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1. 发明申请

WO2012130322A1 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：WO2012130322A1
公开(公告)日：2012-10-04
申请号：PCT/EP2011/055059
申请日：2011-03-31
申请人： ELARA PHARMACEUTICALS GMBH , MÜLBAIER, Marcel , ALONSO, Jorge , THOMSON, Douglas , JANSSEN, Bernd , ENCINAS LOPEZ, Arantxa , WENDT, Bernd , SCHULTES, Christoph
发明人： MÜLBAIER, Marcel , ALONSO, Jorge , THOMSON, Douglas , JANSSEN, Bernd , ENCINAS LOPEZ, Arantxa , WENDT, Bernd , SCHULTES, Christoph
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
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 CH 2 , CH 2 CH 2 or C=O; R 1 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 R 1a which are identical or different; R 2 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 R 2a which are identical or different; R 3 is hydrogen, C 1 -C 6 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkyl C(O)R 4 ; where R 1a , R 2a and R 4 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是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。

2. 发明申请

WO2012130306A1 BICYCLIC 2,3-DIHYRDOBENZAZINE COMPOUNDS FOR USE IN THERAPY 审中-公开
标题翻译：双酚2,3-二羟基苯并嗪化合物用于治疗
公开(公告)号：WO2012130306A1
公开(公告)日：2012-10-04
申请号：PCT/EP2011/054959
申请日：2011-03-30
申请人： ELARA PHARMACEUTICALS GMBH , JANSSEN, Bernd , THOMSON, Douglas , MÜLBAIER, Marcel , ALONSO, Jorge , ENCINAS-LOPEZ, Arantxa , WENDT, Bernd , SCHULTES, Christoph
发明人： JANSSEN, Bernd , THOMSON, Douglas , MÜLBAIER, Marcel , ALONSO, Jorge , ENCINAS-LOPEZ, Arantxa , WENDT, Bernd , SCHULTES, Christoph
IPC分类号： C07D413/04 , C07D417/04 , C07D419/04 , A61K31/538 , A61K31/5415 , A61P29/00
CPC分类号： C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present invention provides novel 2,3-dihydrobenzazine compounds of formula (I) and to their salts. The compounds inhibit cell proliferation and cell division and they also inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions (I) wherein X is O or S(=O)n; n is 0, 1 or 2; R 1 is an optionally substituted C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring having either 1, 2 or 3 nitrogen atoms as heteroatom ring members or 1 oxygen or 1 sulfur atom and 0, 1 or 2 nitrogen atoms as heteroatom ring members, and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring having 1, 2 or 3 heteroatom ring members selected from oxygen, sulfur and nitrogen, where sulfur atoms, if present, may be present as S, S(O) or S(O) 2 and where the saturated or unsaturated carbocyclic or heterocyclic second ring may also have 1 or 2 carbonyl groups or thiocarbonyl groups as ring members; R 2 is an optionally substituted aromatic radical selected from phenyl, C-bound mono- cyclic 5- or 6-membered heteroaryl or C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring.
摘要翻译：本发明提供新的式（I）的2,3-二氢苯并嗪化合物及其盐。这些化合物抑制细胞增殖和细胞分裂，并且还在低氧条件下（I）抑制缺氧诱导因子（HIF）介导的转录和信号传导的活化，其中X是O或S（= O）n; n为0,1或2; R1是任选取代的C结合的双环，其包含第一环，其是苯环或具有1,2或3个氮原子作为杂原子环成员或1个氧或1个硫原子的5或6元杂芳环和0 ，1或2个氮原子作为杂原子环成员，和第二个环，其与第一个环稠合，其中第二个环是5-，6-或7-元碳环或5-，6-或7 含有1,2或3个选自氧，硫和氮的杂原子环成员的杂环，其中硫原子（如果存在）可以S，S（O）或S（O）2存在，其中饱和或不饱和的碳环或杂环第二环也可以具有1或2个羰基或硫代羰基作为环成员; R2是任选取代的芳基，其选自苯基，C-结合的单环5-或6-元杂芳基或C结合的双环，其包含第一环，其是苯环或5-或6-元杂芳环，第二个环与第一个环融合，其中第二个环是5-，6-或7-元的碳环或5-，6-或7-元杂环。

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