treating cancer.

IPC Classes  ?

• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 33/243 - PlatinumCompounds thereof
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• A61K 31/537 - 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 spiro-condensed or forming part of bridged ring systems
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 35/00 - Antineoplastic agents

Abstract

ABSTRACT The present disclosure relates to novel heterotricyclic derivative compounds represented by Formula 1 H R" X dahh, 0 cR2 1111 R3 R5 0 R4 [Formula 11 and the use thereof, and more particularly, to novel heterotricyclic derivative compounds having inhibitory activity against EZH1 (enhancer of zeste homolog 1) and/or EZH2 (enhancer of zeste homolog 2) activity, pharmaceutically acceptable salts thereof, or pharmaceutical compositions containing these compounds. The heterotricyclic derivative compounds have anticancer activity against cancer associated with the activity of EZH1, EZH2 or both EZH1 and EZH2, and may be effectively used as a therapeutic agent against the cancer. 1 Date recue/Date received 2023-05-08

IPC Classes  ?

• C07D 491/04 - Ortho-condensed systems
• A61K 31/4743 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having sulfur as a ring hetero atom
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a novel heterocyclic derivative compound and a use of same, and more specifically, to a novel heterotricyclic derivative compound having inhibitory activity on enhancer of zeste homolog 1 (EZH1) and/or enhancer of zeste homolog 2 (EZH2), a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising said compound.

IPC Classes  ?

• C07D 491/04 - Ortho-condensed systems
• A61K 31/4743 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having sulfur as a ring hetero atom
• A61P 35/00 - Antineoplastic agents

Abstract

This patent documentrelates to the crystalline forms of a quinazoline compound and the hydrochloride salts thereof. More particularly, this patent document relates to a preparation method of the crystalline forms of 1-(4-(4-(3,4-dichloro-2-fluorophenylamino) -7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one and its hydrochloride salts.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

Abstract

This patent documentrelates to the crystalline forms of a quinazoline compound and the hydrochloride salts thereof. More particularly, this patent document relates to a preparation method of the crystalline forms of 1-(4-(4-(3,4-dichloro-2-fluorophenylamino) -7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one and its hydrochloride salts.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

Abstract

Provided are combinations of poziotinib and an anti-HER1, anti-HER2 or anti-HER4 antibody, optionally with other agents, and use of the combinations for treating cancer.

IPC Classes  ?

• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

Abstract

Provided are combinations of poziotinib and an anti-HER1, anti-HER2 or anti-HER4 antibody, optionally with other agents, and use of the combinations for treating cancer.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to an imidazopyridazine compound having cell growth inhibitory activity, and a pharmaceutical composition for preventing or treating cancer or a tumor including the same. The imidazopyridazine compound of Chemical Formula 1 according to the present invention has excellent cell growth inhibitory activity, and thus can be favorably used as a preventive or therapeutic agent for cancer or a tumor.

IPC Classes  ?

• C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings

Abstract

The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-β, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 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
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• C07D 495/04 - Ortho-condensed systems
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61P 19/04 - Drugs for skeletal disorders for non-specific disorders of the connective tissue
• A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to an imidazopyridazine compound having cell growth inhibitory activity and a pharmaceutical composition comprising the imidazopyridazine compound for preventing or treating cancer or a tumor. The imidazopyridazine compound of chemical formula 1 according to the present invention has excellent cell growth inhibitory activity, and thus can be favorably used as a preventive or therapeutic agent for cancer or a tumor.

IPC Classes  ?

• C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

The present invention relates to an imidazopyridazine compound having cell growth inhibitory activity and a pharmaceutical composition comprising the imidazopyridazine compound for preventing or treating cancer or a tumor. The imidazopyridazine compound of chemical formula 1 according to the present invention has excellent cell growth inhibitory activity, and thus can be favorably used as a preventive or therapeutic agent for cancer or a tumor.

IPC Classes  ?

• C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

The present invention relates to a novel heterocyclic derivative compound and a use thereof and, more particularly, to a novel heterocyclic derivative compound having selective inhibitory activity against a fibroblast growth factor receptor (FGFR), and a pharmaceutical composition comprising the same for preventing or treating various diseases associated with the FGFR.

IPC Classes  ?

• C07D 487/14 - Ortho-condensed systems
• C07D 471/14 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

The present invention relates to a novel substituted pyrazole derivative, having the effect of inhibiting the serine/threonine kinase activity, targeting the receptor ALK5 of TGF-β. A pharmaceutical composition containing a compound of the present invention as an active ingredient can be usefully used in the treatment and/or prevention of cancer, an autoimmune disease, a fibrotic disease, an inflammatory disease, a neurodegenerative disease, an infectious disease, a pulmonary disease, a cardiovascular disease or a metabolic disease or other diseases associated with a decrease in TGF family signaling activity.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 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 233/58 - 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 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 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 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
• A61K 31/428 - Thiazoles condensed with carbocyclic rings

Goods & Services

Orally delivered oncology drug.

Goods & Services

Orally delivered oncology drug.

Goods & Services

Orally delivered oncology drug.

Goods & Services

Orally delivered oncology drug.

Abstract

The present invention relates to a compound selected from the group consisting of a compound represented by chemical formula 1 for inhibiting the activity of diacylglycerol 0-acyltransferase type 1, and pharmaceutically acceptable salts thereof, and to a pharmaceutical composition including same as an active ingredient. The compound of the present invention may be used as an effective therapeutic agent for treating, without side effects, diseases such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, etc. induced by the activity of DGAT1. In chemical formula 1, A, B, X and R5-7 are the same as those defined in the present specification.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention relates to a composition for treating obesity-related diseases comprising an insulinotropic peptide conjugate, more particularly, to a composition for treating obesity-related diseases comprising a conjugate prepared by covalently linking the insulinotropic peptide with a carrier substance via a non-peptidyl linker, and a method for treating obesity-related diseases by using the same. In particular, the composition for treating obesity-related diseases according to the present invention remarkably improves the efficacy of suppressing food intake and its duration to reduce body weight and body fat, thereby being useful for the treatment of obesity-related diseases.

IPC Classes  ?

• A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Abstract

The present invention relates to an N-terminal amino acid-modified insulinotropic peptide having a high activity, and to a pharmaceutical composition comprising the same. The insulinotropic peptide derivatives according to the present invention exhibit therapeutic effects, which are not observed in native and other insulinotropic peptide analogs. Therefore, the insulinotropic peptide derivatives and the pharmaceutical composition comprising the same according to the present invention can be effectively provided for the treatment of the diseases.

IPC Classes  ?

• C07K 14/65 - Insulin-like growth factors, i.e. somatomedins, e.g. IGF-1, IGF-2

Abstract

The present invention relates to an Natriuretic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an Natriuretic peptide, a non-peptidyl polymer and a carrier substance, which are covalently linked to each other, and a use of the same. The Natriuretic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half-life, and thus it can be desirably employed in the development of long-acting formulations of various peptide drugs.

IPC Classes  ?

• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

Abstract

The present invention relates to an insulinotropic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an insulinotropic peptide, a non-peptide polymer and an immunoglobulin Fc region, which are covalently linked to each other, and a use of the same. The insulinotropic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half- life, and thus it can be desirably employed in the development of long acting formulations of various peptide drugs.

IPC Classes  ?

• A61K 38/28 - Insulins

Abstract

Disclosed herein is an inducible high-expression cassette comprising a dihydrofolate reductase (DHFR) promoter from which GC-rich repeat sequences are partially or entirely removed, the cassette capable of more effectively improving a gene amplification system. Also disclosed are an expression vector comprising the inducible expression cassette and optionally a gene encoding a recombinant protein of interest, an animal cell line transformed with the expression vector, and a method of mass producing and purifying a recombinant protein by culturing the transformant. The present invention enables the shortening of the time required to establish a cell line producing a recombinant protein of interest at high levels using a low concentration of a DHFR inhibitor, thereby allowing more effective production of the recombinant protein.

IPC Classes  ?

• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12N 15/79 - Vectors or expression systems specially adapted for eukaryotic hosts
• C12N 15/09 - Recombinant DNA-technology

Abstract

Disclosed is a method for the mass production of a monomeric or dimeric immunoglobulin Fc region, free of initial methionine residues, using a recombinant expression vector comprising a nucleotide sequence coding for a recombinant immunoglobulin Fc region comprising an immunoglobulin Fc region linked at the N-terminus thereof to an immunoglobulin Fc region via a peptide bond.

IPC Classes  ?

• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies

Abstract

Disclosed are an Fc fragment modified by a non-peptide polymer, a pharmaceutical composition comprising the Fc fragment modified by the non-peptide polymer as a carrier, a complex of the Fc fragment and a drug via a linker and a pharmaceutical composition comprising such a complex. The Fc fragment modified by a non-peptide peptide according to the present invention lacks immunogenicity and effector functions. Due to these properties, the Fc fragment maintains the in vivo activity of a drug conjugated thereto in high levels, remarkably increases the serum half-life of the drug, and remarkably reduces the risk of inducing immune responses.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies