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21. 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。

22. 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。。

23. 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.

24. 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。

25. 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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