New benzocycloheptenyl-alkanoic acid derivatives and analogs are selective vitronectin receptor antagonists useful e.g. for treating cardiovascular or inflammatory diseases or especially cancer

摘要

Benzocycloheptenyl-alkanoic acid derivatives (including heterocyclic analogs) (I) are new. Benzocycloheptenyl-alkanoic acid derivatives (including heterocyclic analogs) of formula (I), including their enantiomers, diastereomers and acid or base addition salts are new. G = phenyl or aromatic or partially unsaturated 6-membered heterocyclyl (containing 1 or 2 of N and O as heteroatoms), both optionally substituted by at least one R1-R4; G1, G2 = C or N; T1 = -CH2CH2-, -CH=CH- or =CHCH2-, and T2 = a direct bond, or T1 = -CH2- or =CH-, and T2 = -CH2- or =CH-; R1-R4 = halo, alkyl, perhaloalkyl, CN, NO2, OR7, NR6R6', COOR6, CONR6R6', COR6 or S(O)nR6; n = 0-2; R5 = -(CH2)m-COOR6; R6, R6' = H, alkyl, optionally substituted aryl or optionally substituted aralkyl; R7 = H or alkyl; W = -CH-, -C= or =C-, and A = CO, CH2, =CH- or -CH=, or W = N, and A = CO or CH2; X = CO-X1. CO-NR6-X1, SO2-NR6-X1 or S(O)n-X1; X1 = alkylene; Y = Y1, Y2-Y1 or Y1-Y2-Y1; Y1 = alkylene, alkenylene or alkynylene; Y2 = arylene, heteroarylene, cycloalkylene or heterocycloalkylene; Z = Z1, Z10-NR6 or Z10-NR6-CO; Z10 = alkyl or Z1; Z1 = Z2, Z20-C(=NR6), Z20-NR6 or Z20-NR6-CO; Z20 = alkyl, heteroalkyl or Z2; Z2 = heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused aryl-heteroaryl, fused aryl-heterocycloalkyl, fused heteroaryl-heterocycloalkyl or fused heteroaryl-heteroaryl (all optionally substituted); or fused cycloalkyl-heterocycloalkyl; m = 1-6; alkyl or alkylene moieties have 1-6C; heteroalkyl moieties are alkyl having one C replaced by N, O and/or S; alkenylene or alkynylene moieties have 2-6C and 1-3 double or triple bonds; cycloalkyl or cycloalkylene moieties have 3-8C; heterocycloalkyl moieties are 5-7 membered and contain 1-3 of N, O or S; aryl moieties are phenyl or naphthyl; heteroaryl moieties are mono- or bicyclic, partially or completely unsaturated and 5-11 membered, and contain 1-5 of N, O and/or S; the optional substituents on heterocycloalkyl, aryl or heteroaryl moieties are at least one of halo, alkyl, alkoxy, OH, SH, CN, NH2, mono- or dialkylamino, NO2, COOH, alkoxycarbonyl, CONH2, mono- or dialkylcarbamoyl or (in the case of heteroaryl or heterocycloalkyl) oxo. Independent claims are included for the preparation of (I).