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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：EP1987036A1
公开(公告)日：2008-11-05
申请号：EP07704382.6
申请日：2007-02-06
IPC分类号： C07D487/04 , A61K31/407 , A61P29/00 , 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-1) 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 treating diseases mediated by the CCR5 receptor.
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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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公开(公告)号：EP2691399A1
公开(公告)日：2014-02-05
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
摘要： The present invention relates to the use of novel pyrrolopyrazine 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的新型吡咯并吡嗪衍生物的用途：其中所有可变取代基如本文所述定义，其为SYK抑制剂且可用于治疗自身免疫疾病和炎性疾病。
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公开(公告)号：EP2864330A1
公开(公告)日：2015-04-29
申请号：EP13729367.6
申请日：2013-06-18
IPC分类号： C07D487/04 , A61K31/495 , A61K31/4985 , A61P35/00
CPC分类号： C07D487/04
摘要： There are provided compounds of the formula (I), wherein R
1 and R
2 are as described herein. The compounds are useful as inhibitors of tankyrase in the treatment of cancer.摘要翻译： 提供了式（I）的化合物，其中R 1和R 2如本文所述。 该化合物可用作治疗癌症的坦科聚合酶抑制剂。
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公开(公告)号：EP2709997A1
公开(公告)日：2014-03-26
申请号：EP12721812.1
申请日：2012-05-14
发明人： BILLEDEAU, Roland J. , KONDRU, Rama K. , LOPEZ-TAPIA, Francisco Javier , LOU, Yan , OWENS, Timothy D. , QIAN, Yimin , SO, Sung-Sau , THAKKAR, Kshitij Chhabilbhai , WANNER, Jutta , MORALES, Omar Jose
IPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D413/10 , C07D417/10 , C07D471/04 , A61K31/502 , A61P29/00 , A61P37/00
CPC分类号： C07D405/10 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04
摘要： This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
摘要翻译： 该申请公开了根据通式（I）的化合物，其中所有变量如本文所述定义，其抑制Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过度Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎性和自身免疫疾病，如类风湿性关节炎。 还公开了含有式（I）化合物和至少一种载体，稀释剂或赋形剂的组合物。
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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：EP2709997B1
公开(公告)日：2016-06-29
申请号：EP12721812.1
申请日：2012-05-14
发明人： BILLEDEAU, Roland J. , KONDRU, Rama K. , LOPEZ-TAPIA, Francisco Javier , LOU, Yan , OWENS, Timothy D. , QIAN, Yimin , SO, Sung-Sau , THAKKAR, Kshitij Chhabilbhai , WANNER, Jutta , MORALES, Omar Jose
IPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D413/10 , C07D417/10 , C07D471/04 , A61K31/502 , A61P29/00 , A61P37/00
CPC分类号： C07D405/10 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04
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9.发明公开OCTAHYDROPYRROLO [3, 4-C] PYRROLE DERIVATIVES AND THEIR USE AS ANTIVIRAL AGENTS 有权八氢 - 吡咯并[3,4-C]吡咯和它们作为抗病毒剂的
公开(公告)号：EP2066674A1
公开(公告)日：2009-06-10
申请号：EP07803370.1
申请日：2007-09-10
IPC分类号： C07D487/04 , A61K31/407 , 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 and Ar 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).
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10.发明公开PYRAZOLO [1, 5A]PYRIMIDINE AND THIENO [3, 2B]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS 有权吡咯并[1,5A]吡啶并[3,2,2]嘌呤霉素衍生物，IRAK4-MODULATOREN
公开(公告)号：EP2593457A1
公开(公告)日：2013-05-22
申请号：EP11736028.9
申请日：2011-07-08
发明人： ARORA, Nidhi , CHEN, Shaoqing , HERMANN, Johannes, Cornelius , KUGLSTATTER, Andreas , LABADIE, Sharada, Shenvi , LIN, Clara Jeou Jen , LUCAS, Matthew, C. , MOORE, Amy, Geraldine , PAPP, Eva , TALAMAS, Francisco, Xavier , WANNER, Jutta , ZHAI, Yansheng
IPC分类号： C07D487/04 , C07D495/04 , A61K31/4365 , A61K31/519 , A61P11/00 , A61P29/00
CPC分类号： C07D495/04 , C07D487/04
摘要： Compounds of the formula I or II: wherein X, m, Ar, R
1 and R
2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.摘要翻译： 式I或II的化合物：其中X，m，Ar，R 1和R 2如本文所定义。 本发明化合物可用于治疗IRAK介导的病症。
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