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1. 发明授权

US06548694B2 N-(4-carbamimidoyl-phenyl)-glycine derivatives 失效
标题翻译： N-（4-甲脒基 - 苯基） - 甘氨酸衍生物
公开(公告)号：US06548694B2
公开(公告)日：2003-04-15
申请号：US09858535
申请日：2001-05-16
申请人： Leo Alig , Katrin Groebke Zbinden , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Hans Peter Wessel
发明人： Leo Alig , Katrin Groebke Zbinden , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Hans Peter Wessel
IPC分类号： C07C22900
CPC分类号： C07D317/36 , C07C257/18 , C07C259/18 , C07D307/20
摘要： N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: wherein X and R1 to R5 are as defined herein, and includes hydrates or solvates and/or physiologically acceptable salts thereof and/or physiologically acceptable esters thereof.
摘要翻译： N-（4-脒甲酰基 - 苯基） - 甘氨酸衍生物具有下式：其中X和R 1至R 5如本文所定义，并且包括水合物或溶剂化物和/或其生理学上可接受的盐和/或其生理上可接受的酯。

2. 发明授权

US5747522A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5747522A
公开(公告)日：1998-05-05
申请号：US452614
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 , A61K31/40 , A61K31/395
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 prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and 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预防由粘附蛋白与血小板的结合以及血小板聚集和细胞粘附。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。

3. 发明授权

US5663297A Antithrombic peptides 失效
标题翻译：抗血清肽
公开(公告)号：US5663297A
公开(公告)日：1997-09-02
申请号：US454453
申请日：1995-05-30
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 , A61K31/198 , A61K38/05 , A61K38/06 , A61K38/07 , A61P7/02 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/09 , C07K5/10 , C07K5/11 , C07K7/06 , C07K14/47 , C07K14/75
CPC分类号： C07K14/75 , C07K14/47 , C07K5/0202 , C07K5/0815 , C07K5/1019 , A61K38/00 , Y02P20/55
摘要： Disclosed herein are peptide of the formulaR--CONH--CH.sub.2 --CONH--CH(R')--CH.sub.2 COOH Iwherein R and R' are as defined herein. The claimed peptide derivatives inhibit platelet aggregation and as such are useful in the treatment of thrombosis.
摘要翻译：本文公开的是式R-CONH-CH2-CONH-CH（R'）-CH 2 COOH的肽，其中R和R'如本文所定义。要求保护的肽衍生物抑制血小板聚集，因此可用于治疗血栓形成。

4. 发明授权

US5545658A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5545658A
公开(公告)日：1996-08-13
申请号：US452615
申请日：1995-05-25
申请人： Leo Alig , Paul Hadvary , Marianne H urzeler , Marcel M uller , Beat Steiner , Thomas Weller
发明人： Leo Alig , Paul Hadvary , Marianne H urzeler , Marcel M uller , Beat Steiner , Thomas Weller
IPC分类号： C07C257/18 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/46 , C07D211/48 , C07D211/52 , C07D401/06 , C07D401/12 , C07D451/06 , A61K31/40
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
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 prophylaxis 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预防由粘附蛋白与血小板的结合以及血小板聚集和细胞粘附。

5. 发明授权

US5399585A Carboxamides and sulfonamides compounds which have useful pharmaceutical utility 失效
标题翻译：具有有用的药物效用的羧酰胺和磺酰胺化合物
公开(公告)号：US5399585A
公开(公告)日：1995-03-21
申请号：US114415
申请日：1993-08-30
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： C07C257/18 , C07C279/18 , C07C311/17 , C07D213/82 , C07D333/24 , C07D333/10 , A61K31/38
CPC分类号： C07D213/82 , C07C257/18 , C07C279/18 , C07C311/17 , C07D333/24 , Y02P20/55
摘要： Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.
摘要翻译：描述了具有式R1-A-（W）aX-（CH2）b-（Y）cBZ-COOR（I）的新型甲酰胺和磺酰胺，其中R 1，A，W，X，Y，B，Z， R，a，b和c如说明书中所提供。这些化合物可用于治疗血栓形成，中风，心肌梗塞，炎症，动脉硬化以及治疗和预防肿瘤。这些新化合物是通过除去具有被保护的脒基或胍基的相应化合物中的保护基来制备的。

6. 发明授权

US5256812A Carboxamides and sulfonamides 失效
标题翻译：甲酰胺和磺酰胺
公开(公告)号：US5256812A
公开(公告)日：1993-10-26
申请号：US755960
申请日：1991-09-06
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： C07C257/18 , C07C279/18 , C07C311/17 , C07D213/82 , C07D333/24 , C07C143/67
CPC分类号： C07D213/82 , C07C257/18 , C07C279/18 , C07C311/17 , C07D333/24 , Y02P20/55
摘要： Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.
摘要翻译：描述了具有式R1-A-（W）aX-（CH2）b-（Y）cBZ-COOR（I）的新型甲酰胺和磺酰胺，其中R 1，A，W，X，Y，B，Z， R，a，b和c如说明书中所提供。这些化合物可用于治疗血栓形成，中风，心肌梗死，炎症，动脉硬化以及治疗和预防肿瘤。这些新化合物是通过除去具有被保护的脒基或胍基的相应化合物中的保护基来制备的。

7. 发明授权

US5166218A Phenoxypropanolamines and pharmaceutical compositions thereof 失效
标题翻译：苯氧基丙胺胺及其药物组合物
公开(公告)号：US5166218A
公开(公告)日：1992-11-24
申请号：US744624
申请日：1991-08-12
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
CPC分类号： C07D295/088 , C07C229/38 , C07D333/20 , C07D333/24 , C07D333/38
摘要： Tertiary and secondary amines of the formulas ##STR1## and ##STR2## wherein n is the integer 1 or 2,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为整数1或2，R为氢，低级烷酰基或苯基 - 低级 - 烷酰基，X 1为任选单氟化或单 - 在邻位被氯化，X2是低级烷基，在邻位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是氢或甲基，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。

8. 发明授权

US4348327A Process for the preparation of 17.alpha.-hydroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids 失效
标题翻译：制备17α-羟基和17aα-羟基-D-高聚羧酸的方法
公开(公告)号：US4348327A
公开(公告)日：1982-09-07
申请号：US276563
申请日：1981-06-23
申请人： Robert Nickolson , Ulrich Kerb , Rudolf Wiechert , Leo Alig , Andor Furst , Marcel Muller
发明人： Robert Nickolson , Ulrich Kerb , Rudolf Wiechert , Leo Alig , Andor Furst , Marcel Muller
IPC分类号： C07J3/00 , C07J41/00 , C07J63/00 , C07J9/00
CPC分类号： C07J63/008 , C07J3/005 , C07J41/0066 , C07J41/0094
摘要： 17.alpha.-hyroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids of the formula ##STR1## wherein n is 1 or 2,A is ##STR2## and R.sub.1 is H or CH.sub.3are prepared by hydrating the corresponding 17-nitriles with a mixture of a lower carboxylic acid and its anhydride in the presence of perchloric acid. The resultant 17.beta.-N-acylcarboxamide is then treated with an alkali metal hydroxide in a polyhydric alcohol at an elevated temperature. The product acids are intermediates, e.g., for the production of steroids having antiinflammatory activity.
摘要翻译：其中n为1或2的17α-羟基 - 和17α-羟基-D-高聚羧酸，其中n为1或2，A为H，并且R 1为H或CH 3是通过用相应的17-腈水解在高氯酸存在下，低级羧酸及其酸酐的混合物。然后在升高的温度下，用多元醇中的碱金属氢氧化物处理所得的17β-酰基羧酰胺。产物酸是中间体，例如用于生产具有抗炎活性的类固醇。

9. 发明授权

US4197406A D-Homosteroids 失效
标题翻译： D-类固醇
公开(公告)号：US4197406A
公开(公告)日：1980-04-08
申请号：US36476
申请日：1979-05-07
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： A61K31/235 , C07J63/00 , C07C69/78
CPC分类号： C07J63/008
摘要： The present disclosure is concerned with 17a-(m-iodobenzoyloxy) substituted D-homosteroids and a process for their manufacture. The compounds are useful as intermediates and also as hormonal agents, particularly progestational agents.
摘要翻译：本公开涉及17a-（间碘苯氧基）取代的D-类固醇类及其制备方法。这些化合物可用作中间体，也可用作激素，特别是孕激素。

10. 发明授权

US4026921A D-homosteroids 失效
标题翻译： D-类固醇
公开(公告)号：US4026921A
公开(公告)日：1977-05-31
申请号：US507883
申请日：1974-09-20
申请人： Andor Furst , Marcel Muller , Leo Alig , Peter Keller , Ulrich Kerb , Rudolf Wiechert , Klaus Kieslich , Karl Petzoldt
发明人： Andor Furst , Marcel Muller , Leo Alig , Peter Keller , Ulrich Kerb , Rudolf Wiechert , Klaus Kieslich , Karl Petzoldt
IPC分类号： C07J63/00
CPC分类号： C07J63/008 , Y10S435/85 , Y10S514/887 , Y10S514/914 , Y10S514/96
摘要： Novel D-homosteroids of the formula ##STR1## are disclosed. These compounds exhibit anti-inflammatory activity.
摘要翻译：公开了新颖的D-类固醇类化合物（IMAGE）。这些化合物表现出抗炎活性。

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