| 摘要 |
6,7-Disubstituted 4-amino-quinazoline or quinoline derivatives (I) are new. Bicyclic heterocycles of formula (I) and their tautomers, stereoisomers and salts are new. Ra = H or T; T = 1-4C alkyl; Rb = Ph', CH2Ph' or CHMePh'; Ph' = substituted phenyl; Rc, Rd = H, F, Cl or OMe; or Me optionally substituted (os) by OMe, NMe2, NEt2, pyrrolidino, piperidino or morpholino; X = C-CN or N; A = O, NH or NT; B' = CO or SO2; C' = CH=C=CH, C=CH2 or CH=CH (all os by 1 or 2 Me or by CF3); C?=C; or CH=CHCH=CH (os by 1-4 Me or by CF3); D = Q1, COQ1, SO2Q1, COOQ2, CONR4Q2 or SO2NR4Q2 (all bonded to E via Q1 or Q2); or may also be a bond if bonded to C in E or CO or SO2 if bonded to N in E; Q1 = 1-8C alkylene (os by 1-4 F); Q2 = 1-8C alkylene; R4 = H or T; E = NR5Q3COOR6, NR5Q3P(O)(OR7)OR8 or NR5Q3P(O)(OR7)R9; Q3 = optionally substituted 1-6C n-alkylene; R5 = H, optionally substituted T; os Et or propyl, which may be terminally substituted; R6-R8 = H; os 1-8C alkyl or 4-7C cycloalkyl; alkenyl or alkynyl (both not alpha -unsaturated); or -T-cycloalkyl, Ar, -T-Ar or CReRfOCORg; Re, Rf = H or T; Rg = T, cycloalkyl, OT or 5-7C cycloalkoxy; R9 = T, Ar or -T-Ar; substituted imino; or G1; or -D-E = H, F, Cl, T (os by 1-5 F), 3-6C cycloalkyl, Ar, Het, COT, COAr, COOH, COOT, COOCReRfCOOR9, P(O)(OR7)OR8, P(O)(OR7)R9, CONH2, CONHT, CON(T)2 or COQ'4; F' = 1-6C alkylene, 1-6C oxyalkylene (linked to G via C) or O (not linked to N in G); G = G1; or as defined for E; or -F'-G = H, F, Cl, 1-6C alkoxy (os), cycloalkoxy, cycloalkylalkoxy, NH2, NHT, N(T)2 or Q'4 (other than 4-membered alkyleneimino); G1 = substituted 4-7 membered alkyleneimino, morpholino or homomorpholino, piperazino or homopiperazino, pyrrolidinyl, piperidinyl or hexahydroazepinyl; os 2-oxo-morpholinyl (linked to C in F'); morpholino or thiomorpholino 2-substituted or 2,6-disubstituted by OT etc.; Q'4 = 4-7 membered alkyleneimino (where CH2 in the 4-position may be replaced); Ar = os phenyl; Het = 5-membered heteroaryl (containing NH, O or S and optionally 1 or 2 N) os by 1 or 2 Me or Et or 6-membered heteroaryl (containing 1-3 N) os by 1 or 2 Me or Et or by halo, CF3, OH, OMe or OEt; with provisos; unless specified otherwise alkyl moieties have 1-3C, alkenyl or alkynyl moieties 3-5C and cycloalkyl moieties 3-7C. Full Definitions are given in the DEFINITIONS (Full Definitions) field. An Independent claim is included for the preparation of (I).
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