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11. 发明授权

US4207341A Hypoglycaemically and hypolipidaemically active derivatives of phenylacetic acid 失效
标题翻译：低血糖和降血糖活性的苯乙酸衍生物
公开(公告)号：US4207341A
公开(公告)日：1980-06-10
申请号：US701717
申请日：1976-07-01
申请人： Manfred Hubner , Hans Kuhnle , Ernst-Christian Witte , Ruth Heerdt , Rudi Weyer , Volker Hitzel
发明人： Manfred Hubner , Hans Kuhnle , Ernst-Christian Witte , Ruth Heerdt , Rudi Weyer , Volker Hitzel
IPC分类号： A61K31/17 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/27 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/47 , A61K31/495 , A61P3/06 , A61P3/08 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/87 , C07C235/52 , C07C279/26 , C07D209/42 , C07D213/82 , C07D215/48 , C07D241/28 , C07D307/79 , C07D311/22 , C07D333/38 , C07C101/42 , C07C101/44
CPC分类号： C07D213/82 , C07C279/26 , C07D209/42 , C07D215/48 , C07D307/79 , C07D311/22 , C07D333/38 , Y10S514/866
摘要： Phenylacetic acid derivatives of the formula ##STR1## wherein A is an aryl radical optionally substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino or aryloxy, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an optionally branched alkylene radical containing up to 3 carbon atoms, andR.sub.1 and R.sub.2 each independently is hydrogen or a lower alkyl radical,or a physiologically compatible salt or ester thereof, exhibit marked hypoglycaemic and hypolipidaemic activity.
摘要翻译：其中A是任选被卤素，三氟甲基，烷基，烷氧基，烯氧基，烷氧基烷氧基，烷基取代的氨基或芳氧基取代的芳基，或任选被卤素，烷基或烷氧基取代的杂环体系 Y是价态键或含有至多3个碳原子的任意支化的亚烷基，R 1和R 2各自独立地为氢或低级烷基或其生理上相容的盐或酯，表现出显着的低血糖和降血脂活性。

12. 发明授权

US4182775A Benzoic acids and process for their preparation 失效
标题翻译：苯甲酸及其制备方法
公开(公告)号：US4182775A
公开(公告)日：1980-01-08
申请号：US829876
申请日：1977-09-01
申请人： Rudi Weyer , Volker Hitzel , Ernold Granzer
发明人： Rudi Weyer , Volker Hitzel , Ernold Granzer
IPC分类号： A61K31/195 , A61K31/38 , A61K31/381 , A61P3/06 , C07C229/38 , C07C233/81 , C07C235/52 , C07D333/38 , C07C101/42 , A01N9/20
CPC分类号： C07C229/38 , C07D333/38
摘要： Benzoic acids of the general formula I ##STR1## in which R, R.sup.1, R.sup.2 and Y have the meanings as mentioned in the following, and which in the form of the free compounds or in the form of the physiologically tolerated salts and esters possess valuable pharmacological properties, processes for preparing them, pharmaceutical preparations containing them, and their use as or in medicaments.
摘要翻译：其中R，R 1，R 2和Y具有如下所述含义的通式I的苯甲酸，其游离化合物形式或以生理上耐受的盐和酯的形式具有有价值的药理学性质，制备方法，含有它们的药物制剂，以及它们在药物中的用途。

13. 发明授权

US4158063A Acylamino(alkyl)benzene derivatives and process for preparing them 失效
标题翻译：酰基氨基（烷基）苯衍生物及其制备方法
公开(公告)号：US4158063A
公开(公告)日：1979-06-12
申请号：US757290
申请日：1977-01-06
申请人： Volker Hitzel , Rudi Weyer , Elmar Bosies
发明人： Volker Hitzel , Rudi Weyer , Elmar Bosies
IPC分类号： A61K31/165 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/10 , C07C231/12 , C07C233/65 , C07D213/82 , C07D215/48 , C07D307/79 , C07D311/58 , C07D333/38
CPC分类号： C07D213/82 , C07D215/48 , C07D307/79 , C07D311/58 , C07D333/38 , Y10S514/866
摘要： The invention relates to acylamino(alkyl)benzene derivatives of the general formula ##STR1## in which W represents a group which can be converted into a carboxyl group, or an aldehyde group or an oxymethyl group or their derivatives or also a low molecular weight alkyl group, preferably a methyl group,X represents an aromatic or hetero-aromatic ring system,Y represents a single chemical bond or a hydrocarbon bridge, andZ represents hydrogen or one or even several other substituents,To their preparation and to pharmaceutical compositions containing them. The compounds have blood sugar lowering activity and may be used in the therapy of diabetes mellitus.
摘要翻译：本发明涉及通式为“IMAGE”的酰氨基（烷基）苯衍生物，其中W代表可转化为羧基的基团，或醛基或羟甲基或其衍生物或低分子量烷基基团，优选甲基，X表示芳族或杂芳族环系，Y表示单一化学键或烃桥，Z表示氢或一个或甚至几个其它取代基。其制备和含有它们的药物组合物。该化合物具有降血糖活性，可用于治疗糖尿病。

14. 发明授权

US4278680A Hypoglycaemically and hypolipidaemically active derivatives of phenylacetic acid 失效
标题翻译：低血糖和降血糖活性的苯乙酸衍生物
公开(公告)号：US4278680A
公开(公告)日：1981-07-14
申请号：US101978
申请日：1979-12-10
申请人： Manfred Hubner , Hans Kuhnle , Ernst-Christian Witte , Ruth Heerdt , Rudi Weyer , Volker Hitzel
发明人： Manfred Hubner , Hans Kuhnle , Ernst-Christian Witte , Ruth Heerdt , Rudi Weyer , Volker Hitzel
IPC分类号： A61K31/17 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/27 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/47 , A61K31/495 , A61P3/06 , A61P3/08 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/87 , C07C235/52 , C07C279/26 , C07D209/42 , C07D213/82 , C07D215/48 , C07D241/28 , C07D307/79 , C07D311/22 , C07D333/38 , C07D213/56 , A61K31/455 , C07D215/40
CPC分类号： C07D213/82 , C07C279/26 , C07D209/42 , C07D215/48 , C07D307/79 , C07D311/22 , C07D333/38 , Y10S514/866
摘要： Phenylacetic acid derivatives of the formula ##STR1## wherein A is an aryl radical optionally substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino or aryloxy, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an optionally branched alkylene radical containing up to 3 carbon atoms, andR.sub.1 and R.sub.2 each independently is hydrogen or a lower alkyl radical,or a physiologically compatible salt or ester thereof, exhibit marked hypoglycaemic and hypolipidaemic activity.
摘要翻译：其中A是任选被卤素，三氟甲基，烷基，烷氧基，烯氧基，烷氧基烷氧基，烷基取代的氨基或芳氧基取代的芳基，或任选被卤素，烷基或烷氧基取代的杂环体系 Y是价态键或含有至多3个碳原子的任意支化的亚烷基，R 1和R 2各自独立地为氢或低级烷基或其生理上相容的盐或酯，表现出显着的低血糖和降血脂活性。

15. 发明授权

US3962244A Benzene sulfonyl ureas 失效
标题翻译： BENZENE SULFONYL UREAS
公开(公告)号：US3962244A
公开(公告)日：1976-06-08
申请号：US489103
申请日：1974-07-17
申请人： Rudi Weyer , Walter Aumuller , Ruth Heerdt , Volker Hitzel , Helmut Weber , Karl Muth
发明人： Rudi Weyer , Walter Aumuller , Ruth Heerdt , Volker Hitzel , Helmut Weber , Karl Muth
IPC分类号： C07D239/90 , C07D239/96 , C07D239/72
CPC分类号： C07D239/90 , C07D239/96 , Y10S514/866
摘要： Benzene sulfonyl ureas of the formula ##SPC1##In whichR represents a hydrogen, chlorine, or bromine atom, a methoxy or methyl group,--X--Y-- represents --N=CH--, --NH--CH.sub.2 --, --NH--CO--, ##EQU1## the alkyl herein containing from 1 to 4 carbon atoms, R.sup.2 represents an alkyl group having 1 to 4 carbon atomsR.sup.1 represents an alkyl group having from 3 to 6 carbon atoms, a cycloalkyl group having from 5 to 8 carbon atoms, 3-ethyl-cyclopentyl, methyl-cyclopentyl, dimethylcyclopentyl, 4-alkyl-cyclohexyl having from 1 to 3 carbon atoms in the alkyl group, cyclopentenyl, cyclohexenyl, cycloheptenyl, 4-chloro-cyclohexyl, 4,4-dimethylcyclohexyl, 3-methyl-cyclopentenyl, 4-methylcyclohexenyl, endoalkylene-cyclohexyl, endoalkylene-cyclohexenyl, bicyclo-(2.2.1) hept-2-en-7-yl, and their physiologically tolerable salts, useful for lowering blood sugar level in the treatment of diabetes mellitus.

16. 发明授权

US4542139A Sulfonylureas pharmaceutical formulations based on these compounds and their use for treatment of diabetes 失效
标题翻译：基于这些化合物的磺酰脲类药物制剂及其用于治疗糖尿病的用途
公开(公告)号：US4542139A
公开(公告)日：1985-09-17
申请号：US603987
申请日：1984-04-26
申请人： Volker Hitzel , Rudi Weyer , Karl Giesen , Harald Ritzel
发明人： Volker Hitzel , Rudi Weyer , Karl Giesen , Harald Ritzel
IPC分类号： C07D215/48 , A61K31/47 , A61K31/635 , A61P3/08 , A61P3/10 , C07D215/22 , C07D215/54
CPC分类号： C07D215/54
摘要： Sulfonylureas of the formula ##STR1## in which Y denotes alkylene having 2-3 C atoms, R denotes alkyl having 1-4 C atoms, R.sup.1 denotes hydrogen, chlorine or methyl, and R.sup.2 denotes alkyl having 3-6 C atoms, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylcycloalkenyl or cycloalkenylalkyl, each having 5-8 C atoms, and their physiologically tolerated salts, and processes for their preparation and medicaments prepared therefrom.
摘要翻译：其中Y表示具有2-3个C原子的亚烷基，R表示具有1-4个C原子的烷基，R 1表示氢，氯或甲基，R 2表示具有3-6个C原子的烷基，环烷基，烷基环烷基，环烷基烷基，环烯基，烷基环烯基或环烯基烷基，各自具有5-8个C原子，以及它们的生理学耐受的盐及其制备方法和由其制备的药物。

17. 发明授权

US3950524A Hypoglycemic benzenesulfonamido pyrimidines 失效
标题翻译：低血糖苯磺酰胺嘧啶
公开(公告)号：US3950524A
公开(公告)日：1976-04-13
申请号：US540964
申请日：1975-01-14
申请人： Volker Hitzel , Rudi Weyer , Walter Aumuller
发明人： Volker Hitzel , Rudi Weyer , Walter Aumuller
IPC分类号： C07D239/42 , C07C67/00 , C07C301/00 , C07C303/08 , C07C311/64 , C07D239/46 , C07D239/69 , C07D401/12 , A61K31/505 , C07D239/00
CPC分类号： C07D239/69 , Y10S514/866
摘要： Sulfonamidopyrimidines of the formula ##SPC1##In which X is a 6-membered heteroaromatic ring including 1 to 2 nitrogen atoms which may be substituted with 1 or 2 methyl groups and/or fused with benzene and is linked in vicinal position with regard to the nitrogen atom to the rest of the molecule,R is alkyl or alkoxy, having 1 to 4 carbon atoms each, their manufacture and their use as hypoglycemic agents.
摘要翻译：磺酰胺亚胺嘧啶类，其中X是含有1至2个氮原子的6元杂芳环，其可以被1或2个甲基取代和/或与苯稠合并且相对于氮原子连接在邻位分子的其余部分，R为烷基或烷氧基，各自具有1至4个碳原子，其制备及其作为降血糖剂的用途。

18. 发明授权

US4025519A Benzenesulfonyl-ureas 失效
标题翻译：苯磺酰脲
公开(公告)号：US4025519A
公开(公告)日：1977-05-24
申请号：US568268
申请日：1975-04-15
申请人： Rudi Weyer , Walter Aumuller , Volker Hitzel , Felix Helmut Schmidt
发明人： Rudi Weyer , Walter Aumuller , Volker Hitzel , Felix Helmut Schmidt
IPC分类号： C07D215/38
CPC分类号： C07D215/38 , Y10S514/866
摘要： Sulfonyl-ureas of the formula ##STR1## wherein X represents a heteroaromatic 5- or 6-ring substituted, if desired, by one or two methyl groups and/or annellated with benzene, which ring may contain in addition to a nitrogen atom a further nitrogen, oxygen or sulfur atom and which, in vicinal position to the nitrogen atom, is linked to the rest of the molecule portion, R is alkyl having 1 to 3 carbon atoms, R.sup.1 is alkyl having 3 to 6 carbon atoms, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylcycloalkenyl having each 5 to 9 carbon atoms, cyclohexenylmethyl, chlorocyclohexyl, bicycloheptenylmethyl, bicycloheptylmethyl, bicycloheptenyl, bicycloheptyl, nortricyclyl, adamantyl, benzyl, which as substance or in form of the salts thereof have hypoglycemic properties and are distinguished by a strong and continuous lowering of the blood sugar level, process for preparing them as well as pharmaceutical preparations containing the sulfonyl-ureas as an active substance.
摘要翻译：其中X表示如果需要由一个或两个甲基取代（如果需要的话）和/或与环一起取代的芳香族5-或6-环，该环除了氮之外还可含有原子为另外的氮，氧或硫原子，并且在与氮原子相邻的位置连接到分子部分的其余部分，R是具有1至3个碳原子的烷基，R 1是具有3至6个碳原子的烷基，环烷基，烷基环烷基，环烷基烷基，环烯基，具有5至9个碳原子的烷基环烯基，环己烯基甲基，氯代环己基，双环庚烯基甲基，双环庚基甲基，双环庚烯基，双环庚基，中间体，金刚烷基，苄基，其物质或其盐的形式具有降血糖性质，其特征在于血糖水平的强烈和持续降低，其制备方法以及含有磺酰脲类作为活性物质的药物制剂。

19. 发明授权

US3998968A Benzenesulfonyl ureas and process for their manufacture 失效
标题翻译：苯磺酰脲及其制备方法
公开(公告)号：US3998968A
公开(公告)日：1976-12-21
申请号：US559712
申请日：1975-03-19
申请人： Volker Hitzel , Werner Pfaff , Rudi Weyer , Helmut Weber
发明人： Volker Hitzel , Werner Pfaff , Rudi Weyer , Helmut Weber
IPC分类号： C07C311/58 , A61K20060101 , A61K31/00 , A61K31/17 , A61K31/18 , A61K31/64 , C07C20060101 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/38 , C07C303/40 , C07C127/00
CPC分类号： C07C311/58 , Y10S514/866
摘要： N-acylaminoalkyl-benzenesulfonyl-N'-methyl ureas, especially those of the general formula ##STR1## in which R is C.sub.1-- C.sub.4 --alkyl or a phenyl radical substituted in 2-position by alkoxy of 1 to 4 carbon atoms, phenoxy or dimethylamino and in 5-position by H, CH.sub.3, Cl or Br, their manufacture and their use as oral antidiabetics.
摘要翻译： N-酰基氨基烷基 - 苯磺酰基-N'-甲基脲，特别是其中R为C 1 -C 4 - 烷基或2-位被1-4个碳原子的烷氧基取代的苯基的通式为“IMAGE”的那些，苯氧基或二甲基氨基，在H，CH3，Cl或Br的5-位，它们的制备及其作为口服抗糖尿病药的用途。

20. 发明授权

US3984416A Substituted quinoline-8-carboxamido ethyl benzene-sulfonyl N-cyclopentylmethyl urea 失效
标题翻译：取代的喹啉-8-甲酰氨基乙基苯磺酰基N-环戊基甲基脲
公开(公告)号：US3984416A
公开(公告)日：1976-10-05
申请号：US581764
申请日：1975-05-29
申请人： Helmut Weber , Walter Aumuller , Rudi Weyer , Karl Muth , Volker Hitzel
发明人： Helmut Weber , Walter Aumuller , Rudi Weyer , Karl Muth , Volker Hitzel
IPC分类号： C07D215/16 , C07D215/18
CPC分类号： C07D215/16 , C07C311/58 , C07C2101/08 , C07C2102/08 , C07C2102/10
摘要： Sulfonyl-ureas of the formula X--CO--NH--A--SO.sub.2 --NH--CO--NH--R.sup.1, in which R.sup.1 represents cyclopentylmethyl, alkyl-cyclopentylmethyl or dialkyl-cyclopentylmethyl, having up to 2 carbon atoms in the alkyl rest, or cyclopentylethyl, X represents a. ##SPC1##In which R.sup.2 represents hydrogen, F, Cl, Br, CF.sub.3, CH.sub.3 or OCH.sub.3,b. ##SPC2##In which R.sup.3 represents hydrogen, Cl or CH.sub.3,c. ##SPC3##In which R.sup.4 represents hydrogen, Cl or Br,A represents one of the groupings ##SPC4##And their physiologically tolerated salts, process for preparing them and pharmaceutical preparations containing them.
摘要翻译：式X-CO-NH-A-SO2-NH-CO-NH-R1的磺酰脲，其中R1表示烷基休止中具有至多2个碳原子的环戊基甲基，烷基 - 环戊基甲基或二烷基 - 环戊基甲基，或环戊基乙基，X表示a。

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