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公开(公告)号：EP3082822B1
公开(公告)日：2020-01-15
申请号：EP14872521.1
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 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/5377 , A61K31/5375 , A61P31/18 , C07D471/04 , C07D487/04 , C07D513/04
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公开(公告)号：EP2900665B1
公开(公告)日：2018-01-03
申请号：EP13841430.5
申请日：2013-09-24
发明人： MACHACEK, Michelle R. , ROMEO, Eric T. , KATTAR, Solomon D. , CHRISTOPHER, Matthew , ALTMAN, Michael D. , NORTHRUP, Alan B. , ELLIS, John Michael , BOYLE, Brendan O' , DONOFRIO, Anthony , GRIMM, Jonathan , REUTERSHAN, Michael H. , CHILDERS, Kaleen Konrad , OTTE, Ryan D. , CASH, Brandon , DUCHARME, Yves , HAIDLE, Andrew M. , SPENCER, Kerrie , VITHARANA, Dilrukshi , WU, Lingyun , ZHANG, Li , ZHANG, Peng , BEAULIEU, Christian , GUAY, Daniel
IPC分类号： C07D417/12 , C07D417/14 , C07D239/50 , A61K31/506 , A61P11/06 , A61P29/00 , A61P35/00
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
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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：EP3082822A1
公开(公告)日：2016-10-26
申请号：EP14872521.1
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： A61K31/5375
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：EP2863914B1
公开(公告)日：2018-10-03
申请号：EP13807800.1
申请日：2013-06-18
发明人： MACHACEK, Michele, R. , ALTMAN, Michael, D. , ROMEO, Eric, T. , WITHARANA, Dilrukshi , CASH, Brandon , SIU, Tony , ZHOU, Hua , CHRISTOPHER, Matthew , KATTAR, Solomon, D. , HAIDLE, Andrew, M. , CHILDERS, Kaleen Konrad , MADDESS, Matthew, H. , REUTERSHAN, Michael, H. , DUCHARME, Yves , GUERIN, David, J. , SPENCER, Kerrie , BEAULIEU, Christian , TRUONG, Vouy Linh , GUAY, Daniel , NORTHRUP, Alan, B. , TAOKA, Brandon, M. , LIM, Jongwon , FISCHER, Christian , BUTCHER, John, W. , OTTE, Ryan, D. , SUN, Binyuan , ELLIS, John, Michael
IPC分类号： A61K31/50 , A61K31/501 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/14 , C07D409/14 , C07D471/04 , C07D403/12
CPC分类号： C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
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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：EP2863913A1
公开(公告)日：2015-04-29
申请号：EP13807108.9
申请日：2013-06-18
发明人： LIM, Jongwon , REUTERSHAN, Michael, H. , ELLIS, John Michael , CHILDERS, Kaleen Konrad , DONOFRIO, Anthony , ALTMAN, Michael, D. , HAIDLE, Andrew, M. , ZABIEREK, Anna , CHRISTOPHER, Matthew , GRIMM, Jonathan , BURCH, Jason , FRANCESCO, Maria Emilia Di , PETROCCHI, Alessia , BEAULIEU, Christian , TRUONG, Vouy Linh , NORTHRUP, Alan, B. , BLOUIN, Marc
IPC分类号： A61K31/50 , A61K31/501
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14
摘要： The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 本发明提供了式I的新咪唑类似物，它们是脾酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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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：EP3083609A1
公开(公告)日：2016-10-26
申请号：EP14872077.4
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： C07D413/12 , C07D265/32 , C07D413/14
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：EP2863914A1
公开(公告)日：2015-04-29
申请号：EP13807800.1
申请日：2013-06-18
发明人： MACHACEK, Michele, R. , ALTMAN, Michael, D. , ROMEO, Eric, T. , WITHARANA, Dilrukshi , CASH, Brandon , SIU, Tony , ZHOU, Hua , CHRISTOPHER, Matthew , KATTAR, Solomon, D. , HAIDLE, Andrew, M. , CHILDERS, Kaleen Konrad , MADDESS, Matthew, H. , REUTERSHAN, Michael, H. , DUCHARME, Yves , GUERIN, David, J. , SPENCER, Kerrie , BEAULIEU, Christian , TRUONG, Vouy Linh , GUAY, Daniel , NORTHRUP, Alan, B. , TAOKA, Brandon, M. , LIM, Jongwon , FISCHER, Christian , BUTCHER, John, W. , OTTE, Ryan, D. , SUN, Binyuan , ELLIS, John, Michael
IPC分类号： A61K31/50 , A61K31/501
CPC分类号： C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 本发明提供了式I的新型吡唑衍生物，它们是脾酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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