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1. 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。

2. 发明授权

US3939269A Benzenesulfon YL-semicarbazides for lowering blood sugar levels 失效
标题翻译：用于降低血糖水平的苯磺酸YL-氨基脲
公开(公告)号：US3939269A
公开(公告)日：1976-02-17
申请号：US324836
申请日：1973-01-18
申请人： Walter Aumuller , Rudi Weyer , Ruth Heerdt
发明人： Walter Aumuller , Rudi Weyer , Ruth Heerdt
IPC分类号： A61K31/47 , A61K27/00
CPC分类号： A61K31/47 , Y10S514/866 , Y10S514/884
摘要： Hypoglycemically active benzenesulfonyl-semicarbazides of the formula ##SPC1##Wherein X is hydrogen, chlorine, bromine, methyl or methoxy, Y is --CH(CH.sub.3)-CH.sub.2 --, preferably --CH.sub.2 --CH.sub.2 --, Z is hydrogen or a hydrocarbon radical of 1 or 2 carbon atoms, which forms together with Y a 5- or 6-membered ring, R is alkylene-imino of 3 to 7 carbon atoms in the ring which may be unsaturated or substituted by 1 or 2 methyl or lower alkyl or methoxy, pentamethylene-imino substituted by endoalkylene of 1 to 3 carbon atoms, hexamethylene-imino substituted by endoethylene in .beta.- .epsilon.-position, tetrahydro-iso-indoline, 4,7-endoalkylenehexahydro- or -tetrahydro-iso-indoline, the endoalkylene containing 1 or 2 carbon atoms and the double bond of the tetrahydro compound being in 5,6-position, and the salts thereof as pharmaceutical preparations for oral administration and lowering of blood sugar level in the treatment of diabetes mellitus and the process for lowering the blood sugar level in the treatment of diabetes mellitus.
摘要翻译：式WHEREIN X的低分子活性苯磺酰基 - 氨基脲是氢，氯，溴，甲基或甲氧基，Y是-CH（CH 3）-CH 2 - ，优选-CH 2 -CH 2 - ，Z是氢或1或2的烃基碳原子，其与Y一起形成5-或6-元环，R是环中具有3-7个碳原子的亚烷基亚氨基，其可以是不饱和的或被1或2个甲基或低级烷基或甲氧基，五亚甲基 - 四氢异吲哚啉，4,7-内亚烷基六氢或四氢异吲哚啉，含有1〜3个碳原子的亚烷基亚氨基，含有1〜3个碳原子的亚烷基亚烷基，碳原子，四氢化合物的双键为5,6位，其盐作为用于口服给药的药物制剂和降低糖尿病治疗中的血糖水平以及降低血糖水平的方法直接治疗。。

3. 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。

4. 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。

5. 发明授权

US3932658A Composition and method for lower blood sugar containing N-[4-(.beta.-<2-methoxy-5-chloro-benzamido>-ethyl)-benzenesulfonyl]-N'-c yclopentyl-urea 失效
标题翻译：含有N- {8 4 - （{62 - {21 2-甲氧基-5-氯 - 苯甲酰氨基{22-乙基） - 苯磺酰基} {9 -N {40-环戊基 - 脲
公开(公告)号：US3932658A
公开(公告)日：1976-01-13
申请号：US297679
申请日：1972-10-16
申请人： Helmut Weber , Walter Aumuller , Karl Muth , Rudi Weyer
发明人： Helmut Weber , Walter Aumuller , Karl Muth , Rudi Weyer
IPC分类号： A61K31/17 , A61K27/00
CPC分类号： A61K31/17 , Y10S514/866
摘要： N-[4-(.beta.- -ethyl)-benzenesulfonyl]-N'-cyclopentyl-urea of the formula ##SPC1##Having a long-lasting and strong hypoglycemic action in the treatment of diabetes mellitus and a process for its manufacture.
摘要翻译：具有下列通式的N- [4-（β-（2-甲氧基-5-氯 - 苯甲酰氨基） - 乙基） - 苯磺酰基] -N'-环戊基脲在治疗糖尿病的过程中具有长期和强烈的低血糖作用及其制造工艺。

6. 发明授权

US4066639A Benzene-sulfonyl semicarbazides and process for preparing them 失效
标题翻译：苯并噻喃半胱氨酸及其制备方法
公开(公告)号：US4066639A
公开(公告)日：1978-01-03
申请号：US544018
申请日：1975-01-24
申请人： Helmut Weber , Karl Muth , Rudi Weyer , Walter Aumuller , Erich Haack
发明人： Helmut Weber , Karl Muth , Rudi Weyer , Walter Aumuller , Erich Haack
IPC分类号： C07D205/04 , C07D295/22 , C07D307/68 , C07D317/68 , C07D333/38 , A61K31/64 , C07D211/98 , C07D227/12
CPC分类号： C07D317/68 , C07D205/04 , C07D295/22 , C07D307/68 , C07D333/38 , Y10S514/822
摘要： A benzene-sulfonyl semicarbazide of the formula ##STR1## wherein R is such as phenyl and substituted phenyl, cyclohexyl or alkyl, Y is -CH.sub.2 CH.sub.2 - or ##STR2## is alkylene-imino of 3 to carbon atoms which may also be substituted; a representative compound is 4-[4-(.beta.- -ethyl)-benzene-sulfonyl]-1,1-(.gamma.,.gamma.-dimethyl-pentamethylene)-semicarbazide.

7. 发明授权

US4060626A Indole-carboxylic carbon compounds and pharmaceutical compositions containing them 失效
标题翻译：吲哚羧酸碳化合物和含有它们的药物组合物
公开(公告)号：US4060626A
公开(公告)日：1977-11-29
申请号：US683110
申请日：1976-05-04
申请人： Vladimir Hrstka , Manfred Hubner , Manfred Kuhr , Felix Helmut Schmidt , Walter Aumuller
发明人： Vladimir Hrstka , Manfred Hubner , Manfred Kuhr , Felix Helmut Schmidt , Walter Aumuller
IPC分类号： C07D209/42 , C07D209/60 , C07D209/70 , A61K31/40 , C07D209/18
CPC分类号： C07D209/70 , C07D209/42 , C07D209/60 , Y10S514/866
摘要： Indole-carboxylic acid compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl or alkoxy radical or halogen;R.sub.2 is halogen; lower alkyl or alkoxy radical; orR.sub.1 and R.sub.2 can together also form an alkylene bridge containing 3 to 5 carbon atoms, which can optionally contain one or more double bonds; and, but less preferably, when R.sub.1 is a lower alkyl or alkoxy radical, R.sub.2 can also be a hydrogen atom, and physiologically compatible salts and esters thereof,Are outstandingly effective as blood sugar-lowering agents.
摘要翻译：下式的吲哚羧酸化合物：其中R 1是低级烷基或烷氧基或卤素; R2是卤素; 低级烷基或烷氧基; 或者R 1和R 2可以一起形成含有3至5个碳原子的亚烷基桥，其可任选地含有一个或多个双键; 而且较好的是，当R 1为低级烷基或烷氧基时，R 2也可以是氢原子，以及其生理上相容的盐和酯，作为血糖降低剂是非常有效的。

8. 发明授权

US4029666A Benzenesulfonyl-ureas and process for preparing them 失效
标题翻译：苯磺酰脲及其制备方法
公开(公告)号：US4029666A
公开(公告)日：1977-06-14
申请号：US206190
申请日：1971-12-08
申请人： Helmut Weber , Walter Aumuller , Karl Muth , Rudi Weyer , Felix Helmut Schmidt
发明人： Helmut Weber , Walter Aumuller , Karl Muth , Rudi Weyer , Felix Helmut Schmidt
IPC分类号： C07D209/44 , C07D209/70 , C07D209/72 , C07D221/20 , C07D295/215 , C07D333/38 , C07D451/02 , C07D451/14 , C07D453/06 , C07D211/06
CPC分类号： C07D221/20 , C07D209/44 , C07D209/70 , C07D209/72 , C07D295/215 , C07D333/38 , C07D451/02 , C07D451/14 , C07D453/06 , Y10S514/866
摘要： Benzenesulfonyl-ureas of the formula ##STR1## wherein X represents ##STR2## IN WHICH Z represents hydrogen, halogen, a trifluormethyl group, an alkyl or an alkoxyl radical in 4- or 5-position, or ##STR3## Y represents --CH.sub.2 --CH.sub.2 --, --CH--(CH.sub.3)--CH.sub.2 --or --CH.sub.2 --CH--(CH.sub.3)--,R represents a radical ofA. pentamethylene-imine, which may be substituted by 1 to 3 methyl group or by an endoalkylene group of 1 to 3 carbon atoms,B. hexamethylene-imine, which may be substituted by an endoethylene group in .beta.-.epsilon.-position,C. heptamethylene-imine,D. hexahydro-isoindoline, tetrahydro-isoindoline, 4,7-endoalkylene-hexahydro-, 4,7-endoalkylene-tetrahydro-isoindoline, the endoalkylene group of which may contain 1 - 2 carbon atoms and the double linkage of the tetrahydro group being in 5,6-position,E. N-3-azaspiro-[5,5]-undecane,F. the groups ##STR4## and their pharmaceutically acceptable alkali- or alkaline earth-metal salts.
摘要翻译：其中X表示a）其中Z表示氢，卤素，三氟甲基，4-或5-位的烷基或烷氧基，或Y表示 - 具有下式的苯磺酰基 - CH2-CH2-，-CH-（CH3）-CH2-或-CH2-CH-（CH3） - ，R表示可以被1〜3个甲基取代或由内链烷基取代的戊基乙烯 - 1〜3碳原子团，B.HEXAMETHYLENE-IMINE，可以由β-内酰胺基团内的三乙烯基团取代，C.HEPTAMETHYLENE-IMINE，D.HEXAHYDRO-ISOINDOLINE，四氢-2H-吲哚，4,7-内酰胺 -HEXAHYDRO-，4,7-三羟甲基四氢-2H-吲哚，可以含有1〜2个碳原子的四氢呋喃基团和5,6位四氢呋喃基团的双键，E.N-3-氮杂螺环 - [5,5] - 十一烷，F.G组合物＆amp;图像＆gt;及其药学上可接受的碱金属或碱土金属盐。

9. 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.

10. 发明授权

US3932503A Benzenesulfonyl ureas 失效
标题翻译：苯磺酰脲
公开(公告)号：US3932503A
公开(公告)日：1976-01-13
申请号：US41160
申请日：1970-05-25
申请人： Helmut Weber , Walter Aumuller , Karl Muth , Rudi Weyer
发明人： Helmut Weber , Walter Aumuller , Karl Muth , Rudi Weyer
IPC分类号： A61K31/17 , C07C311/59 , C07D333/38 , C07D333/70 , C07C127/16
CPC分类号： A61K31/17 , C07C311/59 , C07D333/38 , C07D333/70 , C07C2101/14 , C07C2101/18 , C07C2102/50 , C07C2103/66 , Y10S514/866
摘要： Benzenesulfonyl-ureas having hypoglycemic activity and corresponding to the formula ##SPC1##Wherein R.sup.1 isA. cyclopentyl, lower alkyl-cyclopentyl, dimethyl-cyclopentyl, tri-methyl-cyclopentyl, tetramethyl-cyclopentyl, chloro-cyclopentyl;B. di-lower-alkyl-cyclohexyl, lower alkoxymethyl-cyclohexyl; chloro-cyclohexyl;C. cycloalkenyl with 5-8 ring carbon atoms; methyl-cyclopentenyl, methyl-cyclohexenyl; di-methyl-cyclohexenyl, tri-methyl-cyclopentenyl; ##SPC2##In whichA stands for hydrogen, halogen, lower alkyl, lower alkoxy, lower alkenoxy, methoxy-loweralkoxy, lower acyl, nitrophenyl or trifluoromethyl,A.sup.1 stands for hydrogen, lower alkoxy, lower alkyl or halogen and B stands for hydrogen, lower alkyl, lower alkoxy, halogen, benzyloxy or methoxy-methoxy;Y is a hydrocarbon chain of 1-3 carbon atoms, or a physiologically tolerable salt thereof.
摘要翻译：苯磺酰脲具有降血糖活性，对应于式WHEREIN R1为A.环戊烯，低级烷基 - 环戊二烯基，二甲基环戊烯基，三 - 甲基环戊烯基，四甲基环戊烯基，氯代环戊烯基; B.二低级烷基 - 环己基，低级烷基甲基 - 环己基; 氯酚 C.环状碳原子与5-8环碳原子; 甲基环丙基，甲基环己基; 二甲基环己基，三 - 甲基环戊烯; 其中A代表氢，卤素，低级烷基，低级烷氧基，低级烯氧基，甲氧基 - 低级烷氧基，低级酰基，硝基苯基或三氟甲基，A1代表氢，低级烷氧基，低级烷基或卤素，B代表氢，低级烷基，低级烷氧基，卤素，苄氧基或甲氧基 - 甲氧基; Y是1-3个碳原子的烃链，或其生理上可耐受的盐。

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