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公开(公告)号：EP1957454A1
公开(公告)日：2008-08-20
申请号：EP06819599.9
申请日：2006-11-20
发明人： CONNOLLY, Terrence Joseph , FARRELL, Robert P. , HUMPHREYS, Eric R. , LYNCH, Stephen M. , SARMA, Keshab
IPC分类号： C07D209/14
CPC分类号： C07D209/14 , C07D209/18
摘要： A method comprising: hydrogenating an indole propionamide compound of formula h with vitride, to form an aminopropyl indole compound of formula I wherein m, Ar, R1 and R2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
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公开(公告)号：EP2763990A1
公开(公告)日：2014-08-13
申请号：EP12761923.7
申请日：2012-08-27
发明人： CHEN, Shaoqing , DE VICENTE FIDALGO, Javier , HAMILTON, Matthew Michael , HERMANN, Johannes Cornelius , KENNEDY-SMITH, Joshua , LI, Hongju , LOVEY, Allen John , LUCAS, Matthew C. , LUK, Kin-Chun Thomas , LYNCH, Stephen M. , O'YANG, Counde , PADILLA, Fernando , SCHOENFELD, Ryan Craig , SIDDURI, Achyutharao , SOTH, Michael , WANG, Ce , WOVKULICH, Peter Michael , ZHANG, Xiaohu
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/5025 , A61P29/00
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量如本文所述定义，其抑制JAK和SYK并可用于治疗自身免疫和炎性疾病。
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公开(公告)号：EP2550273A2
公开(公告)日：2013-01-30
申请号：EP11711061.9
申请日：2011-03-18
发明人： HENDRICKS, Robert Than , HERMANN, Johannes Cornelius , KONDRU, Rama K. , LOU, Yan , LYNCH, Stephen M. , OWENS, Timothy D. , SOTH, Michael
IPC分类号： C07D487/04 , C07D519/00 , A61K31/4985 , A61P29/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables n, p, q, Q, X, X' and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
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公开(公告)号：EP2925765A1
公开(公告)日：2015-10-07
申请号：EP13798328.4
申请日：2013-11-29
CPC分类号： C07F5/025
摘要： The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐。 另外，本发明涉及制备和使用式I化合物的方法以及含有这些化合物的药物组合物。 式I化合物是LMP7抑制剂，并且可用于治疗相关的炎症性疾病和病症，例如类风湿性关节炎，狼疮和肠易激惹起的疾病。
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公开(公告)号：EP1957488B1
公开(公告)日：2009-09-09
申请号：EP06819602.1
申请日：2006-11-20
发明人： GREENHOUSE, Robert , JAIME-FIGUEROA, Saul , LYNCH, Stephen M. , RAPTOVA, Lubica , STEIN, Karin Ann , WEIKERT, Robert James
IPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , A61K31/395 , A61K31/437 , A61P25/22 , A61P25/24
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14
摘要： The present invention provides compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds. The compounds are useful for the treatment of diseases associated with monoamine reuptake inhibitors.
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公开(公告)号：EP2925746A1
公开(公告)日：2015-10-07
申请号：EP13796097.7
申请日：2013-11-29
发明人： LYNCH, Stephen M. , MARTIN, Rainer E. , NEIDHART, Werner , PLANCHER, Jean-Marc , SCHULZ-GASCH, Tanja
IPC分类号： C07D403/12 , A61K31/415 , A61K31/4164 , A61K31/4192 , A61K31/4196 , C07D233/90 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12 , C07D249/04 , C07D249/10 , A61P19/02 , A61P1/00
CPC分类号： C07D249/04 , C07D233/90 , C07D249/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
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公开(公告)号：EP1957454B1
公开(公告)日：2011-07-20
申请号：EP06819599.9
申请日：2006-11-20
发明人： CONNOLLY, Terrence Joseph , FARRELL, Robert P. , HUMPHREYS, Eric R. , LYNCH, Stephen M. , SARMA, Keshab
IPC分类号： C07D209/14
CPC分类号： C07D209/14 , C07D209/18
摘要： A method comprising: hydrogenating an indole propionamide compound of formula h with vitride, to form an aminopropyl indole compound of formula I wherein m, Ar, R1 and R2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
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公开(公告)号：EP2571881A1
公开(公告)日：2013-03-27
申请号：EP11721743.0
申请日：2011-05-17
发明人： HENDRICKS, Robert Than , HERMANN, Johannes Cornelius , KONDRU, Rama K. , LOU, Yan , LYNCH, Stephen M. , OWENS, Timothy D. , SOTH, Michael , YEE, Calvin Wesley
IPC分类号： C07D487/04 , A61K31/4965 , A61K31/497 , A61P29/00 , A61P37/00 , A61P35/00 , A61P25/00 , A61P9/00 , A61P3/00 , A61P11/00 , A61P19/00
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R
1 and R
2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.摘要翻译： 本发明涉及式（I）的新型吡咯并吡嗪衍生物的用途，其中变量Q和R 1和R 2如本文所述定义，其抑制JAK和SYK并可用于治疗自身免疫和炎症 疾病。
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公开(公告)号：EP1957488A1
公开(公告)日：2008-08-20
申请号：EP06819602.1
申请日：2006-11-20
发明人： GREENHOUSE, Robert , JAIME-FIGUEROA, Saul , LYNCH, Stephen M. , RAPTOVA, Lubica , STEIN, Karin Ann , WEIKERT, Robert James
IPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , A61K31/395 , A61K31/437 , A61P25/22 , A61P25/24
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14
摘要： The present invention provides compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds. The compounds are useful for the treatment of diseases associated with monoamine reuptake inhibitors.
摘要翻译： 本发明提供了式I化合物或其药学上可接受的盐，溶剂合物或前药，其中p，Ar，R 1，R 2，R 3，R a，R b，R c，R d和R e如本文所定义。 还提供了药物组合物，使用方法和制备该化合物的方法。 该化合物可用于治疗与单胺再摄取抑制剂有关的疾病。
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