公开(公告)号：US20190233426A1

公开(公告)日：2019-08-01

申请号：US16311575

申请日：2017-06-09

Applicant: Novartis AG

Inventor： Ho Man CHAN ,  Xingnian Fu ,  Xiang-Ju Justin Gu ,  Ying HUANG ,  Ling LI ,  Yuan MI ,  Wei QI ,  Martin SENDZIK ,  Yongfeng SUN ,  Long WANG ,  Zhengtian YU ,  Hailong ZHANG ,  Ji Yue ZHANG ,  Man ZHANG ,  Qiong ZHANG ,  Kehao ZHAO

IPC: C07D487/04 ,  A61P35/00

Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.

公开(公告)号：US20180170917A1

公开(公告)日：2018-06-21

申请号：US15510609

申请日：2015-09-11

Applicant: NOVARTIS AG

Inventor： Robert John AVERSA ,  Matthew T. BURGER ,  Michael Patrick DILLON ,  Thomas A. DINEEN, Jr. ,  Yan LOU ,  Gisele A. NISHIGUCHI ,  Savithri RAMURTHY ,  Alice C. RICO ,  Vivek RAUNIYAR ,  Martin SENDZIK ,  Sharadha SUBRAMANIAN ,  Lina Quattrocchio SETTI ,  Benjamin R. TAFT ,  Huw Rowland TANNER ,  Lifeng WAN

IPC: C07D405/14 ,  C07D405/12 ,  C07D305/06 ,  C07D413/14 ,  A61P35/00

CPC classification number: C07D405/14 ,  A61P35/00 ,  C07D305/06 ,  C07D405/12 ,  C07D413/14

Abstract: The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

公开(公告)号：US20240216378A1

公开(公告)日：2024-07-04

申请号：US18423776

申请日：2024-01-26

Applicant: NOVARTIS AG

Inventor： Ho Man CHAN ,  Xiang-Ju Justin GU ,  Ying HUANG ,  Ling LI ,  Yuan MI ,  Wei QI ,  Martin SENDZIK ,  Yongfeng SUN ,  Long WANG ,  Zhengtian YU ,  Hailong ZHANG ,  Ji Yue (Jeff) ZHANG ,  Man ZHANG ,  Qiong ZHANG ,  Kehao ZHAO

IPC: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D487/04

Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder:






wherein R1, R2, R3, R4, R5, and n are as defined herein.

公开(公告)号：US20200002330A1

公开(公告)日：2020-01-02

申请号：US16309076

申请日：2017-06-12

Applicant: NOVARTIS AG

Inventor： Zhuoliang CHEN ,  Jorge Garcia FORTANET ,  Rajesh KARKI ,  Matthew J. LAMARCHE ,  Dyuti MAJUMDAR ,  Lawrence Blas PEREZ ,  Martin SENDZIK ,  Troy Douglas SMITH ,  Fan YANG ,  Bing YU

IPC: C07D471/04 ,  C07D513/04 ,  C07D495/04 ,  C07D487/04 ,  C07D403/14 ,  C07D519/00 ,  C07D455/02 ,  C07D401/14

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, R1, R2 and R3 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20190202828A1

公开(公告)日：2019-07-04

申请号：US16311621

申请日：2017-06-06

Applicant: Novartis AG

Inventor： Ho Man CHAN ,  Xingnian Fu ,  Xiang-Ju Justin Gu ,  Ying HUANG ,  Ling LI ,  Yuan MI ,  Wei QI ,  Martin SENDZIK ,  Yongfeng SUN ,  Long WANG ,  Zhengtian YU ,  Hailong ZHANG ,  Ji Yue ZHANG ,  Man ZHANG ,  Qiong ZHANG ,  Kehao ZHAO

IPC: C07D471/04 ,  A61P35/00

Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R6, R7 and R8 are as defined herein.

公开(公告)号：US20180051015A1

公开(公告)日：2018-02-22

申请号：US15499824

申请日：2017-04-27

Applicant: NOVARTIS AG

Inventor： Thomas Raymond CAFERRO ,  Zhuoliang CHEN ,  Young Shin CHO ,  Abran Q. COSTALES ,  Julian Roy LEVELL ,  Gang LIU ,  James R. MANNING ,  Martin SENDZIK ,  Cynthia SHAFER ,  Michael David SHULTZ ,  James Clifford SUTTON ,  Yaping WANG ,  Qian ZHAO

IPC: C07D413/14 ,  C07D417/14 ,  C07D413/04 ,  A61K31/506 ,  A61K31/5377

CPC classification number: C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

公开(公告)号：US20250115572A1

公开(公告)日：2025-04-10

申请号：US18729949

申请日：2023-01-20

Applicant: Novartis AG

Inventor： Christopher M. ADAMS ,  Lara C. CZABANIUK ,  Stefanie FLOHR ,  François GESSIER ,  Michael Christoph HEDIGER ,  Konstanze HURTH ,  Nancy LABBE-GIGUERE ,  Fabio LIMA ,  Tajesh PATEL ,  Oliver SIMIC ,  Martin SENDZIK ,  Angela VITREY ,  Anna VULPETTI

IPC: C07D401/06 ,  A61K31/438 ,  A61K31/444 ,  C07D401/14 ,  C07D405/14

Abstract: Provided herein are compounds of formula (I) and pharmaceutical compositions thereof useful for treating diseases or disorders mediated by the complement factor B. (I).

公开(公告)号：US20240199609A1

公开(公告)日：2024-06-20

申请号：US18523565

申请日：2023-11-29

Applicant: NOVARTIS AG

Inventor： Zhuoliang CHEN ,  Jorge Garcia FORTANET ,  Rajesh KARKI ,  Matthew J. LAMARCHE ,  Dyuti MAJUMDAR ,  Lawrence Blas PEREZ ,  Martin SENDZIK ,  Troy Douglas SMITH ,  Fan YANG ,  Bing YU

IPC: C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D455/02 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D455/02 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I:






in which Y1, Y2, R1, R2 and R3 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20230033320A1

公开(公告)日：2023-02-02

申请号：US17505271

申请日：2021-10-19

Applicant: Novartis AG

Inventor： Ho Man CHAN ,  Xiang-Ju Justin GU ,  Ying HUANG ,  Ling LI ,  Yuan MI ,  Wei QI ,  Martin SENDZIK ,  Yongfeng SUN ,  Long WANG ,  Zhengtian YU ,  Hailong ZHANG ,  Ji Yue (Jeff) ZHANG ,  Man ZHANG ,  Qiong ZHANG ,  Kehao ZHAO

IPC: A61K31/519 ,  C07D487/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551

Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.

公开(公告)号：US20220315578A1

公开(公告)日：2022-10-06

申请号：US17020114

申请日：2020-09-14

Applicant: NOVARTIS AG

Inventor： Xin CHEN ,  Marie-Line GOUDE ,  Edmund Martin HARRINGTON ,  Gregory John HOLLINGWORTH ,  Julien LORBER ,  Martin SENDZIK ,  Anna VULPETTI ,  Thomas ZOLLER

IPC: C07D471/04 ,  C07D401/14

Abstract: The disclosure provides BRD9 bifunctional compounds of Formula (A), (BF-I), (BF-II), (BF-III), (BF-IIIa), (BF-IIIb), (BF-IV), (BF-IVa), (BF-IVb), (BF-I′), (BF-II′), (BF-III′), (BF-IV′), or (BF-V′), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, to their preparation, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases and disorders mediated by a bromodomain-containing protein, such as bromodomain-containing protein 9 (BRD9).