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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.

    Herbicide
    7.
    发明授权
    Herbicide 失效
    除草剂

    公开(公告)号：US4211551A

    公开(公告)日：1980-07-08

    申请号：US850468

    申请日：1977-11-10

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Walter Scharen ,  Jacques Meyer

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Walter Scharen ,  Jacques Meyer

    IPC分类号： A01N39/04 ,  A01P13/00 ,  A01N9/24

    CPC分类号： A01N39/04

    摘要： Herbicidal compositions for selective weed control comprising 4-(4'-chlorobenzyl)-phenoxy acetic acid or a salt thereof and the novel salts of 4-(4'-chlorobenzyl)-phenoxy acetic acid.A method for selectively controlling weeds by applying to a crop area an effective amount of 4-(4'-chlorobenzyl)-phenoxy acetic acid or a salt of said acid.

    摘要翻译： 用于选择性杂草控制的除草组合物包含4-（4'-氯苄基） - 苯氧基乙酸或其盐和4-（4'-氯苄基） - 苯氧基乙酸的新型盐。 通过向作物区域施加有效量的4-（4'-氯苄基） - 苯氧基乙酸或所述酸的盐来选择性地控制杂草的方法。

    Theophylline derivatives
    8.
    发明授权
    Theophylline derivatives 失效
    茶碱衍生物

    公开(公告)号：US4603204A

    公开(公告)日：1986-07-29

    申请号：US474230

    申请日：1983-03-11

    申请人： Kurt Thiele ,  Felix Geissmann ,  Ludwig Zirngibl ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Felix Geissmann ,  Ludwig Zirngibl ,  Ulrich Jahn

    IPC分类号： A61K31/52 ,  A61K31/522 ,  A61P25/02 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D295/22 ,  C07D307/02 ,  C07D473/08

    CPC分类号： C07D473/08

    摘要： New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.

    摘要翻译： 具有式（I）的茶碱的新衍生物，其中R表示氢或OH，n为数字0或1，X或> CH-或> N-，Y为-O-或-CO-，R a 在给定的情况下被卤素，短链烷基，烷氧基或卤素 - 烷基取代的五元或六元芳基环或杂芳基环，并且除了其它性质外，还表现出组胺，血清素 - 卡那霉素拮抗剂 ，抗过敏和肾上腺素能刺激作用。

    Antihypertensive 4-(2-imidazolin-2-yl-amino)-2-methyl-indazole
    10.
    发明授权
    Antihypertensive 4-(2-imidazolin-2-yl-amino)-2-methyl-indazole 失效
    抗高血压4-（2-咪唑啉-2-基 - 氨基）-2-甲基 - 吲唑

    公开(公告)号：US4526898A

    公开(公告)日：1985-07-02

    申请号：US530145

    申请日：1983-09-07

    申请人： Istvan Molnar ,  Kurt Thiele ,  Felix Geissmann ,  Ulrich Jahn

    发明人： Istvan Molnar ,  Kurt Thiele ,  Felix Geissmann ,  Ulrich Jahn

    IPC分类号： C07D403/12 ,  A61K31/415

    CPC分类号： C07D403/12

    摘要： 4-(2-Imidazolin-2-yl-amino)-2-methyl-indazole is a highly selective and effective .alpha..sub.2 -antagonist, .alpha..sub.1 -partial agonist and .alpha..sub.1s -agonist and displays anti-hypertensive activity and antagonistic activity on adrenaline and noradrenaline. It is useful as an .alpha.-adrenoceptor influencing and as an anti-hypertensively active drug.

    摘要翻译： 4-（2-咪唑啉-2-基 - 氨基）-2-甲基 - 吲唑是一种高选择性和有效的α2拮抗剂，α1-部分激动剂和α1s激动剂，并且对抗高血压活性和拮抗活性 肾上腺素和去甲肾上腺素。 作为α肾上腺素能受体影响作为抗高血压活性药物是有用的。