公开(公告)号：US20130338141A1

公开(公告)日：2013-12-19

申请号：US13970130

申请日：2013-08-19

申请人： Richard C. Isaacs ,  Wayne J. Thompson ,  Peter D. Williams ,  Dai-Shi Su ,  Shankar Venkatraman ,  Mark W. Embrey ,  Thorsten E. Fisher ,  John S. Wai ,  David C. Dubost ,  Richard G. Ball ,  Eric J. Choi ,  Tao Pei ,  Sarah L. Trice ,  Neil Campbell ,  Matthew Maddes ,  Peter E. Maligres ,  Michael Shevlin ,  Zhiguo Jake Song ,  Dietrich P. Steinhuebel ,  Neil A. Strotman ,  Jingjun Yin

发明人： Richard C. Isaacs ,  Wayne J. Thompson ,  Peter D. Williams ,  Dai-Shi Su ,  Shankar Venkatraman ,  Mark W. Embrey ,  Thorsten E. Fisher ,  John S. Wai ,  David C. Dubost ,  Richard G. Ball ,  Eric J. Choi ,  Tao Pei ,  Sarah L. Trice ,  Neil Campbell ,  Matthew Maddes ,  Peter E. Maligres ,  Michael Shevlin ,  Zhiguo Jake Song ,  Dietrich P. Steinhuebel ,  Neil A. Strotman ,  Jingjun Yin

IPC分类号： C07D498/04 ,  C07D487/04

CPC分类号： C07D498/04 ,  C07D487/04 ,  H01L2924/0002 ,  H01L2924/00

摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

摘要翻译： 式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。 该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。 该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了制备式I化合物的方法及其中间体。

公开(公告)号：US08513234B2

公开(公告)日：2013-08-20

申请号：US12572341

申请日：2009-10-02

申请人： Richard C. A. Isaacs ,  Wayne J. Thompson ,  Peter D. Williams ,  Dai-Shi Su ,  Shankar Venkatraman ,  Mark W. Embrey ,  Thorsten E. Fisher ,  John S. Wai ,  David C. Dubost ,  Richard G. Ball ,  Eric J. Choi ,  Tao Pei ,  Sarah L. Trice ,  Neil Campbell ,  Matthew Maddess ,  Peter E. Maligres ,  Michael Shevlin ,  Zhiguo Jake Song ,  Dietrich P. Steinhuebel ,  Neil A. Strotman ,  Jingjun Yin

发明人： Richard C. A. Isaacs ,  Wayne J. Thompson ,  Peter D. Williams ,  Dai-Shi Su ,  Shankar Venkatraman ,  Mark W. Embrey ,  Thorsten E. Fisher ,  John S. Wai ,  David C. Dubost ,  Richard G. Ball ,  Eric J. Choi ,  Tao Pei ,  Sarah L. Trice ,  Neil Campbell ,  Matthew Maddess ,  Peter E. Maligres ,  Michael Shevlin ,  Zhiguo Jake Song ,  Dietrich P. Steinhuebel ,  Neil A. Strotman ,  Jingjun Yin

IPC分类号： C07D487/12

CPC分类号： C07D498/04 ,  C07D487/04 ,  H01L2924/0002 ,  H01L2924/00

摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

摘要翻译： 式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。 该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。 该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了制备式I化合物的方法及其中间体。

公开(公告)号：US20100087419A1

公开(公告)日：2010-04-08

申请号：US12572341

申请日：2009-10-02

申请人： Richard C. A. Isaacs ,  Wayne J. Thompson ,  Peter D. Williams ,  Dai-Shi Su ,  Shankar Venkatraman ,  Mark W. Embrey ,  Thorsten E. Fisher ,  John S. Wai ,  David C. Dubost ,  Richard G. Ball ,  Eric J. Choi ,  Tao Pei ,  Sarah L. Trice ,  Neil Campbell ,  Matthew Maddess ,  Peter E. Maligres ,  Michael Shevlin ,  Zhiguo Jake Song ,  Dietrich P. Steinhuebel ,  Neil A. Strotman ,  Jingjun Yin

发明人： Richard C. A. Isaacs ,  Wayne J. Thompson ,  Peter D. Williams ,  Dai-Shi Su ,  Shankar Venkatraman ,  Mark W. Embrey ,  Thorsten E. Fisher ,  John S. Wai ,  David C. Dubost ,  Richard G. Ball ,  Eric J. Choi ,  Tao Pei ,  Sarah L. Trice ,  Neil Campbell ,  Matthew Maddess ,  Peter E. Maligres ,  Michael Shevlin ,  Zhiguo Jake Song ,  Dietrich P. Steinhuebel ,  Neil A. Strotman ,  Jingjun Yin

IPC分类号： A61K31/553 ,  C07D487/04 ,  C07D281/10 ,  A61K31/55 ,  A61P31/18

CPC分类号： C07D498/04 ,  C07D487/04 ,  H01L2924/0002 ,  H01L2924/00

摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

摘要翻译： 式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。 该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。 该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了制备式I化合物的方法及其中间体。

公开(公告)号：US09006460B2

公开(公告)日：2015-04-14

申请号：US13817274

申请日：2011-08-08

申请人： John Limanto ,  Gregory L. Beutner ,  Jingjun Yin ,  Artis Klapars ,  Eric R. Ashley ,  Hallena R. Strotman ,  Matthew D. Truppo ,  Cheol K. Chung ,  Gregory Hughes ,  Zhijian Liu ,  Brendan Grau ,  Jacob Janey

发明人： John Limanto ,  Gregory L. Beutner ,  Jingjun Yin ,  Artis Klapars ,  Eric R. Ashley ,  Hallena R. Strotman ,  Matthew D. Truppo ,  Cheol K. Chung ,  Gregory Hughes ,  Zhijian Liu ,  Brendan Grau ,  Jacob Janey

IPC分类号： C07D207/12 ,  C12P17/10

CPC分类号： C07D207/12 ,  C07C217/52 ,  C07D207/416 ,  C12P17/10

摘要： The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-[(3R)-Hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)-cyclohexane as well as various intermediates.

摘要翻译： 本发明涉及制备式I的氨基环己基醚化合物或其药学上可接受的盐和酯的方法。 特别地，本发明涉及制备（1R，2R）-2 - [（3R） - 羟基吡咯烷基] -1-（3,4-二甲氧基苯乙氧基） - 环己烷以及各种中间体的方法。

公开(公告)号：US20130149751A1

公开(公告)日：2013-06-13

申请号：US13817274

申请日：2011-08-08

申请人： John Limanto ,  Gregory L. Beutner ,  Jingjun Yin ,  Artis Klapars ,  Eric R. Ashley ,  Hallena R. Strotman ,  Matthew D. Truppo ,  Cheol K. Chung ,  Gregory Hughes ,  Zhijian Liu ,  Brendan Grau ,  Jacob Janey

发明人： John Limanto ,  Gregory L. Beutner ,  Jingjun Yin ,  Artis Klapars ,  Eric R. Ashley ,  Hallena R. Strotman ,  Matthew D. Truppo ,  Cheol K. Chung ,  Gregory Hughes ,  Zhijian Liu ,  Brendan Grau ,  Jacob Janey

IPC分类号： C12P17/10

CPC分类号： C07D207/12 ,  C07C217/52 ,  C07D207/416 ,  C12P17/10

摘要： The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-[(3R)-Hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)-cyclohexane as well as various intermediates.

公开(公告)号：US20100036135A1

公开(公告)日：2010-02-11

申请号：US11922446

申请日：2006-07-07

申请人： Jeffrey T. Kuethe ,  Jingjun Yin ,  Mark A. Huffman ,  Michel Journet

发明人： Jeffrey T. Kuethe ,  Jingjun Yin ,  Mark A. Huffman ,  Michel Journet

IPC分类号： C07D209/44 ,  C07C303/26

CPC分类号： C07D209/44

摘要： The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

摘要翻译： 本发明涉及一种制备某些可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的水解异吲哚啉化合物的方法。该化合物可用于治疗某些疾病，包括 呕吐，尿失禁，抑郁和焦虑。

公开(公告)号：US20180179223A1

公开(公告)日：2018-06-28

申请号：US15578777

申请日：2016-06-03

申请人： Jingjun Yin ,  Tetsuji Itoh ,  Jianguo Yin ,  Bangping Xiang ,  Kevin R. Campos ,  Alexei Kalinin ,  Zhuqing Liu ,  Melodie Deniz Christensen ,  Kevin M. Belyk ,  Richard J. Varsolona ,  Andrew Brunskill

发明人： Jingjun Yin ,  Tetsuji Itoh ,  Jianguo Yin ,  Bangping Xiang ,  Kevin R. Campos ,  Alexei Kalinin ,  Zhuqing Liu ,  Melodie Deniz Christensen ,  Kevin M. Belyk ,  Richard J. Varsolona ,  Andrew Brunskill

IPC分类号： C07D498/04 ,  C07F5/02 ,  C07D403/04 ,  B01J31/04

CPC分类号： C07D498/04 ,  B01J31/04 ,  C07D403/04 ,  C07F5/025

摘要： The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.

公开(公告)号：US20170166586A1

公开(公告)日：2017-06-15

申请号：US15325392

申请日：2015-07-10

申请人： Hongming LI ,  Jingjun YIN ,  Kevin M. BELYK ,  Kevin R. CAMPOS ,  Qinghao CHEN ,  Alan M. HYDE ,  Tetsuji ITOH ,  Artis KLAPARS ,  Mathew Thomas TUDGE ,  Edward CLEATOR ,  Aaron M. DUMAS ,  Louis-Charles CAMPEAU ,  Yonggang CHEN ,  Ji QI ,  Wensong XIAO ,  MERCK SHARP & DOHME CORP. ,  MERCK SHARP & DOHME LIMITED ,  MSD R&D (CHINA) CO., LTD

发明人： Hongming Li ,  Jingjun Yin ,  Kevin M. Belyk ,  Kevin R. Campos ,  Qinghao Chen ,  Alan M. Hyde ,  Tetsuji Itoh ,  Artis Klapars ,  Matthew Thomas Tudge ,  Edward Cleator ,  Aaron M. Dumas ,  Louis-Charles Campeau ,  Yonggang Chen ,  Ji Qi ,  Wensong Xiao

IPC分类号： C07D498/04 ,  C07F9/6509 ,  C07D265/14 ,  C07D413/04 ,  C07C251/24 ,  C07D417/04

CPC分类号： C07D498/04 ,  C07C251/24 ,  C07D239/74 ,  C07D265/14 ,  C07D265/36 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07F9/650994 ,  C07F17/02

摘要： The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that are useful as synthetic intermediates in the process of the invention.

公开(公告)号：US07544815B2

公开(公告)日：2009-06-09

申请号：US11484208

申请日：2006-07-11

申请人： Jeffrey T. Kuethe ,  Jingjun Yin ,  Mark A. Huffman ,  Michel Journet

发明人： Jeffrey T. Kuethe ,  Jingjun Yin ,  Mark A. Huffman ,  Michel Journet

IPC分类号： C07D209/44

CPC分类号： C07D209/44

摘要： The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

摘要翻译： 本发明涉及一种制备某些可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的水解异吲哚啉化合物的方法。该化合物可用于治疗某些疾病，包括 呕吐，尿失禁，抑郁和焦虑。

公开(公告)号：US20070015923A1

公开(公告)日：2007-01-18

申请号：US11484208

申请日：2006-07-11

申请人： Jeffrey Kuethe ,  Jingjun Yin ,  Mark Huffman ,  Michel Journet

发明人： Jeffrey Kuethe ,  Jingjun Yin ,  Mark Huffman ,  Michel Journet

IPC分类号： C07D209/44

CPC分类号： C07D209/44

摘要： The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

摘要翻译： 本发明涉及制备某些可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的水解异吲哚啉化合物的方法。该化合物可用于治疗某些疾病，包括 呕吐，尿失禁，抑郁和焦虑。