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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：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：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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4.发明公开MACROCYCLIC SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权万家乐CYCLICAL螺哌啶β-分泌酶抑制剂用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP2073635A4
公开(公告)日：2010-12-29
申请号：EP07839182
申请日：2007-10-02
申请人： MERCK SHARP & DOHME
IPC分类号： A01N43/40 , A61K31/415
CPC分类号： C07D471/10 , C07D471/20
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公开(公告)号：EP1879607A4
公开(公告)日：2010-03-31
申请号：EP06751833
申请日：2006-04-28
申请人： MERCK SHARP & DOHME
发明人： HOLLOWAY M KATHARINE , LIVERTON NIGEL J , LUDMERER STEVEN W , MCCAULEY JOHN A , OLSEN DAVID B , RUDD MICHAEL T , VACCA JOSEPH P
IPC分类号： A61K38/12
CPC分类号： C07K5/0808 , C07K5/0806 , C07K5/0812 , C07K5/0815 , C07K5/0821
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6.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：EP2435037A4
公开(公告)日：2012-10-17
申请号：EP10781008
申请日：2010-05-18
申请人： MERCK SHARP & DOHME
CPC分类号： C07D207/14
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