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1. 发明授权

US4182902A Novel cholesterol-lowering compounds 失效
标题翻译：新型胆固醇降低化合物
公开(公告)号：US4182902A
公开(公告)日：1980-01-08
申请号：US942129
申请日：1978-09-13
申请人： Kurt Thiele , Quazi Armed , Rudolf Adrian , Ulrich Jahn
发明人： Kurt Thiele , Quazi Armed , Rudolf Adrian , Ulrich Jahn
IPC分类号： C07C59/68 , C07C59/70 , C07D211/46 , C07D213/30 , C07D473/08 , C07C63/33
CPC分类号： C07D213/30 , C07C59/68 , C07C59/70 , C07D211/46 , C07D473/08
摘要： p-(p'-chlorobenzyl) phenoxyacetic acid.
摘要翻译：对 - （对 - 氯苄基）苯氧基乙酸。

2. 发明授权

US4214095A Chlorobenzyl phenoxy alkoxylates 失效
标题翻译：氯苄基苯氧基烷氧基化物
公开(公告)号：US4214095A
公开(公告)日：1980-07-22
申请号：US6542
申请日：1979-01-25
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： C07C69/712 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61P3/06 , C07C51/00 , C07C59/125 , C07C59/68 , C07C67/00 , C07C69/612 , C07C201/00 , C07C205/37 , C07D213/30 , C07C69/76
CPC分类号： C07D213/30 , C07C205/37 , C07C59/68
摘要： Novel compounds of the formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are different lower alkyls and R.sup.3 is a lower alkyl or a methyl pyridine group, and the acid addition salts of formula (1) compounds when R.sup.3 is methyl pyridine. The novel compounds have an asymmetric C-atom and may be in the form of the D,L racemates or the D or L stereoisomers.These compounds are useful in the treatment of hypercholesterolemia and hyperlipidemia because of their high effectiveness in reducing the level of cholesterol and lipids in the blood combined with very low general toxicities and substantially reduced hepatomegalitic effects.
摘要翻译：式（1）的新型化合物其中R1和R2是不同的低级烷基，R3是低级烷基或甲基吡啶基，当式（1）的酸加成盐化合物当R3是甲基吡啶时。新化合物具有不对称C原子，并且可以是D，L外消旋物或D或L立体异构体的形式。这些化合物可用于治疗高胆固醇血症和高脂血症，因为它们在降低血液中的胆固醇和脂质的水平方面具有很高的有效性，同时具有非常低的一般毒性和显着降低的肝母细胞效应。

3. 发明授权

US4115393A Pyridyl alkyl esters of substituted phenoxy alkanoic acids having the ability to reduce the level of fatty substances in the blood 失效
标题翻译：具有降低血液中脂肪物质水平的能力的取代苯氧基链烷酸的吡啶基烷基酯
公开(公告)号：US4115393A
公开(公告)日：1978-09-19
申请号：US773145
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 , C07D211/46 , C07D213/55 , C07D473/08
CPC分类号： C07C321/00 , C07C59/68 , C07C59/70 , C07D211/46 , C07D473/08
摘要： Compounds of the formula ##STR1## WHEREIN R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;X represents benzyl, benzyloxy or benzylthio, or benzyl, benzyloxy or benzylthio substituted by a said radical R;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl radical containing up to 10 carbon atoms such that the total number of carbon atoms in A.sup.1 and A.sup.2 is not more than 10;n is an integer of from 1 to 3;m is 1 or 2;And pharmacologically acceptable salts thereof.These compounds have pharmaceutical utility by virtue of their ability to reduce the level of fatty substances in the blood.
摘要翻译：式中的R 1表示氢，卤素，羟基或含有1至4个碳原子的烷基或烷氧基; X表示苄基，苄氧基或苄硫基，或被所述基团R取代的苄基，苄氧基或苄硫基; 可以相同或不同的A 1和A 2是氢或含有至多10个碳原子的烷基，使得A1和A2中的碳原子总数不大于10; N是1到3的整数; M IS 1 OR 2; 及其药理学上可接受的药物。

4. 发明授权

US4275068A Lipid lowering alkylene glycols and ester derivatives thereof 失效
标题翻译：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。

5. 发明授权

US4483999A Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood 失效
标题翻译：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。

6. 发明授权

US4153803A 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.

7. 发明授权

US3947584A Novel indolyl alkyl amines, method of producing same, and their use as anorectic agents 失效
标题翻译：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：

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