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1. 发明申请

US20120095012A1 TOLUIDINE SULFONAMIDES AND THEIR USE 审中-公开
标题翻译：托洛芬磺酰胺及其用途
公开(公告)号：US20120095012A1
公开(公告)日：2012-04-19
申请号：US13142518
申请日：2009-12-30
申请人： Jorge Alonson , Arantxa Encinas Lopez , Marcel Muelbaier , Jochen Ammenn , Bernd Wendt , Joe Lewis , Christoph Schultes , Bernd Janssen
发明人： Jorge Alonson , Arantxa Encinas Lopez , Marcel Muelbaier , Jochen Ammenn , Bernd Wendt , Joe Lewis , Christoph Schultes , Bernd Janssen
IPC分类号： A61K31/4436 , A61K31/381 , C07D213/71 , A61K31/44 , C07D333/34 , A61K31/4178 , C07D413/12 , A61K31/422 , A61P9/10 , A61P19/02 , A61P11/06 , A61P1/00 , A61P17/06 , A61P37/06 , A61P35/00 , A61P7/00 , A61P35/02 , A61K31/443 , A61K31/506 , C07D401/12 , A61K31/4439 , A61K31/501 , C07D403/12 , A61K31/4025 , A61K31/4245 , A61K31/444 , A61P17/00 , A61P29/00 , C07D409/12
CPC分类号： C07D409/12 , C07D207/36 , C07D213/71 , C07D239/38 , C07D241/18 , C07D307/64 , C07D333/34 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
摘要翻译：本发明提供式（I）化合物，其中R 1是单环的5或6元杂芳基; R4是苯基或单环的5或6元杂芳基; 和权利要求中定义的其它取代基，其在缺氧条件下抑制细胞和细胞分裂并抑制缺氧诱导因子（HIF）介导的转录和信号传导的活化。一方面，本发明的化合物可用于制备用于治疗或预防选自以下的疾病或病症的药物：炎性疾病，过度增殖性疾病或病症，缺氧相关病理学和一种以血管过度为特征的疾病。还提供了一种药物组合物，其包含可用于治疗或预防所述疾病或病症的本发明化合物和第二治疗剂或辐射。

2. 发明申请

US20140221354A1 IMIDAZO [1,2-a]PYRIDINE COMPOUNDS FOR USE IN THERAPY 审中-公开
标题翻译：咪达唑[1,2-a]吡啶化合物用于治疗
公开(公告)号：US20140221354A1
公开(公告)日：2014-08-07
申请号：US14007613
申请日：2011-03-31
申请人： Marcel Mulbaier , Jorge Alonso , Douglas Thomson , Bernd Janssen , Arantxa Encinas Lopez , Bernd Wendt , Christoph Schultes
发明人： Marcel Mulbaier , Jorge Alonso , Douglas Thomson , Bernd Janssen , Arantxa Encinas Lopez , Bernd Wendt , Christoph Schultes
IPC分类号： C07D471/04 , A61K31/496 , A61K45/06 , A61K31/551
CPC分类号： C07D471/04 , A61K31/496 , A61K31/551 , A61K45/06
摘要： The present invention provides novel imidazo[1,2-a]pyridine compounds that are useful in therapy of diseases and disorders. The novel compounds inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders, wherein X is CH2, CH2CH2 or C═O; R1 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R1a which are identical or different; R2 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R2a which are identical or different; R3 is hydrogen, C1-C6-alkyl, C1-C4-alkoxy-C1-C4-alkyl, fluorinated C1-C2-alkyl C(O)R4; where R1a, R2a and R4 are as defined in the claims and the specification.
摘要翻译：本发明提供可用于治疗疾病和病症的新的咪唑并[1,2-a]吡啶化合物。该新型化合物在低氧条件下抑制缺氧诱导因子（HIF）介导的转录和信号传导的活化。一方面，本发明的化合物可用于制备用于治疗或预防选自以下的疾病或病症的药物：炎性疾病，过度增殖性疾病或病症，缺氧相关病理学和一种以血管过度为特征的疾病。还提供了包含本发明化合物和第二治疗剂或辐射的药物组合物，其可用于治疗或预防所述疾病或病症，其中X为CH 2，CH 2 CH 2或C = O; R 1是苯基或C键的单环5或6元杂芳基，其中苯基和单环5或6元杂芳基是未取代的或带有相同或不同的1,2,3,4或5个基团R 1a; R 2是苯基或C结合的单环5或6元杂芳基，其中苯基和单环5或6元杂芳基是未取代的或带有相同或不同的1,2,3,4或5个基团R2a; R 3是氢，C 1 -C 6烷基，C 1 -C 4烷氧基-C 1 -C 4烷基，氟化C 1 -C 2烷基C（O）R 4; 其中R1a，R2a和R4如权利要求和说明书中所定义。

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