MÜLBAIER, Marcel,ALONSO, Jorge,THOMSON, Douglas,JANSSEN, Bernd,ENCINAS LOPEZ, Arantxa,WENDT, Bernd,SCHULTES, Christoph
申请号：
EPEP2011/055059
公开号：
WO2012/130322A1
申请日:
2011.03.31
申请国别(地区):
EP
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.La présente invention concerne de nouveaux composés d'imidazo[1,2-a]pyridine qui sont utiles dans le traitement de maladies et de troubles. Les nouveaux composés inhibent l'activation de la transcription médiée par le facteur induit par l'hypoxie (HIF) et la signalisation sous des conditions hypoxiques. Dans un aspect, les composés de la présente invention sont utiles pour la préparation d'un médicament pour le traitement ou la prévention d'une maladie ou d'un trouble sélectionnés dans le groupe constitué d'un trouble inflammatoire, d'une maladie ou d'un
