公开(公告)号：US09187434B2

公开(公告)日：2015-11-17

申请号：US14429964

申请日：2013-09-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Patrice Gill ,  Claude A. Quesnelle ,  Mark G. Saulnier ,  Ashvinikumar V. Gavai

IPC: C07D401/04 ,  C07D243/24 ,  C07D243/14 ,  A61K31/5513 ,  A61K45/06

CPC classification number: C07D243/14 ,  A61K31/5513 ,  A61K45/06 ,  C07D243/24 ,  C07D401/04

Abstract: Disclosed are compounds of Formula (I): wherein: R1 is CH2CH2CF3; R2 is CH2CH2CF3, CH2(cyclopropyl), or phenyl; 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：其中：R1是CH2CH2CF3; R 2是CH 2 CH 2 CF 3，CH 2（环丙基）或苯基; R3是H或CH3; 环A是苯基或吡啶基; 并且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）中疾病或病症的发展。

公开(公告)号：US20150274679A1

公开(公告)日：2015-10-01

申请号：US14429964

申请日：2013-09-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Patrice Gill ,  Claude A. Quesnelle ,  Mark G. Saulnier ,  Ashvinikumar V. Gavai

IPC: C07D243/14 ,  C07D401/04 ,  A61K45/06 ,  A61K31/5513

CPC classification number: C07D243/14 ,  A61K31/5513 ,  A61K45/06 ,  C07D243/24 ,  C07D401/04

Abstract: Disclosed are compounds of Formula (I): wherein: R1 is CH2CH2CF3; R2 is CH2CH2CF3, CH2(cyclopropyl), or phenyl; 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：其中：R1是CH2CH2CF3; R 2是CH 2 CH 2 CF 3，CH 2（环丙基）或苯基; R3是H或CH3; 环A是苯基或吡啶基; 并且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）中疾病或病症的发展。

公开(公告)号：US20190185450A1

公开(公告)日：2019-06-20

申请号：US16315800

申请日：2017-07-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Kap-Sun YEUNG ,  Katharine A. Grant-Young ,  Juliang Zhu ,  Mark G. Saulnier ,  David B. Frennesson ,  Zhaoxing Meng ,  Paul Michael Scola

IPC: C07D401/10 ,  C07D413/14 ,  C07D417/14 ,  C07D417/12 ,  C07D405/14 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/4439 ,  A61K31/498

Abstract: The present disclosure generally relates to compounds of formula (I), wherein R2 is a phenyl or pyridinyl moiety, useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

公开(公告)号：US10144706B2

公开(公告)日：2018-12-04

申请号：US15689115

申请日：2017-08-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Kap-Sun Yeung ,  Katharine A. Grant-Young ,  Juliang Zhu ,  Mark G. Saulnier ,  David B. Frennesson ,  David R. Langley ,  Piyasena Hewawasam ,  Tao Wang ,  Zhongxing Zhang ,  Zhaoxing Meng ,  Li-Qiang Sun ,  Eric Mull ,  Paul Michael Scola

IPC: C07D207/12 ,  C07D217/18 ,  C07D237/06 ,  C07D205/04 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/66 ,  C07D211/90 ,  C07D213/38 ,  C07D213/73 ,  C07D213/79 ,  C07D213/85 ,  C07D231/12 ,  C07D239/26 ,  C07D277/28 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/06 ,  C07D417/12 ,  C07D211/46 ,  C07D211/58 ,  C07D211/60 ,  C07D213/42 ,  C07D213/55 ,  C07C237/04 ,  C07C235/08 ,  C07C229/14 ,  C07C217/58 ,  C07C217/28 ,  C07C217/18 ,  C07C237/06 ,  C07C255/24 ,  C07C255/25

Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

公开(公告)号：US20180221342A1

公开(公告)日：2018-08-09

申请号：US15749557

申请日：2016-07-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David B. Frennesson ,  Piyasena Hewawasam ,  Omar D. Lopez ,  Van N. Nguyen ,  Mark G. Saulnier ,  Yong Tu ,  Alan Xiangdong Wang ,  Gan Wang ,  Ningning Xu ,  Roshan Yadavrao Nimje ,  Hasibur Rahaman ,  Samayamunthula Venkata Satya Arun Kumar Gupta ,  Nicholas A. Meanwell ,  Makonen Belema

IPC: A61K31/4178 ,  A61P31/14

CPC classification number: A61K31/4178 ,  A61K31/417 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/7056 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00 ,  A61P31/14

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

公开(公告)号：US20180057455A1

公开(公告)日：2018-03-01

申请号：US15689115

申请日：2017-08-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： KAP-SUN YEUNG ,  Katharine A. Grant-Young ,  Juliang Zhu ,  Mark G. Saulnier ,  David B. Frennesson ,  David R. Langley ,  Piyasena Hewawasam ,  Tao Wang ,  Zhongxing Zhang ,  Zhaoxing Meng ,  Li-Qiang Sun ,  Eric Mull ,  Paul Michael Scola

IPC: C07D207/12 ,  C07D211/66 ,  C07D207/16 ,  C07D403/12 ,  C07D401/12 ,  C07D207/14 ,  C07D211/22 ,  C07D213/38 ,  C07D401/14 ,  C07C237/06 ,  C07D295/088 ,  C07D205/04 ,  C07D213/85 ,  C07C217/18 ,  C07D213/73 ,  C07D405/12 ,  C07C255/24 ,  C07D413/14 ,  C07D405/14 ,  C07D213/79 ,  C07D231/12 ,  C07D239/26 ,  C07D277/28 ,  C07D211/90

CPC classification number: C07D207/12 ,  C07C217/18 ,  C07C217/28 ,  C07C217/58 ,  C07C229/14 ,  C07C235/08 ,  C07C237/04 ,  C07C237/06 ,  C07C255/24 ,  C07C255/25 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D205/04 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/60 ,  C07D211/66 ,  C07D211/90 ,  C07D213/38 ,  C07D213/42 ,  C07D213/55 ,  C07D213/73 ,  C07D213/79 ,  C07D213/85 ,  C07D231/12 ,  C07D239/26 ,  C07D277/28 ,  C07D295/088 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12

Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

公开(公告)号：US10590105B2

公开(公告)日：2020-03-17

申请号：US16315800

申请日：2017-07-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Kap-Sun Yeung ,  Katharine A. Grant-Young ,  Juliang Zhu ,  Mark G. Saulnier ,  David B. Frennesson ,  Zhaoxing Meng ,  Paul Michael Scola

IPC: C07D401/10 ,  C07D413/14 ,  C07D417/12 ,  C07D405/12 ,  C07D401/14 ,  C07D413/12 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/498 ,  A61K45/06 ,  C07D405/14 ,  C07D417/14

Abstract: The present disclosure generally relates to compounds of formula (I), wherein R2 is a phenyl or pyridinyl moiety, useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

公开(公告)号：US09775831B2

公开(公告)日：2017-10-03

申请号：US14904852

申请日：2014-07-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Mark G. Saulnier ,  David B. Frennesson ,  Makonen Belema

IPC: A61K31/415 ,  A61K31/4178 ,  A61K38/21 ,  A61K45/06 ,  A61K31/422 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/7056 ,  C07D401/14 ,  C07D405/14 ,  C07D317/32 ,  C07D233/64 ,  C07D403/14 ,  C07D487/04 ,  A61K31/4545

CPC classification number: A61K31/4178 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/21 ,  A61K45/06 ,  C07D233/64 ,  C07D317/32 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  A61K2300/00

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

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：US20160166545A1

公开(公告)日：2016-06-16

申请号：US14904852

申请日：2014-07-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Mark G. Saulnier ,  David B. Frennesson ,  Makonen Belema

IPC: A61K31/4178 ,  A61K31/496 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/4545

CPC classification number: A61K31/4178 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/21 ,  A61K45/06 ,  C07D233/64 ,  C07D317/32 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  A61K2300/00

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

Abstract translation: 本公开通常涉及抗病毒化合物，更具体地涉及可以抑制丙型肝炎病毒（HCV）编码的NS5A蛋白的功能的化合物的组合，包含这些组合的组合物，以及用于抑制NS5A的功能的方法 蛋白。