New di- or tetrahydro-benzoazulene derivatives, are integrin inhibitors useful e.g. for treating thrombosis, coronary heart disease, arteriosclerosis, tumors, osteoporosis or rheumatoid arthritis

摘要

6,11-Dihydro- or 2,6,11,11a-tetrahydro-benzo (cd, g) azulene derivatives (I) are new. 6,11-Dihydro- or 2,6,11,11a-tetrahydro-benzo (cd, g) azulene derivatives of formula (I) and their salts and solvates (including enantiomers and diastereomers) are new. R1 = OR4, NHR4 or N(A'')2; R2 = H, halo, NO2, NHR4, NA''2, OR4, SO3R4, SO2R4 or SR4; R3 = NH2, C(=NH)NH2 or NHC(=NH)NH2 (in which all primary amino groups are optionally protected) or -NHR5; R4 = H, A, Ar or Aralk; R5 = mono- or bicyclic heterocycle containing 1-4 of N, O and/or S (optionally substituted by 1-3 of halo, A'', COA', OA', CN, COOA', CONH2, NO2, =NH or O); A = 1-15C alkyl or 3-15C cycloalkyl in which 1-3 CH2 may be replaced by N, O and/or S, both optionally substituted by 1-3 R6; R6 = halo, NO2, NHA', NA''2, OA', phenoxy, COA', SO3A', CN, NHCOA', COOA', CONA'2 or SO2A'; A' = H or A''; A'' = 1-6C alkyl; Ar = mono- or bicyclic aromatic ring system containing 0-4 N, O and/or S (optionally substituted by 1-3 A'' and/or R6); Aralk = 7-14C aralkyl in which 1-3 CH2 may be replaced by N, O and/or S (optionally substituted by 1-3 R6); a = single or double bond; m, n = 0-4. An Independent claim is included for the preparation of (I).