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31. 发明授权

US5039805A Novel benzoic and phenylacetic acid derivatives 失效
标题翻译：新型苯甲酸和苯乙酸衍生物
公开(公告)号：US5039805A
公开(公告)日：1991-08-13
申请号：US440949
申请日：1989-11-24
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： A61K31/165 , A61K31/445 , A61K31/4465 , A61K38/00 , A61P7/02 , A61P9/06 , A61P9/08 , A61P9/10 , A61P29/00 , C07C231/12 , C07C237/40 , C07C237/42 , C07C237/44 , C07C249/00 , C07C257/18 , C07C257/22 , C07C271/22 , C07C277/08 , C07C279/14 , C07D211/34 , C07D211/98 , C07K1/06 , C07K5/02 , C07K5/06
CPC分类号： C07C237/42 , C07C237/40 , C07C237/44 , C07C257/18 , C07C271/22 , C07C279/14 , C07D211/34 , C07K5/0205 , C07C2101/14 , C07C2102/08
摘要： The compound of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, can be used as medicaments for the therapy and prophylaxis of disorders such as thromboses, stroke, cardiac infarct, inflammations and arteriosclerosis as well as for the treatment of tumours.
摘要翻译：其中R1，R2和R3具有说明书中给出的含义的化合物可以用作治疗和预防诸如血栓形成，中风，心肌梗塞，炎症和动脉硬化的病症的药物以及治疗肿瘤。

32. 发明授权

US5017619A Phenethanolamine derivatives 失效
标题翻译：苯乙醇胺衍生物
公开(公告)号：US5017619A
公开(公告)日：1991-05-21
申请号：US285269
申请日：1988-12-16
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： A23K1/16 , A61K31/135 , A61K31/27 , C07C217/62
CPC分类号： C07C217/62 , Y10S514/909 , Y10S514/91
摘要： The invention is directed to phenethanolamine derivatives and their pharmaceutically compatible salts, having the formula ##STR1## wherein n is the number 1 or 2; L.sup.1 and L.sup.2 are hydrogen, C.sub.1-3 -(alkyl)carbonyl or C.sub.1-3 (alkoxy) carbonyl; T is hydrogen or methyl; X.sup.1 and X.sup.2 are phenyl or phenyl which is monosubstituted in the m-position by Br, Cl, F, CF.sub.3 and NO.sub.2 ; Y is --(CH.sub.2).sub.1-6 --O--G, --(CH.sub.2).sub.1-6 --CH.dbd.CH--C(O)--Z, --C(O)--Z or --CH(COOR").sub.2 ; G is C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or --(CH.sub.2).sub.1-4 --Q; Q is phenoxy, phenyl, p-fluorophenyl or p-phenoxyphenyl; Z is a --OR or --N(R,R'); R and R' are hydrogen or C.sub.1-4 -alkyl or R and R' together with the N-atom to which they are attached form a 5- or 6-membered saturated ring which optionally contains an O-atom or an additional N-atom; and R" is C.sub.1-4 -alkyl.The compounds of the invention have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals.
摘要翻译：本发明涉及具有下式的苯乙醇胺衍生物及其药学上相容的盐，其中n是数1或2; L 1和L 2是氢，C 1-3 - （烷基）羰基或C 1-3（烷氧基）羰基; T是氢或甲基; X 1和X 2是苯基或在m-位被Br，Cl，F，CF 3和NO 2单取代的苯基; Y是 - （CH 2）1-6 -O-G， - （CH 2）1-6 -CH = CH-C（O）-Z，-C（O）-Z或-CH（COOR“ G是C 1-4 - 烷基，C 1-4 - 烷氧基-C 1-4 - 烷基或 - （CH 2）1-4-Q; Q是苯氧基，苯基，对氟苯基或对苯氧基苯基; Z是-OR或-N（R，R'）; R和R'是氢或C 1-4 - 烷基或R和R'与它们所连接的N-原子一起形成5-或6-元饱和环，其任选地含有O-原子或另外的N- 原子; 和R“是C 1-4 - 烷基。本发明的化合物具有分解代谢活性并且可用于治疗肥胖症和糖尿病或与增加的蛋白质分解有关的病症，或用作育肥动物的饲料添加剂。

33. 发明授权

US5670515A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5670515A
公开(公告)日：1997-09-23
申请号：US452616
申请日：1995-05-25
申请人： Leo Alig , Paul Hadvary , Marianne Hurzeler , Marcel Muller , Beat Steiner , Thomas Weller
发明人： Leo Alig , Paul Hadvary , Marianne Hurzeler , Marcel Muller , Beat Steiner , Thomas Weller
IPC分类号： A61K31/155 , A61K20060101 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/445 , A61K31/451 , A61P7/02 , A61P7/04 , C07C227/00 , C07C229/00 , C07C229/10 , C07C233/76 , C07C237/22 , C07C257/18 , C07C279/18 , C07D20060101 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/22 , C07D211/40 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/52 , C07D401/06 , C07D401/12 , C07D451/06 , C07D453/06 , A61K31/44 , C07D451/10 , C07D451/12
CPC分类号： C07D451/06 , C07C257/18 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/46 , C07D211/48 , C07D211/52 , C07D401/06 , C07D401/12 , C07C2101/12 , Y02P20/55
摘要： N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'" and Q have the definitions given in the specification, are for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets, by blood platelet aggregation and cell-cell adhesion. They are manufactured by cleaving off protecting groups in corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
摘要翻译：其中L，R'至R“'和Q具有本说明书中给出的定义的式”IMAGE“I的N-酰基-α-氨基羧酸衍生物用于治疗或预防由结合引起的疾病通过血小板聚集和细胞粘附，将胶粘蛋白与血小板结合。它们通过在相应的受保护化合物中裂解保护基团或通过将氰基转化成相应的腈中的脒基来制备。

34. 发明授权

US5378712A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5378712A
公开(公告)日：1995-01-03
申请号：US854135
申请日：1992-03-19
申请人： Leo Alig , Paul Hadvary , Marianne Hurzeler , Marcel Muller , Beat Steiner , Thomas Weller
发明人： Leo Alig , Paul Hadvary , Marianne Hurzeler , Marcel Muller , Beat Steiner , Thomas Weller
IPC分类号： A61K31/155 , A61K20060101 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/445 , A61K31/451 , A61P7/02 , A61P7/04 , C07C227/00 , C07C229/00 , C07C229/10 , C07C233/76 , C07C237/22 , C07C257/18 , C07C279/18 , C07D20060101 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/22 , C07D211/40 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/52 , C07D401/06 , C07D401/12 , C07D451/06 , C07D453/06 , C07D211/56 , C07D211/62 , C07D211/92
CPC分类号： C07D451/06 , C07C257/18 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/46 , C07D211/48 , C07D211/52 , C07D401/06 , C07D401/12 , C07C2101/12 , Y02P20/55
摘要： N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or control of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.
摘要翻译：其中L，R'至R“'和Q具有在说明书中给出的含义的式”IMAGE“I的N-酰基-α-氨基羧酸衍生物可用于治疗或控制由粘附蛋白与血小板的结合以及血小板聚集和细胞粘附。

35. 发明授权

US5273982A Acetic acid derivatives 失效
标题翻译：乙酸衍生物
公开(公告)号：US5273982A
公开(公告)日：1993-12-28
申请号：US665110
申请日：1991-03-05
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 , A01N43/40 , C07D207/00
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。

36. 发明授权

US4988714A Pyridine-ethanolamine derivatives 失效
标题翻译：吡啶 - 乙醇胺衍生物
公开(公告)号：US4988714A
公开(公告)日：1991-01-29
申请号：US236802
申请日：1988-08-26
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： A61K31/44 , C07D213/38 , C07D213/61 , C07D409/12 , C07D409/14
CPC分类号： C07D409/12 , C07D213/38 , C07D213/61 , C07D409/14
摘要： Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the physiologically compatible salts thereof are described. The compounds of formula I have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.

37. 发明授权

US4892886A Phenoxypropanolamines 失效
标题翻译：苯氧基丙胺胺
公开(公告)号：US4892886A
公开(公告)日：1990-01-09
申请号：US350056
申请日：1989-05-10
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： A23K20/111 , A61K31/19 , A61P3/04 , A61P3/08 , A61P3/10 , C07C67/00 , C07C213/00 , C07C217/60
CPC分类号： A23K20/111 , Y10S514/866 , Y10S514/909
摘要： [p-[2-[[(S)-2-hydroxy-3-phenoxypropyl]amino]-ethyl]phenoxy]acetic acid and its physiologically compatible salts, which have catabolic activity and can be used for the treatment of obesity, of diabetes and of conditions which are associated with increased protein breakdown or as feed additives for fattening animals, as described. The compounds are prepared starting from esters corresponding to the aforementioned acid.
摘要翻译： [对 - [2 - [[（S）-2-羟基-3-苯氧基丙基]氨基] - 乙基]苯氧基]乙酸及其具有分解代谢活性并可用于治疗肥胖症的生理相容性盐糖尿病和与增加的蛋白质分解有关的病症或作为育肥动物的饲料添加剂，如上所述。从对应于上述酸的酯开始制备化合物。

38. 发明授权

US4871755A Method for treating diabetes obesity and conditions characterized by increased protein breakdown with novel oxazolidines 失效
标题翻译：用于治疗糖尿病肥胖的方法和以新型恶唑啉为特征的增加的蛋白质分解的病症
公开(公告)号：US4871755A
公开(公告)日：1989-10-03
申请号：US152522
申请日：1988-02-05
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： C07D263/04 , C07D263/06 , C07D333/38 , C07D409/06 , C07D413/06
CPC分类号： C07D263/04 , C07D263/06 , C07D333/38 , C07D409/06 , C07D413/06
摘要： The oxazolidines of the formula ##STR1## wherein n signifies the number 1 or 2.T signifies lower carbalkoxy.X signifies phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy.Y signifies hydrogen or methyl, andZ signifies a phenyl or thienyl residue substituted in a defined manner.and the physiologically compatible salts thereof 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. They are manufactured starting from corresponding primary amines.
摘要翻译：其中n表示数字1或2的式[IMAGE] I的恶唑烷.T表示低级烷氧基。 X表示在邻位上任选单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表示氢或甲基，Z表示以限定的方式取代的苯基或噻吩基。其生理上相容的盐具有分解代谢活性，可用于治疗肥胖症和糖尿病，或用于治疗与蛋白质分解增加有关的病症，或作为育肥动物的饲料添加剂。它们是从相应的伯胺开始制造的。

39. 发明授权

US4743604A Oxazolidines and compositions containing the same 失效
标题翻译：恶唑烷及其组合物
公开(公告)号：US4743604A
公开(公告)日：1988-05-10
申请号：US667186
申请日：1984-11-01
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： C07D263/04 , C07D263/06 , C07D333/38 , C07D409/06 , C07D413/06 , A61K31/495 , C07D413/10 , C07D413/12
CPC分类号： C07D263/04 , C07D263/06 , C07D333/38 , C07D409/06 , C07D413/06
摘要： The oxazolidines of the formula ##STR1## wherein n signifies the number 1 or 2,T signifies lower carbalkoxy,X signifies phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y signifies hydrogen or methyl, andZ signifies a phenyl or thienyl residue substituted in a defined manner,and the physiologically compatible salts thereof 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. They are manufactured starting from corresponding primary amines.
摘要翻译：其中n表示数字1或2的恶唑烷，T表示低级烷氧基，X表示在邻位上任选单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，Y表示氢或甲基，Z表示以限定的方式取代的苯基或噻吩基，其生理上相容的盐具有分解代谢活性，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条件，或作为育肥动物的饲料添加剂。它们是从相应的伯胺开始制造的。

40. 发明授权

US4652679A Aziridine and phenethanolamine derivatives having antiobesity and anti-hyperglycaemic acitivity 失效
标题翻译：具有抗肥胖和抗高血糖活性的氮丙啶和苯乙醇胺衍生物
公开(公告)号：US4652679A
公开(公告)日：1987-03-24
申请号：US492981
申请日：1983-05-09
申请人： Leo Alig , Marcel Muller
发明人： Leo Alig , Marcel Muller
IPC分类号： C07D203/08 , C07D295/135 , C07D295/26 , C07D333/22 , C07D333/24 , C07D333/38 , C07D405/06 , A61K31/045 , A61K31/38 , C07C91/06
CPC分类号： C07D295/26 , C07D203/08 , C07D295/135 , C07D333/22 , C07D333/24 , C07D333/38 , C07D405/06
摘要： Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.
摘要翻译：式I和II-1的氮丙啶和苯乙醇胺衍生物其中R 1和R 2是氢或低级烷基; Z1是苯基或以规定方式取代的苯基; Z2和Z21是以定义的方式取代的苯基或噻吩基; n为1-4的整数。所公开的化合物具有分解代谢活性并且可用于治疗肥胖症和/或糖疾病。式I化合物通过使β-氨基醇（例如式II-1的那些）脱水得到，其反过来可以通过向环氧化物中加入胺或通过还原相应的亚氨基酮，亚氨基醇α-酮-β-羟基胺或β 酮类。

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