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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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2.发明授权QUINAZOLONE DERIVATIVES AS ALPHA 1A/B ADRENERGIC RECEPTOR ANTAGONISTS 有权Quinazolones衍生物作为ALFA 1A / B肾上腺素受体拮抗剂
公开(公告)号：EP1363899B1
公开(公告)日：2005-05-11
申请号：EP01985417.3
申请日：2001-12-17
发明人： BECKER, Cyrus, Kephra , CAROON, Jon, Marie , MELVILLE, Chris, Richard , PADILLA, Fernando , PFISTER, Juerg, Roland , ZHANG, Xiaoming
IPC分类号： C07D401/04 , C07D417/04 , C07D471/04 , A61K31/549 , A61P13/08
CPC分类号： C07D417/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/04
摘要： This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by formula (I) wherein Z is -C(O)- or -S(O)2-, X is carbon or nitrogen, Y is carbon, and X-Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatise ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring; chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their preparation and their use as therapeutic agents.
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公开(公告)号：EP2691399B1
公开(公告)日：2016-07-13
申请号：EP12710724.1
申请日：2012-03-26
发明人： HERMANN, Johannes Cornelius , LOWRIE, JR., Lee Edwin , LUCAS, Matthew C. , LUK, Kin-Chun Thomas , PADILLA, Fernando , WANNER, Jutta , XIE, Wenwei , ZHANG, Xiaohu
IPC分类号： C07D513/04 , A61K31/519 , A61P19/02
CPC分类号： C07D513/04 , A61K45/06
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公开(公告)号：EP2802567A1
公开(公告)日：2014-11-19
申请号：EP13700132.7
申请日：2013-01-07
IPC分类号： C07D237/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04 , A61K31/50 , A61K31/501 , A61P11/06 , A61P29/00 , A61P37/00
CPC分类号： C07D471/04 , A61K31/50 , A61K31/501 , A61K45/06 , C07D237/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14
摘要： The present invention relates to the use of novel triazolopyridine derivatives of formula (I): wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型三唑并吡啶衍生物的用途：其中所有可变取代基如本文所述定义，其为SYK抑制剂，并且可用于治疗自身免疫和炎性疾病。
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5.发明公开QUINAZOLONE DERIVATIVES AS ALPHA 1A/B ADRENERGIC RECEPTOR ANTAGONISTS 有权Quinazolones衍生物作为ALFA 1A / B肾上腺素受体拮抗剂
公开(公告)号：EP1363899A1
公开(公告)日：2003-11-26
申请号：EP01985417.3
申请日：2001-12-17
发明人： BECKER, Cyrus, Kephra , CAROON, Jon, Marie , MELVILLE, Chris, Richard , PADILLA, Fernando , PFISTER, Juerg, Roland , ZHANG, Xiaoming
IPC分类号： C07D401/04 , C07D417/04 , C07D471/04 , A61K31/549 , A61P13/08
CPC分类号： C07D417/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/04
摘要： This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by formula (I) wherein Z is -C(O)- or -S(O)2-, X is carbon or nitrogen, Y is carbon, and X-Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatise ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring; chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their preparation and their use as therapeutic agents.
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公开(公告)号：EP2802590A1
公开(公告)日：2014-11-19
申请号：EP13700133.5
申请日：2013-01-07
发明人： CHEN, Shaoqing , HERMANN, Johannes, Cornelius , LE, Nam, T. , LUCAS, Matthew, C. , PADILLA, Fernando
IPC分类号： C07D495/04 , C07D513/04 , C07D519/00 , A61K31/519 , A61P3/10 , A61P17/06 , A61P19/02 , A61P25/28 , A61P35/00
CPC分类号： C07D495/04 , A61K31/519 , A61K45/06 , C07D513/04 , C07D519/00
摘要： The present invention relates to the use of novel compounds of Formula (I), wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式（I）的新化合物的用途，其中所有可变取代基如本文所述定义，其为SYK抑制剂且可用于治疗自身免疫和炎性疾病。
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公开(公告)号：EP2909174A1
公开(公告)日：2015-08-26
申请号：EP13777038.4
申请日：2013-10-15
发明人： BHAGIRATH, Niala , KENNEDY-SMITH, Joshua , LE, Nam, T. , LUCAS, Matthew, C. , PADILLA, Fernando , SOTH, Michael
IPC分类号： C07D213/72 , C07D401/12 , C07D239/42 , A61P35/02 , A61P25/28
CPC分类号： C07D403/12 , A61K31/44 , A61K31/50 , A61K31/501 , A61K31/506 , A61K45/06 , C07D213/72 , C07D237/24 , C07D239/557 , C07D401/12 , C07D403/04
摘要： The present invention relates to the use of novel compounds of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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公开(公告)号：EP1987035A1
公开(公告)日：2008-11-05
申请号：EP07704347.9
申请日：2007-02-05
发明人： LEMOINE, Remy , MELVILLE, Chris, Richard , PADILLA, Fernando , ROTSTEIN, David, Mark , WANNER, Jutta
IPC分类号： C07D487/04 , A61K31/407 , A61P31/12 , A61P31/18
CPC分类号： C07D487/04
摘要： Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R1-R3 R6c and X1 are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula (I).
摘要翻译： 趋化因子受体拮抗剂，特别是其中R 1 -R 3 R 6c和X 1如本文所定义的式（I）的3,7-二氮杂双环[3.3.0]辛烷化合物是趋化因子CCR5受体的拮抗剂，其可用于治疗或预防 人类免疫缺陷病毒（HIV）感染或治疗AIDS或ARC。 本发明进一步提供了用于治疗用CCR5拮抗剂减轻的疾病的方法。 本发明包括药物组合物和使用这些化合物治疗这些疾病的方法。 本发明进一步包括用于制备根据式（I）的化合物的方法。
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公开(公告)号：EP2888262A1
公开(公告)日：2015-07-01
申请号：EP13750700.0
申请日：2013-08-19
发明人： HERMANN, Johannes Cornelius , KENNEDY-SMITH, Joshua , LUCAS, Matthew C. , PADILLA, Fernando , SCHOENFELD, Ryan Craig , WOVKULICH, Peter Michael
IPC分类号： C07D487/04 , A61K31/4985 , A61P37/00 , A61P37/06 , A61P35/00 , A61P25/28 , A61P3/10 , C07D519/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/506 , A61K45/06 , C07D471/04 , C07D519/00
摘要： The present invention relates to the use of novel pyrrolo[2,3-b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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公开(公告)号：EP2773645A1
公开(公告)日：2014-09-10
申请号：EP12783182.4
申请日：2012-10-29
发明人： HERMANN, Johannes Cornelius , KUGLSTATTER, Andreas , LUCAS, Matthew C. , PADILLA, Fernando , WANNER, Jutta , ZHANG, Xiaohu
IPC分类号： C07D487/04 , A61K31/5025 , A61P29/00 , A61P19/02 , A61P17/06 , A61P3/10 , A61P37/00 , A61P11/06 , A61P25/28 , A61P35/00 , A61P35/02
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/5377 , A61K31/625 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the use of novel compounds of formula (I): wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式（I）的新化合物的用途：其中所有可变取代基如本文所述定义，其为SYK抑制剂且可用于治疗自身免疫和炎性疾病。
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