公开(公告)号：US20180030019A1

公开(公告)日：2018-02-01

申请号：US15551006

申请日：2016-02-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Tao Wang ,  Zhiwei Yin ,  John F. Kadow

IPC: C07D307/84 ,  C07D407/12 ,  C07F9/655 ,  C07H7/06 ,  C07D405/12

Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV:

公开(公告)号：US09770439B2

公开(公告)日：2017-09-26

申请号：US14753564

申请日：2015-06-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Piyasena Hewawasam ,  Omar D. Lopez ,  Yong Tu ,  Alan Xiangdong Wang ,  Ningning Xu ,  John F. Kadow ,  Nicholas A. Meanwell ,  Samayamunthula Venkata Satya Arun Kumar Gupta ,  Indasi J. Gopi Kumar ,  Suresh Kumar Ponugupati ,  Makonen Belema

IPC: A61K31/415 ,  A61K31/535 ,  C07D471/04 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4178 ,  A61K38/21 ,  A61K31/4245 ,  A61K31/4725 ,  A61K31/7056 ,  A61K45/06 ,  C07D233/64 ,  C07D403/14 ,  C07D405/14 ,  C07D493/08 ,  A61K31/437 ,  A61K31/439 ,  A61K31/402 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/695 ,  A61K38/20

CPC classification number: A61K31/4178 ,  A61K31/402 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/695 ,  A61K31/7056 ,  A61K38/2013 ,  A61K38/204 ,  A61K38/208 ,  A61K38/21 ,  A61K45/06 ,  C07D233/64 ,  C07D403/14 ,  C07D405/14 ,  C07D493/08 ,  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.

公开(公告)号：US20170247385A1

公开(公告)日：2017-08-31

申请号：US15500110

申请日：2015-08-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Tao Wang ,  Kyle J. Eastman ,  Zhongxing Zhang ,  Kyle E. Parcella ,  John F. Kadow

IPC: C07D491/048 ,  C07B59/00

CPC classification number: C07D491/048 ,  C07B59/002 ,  C07B2200/05

Abstract: Compounds of formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US09434738B2

公开(公告)日：2016-09-06

申请号：US14759684

申请日：2014-01-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Tao Wang ,  Zhongxing Zhang ,  John F. Kadow

IPC: A61K31/343 ,  C07D307/84 ,  C07D491/06 ,  C07D491/04 ,  C07D498/04

CPC classification number: C07D491/06 ,  A61K31/343 ,  C07D307/84 ,  C07D491/04 ,  C07D498/04

Abstract: Compounds of formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US20160207918A1

公开(公告)日：2016-07-21

申请号：US15071329

申请日：2016-03-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Tao Wang ,  Zhongxing Zhang ,  Nicholas A. Meanwell ,  John F. Kadow ,  Zhiwei Yin ,  Qiufen May Xue ,  Alicia Regueiro-Ren ,  John D. Matiskella ,  Yasutsugu Ueda

IPC: C07D471/04 ,  C07D491/048

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K45/06 ,  C07D491/048

Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives having the Formula I: wherein Q is These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

Abstract translation: 本发明提供具有药物和生物影响性质的化合物，其药物组合物和使用方法。 特别地，本发明涉及具有式I的亚硝基二氧乙酰基哌嗪衍生物：其中Q是这些化合物具有独特的抗病毒活性，无论是单独使用还是与其它抗病毒剂，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。

公开(公告)号：US09303020B2

公开(公告)日：2016-04-05

申请号：US13755971

申请日：2013-01-31

Applicant: Bristol-Myers Squibb Company

Inventor： Kap-Sun Yeung ,  John F. Kadow

IPC: C07D405/14 ,  C07D405/04

CPC classification number: C07D405/14 ,  C07D405/04

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US20160052923A1

公开(公告)日：2016-02-25

申请号：US14779638

申请日：2014-03-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/519 ,  A61K31/496 ,  A61K31/551

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K45/06 ,  C07D519/00

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

Abstract translation: 式I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：US20150232480A1

公开(公告)日：2015-08-20

申请号：US14619213

申请日：2015-02-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Kevin Peese ,  Zhongyu Wang ,  John F. Kadow ,  Prasanna Sivaprakasam ,  B. Narasimhulu Naidu

IPC: C07D498/22

CPC classification number: C07D498/22 ,  C07D471/04

Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

Abstract translation: 本公开一般涉及式I化合物，包括用于治疗人类免疫缺陷病毒（HIV）感染的组合物和方法。 本公开提供了HIV的新型抑制剂，含有这些化合物的药物组合物，以及使用这些化合物治疗HIV感染的方法。

公开(公告)号：US20150232414A1

公开(公告)日：2015-08-20

申请号：US14704183

申请日：2015-05-05

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: C07C215/10 ,  C07D471/04

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 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.

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，R1不存在; 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选自本发明另外，本发明提供了可用于制备前药化合物I的中间体化合物II。其中：L和M独立地选自C 1 -C 6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：US20150105394A1

公开(公告)日：2015-04-16

申请号：US14384410

申请日：2013-03-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Tao Wang ,  John F. Kadow ,  Nicholas A. Meanwell ,  Lawrence G. Hamann

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/519 ,  A61K31/501

CPC classification number: C07D471/04 ,  A61K31/501 ,  A61K31/519 ,  A61K45/06 ,  C07D519/00

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

Abstract translation: 提供式I化合物，包括其药学上可接受的盐：其中A选自：其中Z选自：其可用作HIV附着抑制剂。