公开(公告)号：US10143746B2

公开(公告)日：2018-12-04

申请号：US15446298

申请日：2017-03-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Martin Patrick Allen ,  Eric P. Gillis ,  David R. Langley ,  Michael Matthew Miller ,  Eric Mull ,  Li-Qiang Sun ,  Kap-Sun Yeung ,  Katharine A. Grant-Young ,  Nicholas A. Meanwell ,  Paul Michael Scola

IPC: A61K39/39 ,  A61K45/06 ,  C07K7/08 ,  C07K7/56 ,  G01N33/574 ,  A61K39/00

Abstract: The present disclosure provides novel macrocyclic compounds which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

公开(公告)号：US09527885B2

公开(公告)日：2016-12-27

申请号：US14592313

申请日：2015-01-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Sheldon Hiebert ,  Ramkumar Rajamani ,  Li-Qiang Sun ,  Eric Mull ,  Eric P. Gillis ,  Michael S. Bowsher ,  Qian Zhao ,  Nicholas A. Meanwell ,  Kishore V. Renduchintala ,  Kandhasamy Sarkunam ,  Pulicharla Nagalakshmi ,  P.V.K. Suresh Babu ,  Paul Michael Scola

IPC: C07D225/02 ,  C07K5/097 ,  C07D487/04 ,  C07K5/083 ,  C07K5/08 ,  A61K38/20 ,  A61K38/21 ,  A61K45/06 ,  A61K31/13 ,  A61K31/4745 ,  A61K31/7056 ,  A61K38/06 ,  A61K38/00

CPC classification number: C07K5/0823 ,  A61K31/13 ,  A61K31/4745 ,  A61K31/7056 ,  A61K38/00 ,  A61K38/06 ,  A61K38/2013 ,  A61K38/204 ,  A61K38/2053 ,  A61K38/21 ,  A61K38/212 ,  A61K45/06 ,  C07D487/04 ,  C07K5/0804 ,  C07K5/0827 ,  A61K2300/00

Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

公开(公告)号：US20160075703A1

公开(公告)日：2016-03-17

申请号：US14878270

申请日：2015-10-08

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.

公开(公告)号：US09227961B2

公开(公告)日：2016-01-05

申请号：US14488990

申请日：2014-09-17

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 ,  Lawrence G. Hamann

IPC: C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D233/64 ,  C07D405/14 ,  A61K31/4178 ,  A61K45/06

CPC classification number: C07D233/64 ,  A61K31/4178 ,  A61K45/06 ,  C07D207/16 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07F5/025 ,  C07F7/0812

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：US20150259342A1

公开(公告)日：2015-09-17

申请号：US14725298

申请日：2015-05-29

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：US20150210676A1

公开(公告)日：2015-07-30

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

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：US08889854B2

公开(公告)日：2014-11-18

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: C07J53/00 ,  C07D498/08 ,  C07D495/08 ,  C07D495/10 ,  C07D487/10 ,  C07J63/00 ,  C07D491/08 ,  C07D209/52 ,  C07D487/08

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：US20140135342A1

公开(公告)日：2014-05-15

申请号：US14156718

申请日：2014-01-16

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 ,  A61K45/06 ,  A61K31/496

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. 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，本发明涉及氮杂吲哚乙酰基哌嗪衍生物。 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他抗病毒药，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：US20130183269A1

公开(公告)日：2013-07-18

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

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.

公开(公告)号：US20130072465A1

公开(公告)日：2013-03-21

申请号：US13623165

申请日：2012-09-20

Applicant: Bristol-Myers Squibb Company

Inventor： Zheng Liu ,  Nicholas A. Meanwell ,  Alicia Regueiro-Ren

IPC: A61K31/58 ,  A61P31/18 ,  A61P31/12 ,  C07J53/00 ,  A61K31/565

CPC classification number: C07J63/008

Abstract: Compounds of Formula I: that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.

Abstract translation: 提供具有独特抗病毒活性的式I化合物作为HIV成熟抑制剂。 这些化合物可用于治疗艾滋病毒和艾滋病。