The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.
N-[HETEROARYLCARBONYL]-3-THIENYL-L-ALANINE DERIVATIVES AS a5beta1 ANTAGONISTS
申请人:ARNOULD Jean-Claude
公开号:US20080255183A1
公开(公告)日:2008-10-16
The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins.
Compositions useful for carrying physiologically active agents such as therapeutic agents through skin and other body membranes comprising the agent and an effective, non-toxic amount of a compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group, m is 3-7, N is 0-17 and R is --CH.sub.3, phenyl or substituted phenyl or ##STR2## with the proviso that if m is 3 and R is --CH.sub.3, then n is not 0-6.
Compositions useful for carrying physiologically active agents such as therapeutic agents through skin and other body membranes comprising the agent and an effective, non-toxic amount of a compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group, m is 3-7, N is 0-17 and R is --CH.sub.3, phenyl or substituted phenyl or ##STR2## with the proviso that if m is 3 and R is --CH.sub.3, then n is not 0-6.