HETEROCYCLIC INTEGRIN INHIBITOR PRODRUGS

摘要

This invention relates to novel heterocycles which are useful as antagonists of the alpha v beta 3-integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic delivery of such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis. Compounds of formulas (Ia), (Ib), (Ic) including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt forms thereof, wherein X<1>, X<2>, X<3> and X<4> are independently selected from nitrogen or carbon provided that at least two of X<1>, X<2>, X<3> and X<4> are carbon; compounds of formula (Id): R<1>-Q''-W-X-Y, and pharmaceutically acceptable salt forms thereof, wherein: Q'' is selected 'inter alia' from (i), (ii), (iii), (iv), (v), (vi) compounds of formula (Ie) including enantiomeric or diastereomeric forms thereof, or mixtures of enantiomeric or diastereomeric forms thereof, or pharmaceutically acceptable salts form thereof wherein: b, the bond between carbon atoms numbered 4 and 5, is a carbon-carbon single or double bond.