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still to framstella pharmacologically active derivatives of 2 - karboxialkyl - 4,4dimetyl - pyrrolidine - 5 - on
still to framstella pharmacologically active derivatives of 2 - karboxialkyl - 4,4dimetyl - pyrrolidine - 5 - on
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机译:尚对金银花的2-羧基烷基-4,4二甲基-吡咯烷-5-的药理活性衍生物。
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摘要
Compounds of the formula (I) are disclosed (I) wherein preferably n is 4 to 8, X is CO, protected CO or CHOH wherein the OH moiety may be protected; R1 is hydrogen, or CO2R1 represents an ester group in which the R1 moiety contains from 1 to 12 carbon atoms; R3 is hydroxy or protected hydroxy; R2 is H, C1-4 alkyl, phenyl or phenyl substituted with one or more halogen, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy or nitro groups; R4 is C4-9 alkyl, phenyl, phenyl C1-6 alkyl, or phenyl or C1-6 alkyl substituted by one or more halogen, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy or nitro groups; A is hydrogen or methyl; and salts thereof. The compounds have useful pharmacological properties including anti-gastric secretion, bronchodilator and platelet aggregation inhibition activities. Methods of preparation are also disclosed.
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机译:公开了式(I)化合物(I),其中n优选为4至8,X为CO,被保护的CO或CHOH,其中OH部分可以被保护; R 1是氢,或CO 2 R 1代表其中R 1部分含有1至12个碳原子的酯基; R3是羟基或被保护的羟基; R 2是H,C 1-4烷基,苯基或被一个或多个卤素,三氟甲基,C 1-6烷基,C 1-6烷氧基或硝基取代的苯基; R4是C4-9烷基,苯基,苯基C1-6烷基或被一个或多个卤素,三氟甲基,C1-6烷基,C1-6烷氧基或硝基取代的苯基或C1-6烷基; A是氢或甲基;及其盐。该化合物具有有用的药理特性,包括抗胃分泌,支气管扩张剂和血小板聚集抑制活性。还公开了制备方法。
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