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1. 发明授权

US4387104A N-Substituted pyruvic acid hydrazones, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： N-取代的丙酮酸腙，其制备物和含有它们的药物组合物
公开(公告)号：US4387104A
公开(公告)日：1983-06-07
申请号：US292869
申请日：1981-08-14
申请人： Ruth Heerdt , Hans P. Wolff , Fritz Kaiser , Wolfgang Schaumann , Hans Kuhnle
发明人： Ruth Heerdt , Hans P. Wolff , Fritz Kaiser , Wolfgang Schaumann , Hans Kuhnle
IPC分类号： A61K31/15 , A61K31/19 , A61K31/195 , A61P3/08 , A61P3/10 , C07C67/00 , C07C241/00 , C07C251/08 , C07C251/76 , C07C317/14 , C07C109/12
CPC分类号： C07C251/72
摘要： A pyruvic acid hydrazone derivative of the formula: ##STR1## wherein R is an aryl radical optionally substituted by lower alkyl or is an aliphatic hydrocarbon radical which can be substituted by a lower alkoxy, a cycloalkyl or an optionally substituted aryl radical,A is an alkylene radical containing 2 to 8 carbon atoms, with at least 2 carbon atoms between B and the nitrogen atom, andB is an oxygen or sulphur atom;or a physiologically acceptable salt, ester or amide thereof which possesses hypoglycaemic activity.
摘要翻译：一种下式的丙酮酸腙衍生物，其中R是任选被低级烷基取代的芳基，或者是可被低级烷氧基，环烷基或任意取代的芳基取代的脂族烃基，A是含有2至8个碳原子的亚烷基，B和氮原子之间至少有2个碳原子，B是氧或硫原子; 或其具有低血糖活性的生理上可接受的盐，酯或酰胺。

2. 发明授权

US4425360A Pharmacologically active novel O-substituted pyruvic acid oximes 失效
标题翻译：药理活性新型O-取代丙酮酸肟
公开(公告)号：US4425360A
公开(公告)日：1984-01-10
申请号：US300076
申请日：1981-09-08
申请人： Hans P. Wolff , Ruth Heerdt , Manfred Hubner, deceased , Hans Kuhnle , Felix H. Schmidt
发明人： Hans P. Wolff , Ruth Heerdt , Manfred Hubner, deceased , Hans Kuhnle , Felix H. Schmidt
IPC分类号： A61K31/15 , A61K31/19 , A61K31/195 , A61P3/06 , A61P3/08 , A61P3/10 , C07C249/08 , C07C251/32 , C07C251/36 , C07C251/50 , C07C251/52 , C07C251/54 , C07C251/60 , C07C253/30 , C07C255/50 , C07D295/185 , C07C131/00
CPC分类号： C07D295/185 , Y10S514/866
摘要： The present invention provides pyruvic acid oximes of the general formula: ##STR1## wherein R is a hydrogen atom, a C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, cinnamyloxy, phenylamino, phenyl-N-alkylamino or phenylthio radical or an aryl or aryloxy radical, the aryl moiety of which can be substituted one or more times by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, hydroxyl, trifluoromethyl, amino, acetylamino, nitrile, nitro or methylenedioxy, A is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon chain containing up to 10 carbon atoms, which can be substituted one or more times by halogen or hydroxyl, and R.sub.1 is a C.sub.1 -C.sub.8 alkyl radical, which can be substituted one or more times by halogen, hydroxyl, nitrile, phenyl or carboxyl, or is a nitrile or formyl group, with the proviso that when R--A-- is a methyl or ethyl radical, R.sub.1 is not a methyl radical or a nitrile group and when R--A-- is a benzyl radical, R.sub.1 is not a methyl or benzyl radical; and the physiologically acceptable salts, carboxylic acid esters and amides thereof. The invention also provides processes for the preparation of these compounds pharmaceutical compositions containing them, and their use in combating hypoglycaemia.
摘要翻译：本发明提供以下通式的丙酮酸肟：其中R为氢原子，C 3 -C 8环烷基，C 1 -C 6烷氧基，肉桂氧基，苯基氨基，苯基-N-烷基氨基或苯硫基或芳基或芳氧基，其芳基部分可以被C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，羟基，三氟甲基，氨基，乙酰氨基，腈，硝基或亚甲二氧基取代一次或多次，A是直链或含有至多10个碳原子的支链，饱和或不饱和脂族烃链，其可以被卤素或羟基取代一次或多次，并且R 1是可被卤素取代一次或多次的C 1 -C 8烷基，羟基，腈，苯基或羧基，或者是腈或甲酰基，条件是当RA-是甲基或乙基时，R 1不是甲基或腈基，当RA-是苄基时，R 1 不是甲基或苄基; 和其生理上可接受的盐，羧酸酯和酰胺。本发明还提供了制备这些化合物的方法，含有它们的药物组合物及其在抗低血糖中的应用。

3. 发明授权

US4136197A Hypoglycaemically and hypolipidaemically effective n-substituted carboxylic acid amides 失效
标题翻译：高效和高效的N-取代的羧酸酰胺
公开(公告)号：US4136197A
公开(公告)日：1979-01-23
申请号：US785255
申请日：1977-04-06
申请人： Manfred Hubner , Ruth Heerdt , Elmar Bosies , Hans Kuhnle , Felix H. Schmidt
发明人： Manfred Hubner , Ruth Heerdt , Elmar Bosies , Hans Kuhnle , Felix H. Schmidt
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/55 , A61P3/08 , C07C233/12 , C07C233/60 , C07C233/63 , C07D311/82 , C07D311/84 , C07D311/90 , C07D313/12 , C07D335/12 , C07D335/20 , C07D337/12 , C07C63/44
CPC分类号： C07D335/20 , A61K31/165 , C07C233/12 , C07D311/82 , C07D311/84 , C07D311/90 , C07D313/12 , C07D335/12 , C07D337/12 , C07C2103/18 , Y10S514/884
摘要： An N-substituted carboxylic acid amide of the formula ##STR1## wherein A is a valency bond or an oxygen or sulphur atom or a methylene, ethylene, vinylene, ethyleneoxa or ethylenethia radical,V is a trivalent hydrocarbon radical containing up to 4 carbon atoms,R.sub.1 and R.sub.2 each independently is hydrogen, a halogen atom, a hydroxyl group or an alkyl or alkoxy radical,R.sub.3 is hydrogen, a hydroxyl group or an alkoxy radical,Y is an alkylene radical containing up to 3 carbon atoms,X is a valency bond or a divalent aliphatic hydrocarbon radical containing up to 6 carbon atoms, andD is a hydroxymethyl, formyl, free or esterified carboxyl or an N-substituted carbamoyl radical, or a physiologically compatible salt thereof, characterized by hypoglycaemic and hypolipidaemic activity.

4. 发明授权

US4136196A Hypoglycaemically active 2-(phenylalkyl- or -alkenyl hydrazono)-propionic acid derivatives 失效
标题翻译：高分子活性2-（苯乙烯基或间苯二酚）丙酸衍生物
公开(公告)号：US4136196A
公开(公告)日：1979-01-23
申请号：US835939
申请日：1977-09-22
申请人： Rainer Haeckel , Michael Oellerich , Ruth Heerdt , Manfred Hubner , Hans Kuhnle
发明人： Rainer Haeckel , Michael Oellerich , Ruth Heerdt , Manfred Hubner , Hans Kuhnle
IPC分类号： A61K31/16 , A61K20060101 , A61K31/00 , A61K31/15 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/357 , A61K31/36 , A61P3/08 , A61P3/10 , C07C20060101 , C07C67/00 , C07C241/00 , C07C249/16 , C07C251/76 , C07D317/16 , C07D317/48 , C07D317/58 , C07D317/60 , C07C101/28
CPC分类号： C07C251/72
摘要： A 2-hydrazono-propionic acid derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently is hydrogen, halogen, trifluoromethyl, alkyl, hydroxyl, acyloxy or alkoxy or together are methylenedioxy, andX is an aliphatic hydrocarbon radical containing 2-4 carbon atoms and is optionally substituted by an alkyl radical in the .beta.- or .gamma.-position to the nitrogen atom,Or a physiologically compatible salt, ester or amide thereof, which exhibit hypoglycaemically activity.

5. 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。

6. 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。

7. 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。。

8. 发明授权

US4376731A 1-Aziridine carboxylic acid derivatives with immunostimulant activity 失效
标题翻译：具有免疫刺激活性的1-氮杂环丁烷羧酸衍生物
公开(公告)号：US4376731A
公开(公告)日：1983-03-15
申请号：US859633
申请日：1978-01-31
申请人： Elmar Bosies , Ruth Heerdt , Rudi Gall , Uwe Bicker , Anna E. Ziegler
发明人： Elmar Bosies , Ruth Heerdt , Rudi Gall , Uwe Bicker , Anna E. Ziegler
IPC分类号： C07D203/20 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/395
CPC分类号： C07D403/12 , C07D203/20 , C07D405/12 , C07D409/12
摘要： 2-Substituted-1-aziridine-carboxylic acid esters exhibiting immuno-stimulant activity and of the formula ##STR1## wherein X is a carbamoyl or alkoxycarbonyl radical, andR.sup.1 is an aliphatic hydrocarbon radical optionally substituted by halogen, alkoxy, amino, carbamoyloxy, cycloalkyl, hydroxyl, an imido or heterocyclic radical, cycloalkyl; or aryl, aralkyl, aryloxyalkyl or arylthioalkyl wherein the aryl moiety is optionally substituted by halogen, alkyl, alkoxy, hydroxyl, amino, nitro, cyano, acyl, carbalkoxy, thioalkyl, alkylsulphonyl, phenyl or trifluoromethyl. Counterparts where X is --CN and R.sup.1 is as above, except for ethyl, are also new.
摘要翻译： 2-取代的1-氮丙啶 - 羧酸酯，其具有免疫刺激活性，并且具有下式：其中X是氨基甲酰基或烷氧基羰基，R1是任选被卤素，烷氧基，氨基，氨基甲酰氧基取代的脂族烃基，环烷基，羟基，亚氨基或杂环基，环烷基; 芳基，芳烷基，芳氧基烷基或芳硫基烷基，其中芳基部分任选被卤素，烷基，烷氧基，羟基，氨基，硝基，氰基，酰基，烷氧基，硫代烷基，烷基磺酰基，苯基或三氟甲基取代。对应物，其中X为-CN和R1如上所述，除乙基以外，也是新的。

9. 发明授权

US4206231A Hypoglycaemically active 2-alkyl- or -alkenyl-hydrazono propionic acid derivatives 失效
标题翻译：低血糖活性2-烷基 - 或 - 烯基 - 亚氨基丙酸衍生物
公开(公告)号：US4206231A
公开(公告)日：1980-06-03
申请号：US934291
申请日：1978-08-17
申请人： Rainer Haeckel , Michael Oellerich , Ruth Heerdt , Manfred Hubner , Felix H. Schmidt
发明人： Rainer Haeckel , Michael Oellerich , Ruth Heerdt , Manfred Hubner , Felix H. Schmidt
IPC分类号： A61K31/19 , A61K20060101 , A61K31/15 , A61K31/16 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/22 , A61P3/08 , C07C20060101 , C07C67/00 , C07C241/00 , C07C249/16 , C07C251/74 , C07C251/76 , C07D20060101 , C07C101/02
CPC分类号： C07C251/72
摘要： A 2-hydrazonopropionic acid derivative of the formula ##STR1## wherein R is an aliphatic hydrocarbon radical, andX is a valency bond or a divalent aliphatic hydrocarbon radical containing up to 4 carbon atoms, with the proviso that when X is a valency bond, R cannot be saturated cycloalkyl, ora physiologically compatible salt, lower alkyl ester or amide thereof, which exhibit hypoglycaemic activity.
摘要翻译：其中R是脂族烃基，X是价键或含有至多4个碳原子的二价脂族烃基，其条件是当X是价键时， R不能是表现出低血糖活性的饱和环烷基或其生理上相容的盐，低级烷基酯或酰胺。

10. 发明授权

US3996241A 2-Hydroxymethyl indole compounds and blood sugar lowering compositions 失效
标题翻译： 2-羟甲基吲哚化合物和降血糖组合物
公开(公告)号：US3996241A
公开(公告)日：1976-12-07
申请号：US516947
申请日：1974-10-22
申请人： Ruth Heerdt , Manfred Hubner , Felix Helmut Schmidt , Kurt Stach
发明人： Ruth Heerdt , Manfred Hubner , Felix Helmut Schmidt , Kurt Stach
IPC分类号： C07D209/12 , C07D209/60
CPC分类号： C07D209/12 , C07D209/60 , Y10S514/866
摘要： New indole derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are hydrogen or halogen or lower alkyl or, taken together, represent a --CH=CH-CH=CH- bridge, with the proviso that R.sub.1 and R.sub.2 are not both hydrogen, and wherein, when R.sub.2 is halogen or alkyl, R.sub.1 can also be alkoxy;Are outstandingly effective in blood sugar lowering action in mammals.
摘要翻译：式（I）的新的吲哚衍生物其中R 1和R 2可以相同或不同，为氢或卤素或低级烷基，或一起表示-CH = CH-CH = CH-桥，条件是R 1和R 2不是氢，并且其中当R 2是卤素或烷基时，R 1也可以是烷氧基; 在牛奶中降低血糖的作用非常有效。

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