| 摘要 |
(A) Carbacycline derivs. of formulae (X) and (X1) are new. n is 1 or 2. L1 is alpha-R3, beta-R4; beta-R3 or a mixt. of both; R3 and R4 being each H, methyl or fluoro, M1 is alpha-hydroxy, beta-R5 or alpha-R5, beta-hydroxy; R5 being H or methyl. R7 is CmH2m. CH3 (m is 1-5); phenoxy opt. substd. by 1-3 of chloro, fluoro, trifluoromethyl, 1-3C alkyl or alkoxy phenyl, benzyl, phenethyl or phenylpropyl, all opt. ring-substd. as phenoxy; cis-CH=CH.CH2.CH3; (CH2)2. CH(OH).CH3 or (CH2)3.CH=C(CH3)2. R8 is H, hydroxymethyl or hydroxy. R15 is H or fluoro R16 is hydrogen or together with R17 is methylene. R17 is H or 1-4C alkyl. R20, R21, R22, R23 or R4 can all be H (2 R22 alpha or beta); or R20 is H, R21 and R33 form a second C-C bond, and R23 and R24 form a second bond or are both H; or R22, R23 and R24 are all H (R22 alpha or beta) and R21 and R20 are together oxo, or R20 is H and R21 alpha or beta hydroxy. X1 is COOR1, hydroxymethyl, COL4, or CH2NL2L3 or R1 is a cation. L4 is NR51R52; pyrrolidino, piperidino, morpholino, piperazino, hexamethyl eneimino, pyrrolino or 3,4-didehhydropiperidinyl (opt. substd). N(R53).COR51 or N(R53).SO2.R51 R51 and R52 are H, 1-12C alkyl, 3-10C cycloalkyl, 7-12C aralkyl, phenyl (opt. substd. by 1-3 chloro, 1-3C alkyl, hydroxy, carboxy, 2-5C alkoxycarbonyl or nitro), 2-5C (carboxy-, carbamoyl- or cyano) alkyl, 3-6C acetyl alkyl, 7-11C benzo(sic)alkyl (opt.substd) pyridyl (opt. substd). 6-9C pyridylalkyl (opt. substd.) or is 1-4C mono- di- or tri-hydroxyalkyl; at most one of R51 and R52 is H or alkyl. R53 is H or 1-4C alkyl, and is N(R3). COR51, R51 cannot be H. L2 and L3 are H or 1-4C alkyl. Y is cis or trans vinylene, ethylene or CC Z1 is CH2.(CH2)f. C(R2)2; trans-CH2. CH=CH, or -Ph-(CH2)g R2 is H or fluoro f is 0-3, Ph is 1,2-,1,3- or 1,4-phenylene. g is 0-3. (X) and (X1) are useful in human and veterinary medicine as antithromotics, antiulcer agents (reducing acid secretion and counteracting effects of non-steroidal antiinflam |
