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    • 11. 发明授权
    • Lipid lowering alkylene glycols and ester derivatives thereof
    • 脂质降解亚烷基二醇及其酯衍生物
    • US4275068A
    • 1981-06-23
    • US48536
    • 1979-04-23
    • Kurt ThieleQuazi AhmedUlrich JahnRudolf Adrian
    • Kurt ThieleQuazi AhmedUlrich JahnRudolf Adrian
    • C07D213/80A61K31/455A61K31/60C07C69/90
    • C07D213/80
    • Novel alkylene glycol derivatives of the formula (1) ##STR1## in which R.sup.1 is the hydrogen atom, an alkyl group having 1-4 C-atoms or an aryl group, R.sup.2 is the hydrogen atom or an alkyl group having 1-4 C-atoms, R.sup.3 is the hydrogen atom or a group of the formula ##STR2## in which Z is an alkyl residue, an optionally substituted aryl residue or a heterocyclic residue and R.sup.4 is a residue of the formula ##STR3## in which R.sup.5 is the hydrogen atom or chlorine atom, or the methyl group, exhibit an advantageous activity in regard of lowering the cholesterol and triglyceride level in the blood. Production of the novel derivatives by reduction of the corresponding acids, or by reacting a phenol of the formula ##STR4## and an alcohol of the formula ##STR5## optionally with subsequent esterification, is described.
    • 式(1)的新型亚烷基二醇衍生物其中R1是氢原子,具有1-4个碳原子的烷基或芳基,R2是氢原子或具有1个碳原子的烷基 -4个C原子,R3是氢原子或其中Z是烷基残基,任选取代的芳基残基或杂环残基的式“IMAGE”的基团,R4是式“IMAGE”的残基,其中 R5是氢原子或氯原子或甲基,在降低血液中的胆固醇和甘油三酯水平方面表现出有利的活性。 描述了通过还原相应的酸或通过使式(IMAGE)的酚与式(IMAGE)的醇任选地随后的酯化反应制备新衍生物。
    • 19. 发明授权
    • Cholesterol-lowering phenoxyalkanoic acid esters
    • US4153803A
    • 1979-05-08
    • US773144
    • 1977-03-01
    • Kurt ThieleQuazi AhmedRudolf AdrianUlrich Jahn
    • Kurt ThieleQuazi AhmedRudolf AdrianUlrich Jahn
    • A61K31/22C07C59/68C07C59/70C07C69/712C07C69/736C07D211/46C07D213/30C07D473/08C07C69/76
    • C07C321/00C07C59/68C07C59/70C07D211/46C07D473/08
    • Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: ##STR1## wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A.sup.1 and A.sup.2 contain together not more than 10 carbon atoms,Y is oxygen, in which case X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiary aminoalkoxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, or X is hydrogen and Z is pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, orY is oxygen, X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is alkoxy containing from 1 to 4 carbon atoms, hydroxy or O.sup.- M.sup.+, M being a metal cation of Main Groups I, II or III of the Periodic System of the Elements or an organic base cation or ammonium ion, A.sup.1 and A.sup.2 being the same and being as aforesaid or being different with one of A.sup.1 and A.sup.2 being hydrogen or both being hydrogen and X being a para substituent with respect to Y in the benzene ring in the same general formula,Y is oxygen, X is hydrogen and Z is amine, azacyclohydrocarbyloxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms,Or Y is sulphur, in which case X is hydrogen, benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy, alkoxy containing from 1 to 4 carbon atoms, hydroxy, O.sup.- M.sup.+ wherein M is a metal cation of Main Groups I, II or III of the Periodic System of The Elements or an organic base cation or ammonium ion, cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiaryaminoalkoxy, pivaloyloxyalkoxy or pyridyl-C-alkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, and pharmacologically acceptable acid addition and quaternary ammonium salts of compounds containing basic groups, and optical isomers of said compounds when A.sup.1 and A.sup.2 are different.