公开(公告)号：US20150080440A1

公开(公告)日：2015-03-19

申请号：US14553081

申请日：2014-11-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Soong-Hoon Kim ,  Robert M. Borzilleri ,  Gregory D. Vite ,  James A. Johnson

IPC: C07D491/044 ,  C07D417/06

CPC classification number: C07D491/044 ,  C07D417/06 ,  C07D491/04 ,  C07D493/04

Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract translation: 本发明涉及下列化合物，其中变量G，W，Q，X，Y，B1，B2，Z1，Z2和R1-R7如本文所定义，衍生物及其中间体的制备方法 。

公开(公告)号：US20140357605A1

公开(公告)日：2014-12-04

申请号：US14444682

申请日：2014-07-28

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ashvinikumar V. Gavai ,  Claude A. Quesnelle ,  Soong-Hoon Kim

IPC: C07D243/24 ,  A61K31/506 ,  A61K31/282 ,  A61K31/138 ,  A61K31/573 ,  A61K31/5513 ,  A61K31/337

CPC classification number: C07D243/24 ,  A61K31/138 ,  A61K31/282 ,  A61K31/337 ,  A61K31/506 ,  A61K31/5513 ,  A61K31/555 ,  A61K31/573 ,  A61K45/06 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds 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）的化合物或其前药; 其中：R1是-CH2CF3或-CH2CH2CF3; R2是-CH2CF3，-CH2CH2CF3或-CH2CH2CH2CF3; R3是H或-CH3; 每个R a独立地是F，Cl，-CN，-OCH 3和/或-NHCH 2 CH 2 OCH 3; 并且z为零，1或2.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）中疾病或病症的发展。

公开(公告)号：US20140100365A1

公开(公告)日：2014-04-10

申请号：US14100896

申请日：2013-12-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ashvinikumar V. Gavai ,  Claude A. Quesnelle ,  Soong-Hoon Kim ,  Francis Y. Lee

IPC: C07D243/24

CPC classification number: C07D243/24 ,  A61K31/138 ,  A61K31/337 ,  A61K31/5513 ,  A61K31/555 ,  A61K31/573 ,  A61K45/06 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds 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）的化合物或其前药; 其中：R1是-CH2CF3或-CH2CH2CF3; R2是-CH2CF3，-CH2CH2CF3或-CH2CH2CH2CF3; R3是H或-CH3; 每个R a独立地为F，Cl，-CN，-OCH 3和/或-NHCH 2 CH 2 OCH 3; 并且z为零，1或2.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）中疾病或病症的发展。

公开(公告)号：US08680090B2

公开(公告)日：2014-03-25

申请号：US13936311

申请日：2013-07-08

Applicant: Bristol-Myers Squibb Company

Inventor： James A. Johnson ,  Ji Jiang ,  Soong-Hoon Kim ,  Zulan Pi ,  Jennifer X. Qiao ,  George O. Tora ,  Tammy C. Wang ,  Heather Finlay

IPC: A61K31/397 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/506 ,  A61K31/4436 ,  A61K31/4535 ,  A61K31/4245 ,  A61K31/433 ,  C07D417/14 ,  C07D413/14 ,  C07D401/14 ,  C07D285/12 ,  C07D271/10

CPC classification number: C07D417/06 ,  C07D417/14

Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.

Abstract translation: 本发明提供式（I）化合物：如说明书中所定义和包含任何这些新化合物的组合物。 这些化合物是可用作药物的内皮脂肪酶抑制剂。

公开(公告)号：US20190263791A1

公开(公告)日：2019-08-29

申请号：US16411221

申请日：2019-05-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James A. Johnson ,  Soong-Hoon Kim ,  R. Michael Lawrence ,  Michael C. Myers ,  Hannguang J. Chao ,  Monique Phillips ,  Ji Jiang

IPC: C07D413/04 ,  C07D417/14 ,  C07D498/04 ,  C07D413/14 ,  C07D401/04

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

公开(公告)号：US09427442B2

公开(公告)日：2016-08-30

申请号：US14429958

申请日：2013-09-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yufen Zhao ,  Ashvinikumar V. Gavai ,  Patrice Gill ,  Soong-Hoon Kim ,  Brian E. Fink ,  Libing Chen ,  Mark G. Saulnier ,  Wen-Ching Han

IPC: C07D243/24 ,  A61K31/5513 ,  A61K45/06

CPC classification number: A61K31/5513 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/555 ,  A61K45/06 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is —CH2CH2CF3; R2 is —CH2CH2CH2F, —CH2CF2CH3, —CH2CH2CF3, —CH2CH(CH3)CF3, —CH2CH2CF2CH3, (Formulae (II), (III), (IV), (V) or (VI): R3 is H or —CH3; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds 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：（式（I））其中：R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CH2F，-CH2CF2CH3，-CH2CH2CF3，-CH2CH（CH3）CF3，-CH2CH2CF2CH3，（式（Ⅱ），（Ⅲ），（Ⅳ），（Ⅴ）或（Ⅵ）：R3是H或-CH3; 环A是苯基或吡啶基; Rx，Ry，Ra，Rb，y和z在本文中定义。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）中的疾病或病症的发展。

公开(公告)号：US20150231152A1

公开(公告)日：2015-08-20

申请号：US14429958

申请日：2013-09-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yufen Zhao ,  Ashvinikumar V. Gavai ,  Patrice Gill ,  Soong-Hoon Kim ,  Brian E. Fink ,  Libing Chen ,  Mark G. Saulnier ,  Wen-Ching Han

IPC: A61K31/5513 ,  A61K45/06 ,  C07D243/24

CPC classification number: A61K31/5513 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/555 ,  A61K45/06 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is —CH2CH2CF3; R2 is —CH2CH2CH2F, —CH2CF2CH3, —CH2CH2CF3, —CH2CH(CH3)CF3, —CH2CH2CF2CH3, (Formulae (II), (III), (IV), (V) or (VI): R3 is H or —CH3; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds 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：（式（I））其中：R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CH2F，-CH2CF2CH3，-CH2CH2CF3，-CH2CH（CH3）CF3，-CH2CH2CF2CH3，（式（Ⅱ），（Ⅲ），（Ⅳ），（Ⅴ）或（Ⅵ）：R3是H或-CH3; 环A是苯基或吡啶基; Rx，Ry，Ra，Rb，y和z在本文中定义。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）中的疾病或病症的发展。

公开(公告)号：US08822454B2

公开(公告)日：2014-09-02

申请号：US14100896

申请日：2013-12-09

Applicant: Bristol-Myers Squibb Company

Inventor： Ashvinikumar V. Gavai ,  Claude A. Quesnelle ,  Soong-Hoon Kim

IPC: C07D243/24 ,  A61K31/5513 ,  A61K31/337 ,  A61K31/138 ,  A61K45/06 ,  A61K31/555 ,  A61K31/573

CPC classification number: C07D243/24 ,  A61K31/138 ,  A61K31/337 ,  A61K31/5513 ,  A61K31/555 ,  A61K31/573 ,  A61K45/06 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds 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）的化合物或其前药; 其中：R1是-CH2CF3或-CH2CH2CF3; R2是-CH2CF3，-CH2CH2CF3或-CH2CH2CH2CF3; R3是H或-CH3; 每个R a独立地是F，Cl，-CN，-OCH 3和/或-NHCH 2 CH 2 OCH 3; 并且z为零，1或2.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）中疾病或病症的发展。

公开(公告)号：US20140179674A1

公开(公告)日：2014-06-26

申请号：US14191861

申请日：2014-02-27

Applicant: Bristol-Myers Squibb Company

Inventor： Brian E. Fink ,  Libing Chen ,  Ashvinikumar V. Gavai ,  Liqi He ,  Soong-Hoon Kim ,  Andrew James Nation ,  Yufen Zhao ,  Litai H. Zhang

IPC: C07D487/04 ,  C07D498/04

CPC classification number: C07D487/04 ,  C07D498/04

Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 式（I）咪唑并哒嗪抑制蛋白激酶活性，从而使其成为抗癌剂。

公开(公告)号：US20140011799A1

公开(公告)日：2014-01-09

申请号：US13936311

申请日：2013-07-08

Applicant: Bristol-Myers Squibb Company

Inventor： James A. Johnson ,  Ji Jiang ,  Soong-Hoon Kim ,  Zulan Pi ,  Jennifer X. Qiao ,  George O. Tora ,  Tammy C. Wang ,  Heather Finlay

IPC: C07D417/06 ,  C07D417/14

CPC classification number: C07D417/06 ,  C07D417/14

Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.

Abstract translation: 本发明提供式（I）化合物：如说明书中所定义和包含任何这些新化合物的组合物。 这些化合物是可用作药物的内皮脂肪酶抑制剂。