MULBAIER, MARCEL,ALONSO, JORGE,THOMSON, DOUGLAS,JANSSEN, BERND,ENCINAS LOPEZ, ARANTXA,WENDT, BERND,SCHULTES, CHRISTOPH
申请号：
CA2831356
公开号：
CA2831356A1
申请日:
2011.03.31
申请国别(地区):
CA
年份:
2012
代理人:
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.
