公开(公告)号：US20240043428A1

公开(公告)日：2024-02-08

申请号：US18069646

申请日：2022-12-21

Applicant: Novartis AG ,  Astex Therapeutics Ltd.

Inventor： Gilbert BESONG ,  Christopher Thomas BRAIN ,  Clinton A. BROOKS ,  Miles Stuart CONGREVE ,  Claudio DAGOSTIN ,  Guo HE ,  Ying HOU ,  Steven HOWARD ,  Yue LI ,  Yipin LU ,  Paul MORTENSON ,  Troy SMITH ,  Moo Je SUNG ,  Steven WOODHEAD ,  Wojciech WRONA ,  Bharat LAGU

IPC: C07D487/04 ,  A61K31/519 ,  C07D487/08 ,  A61P35/00

CPC classification number: C07D487/04 ,  A61P35/00 ,  C07D487/08 ,  A61K31/519

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

公开(公告)号：US20210253578A1

公开(公告)日：2021-08-19

申请号：US17023041

申请日：2020-09-16

Applicant: Novartis AG ,  Astex Therapeutics Ltd.

Inventor： Gilbert BESONG ,  Christopher Thomas BRAIN ,  Clinton A. BROOKS ,  Miles Stuart CONGREVE ,  Claudio DAGOSTIN ,  Guo HE ,  Ying HOU ,  Steven HOWARD ,  Yue LI ,  Yipin LU ,  Paul MORTENSON ,  Troy SMITH ,  Moo Je SUNG ,  Steven WOODHEAD ,  Wojciech WRONA ,  Bharat LAGU

IPC: C07D487/04 ,  C07D487/08 ,  A61K31/519 ,  A61P35/00

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

公开(公告)号：US20250145600A1

公开(公告)日：2025-05-08

申请号：US18836800

申请日：2023-02-10

Applicant: Novartis AG

Inventor： Martin ALLAN ,  Matthew CARSON ,  Thomas CAYA ,  Tanzina FAZAL ,  Ming QIAN ,  Troy SMITH ,  Liansheng SU ,  Lihua YANG ,  Ping ZHANG

IPC: C07D413/14 ,  A61K31/454 ,  A61K31/4545 ,  A61K45/06 ,  C07D405/14 ,  C07D417/14

Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds, as well as methods and uses of these compounds in the treatment of diseases.

公开(公告)号：US20240182456A1

公开(公告)日：2024-06-06

申请号：US18554778

申请日：2022-04-11

Applicant: Novartis AG

Inventor： Martin ALLAN ,  Matthew CARSON ,  Thomas CAYA ,  Lara CZABANIUK ,  Ming QIAN ,  Daniel SMITH ,  Troy SMITH ,  Liansheng SU ,  Chung-Yeh WU ,  Lihua YANG ,  Chun ZHANG ,  Ping ZHANG ,  Xilin ZHOU

IPC: C07D405/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds of formula (I) as activators of glucagon-like peptide 1 (GLP1) receptor for the treatment of obesity, type 2 diabetes mellitus, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, one or more diabetic complications, diabetic nephropathy, dyslipidemia, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hypertension, atherosclerosis, peripheral arterial disease, stroke, cardiomyopathy, atrial fibrillation, heart failure, coronary heart disease and neuropathy. Preferred compounds are e.g. 2-((4-((S)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-imidazole derivatives and similar compounds, such as e.g. C-1, C-2, C-3, C-4 and other compounds.