| 摘要 |
Amino substituted heterobicyclic and heteropolycyclic compounds of formula (I) and their salts are new: A = 5-10 membered mono- or polycyclic, aromatic or non-aromatic ring (optionally containing 1-4 N, O and/or S and optionally substituted by one or more of R<12>-R<15>; B = direct bond; or alkyl, -CR<2>=CR<2>-, 5-10C aryl, 3-8C cycloalkyl, -C</>C-, -NR<2>-, -NR<2>-C(O)-, -NR<2>-C(Q)-NR<2>-, -O-C(O)-, -NR<2>-S(O)n-, -Q- or -CR<2>=CR<3>- (all optionally mono- or disubstituted by alkyl), e.g. Me-Ph-Me or -Et-NR<2>-C(O)-; Q = O or S; n = 1 or 2; D, F = direct bond or alkyl, 5-10C aryl, -Q-; -NR<2>-, -CO-NR<2>-, -NR<2>-CO-, -NR<2>-C(Q)-NR<2>-, -O-C(O)-,-C(O)-O-, -S(O)n, -S(O)n-NR<2>, -NR<2>-S(O)n, -CR<2>=CR<3>- or -C IDENTICAL C- (all optionally mono- or disubstituted by alkyl, -CR<2>-CR<2>- or 5-6C aryl); provided that D is not -CO-NR<2>-, -C(O)-O-, -S(O)n or -S(O)n-NR<2> if B is a direct bond; E = template of a fibrinogen receptor antagonist; G = -CR<4>R<5>-(CR<6>R<7>)p-(CH2)q-R<10>; R<2>, R<3> = H; 1-10C alkyl (optionally substituted by 1 or more F); 3-12C cycloalkyl; 3-12C cycloalkyl-alkyl; aryl; aryl-alkyl; R<8>OC(O)R<9>; R<8>R<8>NC(O)R<9>; or R<6>C(O)R<9>; R<4>-R<7> = H; F; OH; alkyl; cycloalkyl; cycloalkyl-alkyl; R<8>QR<9>; R<8>CO2R<9>; R<8>OC(O)R<9>; R<8>-aryl-R<9>; R<8>N(R<2>)R<9>; R<8>R<8>NR<9>; R<8>N(R<2>)CO(O)R<9>; R<8>S(O)-N(R<2>)R<9>; R<8>QC(O)N(R<2>)R<9>; R<8>C(O)N(R<2>)R<9>; R<8>N(R<2>)C(O)N(R<2>)R<9>; R<8>N(R<2>)S(O)N(R<2>)R<9>; R<8>S(O)nR<9>; R<8>C(O)R<9>; R<8>N(R<2>)C(O)R<9>; or R<8>N(R<2>)S(O)nR<9>; R<8> = H; Alk; cycloalkyl; cycloalkyl-Alk; aryl; or aryl-Alk; Alk = alkyl (optionally substituted by one or more F); R<9> = direct bond or alkyl; R<10> = C(Q)R<11>; S(O)-NR<11>; P(O)nR<11>; or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S, e.g. tetrazolyl, imidazolyl, pyrazolyl, oxazolyl or thiadiazolyl; R<11> = OH; alkoxy, aryl-alkoxy; aryloxy; alkylcarbonyloxy-(1-4C) alkoxy; aryl-alkylcarbonyloxy-(1-6C) alkoxy; NH2; NH(alkyl); N(alkyl)2; aryl-alkylamino; dialkylaminocarbonylmethoxy; aryl-dialkylaminocarbonylmethoxy; arylamino; or a L- or D-aminoacid; R<12>-R<15> = H; 1-10C alkyl (optionally substituted by one or more F); 3-12C cycloalkyl; 3-12C cycloalkyl-alkyl; aryl; aryl-alkyl; NH2; R<8>ONR<9>; R<8>OR<9>; R<8>OC(O)R<9>; R<8>R<8>NR<9>; R<8>-aryl-R<9>; HO-alkyl-N(R<2>)R<9>; R<8>N(R<2>)C(O)R<9>; R<8>C(O)N(R<2>)R<9>; R<8>C(O)R<9>; R<2>R<3>N-C(=NR<2>)-NR<2>; R<2>R<3>N-C(=NR<2>); or Q; or two adjacent R<12>-R<15> substituents form -O-(CH2)n-O-; Y = NR<2> or Q; p, q = 0 or 1; unless specified otherwise alky moieties have 1-8C, cycloalkyl moieties 3-14C and aryl moieties 5-14C; the compounds where E is a 6-membered aromatic ring (optionally containing 1-4 N atoms and/or 1-4 substituents) and the compound 4-methyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine are excluded. |
