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21. 发明授权

US3939193A D-Homosteroids 失效
标题翻译： D-类固醇
公开(公告)号：US3939193A
公开(公告)日：1976-02-17
申请号：US501558
申请日：1974-08-29
申请人： Leo Alig , Andor Furst , Marcel Muller
发明人： Leo Alig , Andor Furst , Marcel Muller
IPC分类号： A61K31/12 , A61K31/56 , A61K31/573 , A61P29/00 , C07J63/00 , C07C141/12 , C07C49/45
CPC分类号： C07J63/008
摘要： A novel class of D-homosteroids is disclosed. These compounds have potent endocrinal activity, particularly as anti-inflammatory agents.
摘要翻译：公开了一类新的D-类固醇激素。这些化合物具有有效的内分泌活性，特别是抗炎剂。

22. 发明授权

US5726185A Acetic acid derivatives 失效
标题翻译：乙酸衍生物
公开(公告)号：US5726185A
公开(公告)日：1998-03-10
申请号：US347736
申请日：1994-12-01
申请人： Leo Alig , Paul Hadvary , Marianne Hurzeler Muller , Marcel Muller , Beat Steiner , Thomas Weller
发明人： Leo Alig , Paul Hadvary , Marianne Hurzeler Muller , Marcel Muller , Beat Steiner , Thomas Weller
IPC分类号： C07D401/12 , A61K31/00 , A61K31/19 , A61K31/22 , A61K31/24 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/395 , A61K31/4418 , A61K31/445 , A61K31/47 , A61K31/472 , A61P7/00 , A61P7/02 , A61P19/00 , C07C237/32 , C07C251/24 , C07C251/48 , C07C257/18 , C07C259/18 , C07C271/06 , C07C271/62 , C07C271/64 , C07C323/42 , C07C323/50 , C07C333/04 , C07D207/12 , C07D211/00 , C07D211/20 , C07D211/34 , C07D211/46 , C07D211/58 , C07D211/94 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D267/14 , C07D271/06 , C07D271/07 , C07D307/68 , C07D309/12 , C07D413/02 , C07D413/06 , C07D413/10 , C07D413/12 , C07F9/24 , A61K31/43 , C07D211/08 , C07D211/92
CPC分类号： C07D213/82 , C07C237/32 , C07C257/18 , C07C259/18 , C07C271/64 , C07C323/42 , C07C333/04 , C07D207/12 , C07D211/46 , C07D217/02 , C07D271/07 , C07D309/12 , C07D401/12 , C07D413/12 , C07F9/2491 , C07C2101/02 , C07C2101/14 , Y02P20/55
摘要： Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
摘要翻译：其中L，M，T和Q具有在说明书中给出的含义的式“IMAGE”I的乙酸衍生物可用于治疗或预防由粘合蛋白与血小板结合引起的疾病，血小板聚集和细胞粘附，并通过裂解相应的保护化合物中的保护基团或通过将氰基转化为相应的腈中的脒基来制备。

23. 发明授权

US5430024A Peptides bearing N-terminal amidino moieties and their use as inhibitors of platelet aggregation 失效
标题翻译：具有N-末端脒基部分的肽及其作为血小板聚集抑制剂的用途
公开(公告)号：US5430024A
公开(公告)日：1995-07-04
申请号：US123826
申请日：1993-09-20
申请人： Leo Alig , Albrecht Edenhofer , Marcel Muller , Arnold Trzeciak , Thomas Weller
发明人： Leo Alig , Albrecht Edenhofer , Marcel Muller , Arnold Trzeciak , Thomas Weller
IPC分类号： A61K38/00 , C07C257/18 , C07C271/64 , C07D207/08 , C07D207/16 , C07D211/34 , C07D211/60 , C07K5/02 , C07K5/062 , C07K5/065 , C07K14/75 , A61K38/06
CPC分类号： C07D207/08 , C07C257/18 , C07C271/64 , C07D207/16 , C07D211/34 , C07D211/60 , C07K14/75 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06026 , C07K5/06113 , A61K38/00
摘要： Acetic acid derivatives of formulaH.sub.2 N(NH)C--X--Y--CO--Z--CH(Q.sup.1)COOQ.sup.2 Iand hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of adhesive proteins to blood platelets and also to inhibit blood platelet aggregation and cell-cell adhesion.
摘要翻译：式H2N（NH）CXY-CO-Z-CH（Q1）COOQ2I的乙酸衍生物及其水合物，溶剂合物及其生理学上可接受的盐可用于抑制粘合蛋白与血小板结合并抑制血小板聚集和细胞细胞粘附。

24. 发明授权

US5064863A Phenoxypropanolamines and pharmaceutical use 失效
标题翻译：苯氧基丙胺酸酯和药物用途
公开(公告)号：US5064863A
公开(公告)日：1991-11-12
申请号：US130929
申请日：1987-12-10
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： C07C229/38 , C07D295/092 , C07D333/20 , C07D333/24 , C07D333/38 , A61K31/135 , C07C217/72
CPC分类号： C07D295/088 , C07C229/38 , C07D333/20 , C07D333/24 , C07D333/38
摘要： Tertiary and secondary amines of the formulas ##STR1## wherein n is the integer 1 or 2, p0 R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.
摘要翻译：式（I）＆lt; IMAGE＆gt; V-1的叔胺和仲胺，其中n为1或2的整数，p O为氢，低级烷酰基或苯基 - 低级 - 烷酰基，X 1为任选单氟化的苯氧基甲基，在邻位单氯化，X2为低级烷基，任选在邻位单一氟化或单氯化的苯氧基甲基或任选被氟，氯，三氟甲基或低级烷氧基单取代的苯基，Y为氢或甲基，并且Z是如下文所述取代的苯基或噻吩基，并且描述了生理和药学上相容的盐。式I和V-1的化合物具有分解代谢活性，可用于治疗肥胖症和糖尿病，或用于治疗与增加的蛋白质分解相关的病症，或作为育肥动物的饲料添加剂。式I和V-1的化合物可以从相应的伯胺开始制备。

25. 发明授权

US4585796A Novel phenethanolamines 失效
标题翻译：新型苯乙醇胺
公开(公告)号：US4585796A
公开(公告)日：1986-04-29
申请号：US518990
申请日：1983-08-01
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： A61K31/165 , C07C13/18 , C07C229/38 , C07C233/00 , C07C309/63 , C07C311/15 , C07C317/04 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/38 , A61K31/38 , C07C103/28
CPC分类号： C07C255/00 , C07C229/38 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/38 , Y10S514/866 , Y10S514/909
摘要： The tertiary amines of the formula ##STR1## wherein n represents a whole number of 1 to 5;X.sup.1 represents phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;X.sup.2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower-alkoxycarbonyl;Z represents a group of the formula ##STR2## R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl;R.sup.4, R.sup.5 and R.sup.51 represent hydrogen, lower-alkyl, lower-alkoxy, lower alkanoyl, carboxy, cyano, hydroxy, hydroxy-lower-alkyl, acyloxy or a group --C(R.sup.6).dbd.C(R.sup.7)COOR.sup.8, --SO.sub.2 R.sup.9, --C(O)R.sup.9 or --CH.sub.2 R.sup.10, with the proviso that R.sup.4 does not represent hydrogen when R.sup.5 represents hydroxy, lower-alkyl or lower-alkoxy;R.sup.6, R.sup.7 and R.sup.8 represent hydrogen or lower-alkyl;R.sup.9 represents amino, mono-lower-alkylamino or a group R;R represents di-lower-alkylamino, piperidino, morpholino, thiamorpholino, piperazino or the ether group of a lower aliphatic, cycloaliphatic or araliphatic alcohol or of a phenol; andR.sup.10 represents a group R and, where R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, lower-alkoxybenzylamino or trifluoromethyl and simultaneously Y represents hydrogen, lower-alkyl or hydroxymethyl, R.sup.10 can also represent amino or mono-lower-alkylamino,have hypoglycaemic activity and reduce glycosuria. They are manufactured from corresponding primary or secondary amines.
摘要翻译：式Ⅰ的叔胺其中n表示1至5的整数; X1表示苯基或被R1，R2和R3单，二或三取代的苯基; X2代表氢，低级烷基，苯基或被R1，R2和R3单，二或三取代的苯基; Y表示氢，低级烷基，羟甲基，羧基或低级烷氧基羰基; Z表示式（Z）R1的基团，R2和R3表示氢，卤素，羟基，苄氧基，低级烷基，低级烷氧基，羟甲基，氨基，酰氨基，低级烷氧基苄氨基，硝基，氨基甲酰基，三氟甲基或低级烷基磺酰基甲基; R4，R5和R5表示氢，低级烷基，低级烷氧基，低级烷酰基，羧基，氰基，羟基，羟基 - 低级 - 烷基，酰氧基或基团-C（R6）= C（R7）COOR8，-SO2R9， -C（O）R 9或-CH 2 R 10，条件是当R 5表示羟基，低级烷基或低级烷氧基时，R 4不表示氢; R6，R7和R8表示氢或低级烷基; R9表示氨基，单低级烷基氨基或基团R; R代表二低级烷基氨基，哌啶子基，吗啉代，硫代吗啉代，哌嗪子基或低级脂肪族，脂环族或芳脂族醇或苯酚的醚基; R 10表示基团R，并且其中R 1，R 2和R 3表示氢，卤素，羟基，苄氧基，低级烷基，低级烷氧基，羟甲基，氨基，低级烷氧基苄氨基或三氟甲基，同时Y表示氢，低级烷基或羟甲基，R10也可以代表氨基或单低级烷基氨基，具有低血糖活性并降低糖尿。它们由相应的伯胺或仲胺制成。

26. 发明授权

US4137269A D-homosteroids 失效
标题翻译： D-类固醇
公开(公告)号：US4137269A
公开(公告)日：1979-01-30
申请号：US731238
申请日：1976-10-12
申请人： Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Klaus Kieslich , Rudolf Wiechert
发明人： Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Klaus Kieslich , Rudolf Wiechert
IPC分类号： A61K31/12 , A61K31/56 , A61P29/00 , C07J63/00
CPC分类号： C07J63/008 , C07J63/00
摘要： The present disclosure relates to steroids. More particularly, the disclosure is concerned with D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same. The subject D-homosteroids have high endocrinal activity and are particularly active as anti-inflammatory agents.
摘要翻译：本公开涉及类固醇。更具体地，本公开涉及D-类固醇，其制备方法和含有它们的药物制剂。受试者D-类固醇具有高的内分泌活性，并且作为抗炎剂特别有活性。

27. 发明授权

US4036874A D-homopregnanes 失效
标题翻译： D-己内酯
公开(公告)号：US4036874A
公开(公告)日：1977-07-19
申请号：US639939
申请日：1975-12-11
申请人： Leo Alig , Andor Furst , Marcel Muller
发明人： Leo Alig , Andor Furst , Marcel Muller
IPC分类号： C07J63/00 , C12P33/00
CPC分类号： C07J63/008 , C12P33/00 , Y10S435/83 , Y10S435/896 , Y10S435/911
摘要： D-homosteroids of the formula ##STR1## wherein R.sup.6 is hydrogen, fluorine, chlorine or methyl; R.sup.9 is hydrogen, fluorine, chlorine or bromine; R.sup.17 and R.sup.21 each independently are hydroxy or acyloxy, and U represents optional olefinic unsaturation are endocrine agents having anti-inflammatory properties.
摘要翻译： D-类固醇，其中R6是氢，氟，氯或甲基; R9是氢，氟，氯或溴; R17和R21各自独立地是羟基或酰氧基，U代表任选的烯属不饱和键是具有抗炎特性的内分泌剂。

28. 发明授权

US4028400A D-homosteroids 失效
标题翻译： D-类固醇
公开(公告)号：US4028400A
公开(公告)日：1977-06-07
申请号：US507884
申请日：1974-09-20
申请人： Leo Alig , Andor Furst , Peter Keller , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人： Leo Alig , Andor Furst , Peter Keller , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
IPC分类号： C07J63/00
CPC分类号： C07J63/008
摘要： The present invention relates to steroids. More particularly, the invention is concerned with D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same.
摘要翻译：本发明涉及类固醇。更具体地，本发明涉及D-类固醇，其制备方法和含有它的药物制剂。

29. 发明授权

US4026922A D-Homo-pregnene steroids 失效
标题翻译： D-异孕烯类固醇
公开(公告)号：US4026922A
公开(公告)日：1977-05-31
申请号：US619065
申请日：1975-10-02
申请人： Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人： Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
IPC分类号： C07C69/013 , A61K31/12 , A61K31/215 , A61K31/22 , A61K35/56 , B01J23/00 , C07B61/00 , C07C45/00 , C07C49/587 , C07C67/00 , C07J63/00 , C07J71/00 , C12P33/02
CPC分类号： C07J71/001 , C07J63/00 , C07J63/008 , Y10S514/96
摘要： The present disclosure relates to novel D-homo-pregnene steroids useful as progestational agents.
摘要翻译：本公开内容涉及可用作促孕剂的新型D-同型孕激素类固醇。

30. 发明授权

US3965128A 6.beta.,7.beta.-Epoxy-1.alpha.,2.alpha.-methylen-D-homo-4-pregnen-3,20-di ones 失效
标题翻译： 6 {62,7 {62-环氧-1 {60,2 {60-亚甲基-D-同-4-孕烯-3,20-二酮
公开(公告)号：US3965128A
公开(公告)日：1976-06-22
申请号：US508492
申请日：1974-09-23
申请人： Andor Furst , Marcel Muller , Leo Alig , Peter Keller , Ulrich Kerb , Rudolf Wiechert
发明人： Andor Furst , Marcel Muller , Leo Alig , Peter Keller , Ulrich Kerb , Rudolf Wiechert
IPC分类号： C07D303/32 , C07J63/00 , C07D303/44
CPC分类号： C07J63/008
摘要： New 6.beta.,7.beta.-epoxy-17.alpha.-hydroxy or acyloxy-1.alpha.,2.alpha.-methylen-D-homo-4-pregnen-3,20-diones having surprising progestational activity are disclosed.
摘要翻译：公开了具有惊人刺激活性的新的6β，7β-环氧-17α-羟基或酰氧基-1α，2α-亚甲基-D-同-4-孕烯-3,20-二酮。

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