公开(公告)号：US20160176864A1

公开(公告)日：2016-06-23

申请号：US14580355

申请日：2014-12-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Derek J. Norris ,  George V. Delucca ,  Ashvinikumar V. Gavai ,  Claude A. Quesnelle ,  Patrice Gill ,  Daniel O'Malley ,  Wayne Vaccaro ,  Francis Y. Lee ,  Mikkel V. DeBenedetto ,  Andrew P. Degnan ,  Haiquan Fang ,  Matthew D. Hill ,  Hong Huang ,  William D. Schmitz ,  John E. Starrett, JR. ,  Wen-Ching Han ,  John S. Tokarski ,  Sunil Kumar Mandal

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US20160060232A1

公开(公告)日：2016-03-03

申请号：US14938284

申请日：2015-11-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D243/24

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.

公开(公告)号：US09273014B2

公开(公告)日：2016-03-01

申请号：US14627573

申请日：2015-02-20

Applicant: Bristol-Myers Squibb Company

Inventor： Ashvinikumar V. Gavai ,  George V. DeLucca ,  Daniel O'Malley ,  Patrice Gill ,  Claude A. Quesnelle ,  Brian E. Fink ,  Yufen Zhao ,  Francis Y. Lee

IPC: A61K38/00 ,  A61K47/00 ,  C07D243/24 ,  A61K31/5513 ,  A61K31/573 ,  A61K31/675 ,  A61K38/05 ,  A61K45/06 ,  C07D401/04 ,  C07F9/645 ,  C07K5/062 ,  C07D243/18 ,  C07D243/26 ,  C07F9/12 ,  A61K9/00 ,  A61K9/08 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/555 ,  C07F7/18 ,  C07F9/38 ,  A61K9/48 ,  A61K47/48

CPC classification number: C07D243/24 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/08 ,  A61K9/4866 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/5513 ,  A61K31/555 ,  A61K31/573 ,  A61K31/675 ,  A61K45/06 ,  A61K47/64 ,  C07D243/18 ,  C07D243/26 ,  C07D401/04 ,  C07F7/1804 ,  C07F9/12 ,  C07F9/38 ,  C07F9/645 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; 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; or as prodrugs of such compounds.

公开(公告)号：US20140087992A1

公开(公告)日：2014-03-27

申请号：US14032333

申请日：2013-09-20

Applicant: Bristol-Myers Squibb Company

Inventor： Ashvinikumar V. Gavai ,  George V. DeLucca ,  Daniel O'Malley ,  Patrice Gill ,  Claude A. Quesnelle ,  Brian E. Fink ,  Yufen Zhao ,  Francis Y. Lee

IPC: C07D243/24 ,  A61K45/06 ,  A61K31/573 ,  C07K5/062 ,  A61K31/675 ,  C07D401/04 ,  A61K38/05 ,  A61K31/5513 ,  C07F9/645

CPC classification number: C07D243/24 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/08 ,  A61K9/4866 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/5513 ,  A61K31/555 ,  A61K31/573 ,  A61K31/675 ,  A61K45/06 ,  A61K47/64 ,  C07D243/18 ,  C07D243/26 ,  C07D401/04 ,  C07F7/1804 ,  C07F9/12 ,  C07F9/38 ,  C07F9/645 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; 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; or as prodrugs of such compounds.

Abstract translation: 公开了式（I）和/或其盐的化合物：其中R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CF3或-CH2CH2CH2CF3; R3是H，-CH3或Rx; R4是H或Ry; 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; 或作为这些化合物的前药。

公开(公告)号：US20160318928A1

公开(公告)日：2016-11-03

申请号：US15107652

申请日：2014-12-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Derek J. Norris ,  George V. Delucca ,  Ashvinikumar V. Gavai ,  Claude A. Quesnelle ,  Patrice Gill ,  Daniel O'Malley ,  Wayne Vaccaro ,  Francis Y. Lee ,  Mikkel V. DeBenedetto ,  Andrew P. Degnan ,  Haiquan Fang ,  Matthew D. Hill ,  Hong Huang ,  William D. Schmitz ,  John E. Starrett, JR. ,  Wen-Ching Han ,  John S. Tokarski ,  Sunil Kumar Mandal

IPC: C07D471/04 ,  A61K31/501 ,  A61K31/506 ,  A61K31/437 ,  A61K31/444

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506

Abstract: The present invention is directed to tricyclic compounds (I), pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

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：US20140256700A1

公开(公告)日：2014-09-11

申请号：US14190477

申请日：2014-02-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Michael A. Poss ,  David R. Tortolani ,  Dharmpal S. Dodd ,  Christopher P. Mussari ,  John S. Tokarski ,  Ashvinikumar V. Gavai ,  Yufen Zhao ,  George V. Delucca ,  Daniel O'Malley ,  Derek J. Norris ,  Patrice Gill ,  Claude A. Quesnelle ,  Wen-Ching Han

IPC: A61K31/553 ,  A61K31/5377 ,  C07D417/14 ,  C07D413/14 ,  A61K31/422 ,  A61K31/4192 ,  A61K31/496 ,  A61K31/427 ,  A61K31/5355 ,  A61K31/541 ,  C07D405/14 ,  C07D413/04 ,  A61K31/454

CPC classification number: A61K31/553 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Abstract translation: 本发明涉及咔唑化合物，包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。

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：US10683290B2

公开(公告)日：2020-06-16

申请号：US15573141

申请日：2016-05-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Claude A. Quesnelle ,  Lalgudi S. Harikrishnan ,  Matthew D. Hill

IPC: C07D471/04 ,  A61P35/02

Abstract: The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US20150218111A1

公开(公告)日：2015-08-06

申请号：US14429941

申请日：2013-09-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ashvinikumar V. Gavai ,  Weifang Shan ,  James Aaron Balog ,  Claude A. Quesnelle ,  Wen-Ching Han ,  George V. DeLucca ,  Daniel O'Malley ,  Brian E. Fink

IPC: C07D243/24 ,  C07D413/12 ,  A61K45/06 ,  C07D413/14 ,  C07D401/04 ,  C07D491/056 ,  A61K31/5513 ,  C07D401/12

CPC classification number: C07D243/24 ,  A61K31/5513 ,  A61K45/06 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D491/04 ,  C07D491/056

Abstract: Disclosed are compounds of Formula (I): wherein: R2 is phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, or pyridinyl; R3 is H, CH3, CH2(cyclopropyl), pyridinyl, chloropyridinyl, or methoxypyridinyl: and 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：R 2是苯基，氟苯基，氯苯基，三氟苯基，甲基异恶唑基或吡啶基; R 3是H，CH 3，CH 2（环丙基），吡啶基，氯吡啶基或甲氧基吡啶基：和R a，R b，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。