公开(公告)号：US20190307753A1

公开(公告)日：2019-10-10

申请号：US16301935

申请日：2017-05-11

Applicant: Alan WHITEHEAD ,  Olga ORNOSKI ,  Subharekha RAGHAVAN ,  Raphaelle BERGER ,  Joie GARFUNKLE ,  Zhiqiang YANG ,  Gang JI ,  Falong JIANG ,  Jianmin FU ,  Merck Sharp & Dohme Corp.

Inventor： Alan Whitehead ,  Olga Ornoski ,  Subharekha Raghavan ,  Raphaelle Berger ,  Joie Garfunkle ,  Zhiqiang Yang ,  Gang JI ,  Falong Jiang ,  Jianmin Fu

IPC: A61K31/519 ,  C07D519/00 ,  A61P9/12

Abstract: The invention provides certain fused pyrazine compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, R1, R3, R4a, R5a, R5b, R6, and the subscript t are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases or disorders which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and disorders and for preparing pharmaceutical s for this purpose.

公开(公告)号：US10780092B2

公开(公告)日：2020-09-22

申请号：US16301935

申请日：2017-05-11

Applicant: Merck Sharp & Dohme Corp. ,  Alan Whitehead ,  Olga Ornoski ,  Subharekha Raghavan ,  Raphaelle Berger ,  Joie Garfunkle ,  Zhiqiang Yang ,  Gang Ji ,  Falong Jiang ,  Jianmin Fu

Inventor： Alan Whitehead ,  Olga Ornoski ,  Subharekha Raghavan ,  Raphaelle Berger ,  Joie Garfunkle ,  Zhiqiang Yang ,  Gang Ji ,  Falong Jiang ,  Jianmin Fu

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61P9/12

Abstract: The invention provides certain fused pyrazine compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, R1, R3, R4a, R5a, R5b, R6, and the subscript t are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases or disorders which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and disorders and for preparing pharmaceuticals for this purpose.

公开(公告)号：US20170174693A1

公开(公告)日：2017-06-22

申请号：US15384429

申请日：2016-12-20

Applicant: Raphaelle Berger ,  Yi-Heng Chen ,  Guoqing Li ,  Joie Garfunkle ,  Hong-Dong Li ,  Shouwu Miao ,  Subharekha Raghavan ,  Cameron J. Smith ,  John Stelmach ,  Alan Whitehead ,  Rui Zhang ,  Yong Zhang ,  Jianmin Fu ,  Gang Ji ,  Falong Jiang

Inventor： Raphaelle Berger ,  Yi-Heng Chen ,  Guoqing Li ,  Joie Garfunkle ,  Hong-Dong Li ,  Shouwu Miao ,  Subharekha Raghavan ,  Cameron J. Smith ,  John Stelmach ,  Alan Whitehead ,  Rui Zhang ,  Yong Zhang ,  Jianmin Fu ,  Gang Ji ,  Falong Jiang

IPC: C07D487/04 ,  A61K31/519 ,  C07D519/00 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  C07D519/00

Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.