公开(公告)号：US20130210787A1

公开(公告)日：2013-08-15

申请号：US13760726

申请日：2013-02-06

Applicant: Bristol-Myers Squibb Company

Inventor： Jacob Swidorski ,  Nicholas A. Meanwell ,  Alicia Regueiro-Ren ,  Sing-Yuen Sit ,  Jie Chen ,  Yan Chen

IPC: C07J53/00 ,  A61K45/06 ,  A61K31/58

CPC classification number: C07J53/002 ,  A61K31/58 ,  A61K45/06 ,  C07J63/008 ,  A61K2300/00

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.

Abstract translation: 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的C-3环烯基三萜类化合物作为HIV成熟抑制剂提供，如式I，II，III和IV化合物所示：其中X可以是C 4-8环烷基，C 4-8环烯基，C 4 -9螺环烷基，C4-9螺环烯基，C4-8氧杂环烷基，C4-8二氧杂环烷基，C6-8氧杂环烯基，C6-8二氧杂环烯基，C6-9氧杂螺环烷基或C6-9氧杂环烯烯基环。 这些化合物可用于治疗艾滋病毒和艾滋病。

公开(公告)号：US12172975B2

公开(公告)日：2024-12-24

申请号：US17274220

申请日：2019-09-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Junqing Guo ,  Jie Chen ,  Carolyn Diane Dzierba ,  Amy C. Hart ,  Guanglin Luo ,  John E. Macor ,  William J. Pitts ,  Sing-Yuen Sit

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14

Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, (I) are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

公开(公告)号：US20190389859A1

公开(公告)日：2019-12-26

申请号：US16484604

申请日：2018-02-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Junqing Guo ,  Amy C. Hart ,  John E. Macor ,  Michael E. Mertzman ,  William J. Pitts ,  Steven H. Spergel ,  Scott Hunter Watterson ,  Murugaiah Andappan Murugaiah Subbaiah ,  Jie Chen ,  Carolyn Diane Dzierba ,  Guanglin Luo ,  Jianliang Shi ,  Sing-Yuen Sit

IPC: C07D471/04

Abstract: Compounds having formula (I) (IX), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).

公开(公告)号：US09227940B2

公开(公告)日：2016-01-05

申请号：US14477594

申请日：2014-09-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alan Xiangdong Wang ,  Li-Qiang Sun ,  Sing-Yuen Sit ,  Ny Sin ,  Paul Michael Scola ,  Yan Chen

IPC: C07D207/16 ,  A61K31/40 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/062 ,  C07K5/083 ,  C07K5/08 ,  A61K45/06 ,  A61K38/00

CPC classification number: A61K38/06 ,  A61K31/40 ,  A61K38/00 ,  A61K38/005 ,  A61K45/06 ,  C07D207/16 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/0827 ,  A61K2300/00

Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract translation: 公开了具有以下通式的丙型肝炎病毒抑制剂：其中R1，R2，R3，R'，B，Y和X在说明书中描述。 还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。

公开(公告)号：US20150291655A1

公开(公告)日：2015-10-15

申请号：US14682179

申请日：2015-04-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Sing-Yuen Sit ,  Yan Chen ,  Jie Chen ,  Jacob Swidorski ,  Brian Lee Venables ,  Ny Sin ,  Nicholas A. Meanwell ,  Alicia Regueiro-Ren ,  Richard A. Hartz ,  Li Xu ,  Zheng Liu

IPC: C07J63/00 ,  C07F5/04 ,  C07C309/65

CPC classification number: A61K31/58 ,  A61K45/06 ,  C07C309/65 ,  C07C2601/16 ,  C07F5/025 ,  C07F5/04 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.

Abstract translation: 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的三萜类化合物作为HIV成熟抑制剂提供，如式I化合物所示：X选自C 4-8环烷基，C 4-8环烯基，C 4-9螺环烷基，C 4-9螺环烯基，C 4 - 8个氧杂环烷基，C4-8二氧杂环烷基，C6-8氧杂环烯基，C6-8二氧杂环烯基，C6环二烯基，C6氧杂环辛烯基，C6-9氧杂螺环烷基和C6-9氧杂环烯烯基环，使得X被A取代，其中A是-C1-6 烷基卤 这些化合物可用于治疗艾滋病毒和艾滋病。

公开(公告)号：US20140163231A1

公开(公告)日：2014-06-12

申请号：US14183247

申请日：2014-02-18

Applicant: Bristol-Myers Squibb Company

Inventor： Alan Xiangdong Wang ,  Li-Qiang Sun ,  Sing-Yuen Sit ,  Ny Sin ,  Paul Michael Scola ,  Yan Chen

IPC: C07D401/12

CPC classification number: A61K38/06 ,  A61K31/40 ,  A61K38/00 ,  A61K38/005 ,  A61K45/06 ,  C07D207/16 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/0827 ,  A61K2300/00

Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract translation: 公开了具有以下通式的丙型肝炎病毒抑制剂：其中R1，R2，R3，R'，B，Y和X在说明书中描述。 还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。

公开(公告)号：US20130296554A1

公开(公告)日：2013-11-07

申请号：US13799479

申请日：2013-03-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ny Sin ,  Zheng Liu ,  Jacob Swidorski ,  Sing-Yuen Sit ,  Jie Chen ,  Yan Chen ,  Nicholas A. Meanwell ,  Alicia Regueiro-Ren

IPC: C07D487/08 ,  C07D495/08 ,  C07D495/10 ,  C07D487/10 ,  C07D498/08 ,  C07D209/52 ,  C07D491/08

CPC classification number: C07D487/08 ,  C07D209/52 ,  C07D487/10 ,  C07D491/08 ,  C07D495/08 ,  C07D495/10 ,  C07D498/08 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.

Abstract translation: 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的三萜类化合物的C-17二环胺作为HIV成熟抑制剂提供，如式I，II和III化合物所示：这些化合物可用于治疗HIV和AIDS。