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公开(公告)号：US20130034520A1
公开(公告)日：2013-02-07
申请号：US13650374
申请日：2012-10-12
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: A61K31/4178 , C07D413/14 , A61K31/5377 , A61K31/496 , C07D401/14 , A61P31/14 , A61K38/05 , A61K38/21 , A61K31/7056 , A61K38/20 , A61K31/713 , C07D403/14 , A61K31/454
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.
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公开(公告)号：US09856292B2
公开(公告)日：2018-01-02
申请号：US14938327
申请日：2015-11-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Kevin W. Gillman , Jason Goodrich , Kenneth M. Boy , Yunhui Zhang , Claudio Mapelli , Michael A. Poss , Paul Michael Scola , David R. Langley , Nicholas A. Meanwell
CPC classification number: C07K7/08 , A61K38/00 , A61K38/10 , A61K45/06 , A61K51/088 , C07K7/56 , Y02A50/463
Abstract: The present disclosure provides compounds which are immunomodulators and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
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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.
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公开(公告)号：US09758487B2
公开(公告)日：2017-09-12
申请号：US15194980
申请日：2016-06-28
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: A61K38/20 , A61K31/4164 , A61K31/517 , A61K31/715 , A61K38/46 , A61P31/00 , C07D403/02 , C07D401/00 , C07D233/64 , C07D401/14 , C07D403/14 , A61K31/4178 , A61K45/06 , C07D405/14 , C07D413/14 , C07D409/14 , C07D417/14
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.
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15.发明申请SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES WITH PROTEASE INHIBITORS 审中-公开带有蛋白酶抑制剂的取代的氮杂双环戊哌嗪衍生物公开(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。
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Patent Agency Ranking
16.发明申请PIPERAZINE AND HOMOPIPERAZINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS 审中-公开作为艾滋病毒药物抑制剂的哌嗪和异丙肾上腺素衍生物公开(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。
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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。
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18.发明申请公开(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。
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公开(公告)号：US20150125422A1
公开(公告)日：2015-05-07
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
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.
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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。
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