New 2-substd. thieno-triazolo-di:azepine derivs. - are inhibitors of platelet activating factor for treating inflammation etc., and new organo-metallic intermediates

摘要

Thienodiazepine derivs of formulae (Ia) and (Ib) their racemates, enantiomers, diastereomers (or mixts) and their physiologically acceptable acid addn salts are new, R1 = H, 1-4C alkyl (opt substd by halo or 0H), cyclopropyl, cyclobutyl, 1-4C alkoxy, or halo; R2 = Ra-A-C(Rb)(0H)-, Ra-B Ra-B-CRc=CRb-, Rd-N=CH-, Re-D-CH2-; Rf-0-S02-, R8R9N-S02-, CH0 or C00H; R3 = phenyl (opt substd by 1 or more Me, halo, N02 and/or CF3) etc, R4 = H, 1-4C alkyl or acyl or HC0; R5 = H, 0H, 1-6C alkyl (opt substd by 0H, alkylsulphonyl oxy, NR8R9 or C0NR12R13), 1-4C alkylcarbonyloxy, 1-4C alkoxycarbonyl, 1-4C carboxy- or alkoxycarbonyl-substd alkyl; X and Y = CR1 or N, but not both CR1; or Y = C-C00R1 and X=N; A = 0-8C opt branched alkylene; B= 0-7C opt branched alkylene; D = 0, S or NH+ Ra = H; 1-4C alkyl (opt substd by halo) etc; Rc = H, aryl, substd phenyl or 1-4C alkyl; Rd = 1-10C alkyl, alkenyl or alkynyl etc; Re is as Rd when D = NH, but otherwise is 1-8C alkyl (opt substd by phenyl, opt substd) or opt substd phenyl; R6 and R7 = H; 1-10C alkyl, alkenyl or alkynyl (opt substd by halo, C00H, 1-6C alkoxycarbonyl, phenyl (opt substd); Rf = opt substd phenyl or heteroaryl; R8 = H; 1-10C alkyl, alkenyl or alkynyl etc; R9 is as R8, or R9 and R8 together are a heterocycle as R6 and R7; R10 and R11 = H; phenyl (opt substd); 3-6C cycloalkyl (opt substd); 1-10C alkyl alkenyl or alkynyl R10' and R11' = R10 and R11 R1r = H,C& @- &DH-) --"+"N---FTAI D---j-- -R"l---C'd-< -R(C(--c H-W$ 1-4C alkyl or alkoxy, or (i) P1 = 01-18C alkyl, alkenyl or alkynyl (opt substd by halo, 0H, N02, opt substd amine, alkoxy, or when R13 = H or alkyl, by ester residue; R13 is as R12 or a C- or N-bound, 5-7 membered heterocycle, satd or unsatd and opt substd by 1 or more 1-4C alkyl; R12 and R13 may together be a heterocycle as R6 and R7; R112 and R113 are as R12 and R13; R1 = H or alkyl. USE - (Ia)and (Ib), are antagonists of platelet-inhibiting factor.