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公开(公告)号：US08637449B2
公开(公告)日：2014-01-28
申请号：US13392168
申请日：2010-08-26
IPC分类号： A61K38/00
CPC分类号： C07K5/0808 , C07K5/0812 , C07K5/0827
摘要： The present invention relates to synthetic processes useful in the preparation of macrocyclic compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus NS3 protease and have application in the treatment of conditions caused by the hepatitis C virus. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
摘要翻译： 本发明涉及可用于制备式（I）的大环化合物的合成方法，其可用作丙型肝炎病毒NS3蛋白酶的抑制剂，并且可用于治疗由丙型肝炎病毒引起的病症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。
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公开(公告)号：US20120232247A1
公开(公告)日：2012-09-13
申请号：US13392168
申请日：2010-08-26
IPC分类号： C07K5/12
CPC分类号： C07K5/0808 , C07K5/0812 , C07K5/0827
摘要： The present invention relates to synthetic processes useful in the preparation of macrocyclic compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus NS3 protease and have application in the treatment of conditions caused by the hepatitis C virus. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
摘要翻译： 本发明涉及可用于制备式（I）的大环化合物的合成方法，其可用作丙型肝炎病毒NS3蛋白酶的抑制剂，并且可用于治疗由丙型肝炎病毒引起的病症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。
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公开(公告)号：US20110319627A1
公开(公告)日：2011-12-29
申请号：US12969371
申请日：2010-12-15
IPC分类号： C07D213/75
CPC分类号： C07D213/75
摘要： Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.
摘要翻译： 本文描述了制备式II化合物或其药学上可接受的盐的新方法。 在一些实施方案中，该方法用于制备betrixaban或其药学上可接受的盐。 还描述了包含基本上纯的双倍他卡巴游离碱或其盐的组合物。
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公开(公告)号：US09238604B2
公开(公告)日：2016-01-19
申请号：US14239393
申请日：2012-08-16
申请人： Feng Xu , Guy Humphrey , Tao Pei , Zhiguo Jake Song , Tao Wang , Laura Artino
发明人： Feng Xu , Guy Humphrey , Tao Pei , Zhiguo Jake Song , Tao Wang , Laura Artino
IPC分类号： C07K5/08 , C07K5/10 , C07K5/12 , C07D401/12 , C07C35/04 , C07K5/083 , C07D403/12 , C07D498/16 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , A61K38/00
CPC分类号： C07C35/04 , A61K38/00 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , C07D403/12 , C07D498/16 , C07K5/0808 , C07K5/126
摘要： The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.
摘要翻译： 本发明包括可用作制备中性物质的中间体的化合物，制备中间体的方法，以及从中间体制备大环内酯的方法。 本文描述的方法和中间体的一个用途是制备能够抑制HCV NS3蛋白酶活性的大环内酰胺化合物。 HCV NS3抑制化合物具有治疗和研究应用。
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公开(公告)号：US08394964B2
公开(公告)日：2013-03-12
申请号：US12969371
申请日：2010-12-15
IPC分类号： C07D213/75
CPC分类号： C07D213/75
摘要： Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.
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公开(公告)号：US20170233382A1
公开(公告)日：2017-08-17
申请号：US15503035
申请日：2015-08-10
申请人： Steven P. MILLER , Carmela MOLINARO , David THAISRIVONGS , Feng XU , Richard DESMOND , Hongming LI , Qinghao CHEN , Andrew STAMFORD , Zhiguo Jake SONG , Lushi TAN , Merck Sharp & Dohme Corp.
发明人： Steven P. Miller , Carmela Molinaro , David Thaisrivongs , Feng Xu , Richard Desmond , Hongming Li , Qinghao Chen , Andrew W. Stamford , Zhiguo Jake Song , Lushi Tan
IPC分类号： C07D417/12 , C07C313/06 , C07C311/33 , C07D213/81
CPC分类号： C07D417/12 , C07C303/40 , C07C311/33 , C07C311/35 , C07C313/06 , C07D213/81
摘要： This invention provides processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2. In addition, the invention provides certain synthetic intermediates which are useful, among other things, for the preparation of the Compound of Formula (I).
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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。
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公开(公告)号：US20140200343A1
公开(公告)日：2014-07-17
申请号：US14239393
申请日：2012-08-16
申请人： Feng Xu , Guy Humphrey , Tao Pei , Zhiguo Jake Song , Tao Wang , Laura Artino
发明人： Feng Xu , Guy Humphrey , Tao Pei , Zhiguo Jake Song , Tao Wang , Laura Artino
IPC分类号： C07D498/16 , C07D403/12
CPC分类号： C07C35/04 , A61K38/00 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , C07D403/12 , C07D498/16 , C07K5/0808 , C07K5/126
摘要： The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.
摘要翻译： 本发明包括可用作制备大新戊酰胺的中间体的化合物，制备中间体的方法和从中间体制备大环内酯的方法。 本文描述的方法和中间体的一个用途是制备能够抑制HCV NS3蛋白酶活性的大环内酰胺化合物。 HCV NS3抑制化合物具有治疗和研究应用。
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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。
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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。
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