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公开(公告)号：EP3038466B1
公开(公告)日：2018-05-23
申请号：EP14840648.1
申请日：2014-08-25
发明人： ALI, Amjad , GALLO, Gioconda, V. , HENDERSON, Timothy, J. , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , METZGER, Edward , RUIZ, Manuel de Lera , STAMFORD, Andrew , TEMPEST, Paul , WHITEHEAD, Brent , WU, Heping
IPC分类号： C07D519/00 , C07D491/147 , A61K31/519 , A61P25/00 , A61P25/16 , A61P25/28
CPC分类号： C07D519/00 , C07D491/147
摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.
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2.发明授权
公开(公告)号：EP1945617B1
公开(公告)日：2012-12-26
申请号：EP06836623.6
申请日：2006-10-30
发明人： CLOSE, Joshua , HEIDEBRECHT, Richard W. , KATTAR, Solomon , MILLER, Thomas A. , SLOMAN, David , STANTON, Matthew G. , TEMPEST, Paul , WITTER, David J.
IPC分类号： C07D231/40 , C07D401/12 , C07D409/14 , C07D409/04 , C07D413/12 , C07D417/12 , A61K31/415 , A61K31/4245 , A61K31/427 , A61K31/4406 , A61P35/00
CPC分类号： C07D401/12 , C07D231/40 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12
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3.发明公开4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 有权4-羧基苯甲酰胺衍生物ALS HISTONDEACETYLASE-HEMMER
公开(公告)号：EP2170076A1
公开(公告)日：2010-04-07
申请号：EP08794378.3
申请日：2008-06-24
发明人： HARRINGTON, Paul , HEIDEBRECHT, Richard, W., Jr. , KATTAR, Solomon , MILLER, Thomas, A. , OTTE, Karin, M. , SILIPHAIVANH, Phieng , TEMPEST, Paul , WILSON, Kevin, J. , WITTER, David, J.
CPC分类号： C07D295/155 , C07C237/40 , C07C237/42 , C07C271/22 , C07C271/38 , C07C271/54 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/14 , C07D207/16 , C07D209/44 , C07D209/48 , C07D211/14 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/74 , C07D217/04 , C07D231/12 , C07D233/64 , C07D241/12 , C07D263/20 , C07D277/28 , C07D295/125 , C07D307/22 , C07D333/10 , C07D333/20 , C07D401/04 , C07D409/12 , C07D413/12
摘要： The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.
摘要翻译： 本发明涉及一类新的4-羧基苄基氨基衍生物。 4-羧基苄基氨基化合物可用于治疗癌症。 4-羧基苄基氨基化合物还可以抑制组蛋白脱乙酰酶，并且适用于选择性诱导末端分化，并阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如 神经退行性疾病 本发明进一步提供包含4-羧基苄基氨基衍生物和这些药物组合物的安全投药方案的药物组合物，其易于遵循，并且其在体内导致治疗有效量的4-羧基苄基氨基衍生物。
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公开(公告)号：EP2964220B1
公开(公告)日：2017-10-04
申请号：EP14760553.9
申请日：2014-02-27
发明人： MILLER, Michael , BASU, Kallol , DEMONG, Duane , SCOTT, Jack , LIU, Hong , DAI, Xing , STAMFORD, Andrew , POIRIER, Marc , TEMPEST, Paul
IPC分类号： A61K31/416 , C07D231/56 , C07D401/04 , C07D405/14 , C07D498/08 , C07D413/14 , C07D401/14 , C07D417/14 , A61P25/08
CPC分类号： C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/08 , C07D495/08 , C07D498/04 , C07D498/08
摘要： The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.
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公开(公告)号：EP2964223B1
公开(公告)日：2017-09-13
申请号：EP14761162.8
申请日：2014-02-27
发明人： MILLER, Michael , BASU, Kallol , DEMONG, Duane , SCOTT, Jack , LI, Wei , STAMFORD, Andrew , POIRIER, Marc , TEMPEST, Paul
IPC分类号： C07D403/14 , C07D413/14 , C07D405/14 , C07D401/14 , C07D498/08 , C07D471/04 , C07D487/04 , C07D417/14 , C07D409/14 , A61K31/506 , A61P25/16
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107 , C07D498/04 , C07D498/08 , C07D498/10
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6.发明授权4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 有权4- carboxybenzylamino衍生物作为组蛋白脱乙酰酶抑制剂
公开(公告)号：EP2170076B1
公开(公告)日：2016-05-18
申请号：EP08794378.3
申请日：2008-06-24
发明人： HARRINGTON, Paul , HEIDEBRECHT, Richard, W., Jr. , KATTAR, Solomon , MILLER, Thomas, A. , OTTE, Karin, M. , SILIPHAIVANH, Phieng , TEMPEST, Paul , WILSON, Kevin, J. , WITTER, David, J.
IPC分类号： C07C237/40 , C07D207/08 , A61K31/17 , A61P35/00
CPC分类号： C07D295/155 , C07C237/40 , C07C237/42 , C07C271/22 , C07C271/38 , C07C271/54 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/14 , C07D207/16 , C07D209/44 , C07D209/48 , C07D211/14 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/74 , C07D217/04 , C07D231/12 , C07D233/64 , C07D241/12 , C07D263/20 , C07D277/28 , C07D295/125 , C07D307/22 , C07D333/10 , C07D333/20 , C07D401/04 , C07D409/12 , C07D413/12
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公开(公告)号：EP2964223A1
公开(公告)日：2016-01-13
申请号：EP14761162.8
申请日：2014-02-27
发明人： MILLER, Michael , BASU, Kallol , DEMONG, Duane , SCOTT, Jack , LI, Wei , STAMFORD, Andrew , POIRIER, Marc , TEMPEST, Paul
IPC分类号： A61K31/415 , C07D231/56
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107 , C07D498/04 , C07D498/08 , C07D498/10
摘要： The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
摘要翻译： 本发明涉及作为LRRK2激酶的有效抑制剂的吲唑化合物，其可用于治疗或预防其中涉及LRRK2激酶的疾病，例如帕金森病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及LRRK-2激酶的疾病中的用途。
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公开(公告)号：EP2166846B1
公开(公告)日：2012-10-17
申请号：EP08768504.6
申请日：2008-06-16
发明人： ALTMAN, Michael , CHRISTOPHER, Matthew , GRIMM, Jonathan, B. , HAIDLE, Andrew , KONRAD, Kaleen , LIM, Jongwon , MACCOSS, Rachel, N. , MACHACEK, Michelle , OSIMBONI, Ekundayo , OTTE, Ryan, D. , SIU, Tony , SPENCER, Kerrie , TAOKA, Brandon , TEMPEST, Paul , WILSON, Kevin , WOO, Hyun Chong , YOUNG, Jonathan , ZABIEREK, Anna
IPC分类号： C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/6558 , A61K31/381 , A61K31/44 , A61P35/00
CPC分类号： C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/65586 , C07F9/65685
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9.发明公开CYCLOBUTYL SULFONES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权CYCLOBUTYL SULFONES作为NOTCH SPARING GAMMA SECRETASE抑制剂
公开(公告)号：EP2273877A1
公开(公告)日：2011-01-19
申请号：EP09734395.8
申请日：2009-04-17
发明人： HEIDEBRECHT, Richard, W. , LI, Chaomin , MUNOZ, Benito , ROSENAU, Andrew , SURDI, Laura, M. , TEMPEST, Paul , SILIPHAIVANH, Phieng , BRUBAKER, Jason
CPC分类号： C07C317/30 , C07C2601/04 , C07D309/12
摘要： The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-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环丁基砜衍生物，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氏病而不发展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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10.发明公开
公开(公告)号：EP3525790A2
公开(公告)日：2019-08-21
申请号：EP17859539.3
申请日：2017-10-09
发明人： RUDD, Michael, T. , MENG, Zhaoyang , WAI, Jenny , BENNETT, David Jonathan , BRNARDIC, Edward, J. , LIVERTON, Nigel, J. , STACHEL, Shawn, J. , HAN, Yongxin , TEMPEST, Paul , ZHU, Jiuxiang , XU, Xuewang , ZHU, Bin , HUANG, Chuanman
IPC分类号： A61K31/4545 , C07D401/12
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