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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：EP2900665A4
公开(公告)日：2016-03-23
申请号：EP13841430
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 , A61K31/506 , A61P11/06 , A61P29/00 , A61P35/00 , C07D239/50 , C07D417/14
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.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物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：EP2863914A4
公开(公告)日：2015-12-16
申请号：EP13807800
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 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
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，其是脾脏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：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：EP2863913A4
公开(公告)日：2015-12-16
申请号：EP13807108
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 , C07D401/14 , C07D403/12 , C07D403/14
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的新型咪唑类似物，其是脾脏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：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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7.发明公开CATHEPSIN CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF VARIOUS DISEASES 审中-公开组织蛋白酶半胱氨酸蛋白酶抑制剂用于治疗各种疾病的治疗
公开(公告)号：EP2445872A4
公开(公告)日：2012-12-05
申请号：EP10791096
申请日：2010-06-16
申请人： MERCK CANADA INC
发明人： BLACK CAMERON , BEAULIEU CHRISTIAN
IPC分类号： C07C317/48 , A61K31/277 , A61K31/425 , A61K31/433 , A61P33/00 , C07C255/29 , C07C255/41 , C07C317/28 , C07C317/32 , C07C323/60 , C07D277/36 , C07D277/76 , C07D285/125 , C07D333/28
CPC分类号： C07D277/76 , C07C255/29 , C07C255/41 , C07C317/32 , C07C317/48 , C07C323/60 , C07C2601/02 , C07C2601/10 , C07D277/36 , C07D285/125 , C07D333/28
摘要： The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.
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公开(公告)号：EP2225196A4
公开(公告)日：2012-02-29
申请号：EP08853988
申请日：2008-11-26
申请人： MERCK CANADA INC
IPC分类号： C07C31/32 , A61K31/277 , A61P33/00 , C07C255/60 , C07C323/29 , C07D207/335 , C07D213/38 , C07D213/57 , C07D213/89 , C07D271/06 , C07D295/135 , C07D295/185
CPC分类号： C07C255/60 , A61K31/277 , A61K31/4418 , A61K31/5375 , A61K45/06 , C07C255/44 , C07C255/46 , C07C311/37 , C07C317/32 , C07C323/32 , C07C2601/02 , C07D207/335 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/89 , C07D271/06 , C07D295/135 , C07D295/185 , C07D295/192
摘要： Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis. Compounds of formula I of the invention are capable of treating and/or preventing the above-identified diseases:
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