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公开(公告)号：EP3113780B1
公开(公告)日：2019-08-14
申请号：EP15759159.5
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 , C07D265/30 , C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D498/10 , C07D487/04 , C07D471/04 , A61K45/06
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公开(公告)号：EP2895482A1
公开(公告)日：2015-07-22
申请号：EP13763164.4
申请日：2013-09-09
发明人： MCCAULEY, John, A. , CRANE, Sheldon , BEAULIEU, Christian , BENNETT, David, J. , BUNGARD, Christopher, J. , CHANG, Ronald, K. , GRESHOCK, Thomas, J. , HAO, Li , HOLLOWAY, Kate , MANIKOWSKI, Jesse, J. , MCKAY, Daniel , MOLINARO, Carmela , MORADEI, Oscar Miguel , NANTERMET, Philippe, G. , NADEAU, Christian , SATYANARAYANA, Tummanapalli , SHIPE, William , SINGH, Sanjay Kumar , TRUONG, Vouy Linh , VIJAYASARADHI, Sivalenka , WILLIAMS, Peter, D. , WISCOUNT, Catherine, M.
IPC分类号： C07D413/14 , C07D413/06 , C07D413/12 , C07D265/30 , C07D265/32 , A61K31/5377 , A61P31/18
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
摘要： 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： 式I所涵盖的化合物包括为HIV蛋白酶抑制剂的化合物和可在体内代谢为HIV蛋白酶抑制剂的其它化合物。 这些化合物及其可药用盐可用于预防或治疗HIV感染和预防，治疗或延缓AIDS发作。 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：EP3113780A1
公开(公告)日：2017-01-11
申请号：EP15759159.5
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
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.
摘要翻译： 本发明涉及式（I）的2,6-吗啉衍生物及其药学上可接受的盐，其中Z1，Z2，V1，V2，V3，R6，R6A和X在本文中定义。 本发明还涉及使用本发明的2,6-吗啉衍生物用于抑制HIV蛋白酶，HIV复制的抑制，HIV预防感染，HIV感染治疗以及预防，治疗 ，并延迟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：EP2895482B1
公开(公告)日：2016-10-19
申请号：EP13763164.4
申请日：2013-09-09
发明人： MCCAULEY, John, A. , CRANE, Sheldon , BEAULIEU, Christian , BENNETT, David, J. , BUNGARD, Christopher, J. , CHANG, Ronald, K. , GRESHOCK, Thomas, J. , HAO, Li , HOLLOWAY, Kate , MANIKOWSKI, Jesse, J. , MCKAY, Daniel , MOLINARO, Carmela , MORADEI, Oscar Miguel , NANTERMET, Philippe, G. , NADEAU, Christian , SATYANARAYANA, Tummanapalli , SHIPE, William , SINGH, Sanjay Kumar , TRUONG, Vouy Linh , VIJAYASARADHI, Sivalenka , WILLIAMS, Peter, D. , WISCOUNT, Catherine, M.
IPC分类号： C07D413/14 , C07D413/06 , C07D413/12 , C07D265/30 , C07D265/32 , A61K31/5377 , A61P31/18
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
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公开(公告)号：EP2391212A1
公开(公告)日：2011-12-07
申请号：EP10736272.5
申请日：2010-01-25
发明人： VENKATRAMAN, Shankar , WAI, John, S. , THOMPSON, Wayne , KIM, Boyoung , ISAACS, Richard C.A. , LOUGHRAN, H. Marie , SU, Dai-Shi , LIM, John , EMBREY, Mark, W. , WILLIAMS, Peter, D.
CPC分类号： C07D487/18 , C07D471/18 , C07D491/18
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X
1 , X
2 , χ
3 , Y, Z, R
1 , R
2 and R
3 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.-
公开(公告)号：EP2349276A2
公开(公告)日：2011-08-03
申请号：EP09740569.0
申请日：2009-10-02
发明人： ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L. , CAMPBELL, Neil , MADDESS, Matthew , MALIGRES, Peter, E. , SHEVLIN, Michael , SONG, Zhiguo Jake , STEINHUEBEL, Dietrich, P. , STROTMAN, Neil, A. , YIN, Jingjun
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整合酶抑制剂和HIV复制抑制剂：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HIV感染以及预防，治疗或延迟AIDS的发作或进展。 这些化合物作为化合物本身（或其水合物或溶剂合物）或以药学上可接受的盐的形式用于抗HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了制备式I化合物及其中间体的方法。
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公开(公告)号：EP2349276B1
公开(公告)日：2019-11-27
申请号：EP09740569.0
申请日：2009-10-02
发明人： ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L. , CAMPBELL, Neil , MADDESS, Matthew , MALIGRES, Peter, E. , SHEVLIN, Michael , SONG, Zhiguo Jake , STEINHUEBEL, Dietrich, P. , STROTMAN, Neil, A. , YIN, Jingjun
IPC分类号： A61K31/553 , C07D487/04 , C07D281/10 , A61K31/55 , A61P31/18
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公开(公告)号：EP3558305A1
公开(公告)日：2019-10-30
申请号：EP17883610.2
申请日：2017-12-19
发明人： MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu , WILLIAMS, Peter, D. , KIM, Jae-Hun , NOLT, M. Brad , CAPLEN, Mary Ann
IPC分类号： A61K31/4178 , C07D403/06 , C07D493/04
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9.发明公开
公开(公告)号：EP2488031A1
公开(公告)日：2012-08-22
申请号：EP10823842.9
申请日：2010-10-05
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： A01N43/56 , A61K31/415
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
摘要： The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ϒ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括一类新的二芳基醚衍生物，其抑制由推定的γ-分泌酶加工APP而同时保留Notch信号传导途径，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠问题。 药物组合物和使用方法也包括在内。
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