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：US20210300919A1

公开(公告)日：2021-09-30

申请号：US17130374

申请日：2020-12-22

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 ,  C07D401/14 ,  C07D519/00 ,  C07D455/02 ,  C07D403/14 ,  A61P35/00

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：US20180169063A1

公开(公告)日：2018-06-21

申请号：US15898561

申请日：2018-02-17

Applicant: NOVARTIS AG

Inventor： Heather Elizabeth BURKS ,  Michael A. DECHANTSREITER ,  Guo HE ,  Jill NUNEZ ,  Stefan PEUKERT ,  Clayton SPRINGER ,  Yingchuan SUN ,  Noel Marie-France THOMSEN ,  George Scott TRIA ,  Bing YU

IPC: A61K31/381 ,  A61K45/06 ,  C07D409/04 ,  A61K31/4436 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/4196 ,  C07D413/12 ,  C07D413/04 ,  C07D409/12 ,  C07D333/66 ,  C07D333/64 ,  A61K31/5377 ,  A61K31/404 ,  A61K31/41 ,  A61K31/428 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/4745 ,  C07D417/12 ,  C07D409/10 ,  A61K31/506

CPC classification number: A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. 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 aberrant estrogen receptor activity.

公开(公告)号：US20170112805A1

公开(公告)日：2017-04-27

申请号：US15399562

申请日：2017-01-05

Applicant: NOVARTIS AG

Inventor： Heather Elizabeth BURKS ,  Michael A. DECHANTSREITER ,  Guo HE ,  Jill NUNEZ ,  Stefan PEUKERT ,  Clayton SPRINGER ,  Yingchuan SUN ,  Noel Marie-France THOMSEN ,  George Scott TRIA ,  Bing YU

IPC: A61K31/381 ,  A61K31/4745 ,  A61K45/06 ,  A61K31/5377

CPC classification number: A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. 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 aberrant estrogen receptor activity.

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：US20230091510A1

公开(公告)日：2023-03-23

申请号：US17612280

申请日：2020-05-19

Applicant: Novartis AG

Inventor： Zhuoliang CHEN ,  Katsumasa NAKAJIMA ,  Matthew T. BURGER ,  Joseph Anthony D'ALESSIO ,  Eric MCNEILL ,  Mark G, PALMERO ,  Bing YU ,  Qiang ZHANG

IPC: A61K47/68 ,  A61K47/54 ,  A61K47/60 ,  A61K47/61 ,  A61P35/00 ,  C07K16/28 ,  C07K5/062

Abstract: Provided herein are linkers, linker-drug groups and anti-body-drug conjugates comprising hydrophilic groups.