JANSSEN, Bernd,THOMSON, Douglas,MÜLBAIER, Marcel,ALONSO, Jorge,ENCINAS-LOPEZ, Arantxa,WENDT, Bernd,SCHULTES, Christoph
申请号：
EPEP2011/054959
公开号：
WO2012/130306A1
申请日:
2011.03.30
申请国别(地区):
WO
年份:
2012
代理人:
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 R1 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 R2 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.La présente invention concerne des nouveaux composés de 2,3-dihydrobenzazine de formule I et leurs sels. Les composés inhibent la prolifération cellulaire et la division cellulaire ils inhibent également lactivation de la transcription induite par le facteur inductible par lhypoxie (HIF) et de la signalisation dans des conditions dhypoxie. Dans la formule (I) X représente O ou S(=O)n n vaut 0, 1 ou 2 R1 représente bicyclyle lié par C éventuellement substitué comprenant un premier cycle qui est un cycle b
