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：US20220306617A1

公开(公告)日：2022-09-29

申请号：US17638106

申请日：2020-08-24

Applicant: NOVARTIS AG

Inventor： Claire ADCOCK ,  Jake AXFORD ,  Ying HOU ,  Hyungchul KIM ,  Yiping SHEN ,  Nichola SMITH ,  Catherine Fooks SOLOVAY ,  Moo Je SUNG ,  Megan LIGHTFOOT ,  Alessandro MAZZACANI ,  Emily STANLEY ,  Lewis WHITEHEAD

IPC: C07D413/10 ,  A61K31/422 ,  A61K45/06 ,  C07D413/14 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/675 ,  C07F9/6558 ,  A61P11/00

Abstract: The invention relates to heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification; capable of modulating the ctivity of TMEM16a. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including COPD, bronchiectasis, asthma, cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, cystic fibrosis, primary ciliary dyskinesia, respiratory tract infections (acute and chronic; viral and bacterial), lung carcinoma.

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.