公开(公告)号：US20160022723A1

公开(公告)日：2016-01-28

申请号：US14782235

申请日：2014-04-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Francis Y. Lee

IPC: A61K31/7068 ,  A61K31/5513

CPC classification number: A61K31/7068 ,  A61K31/5513 ,  A61K31/706 ,  A61K31/7064 ,  A61K2300/00

Abstract: A method of treating a proliferative disease, such as cancer, is disclosed. The method comprises administering to a mammal in need thereof synergistically therapeutically effective amounts of: (i) (2R,3S)—N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-di-hydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide; (ii) 2-deoxy-2,2-difluorocytidine monohydrochloride (beta-isomer); and (iii) optionally, one or more additional anticancer agents.

Abstract translation: 公开了治疗增殖性疾病如癌症的方法。 该方法包括向有需要的哺乳动物施用协同治疗有效量的：（i）（2R，3S）-N - （（3S）-1-甲基-2-氧代-5-苯基-2,3-二 - 氢-3H-1,4-苯并二氮杂-3-基）-2,3-双（3,3,3-三氟丙基）琥珀酰胺; （ii）2-脱氧-2,2-二氟胞苷一盐酸盐（β-异构体）; 和（iii）任选的一种或多种另外的抗癌剂。

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：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：US20140135367A1

公开(公告)日：2014-05-15

申请号：US14162286

申请日：2014-01-23

Applicant: Bristol-Myers Squibb Company

Inventor： Charles F. Albright ,  Donna Marie Barten ,  Francis Y. Lee

IPC: A61K31/427

CPC classification number: A61K31/427

Abstract: Methods of treating Tau-associated diseases, preferably tauopathies, are described using epothilone D that exhibit good brain penetration, long half-life, and high selective retention in brain, and provides effective therapies in treating tauopathies including Alzheimer's disease.

Abstract translation: 使用表现出良好的脑渗透性，长半衰期和高选择性保留在脑中的埃坡霉素D来描述治疗Tau相关疾病，优选tau蛋白病的方法，并且提供治疗包括阿尔茨海默氏病在内的tau蛋白病的有效疗法。

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：US20130142805A1

公开(公告)日：2013-06-06

申请号：US13766900

申请日：2013-02-14

Applicant: Bristol-Myers Squibb Company

Inventor： Maria Jure-Kunkel ,  Francis Y. Lee

IPC: A61K39/395 ,  A61K33/24 ,  A61K31/555 ,  A61K31/7068

CPC classification number: A61K31/555 ,  A61K31/505 ,  A61K31/7068 ,  A61K33/24 ,  A61K39/39541 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00

Abstract: Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.

Abstract translation: 公开了可用于治疗和预防增殖性疾病的组合物和方法。