Patent ES-8707183-A1 (ES)
Title: Benzyl, benzyloxy or benzyl:thio-di:peptide derivs.
IPC: A61K31/405
Filed: 1986-01-08
Abstract: Benzyl, benzyloxy- or benzylthio-dipeptide derivs. of the formula (I) and their salts are new W = gp. n = 0 or 1; m = 0 to 2; p and q = 0, 1 or 2 provided the sum of p and q is 1 or 2 and that in formula (V), p is not O Y = CH2, -CH2-O-, -CH2-S-attached to position 2 or 4 of the phenyl gp. Z = gp. (VI) or (VII) A = Cl or Cf3; D = -(CH2)n-, -CH2O-, -CH2S-, -CH2CONH-G = -CONR7(CH2)t- or -SO2NR7(CH2)t-; t = 0 or 1; R1 and R4 = OH, 1-8C alkoxy, K-Xr-(CH2)s-O-, -OCH2OCO(3-8C)alkyl or K = XI or XII X = 0 or S; r = 0 or 1; S = 0 to 4; M = H, halo, OH, CF3 1-6C alkoxy, 2- or 3-furyl, 2 or 3 thienyl or phenyl (opt. substd. by halo, OH, CF3, 1-6C alkoxy or 1-6C alkyl) with the proviso that when S is O then r is O; R2,R5,R6 and R9 = H or lower alkyl; R3 = H, lower alkyl or amino lower alkyl.  (12pp Dwg.No.0/0) EPAB- EP-236307 B A compound represented by formula (I) wherein W is (II)-(V); n is 0 or 1; m is 0 to 2; p and q are each 0, 1 or 2, provided that the sum of p and q is 1 or 2, and that in formula (V), p is not 0; Y is -CH2-, -CH2O-, or -CH2S-, attached at the 2 or 4 position of phenyl group; Z is (VI) or (VII) wherein A is Cl or CF3; D is -(CH2)u-, -CH2O-, -CH2S-; -CH2C(O)NH-; G is -CONR7(CH2)t-, or -SO2NR7(CH2)t-; t is 0 or 1; R1 and R4 are y hydroxy, alkoxy having from 1 to 8 carbon atoms, K-Xf-(CH2)s-O-, wherein K is phenyl, substituted phenyl, 1- or 2-naphthyl, X is oxygen or sulphur, r is 0 or 1 and s is 0 to 4, and wherein the substituents on the phenyl are chosen from group M, wherein M is halogen,  trifluoromethyl, alkoxy having 1 to 6 carbon atoms, 2-and 3-furanyl, 2- and 3-thienyl and phenyl (which phenyl group may be substituted with halogen, hydroxy, trifluoromethyl, alkoxy having from 1 to 6 carbon atoms or alkyl having from 1 to 6 carbons atoms), provided that when s is zero, r is zero, -OCH2OCO-alkyl wherein the alkyl has from 3 to 8 carbon atoms, -OCH2CO-phenyl, wherein the phenyl may be substituted with group M, 1-glyceryl, (VIII) or (IX), R2, R5, R6 and R9 are hydrogen or C1-C6 alkyl; R3 is hydrogen, C1-C6 alkyl or amino C1-C6 alkyl; R7 is hydrogen, C1-C6 alkyl or phenyl(C1-C6)alkyl; R8 is hydrogen, C1-C6 alkyl, phenyl or phenyl substituted by group M; u is 1 or 2; and the pharmaceutically acceptable salts thereof.   (36pp) - EP-236307 B A compound represented by formula (I) wherein W is (II)-(V); n is 0 or 1; m is 0 to 2; p and q are each 0, 1 or 2, provided that the sum of p and q is 1 or 2, and that in formula (V), p is not 0; Y is -CH2-, -CH2O-, or -CH2S-, attached at the 2 or 4 position of phenyl group; Z is (VI) or (VII) wherein A is Cl or CF3; D is -(CH2)u-, -CH2O-, -CH2S-; -CH2C(O)NH-; G is -CONR7(CH2)t-, or -SO2NR7(CH2)t-; t is 0 or 1; R1 and R4 are y hydroxy, alkoxy having from 1 to 8 carbon atoms, K-Xf-(CH2)s-O-, wherein K is phenyl, substituted phenyl, 1- or 2-naphthyl, X is oxygen or sulphur, r is 0 or 1 and s is 0 to 4, and wherein the substituents on the phenyl are chosen from group M, wherein M is halogen, trifluoromethyl, alkoxy having 1 to 6 carbon atoms, 2-and 3-furanyl, 2- and 3-thienyl and phenyl (which phenyl group may be substituted with halogen, hydroxy, trifluoromethyl, alkoxy having from 1 to 6 carbon atoms or alkyl having from 1 to 6 carbons atoms), provided that when s is zero, r is zero, -OCH2OCO-alkyl wherein the alkyl has from 3 to 8 carbon atoms, -OCH2CO-phenyl, wherein the phenyl may be substituted with group M, 1-glyceryl, (VIII) or (IX), R2, R5, R6 and R9 are hydrogen or C1-C6 alkyl; R3 is hydrogen, C1-C6 alkyl or amino C1-C6 alkyl; R7 is hydrogen, C1-C6 alkyl or phenyl(C1-C6)alkyl; R8 is hydrogen, C1-C6 alkyl, phenyl or phenyl substituted by group M; u is 1 or 2; and the pharmaceutically acceptable salts thereof. (36pp)