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prostacyclinanalog, this active component containing the blutumlauf corrective means and against magengeschwuere acting means.

机译:前列环素类似物,该活性成分含有blutumlauf矫正剂和抗magengeschwuere作用剂。

摘要

A prostacyclin analogue having the formula: IMAGE (I) wherein R1 is -CO2R5 (wherein R5 is a hydrogen atom, a straight chain or branched alkyl group having from 1 to 12 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted phenyl group, or one equivalent of a cation), or -CONR6R7 (wherein each of R6 and R7 is a hydrogen atom or an alkyl group having from 1 to 10 carbon atoms, or R6 and R7 together with the adjacent nitrogen atom, form a 5- or 6-membered substituted or unsubstituted hetero ring which may contain a hetero atom other than said nitrogen atom); A is -CH2CH2CH2-, CH2-O-CH2CH2-, -CH2CH2CH2CH2-, -CH2CH2-O-CH2- or -CH=CHCH2CH 2-; B is trans -CH=CH- or -C 3BOND C-; R2 is a straight chain or branched alkyl group having from 3 to 10 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a straight chain or branched alkenyl group having from 3 to 12 carbon atoms, a straight chain or branched alkynyl group having from 3 to 8 carbon atoms, or an alkyl group having from 1 to 3 carbon atoms substituted by a substituted or unsubstituted phenyl or phenoxy group, by an alkoxy group having from 1 to 6 carbon atoms or by a cycloalkyl group having from 5 to 8 carbon atoms; R3 is a hydrogen atom, a methyl group or a vinyl group; and R4 is a hydrogen atom, an acyl group having from 1 to 7 carbon atoms, a tri-C1-C7 hydrocarbon-silyl group or a group capable of forming an acetal bond together with the oxygen atom of a hydroxyl group; provided that the double bond in a substituent for A is E or Z, or a mixture thereof; the asymmetric center in a substituent for R2 assumes a R-conformation or a S-conformation, or a mixture thereof; and the bonds shown by dotted lines at the 2-3 and 3-4 positions mean that either one of them is a double bond.
机译:具有下式的前列环素类似物:(I)其中R1为-CO2R5(其中R5为氢原子,具有1至12个碳原子的直链或支链烷基,具有7至12个碳原子的芳烷基原子,具有4至7个碳原子且未被取代或被至少一个具有1至4个碳原子的烷基取代的环烷基,经取代或未经取代的苯基或一当量的阳离子)或-CONR6R7(其中R 6和R 7各自为氢原子或具有1至10个碳原子的烷基,或R 6和R 7与相邻的氮原子一起形成可含有杂原子的5或6元取代或未取代的杂环所述氮原子以外的原子); A为-CH 2 CH 2 CH 2-,CH 2 -O-CH 2 CH 2-,-CH 2 CH 2 CH 2 CH 2-,-CH 2 CH 2 -O-CH 2-或-CH = CHCH 2 CH 2-。 B是反式-CH = CH-或-C 3BOND C-; R 2为具有3至10个碳原子的直链或支链烷基,具有4至7个碳原子并且未被取代或被至少一个具有1至4个碳原子的烷基取代的环烷基,直链或支链具有3至12个碳原子的烯基,具有3至8个碳原子的直链或支链炔基,或具有1至3个碳原子的被取代或未取代的苯基或苯氧基取代的烷基,被烷氧基取代具有1至6个碳原子的基团或具有5至8个碳原子的环烷基; R3是氢原子,甲基或乙烯基; R4为氢原子,碳原子数为1至7的酰基,三碳原子数为1〜7的烃基甲硅烷基或能够与羟基的氧原子一起形成缩醛键的基团。前提是A的取代基中的双键是E或Z,或其混合物; R 2的取代基中的不对称中心为R构型或S构型,或它们的混合物。并且在2-3和3-4位置用虚线显示的键表示其中一个是双键。

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