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公开(公告)号:EP2632895A4
公开(公告)日:2015-12-16
申请号:EP11835398
申请日:2011-10-27
申请人: MERCK CANADA INC
IPC分类号: C07C311/41 , A61K31/27 , A61K31/428 , A61P31/18 , C07C311/29 , C07D277/62 , C07D413/12 , C07D417/12
CPC分类号: C07C311/39 , C07C311/29 , C07C311/41 , C07D277/62 , C07D413/12 , C07D417/12
摘要: Compounds of Formula I are disclosed wherein R1, R2, R3A, R3B, R4A, R4B, R5A, R5B, R6A, R6B, R7, R8 and R9 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 公开了其中R1,R2,R3A,R3B,R4A,R4B,R5A,R5B,R6A,R6B,R7,R8和R9在本文中定义的式I化合物。 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防,治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分,任选地与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:EP3082822A4
公开(公告)日:2017-05-24
申请号:EP14872521
申请日:2014-12-17
发明人: MCCAULEY JOHN A , BEAULIEU CHRISTIAN , BENNETT DAVID JONATHAN , BUNGARD CHRISTOPHER J , CRANE SHELDON , GRESHOCK THOMAS J , HOLLOWAY M KATHARINE , MCKAY DANIEL , MOLINARO CARMELA , MORADEI OSCAR MIGUEL , TUMMANAPALLI SATYANARAYANA , TRUONG VOUY LINH , WILLIAMS PETER D
IPC分类号: C07D265/30 , A61K31/5375 , A61K31/5377 , A61P31/18 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号: C07D265/30 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 本发明涉及2,5,6-取代的吗啉衍生物及其在抑制HIV蛋白酶,抑制HIV复制,预防HIV感染,治疗HIV感染以及预防,治疗 并延缓艾滋病的发病或进展。 化合物及其盐可以用作药物组合物中的成分,任选地与其他抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:EP3113780A4
公开(公告)日:2018-02-21
申请号:EP15759159
申请日:2015-03-02
发明人: MCCAULEY JOHN A , BEAULIEU CHRISTIAN , BENNETT DAVID JONATHAN , BUNGARD CHRISTOPHER J , CRANE SHELDON , GRESHOCK THOMAS J , HOLLOWAY M KATHARINE , LESSARD STEPHANIE , MCKAY DANIEL , MOLINARO CARMELA , MORADEI OSCAR MIGUEL , SIVALENKA VIJAYASARADHI , TRUONG VOUY LINH , TUMMANAPALLI SATYANARAYANA , WILLIAMS PETER D
IPC分类号: A61K31/5377 , A61K31/5375 , A61K31/5386 , A61K45/06 , C07D265/30 , C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/10
CPC分类号: C07D498/10 , A61K31/5375 , A61K31/5377 , A61K31/5386 , A61K45/06 , C07D265/30 , C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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公开(公告)号:EP3083609A4
公开(公告)日:2017-05-31
申请号:EP14872077
申请日:2014-12-17
发明人: MCCAULEY JOHN A , BEAULIEU CHRISTIAN , BENNETT DAVID JONATHAN , BUNGARD CHRISTOPHER J , CRANE SHELDON , GRESHOCK THOMAS J , HOLLOWAY M KATHARINE , JUTEAU HELEN , MCKAY DANIEL , MOLINARO CARMELA , MORADEI OSCAR MIGUEL , NADEAU CHRISTIAN , SIMARD DANIEL , TUMMANAPALLI SATYANARAYANA , TRUONG VOUY LINH , VILLENEUVE KARINE M , WILLIAMS PETER D
IPC分类号: C07D413/04 , A61K31/5377 , A61P31/18 , C07D265/32 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
CPC分类号: A61K31/5377 , A61K45/06 , C07D265/30 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要: The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 本发明涉及5-杂芳基吗啉衍生物及其在抑制HIV蛋白酶,抑制HIV复制,预防HIV感染,治疗HIV感染以及预防,治疗和延缓 艾滋病的发病或进展。 化合物及其盐可以用作药物组合物中的成分,任选地与其他抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:EP2413941A4
公开(公告)日:2012-10-10
申请号:EP10759391
申请日:2010-04-01
发明人: MCKAY DANIEL J , ARBOUR MELISSA , ASPIOTIS RENEE , CHEN AUSTIN , DOLMAN SARAH JENNIFER , FOURNIER PIERRE-ANDRE , GALLANT MICHEL , HAN YONGXIN , HUGHES GREG , JANEY JACOB , JUTEAU HELENE , LACOMBE PATRICK , LALIBERTE SEBASTIEN , LAUZON SOPHIE , MACDONALD DWIGHT , MACKAY BRUCE , MELLON CHRISTOPHE , MOLINARO CARMELA , MORLEY KRISTA L , O'SHEA PAUL
IPC分类号: A61K31/535
CPC分类号: C07D211/26 , C07D211/22 , C07D211/28 , C07D211/52 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14
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