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公开(公告)号：EP2044068A4
公开(公告)日：2010-07-21
申请号：EP07796862
申请日：2007-07-13
申请人： MERCK SHARP & DOHME
发明人： WILLIAMS PETER D , VENKATRAMAN SHANKAR , LANGFORD H MARIE , KIM BOYOUNG , BOOTH THERESA M , GROBLER JAY A , STAAS DONNETTE , RUZEK ROWENA D , EMBREY MARK W , WISCOUNT CATHERINE M , LYLE TERRY A
IPC分类号： C07D471/04
CPC分类号： C07D471/04
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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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3.发明公开DIARYL ETHER DERIVATIVES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 审中-公开二芳基醚衍生物作为抗缺损型的GAMMETETETER抑制剂
公开(公告)号：EP2488031A4
公开(公告)日：2014-07-23
申请号：EP10823842
申请日：2010-10-05
申请人： MERCK SHARP & DOHME
发明人： BROWN WILLIAM COLBY , HEIDEBRECHT RICHARD W , BRUBAKER JASON , FISCHER CHRISTIAN , HENDRIX JOHN T , KELLEY ELIZABETH H , MACCOSS RACHEL N , METHOT JOEY L , MILLER THOMAS , OTTE KARIN M , SILIPHAIVANH PHIENG , REGER THOMAS , WILLIAMS PETER D , WISCOUNT CATHERINE M
IPC分类号： C07D231/20 , A61K31/415 , A61P25/28 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
CPC分类号： C07D231/22 , C07D231/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
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4.发明公开
公开(公告)号：EP3116862A4
公开(公告)日：2017-08-30
申请号：EP15760695
申请日：2015-03-06
发明人： WILLIAMS PETER D , MCCAULEY JOHN A , BUNGARD CHRISTOPHER J , BENNETT DAVID JONATHAN , WADDELL SHERMAN T , MORRIELLO GREGORI J , CHANG LEHUA , DWYER MICHAEL P , HOLLOWAY M KATHARINE , CRESPO ALEJANDRO , CHU XIN-JIE , WISCOUNT CATHERINE , LOUGHRAN H MARIE , MANIKOWSKI JESSE J , KEERTIKAR KARTIK M , HU BIN , ZHONG BIN , JI TAO
IPC分类号： C07D513/08 , A61K31/554 , A61P31/18
CPC分类号： C07D513/08 , A61K31/554 , A61K45/06
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, 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.
摘要翻译： 本发明涉及式I化合物，包含其的药物组合物，以及它们在抑制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。
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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：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：EP3027593A4
公开(公告)日：2017-03-29
申请号：EP14832049
申请日：2014-07-29
发明人： WILLIAMS PETER D , MCCAULEY JOHN A , BENNETT DAVID J , BUNGARD CHRISTOPHER J , CHANG LEHUA , CHU XIN-JIE , DWYER MICHAEL P , HOLLOWAY M KATHERINE , KEERTIKAR KARTIK M , LOUGHRAN H MARIE , MANIKOWSKI JESSE J , MORRIELLO GREGORI J , SHEN DONG-MING , SHERER EDWARD C , SCHULZ JURGEN , WADDELL SHERMAN TIM , WISCOUNT CATHERINE M , ZORN NICOLAS , SATYANARAYANA TUMMANAPALLI , VIJAYASARADHI SIVALENKA , HU BIN , JI TAO , ZHONG BIN
IPC分类号： C07D401/14 , A61K31/496 , A61P31/18 , C07D241/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, 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.
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