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：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。

公开(公告)号：US20160151387A1

公开(公告)日：2016-06-02

申请号：US15015741

申请日：2016-02-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: A61K31/565 ,  A61K31/58 ,  A61K31/704 ,  A61K45/06

CPC classification number: A61K31/565 ,  A61K31/56 ,  A61K31/58 ,  A61K31/704 ,  A61K45/06 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified 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C-17和C-3修饰的三萜类化合物作为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。

公开(公告)号：US20140243298A1

公开(公告)日：2014-08-28

申请号：US14186533

申请日：2014-02-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07J53/00 ,  A61K31/568 ,  A61K31/58

CPC classification number: C07J53/002 ,  A61K31/568 ,  A61K31/58 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV:a compound of Formula I a compound of Formula II a compound of Formula III and a compound of Formula IV 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烷基和烯基C-3修饰的桦木酸衍生物作为HIV成熟抑制剂提供，如式I，II，III和IV化合物所示：式I化合物式IIa化合物 式III化合物和式IV化合物这些化合物可用于治疗艾滋病毒和艾滋病。

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。