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：US09326973B2

公开(公告)日：2016-05-03

申请号：US13735224

申请日：2013-01-07

Applicant: Bristol-Myers Squibb Company

Inventor： Piyasena Hewawasam ,  John F. Kadow ,  Omar D. Lopez ,  Nicholas A. Meanwell ,  Yong Tu ,  Alan Xiangdong Wang ,  Ningning Xu ,  Samayamunthula Venkata Satya Arun Kumar Gupta ,  Pothukanuri Srinivasu ,  Indasi Gopi Kumar ,  Ponugupati Suresh Kumar ,  Makonen Belema ,  Robert A. Fridell ,  Min Gao ,  Julie A. Lemm ,  Donald R. O'Boyle, II ,  Jin-Hua Sun ,  Chunfu Wang ,  Ying-Kai Wang

IPC: A61K31/415 ,  A61K31/675 ,  A61K38/00 ,  A61K31/4178 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/21 ,  A61K45/06 ,  C07D403/14 ,  C07D491/113

CPC classification number: A61K31/4178 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/21 ,  A61K38/212 ,  A61K38/217 ,  A61K45/06 ,  C07D403/14 ,  C07D491/113 ,  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。

公开(公告)号：US20160052924A1

公开(公告)日：2016-02-25

申请号：US14779648

申请日：2014-03-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Tao Wang ,  Zhiwei Yin ,  Zhongxing Madison ,  John A. Bender ,  Barry L. Johnson ,  Jhon F. Kadow ,  Nicholas A. Meanwell

IPC: C07D471/04 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/06 ,  A61K31/454 ,  A61K31/437 ,  A61K31/55

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/55 ,  A61K45/06 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: I useful as HIV attachment inhibitors.

Abstract translation: 式I的化合物，包括其药学上可接受的盐：可用作HIV附着抑制剂。

公开(公告)号：US20150315218A1

公开(公告)日：2015-11-05

申请号：US14800315

申请日：2015-07-15

Applicant: Bristol-Myers Squibb Company

Inventor： Yasutsugu Ueda ,  Timothy P. Connolly ,  John F. Kadow ,  Nicholas A. Meanwell ,  Tao Wang ,  Chung-Pin H. Chen ,  Kap-Sun Yeung ,  Zhongxing Zhang ,  David Kenneth Leahy ,  Shawn K. Pack ,  Nachimuthu Soundararajan ,  Pierre Sirard ,  Kathia Levesque ,  Dominique Thoraval

IPC: C07F9/6561

CPC classification number: A61K31/675 ,  A61K31/497 ,  A61K31/519 ,  A61K45/06 ,  C07C215/10 ,  C07D471/04 ,  C07F9/062 ,  C07F9/5728 ,  C07F9/65515 ,  C07F9/65586 ,  C07F9/6561

Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection: wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

Abstract translation: 本发明提供前药化合物I，其药物组合物及其在治疗HIV感染中的用途：其中：X为C或N，条件是当X为N时，不存在R1; W为C或N，条件是当W为N时，R2不存在; V是C; E是氢或其药学上可接受的盐; 并且Y选自其中：L和M独立地选自C1-C6烷基，苯基，苄基，三烷基甲硅烷基，-2,2,2-三氯乙氧基和2-三甲基甲硅烷基乙氧基。

公开(公告)号：US09156828B2

公开(公告)日：2015-10-13

申请号：US14419568

申请日：2013-08-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Tao Wang ,  Zhongxing Zhang ,  Zhiwei Yin ,  John F. Kadow ,  Nicholas A. Meanwell

IPC: A61K31/553 ,  C07D471/00 ,  C07D413/12 ,  C07D403/12 ,  A61K31/5513 ,  C07D471/04 ,  A61K45/06

CPC classification number: C07D413/12 ,  A61K31/5513 ,  A61K31/553 ,  A61K45/06 ,  C07D403/12 ,  C07D471/04

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: (F) wherein A is selected from the group consisting of: (F) and; (F) and wherein Z is: (F) are useful as HIV attachment inhibitors.

Abstract translation: 式I化合物，包括其药学上可接受的盐：（F）其中A选自：（F）和 （F），其中Z是：（F）可用作HIV附着抑制剂。

公开(公告)号：US08846023B2

公开(公告)日：2014-09-30

申请号：US14021686

申请日：2013-09-09

Applicant: Bristol-Myers Squibb Company

Inventor： Carol Bachand ,  Makonen Belema ,  Daniel H. Deon ,  Andrew C. Good ,  Jason Goodrich ,  Clint A. James ,  Rico Lavoie ,  Omar D. Lopez ,  Alain Martel ,  Nicholas A. Meanwell ,  Van N. Nguyen ,  Jeffrey Lee Romine ,  Edward H. Ruediger ,  Lawrence B. Snyder ,  Denis R. St. Laurent ,  Fukang Yang ,  David R. Langley ,  Gan Wang ,  Lawrence G. Hamann

IPC: C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  A61K31/506 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/13 ,  A61K31/7105 ,  A61K31/4745 ,  A61K31/7056 ,  A61K38/20 ,  A61K38/21 ,  C07D401/14

CPC classification number: A61K31/506 ,  A61K31/13 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/4745 ,  A61K31/7056 ,  A61K31/7105 ,  A61K38/2013 ,  A61K38/204 ,  A61K38/208 ,  A61K38/21 ,  A61K38/212 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

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：US20130253196A1

公开(公告)日：2013-09-26

申请号：US13861804

申请日：2013-04-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yasutsugu Ueda ,  Timothy P. Connolly ,  John F. Kadow ,  Nicholas A. Meanwell ,  Tao Wang ,  Chung-Pin H. Chen ,  Kap-Sun Yeung ,  Zhongxing Zhang ,  David Kenneth Leahy ,  Shawn K. Pack ,  Nachimuthu Soundararajan ,  Pierre Sirard ,  Kathia Levesque ,  Dominique Thoraval

IPC: C07F9/6561

CPC classification number: A61K31/675 ,  A61K31/497 ,  A61K45/06 ,  C07D471/04 ,  C07F9/062 ,  C07F9/5728 ,  C07F9/65515 ,  C07F9/65586 ,  C07F9/6561

Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

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。