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    Lipid lowering alkylene glycols and ester derivatives thereof
    1.
    发明授权
    Lipid lowering alkylene glycols and ester derivatives thereof 失效
    脂质降解亚烷基二醇及其酯衍生物

    公开(公告)号：US4275068A

    公开(公告)日：1981-06-23

    申请号：US48536

    申请日：1979-04-23

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

    IPC分类号： C07D213/80 ,  A61K31/455 ,  A61K31/60 ,  C07C69/90

    CPC分类号： C07D213/80

    摘要： 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.

    摘要翻译： 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。

    Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood
    4.
    发明授权
    Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood 失效
    具有降低血液中脂肪物质水平的能力的苯氧基链烷酸衍生物

    公开(公告)号：US4483999A

    公开(公告)日：1984-11-20

    申请号：US773148

    申请日：1977-03-01

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    IPC分类号： C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07D211/46 ,  C07D473/08 ,  C07C69/76

    CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

    摘要： Novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, or alkyl or alkoxy containing from 1 to 4 carbon atoms,R.sup.2 is hydrogen, halogen, hydroxy or alkyl of alkoxy containing from 1 to 4 carbon atoms,n and m are integers such that the sum (n+m) lies in the range from 3 to 10 inclusive and n differs from m, andx is alkyl containing from 1 to 4 carbon atoms, hydrogen or a cation which is a metal cation of main Groups 1, 2 and 3 of the Periodic System of the Elements, an organic base cation or an ammonium ion. These compounds have pharmaceutical utility by virtue of their considerable ability to reduce the level of fatty substances in the blood.

    摘要翻译： 式中，R 1为氢，卤素，含有1至4个碳原子的烷基或烷氧基，R2为氢，卤素，羟基或含有1至4个碳原子的烷氧基烷基，n和m的新型化合物 整数，使得和（n + m）在3〜10的范围内，n与m不同，x是含有1〜4个碳原子的烷基，氢或作为主体1的金属阳离子的阳离子 ，元素周期系统的2和3，有机碱性离子或铵离子。 这些化合物由于其相当的降低血液中脂肪物质含量的能力而具有药用效用。

    Cholesterol-lowering phenoxyalkanoic acid esters
    5.
    发明授权
    Cholesterol-lowering phenoxyalkanoic acid esters 失效

    公开(公告)号：US4153803A

    公开(公告)日：1979-05-08

    申请号：US773144

    申请日：1977-03-01

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    IPC分类号： A61K31/22 ,  C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07C69/736 ,  C07D211/46 ,  C07D213/30 ,  C07D473/08 ,  C07C69/76

    CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

    摘要： 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.

    Novel indolyl alkyl amines, method of producing same, and their use as anorectic agents
    7.
    发明授权
    Novel indolyl alkyl amines, method of producing same, and their use as anorectic agents 失效
    新型吲哚基烷基胺，其制备方法及其作为厌食剂的用途

    公开(公告)号：US3947584A

    公开(公告)日：1976-03-30

    申请号：US397779

    申请日：1973-09-17

    申请人： Ludwig Zirngibl ,  Rudolf Adrian ,  Ulrich Jahn

    发明人： Ludwig Zirngibl ,  Rudolf Adrian ,  Ulrich Jahn

    IPC分类号： C07D209/14 ,  C07D209/16 ,  A61K31/40

    CPC分类号： C07D209/16 ,  Y10S514/91

    摘要： Indolyl alkyl amines of the following formula: ##SPC1##And their salts with organic or inorganic acids. In this formula I, A and A.sup.1 denote identical or different alkyl radicals which both together have a total of 3-8 C-atoms. R.sup.1 denotes hydrogen, a lower alkyl radical having up to 4 C-atoms or a possibly substituted benzyl or benzoyl radical. R.sup.2 and R.sup.3 may be the same or different and denote hydrogen, a halogen (more particularly chlorine, bromine or fluorine) or (possibly halogenated) lower alkyl radicals or (possibly etherified) hydroxy radicals. R.sup.4 denotes hydrogen, a lower alkyl radical, an acyl group or a (possibly substituted) benzyl radical or the cyano-ethyl group. The compounds are useful as anoretics (appetite inhibitors) and can be made by various disclosed methods.

    摘要翻译： 下式的吲哚基烷基胺：