公开(公告)号：US20150232491A1

公开(公告)日：2015-08-20

申请号：US14429930

申请日：2013-09-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ashvinikumar V. Gavai ,  Wen-Ching Han ,  Brian E. Fink ,  Victor R. Guarino

IPC: C07F9/645 ,  A61K45/06 ,  A61K31/5513 ,  C07D401/12 ,  A61K31/675 ,  C07D243/24

CPC classification number: C07F9/645 ,  A61K31/5513 ,  A61K31/675 ,  A61K45/06 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  C07D401/12 ,  C07F9/12 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are prodrugs of compounds that are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

Abstract translation: 公开了式（I）的化合物及其盐，其中：a）R1是H或CH3，R2是Ry; 或b）R1是Rx，R2是H; 其中Rx和Ry在本文中公开。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物是可用于治疗，预防或减缓各种治疗领域（例如癌症）中的疾病或病症进展的化合物的前药。

公开(公告)号：US09273075B2

公开(公告)日：2016-03-01

申请号：US14429930

申请日：2013-09-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ashvinikumar V. Gavai ,  Wen-Ching Han ,  Brian E. Fink ,  Victor R. Guarino

IPC: C07D243/18 ,  C07D243/26 ,  C07F9/645 ,  A61K31/675 ,  C07D243/24 ,  A61K31/5513 ,  C07D401/12 ,  A61K45/06

CPC classification number: C07F9/645 ,  A61K31/5513 ,  A61K31/675 ,  A61K45/06 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  C07D401/12 ,  C07F9/12 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are prodrugs of compounds that are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

Abstract translation: 公开了式（I）的化合物及其盐，其中：a）R1是H或CH3，R2是Ry; 或b）R1是Rx，R2是H; 其中Rx和Ry在本文中公开。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物是可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症进展的化合物的前药。