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11. 发明授权

US5137897A 2-substituted 4-(3-alkyl-5-tert.-butyl-4-hydroxyphenyl) thiazoles, processes for their preparation, pharmaceuticals containing them and their use 失效
标题翻译： 2-取代的4-（3-烷基-5-叔丁基-4-羟基苯基）噻唑，其制备方法，包含它们的药物及其用途
公开(公告)号：US5137897A
公开(公告)日：1992-08-11
申请号：US626784
申请日：1990-12-13
申请人： Werner Thorwart , Rudolf Schleyerbach , Robert Bartlett , Klaus U. Weithmann
发明人： Werner Thorwart , Rudolf Schleyerbach , Robert Bartlett , Klaus U. Weithmann
IPC分类号： A61K31/425 , A61K31/426 , A61P29/00 , A61P37/00 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/30 , C07D417/06 , C07D417/12
CPC分类号： C07D417/06 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/30
摘要： Novel substituted thiazoles of the formula I ##STR1## in which R.sup.1 is a saturated or unsaturated, straight-chain or branched C.sub.1 -C.sub.5 -alkyl group,R.sup.2 is a hydrogen atom or an alkyl radical having 1 to 3 carbon atoms,A is an intermediate chain of the formula--(CH.sub.2).sub.n --Y--CR.sup.3 R.sup.4 --; --CH.dbd.CR.sup.3 --(CH.sub.2).sub.m -- or --CH.dbd.N--O--(CH.sub.2).sub.n -- whereY is a single bond, an oxygen or sulfur atom or a carbonyl group,R.sup.3 and R.sup.4 are identical or different and are a hydrogen atom or an alkyl radical having up to two carbon atoms, m is a number from 0 to 3 and n is a number from 1 to 4, andZ is a tetrazole or CN group, or a radical of the formula ##STR2## X is a hydroxyl group or a radical of the formula R.sup.5 O-- or R.sup.6 R.sup.7 N--, where R.sup.5 is a straight-chain or branched C.sub.1 -C.sub.4 -alkyl radical which is optionally substituted by hydroxyl, C.sub.1 -C.sub.3 -alkoxy or C.sub.1 -C.sub.3 -alkylamino,R.sup.6 and R.sup.7 are identical or different and are a hydrogen atom, a straight-chain or branched C.sub.1 -C.sub.6 -alkyl radicall or, for the case in which R.sup.6 is a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.7 is a hydroxyl, a C.sub.1 -C.sub.3 -alkoxy or a tetrazol-5-yl group or X, together with the structural element --A--(C.dbd.O)--, is a radical of the formula II ##STR3## where R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.3 -alkyl radical or a C.sub.1 -C.sub.3 -alkoxy radical, and physiologically tolerable salts of such compounds of the formula I in which X is a hydroxyl or hydroxyamino group,are prepared by various processes.They are preferably suitable for the treatment and prophylaxis of inflammatory diseases - in particular inflammatory rheumatic diseases.
摘要翻译： R1是饱和或不饱和的直链或支链C1-C5-烷基，R2是氢原子或具有1至3个碳原子的烷基的式I（I）的新型取代的噻唑， A是式 - （CH 2）n Y-CR 3 R 4 - 的中间链; -CH = CR 3 - （CH 2）m - 或-CH = NO-（CH 2）n - ，其中Y为单键，氧或硫原子或羰基，R 3和R 4相同或不同，为氢原子或具有至多两个碳原子的烷基，m为0至3的数，n为1至4的数，Z为四唑或CN基团，或式X的基团为羟基或式R5O-或R6R7N-的基团，其中R5是任选被羟基，C 1 -C 3 - 烷氧基或C 1 -C 3 - 烷基氨基取代的直链或支链C 1 -C 4烷基，R 6和 R7相同或不同，为氢原子，直链或支链C1-C6烷基，或对于R6为氢原子或C1-C4烷基的情况，R7为羟基， C 1 -C 3 - 烷氧基或四唑-5-基或X与结构元件-A-（C = O） - 一起是式II（II）的基团，其中R 8是氢原子，C 1 -C 3 - 烷基或C 1 -C 3 - 烷氧基，以及生理上的耐受性这些其中X是羟基或羟基氨基的式I化合物的盐通过各种方法制备。它们优选适用于治疗和预防炎症性疾病，特别是炎性风湿性疾病。

12. 发明授权

US4829061A 1-(4-Hydroxy-3,5-di-tert.-butylbenzoyl)homopiperazine, various derivatives thereof, processes for the preparation of these compounds, medicaments containing them, and their use 失效
标题翻译： 1-（4-羟基-3,5-二叔丁基苯甲酰基）高哌嗪，其各种衍生物，这些化合物的制备方法，含有它们的药物及其用途
公开(公告)号：US4829061A
公开(公告)日：1989-05-09
申请号：US149602
申请日：1988-01-28
申请人： Erhard Wolf , Erhard Rossmanith , Robert R. Bartlett , Rudolf Schleyerbach
发明人： Erhard Wolf , Erhard Rossmanith , Robert R. Bartlett , Rudolf Schleyerbach
IPC分类号： A61K31/55 , A61P29/00 , A61P37/00 , C07D243/08
CPC分类号： C07D243/08
摘要： 1-(4-Hydroxy-3,5-di-tert.-butylbenzoyl)homopiperazine and various derivatives thereof substituted on the nitrogen are prepared starting from 4-hydroxy-3,5-di-tert.-butylbenzoic acid or its derivatives and homopiperazine or appropriate derivatives thereof.The compounds and their physiologically tolerated acid addition salts are suitable for the treatment of inflammatory and painful, in particular inflammatory rheumatic, disorders.
摘要翻译：从4-羟基-3,5-二叔丁基苯甲酸或其衍生物开始制备1-（4-羟基-3,5-二叔丁基苯甲酰基）高哌嗪及其在氮上取代的各种衍生物，以及高哌嗪或其适当的衍生物。化合物及其生理耐受的酸加成盐适用于治疗炎性和疼痛，特别是炎性风湿性疾病。

13. 发明授权

US5773470A Medicinal use of n-phenyl-2-cyano-3-hydroxycrotonamide derivatives 失效
标题翻译： N-苯基-2-氰基-3-羟基巴豆酰胺衍生物的药用
公开(公告)号：US5773470A
公开(公告)日：1998-06-30
申请号：US902626
申请日：1997-07-29
申请人： Rudolf Schleyerbach , Robert Ryder Bartlett , Elizabeth Anne Kuo , Edward James Little
发明人： Rudolf Schleyerbach , Robert Ryder Bartlett , Elizabeth Anne Kuo , Edward James Little
IPC分类号： C07C255/30 , A61K31/16 , A61K31/275 , A61K31/277 , A61P29/00 , A61P37/00 , A61P37/06 , C07C253/00 , C07C255/20 , C07C255/21 , C07C255/23 , C07C255/27 , C07C323/36
CPC分类号： A61K31/277 , A61K31/275 , C07C255/23
摘要： N-Phenyl-2-cyano-3-hydroxycrotonamide derivatives and their use as pharmaceuticals having an immunomodulatory property. The use of N-phenyl-2-cyano-3-hydroxycrotonamide derivatives of the formula I ##STR1## in which R.sup.1 is a hydrogen atom or (C.sub.1 -C.sub.4)-alkyl, R.sup.2 is CN, CX.sub.3, WCX.sub.3, W(CH.sub.2).sub.n CX.sub.3, NO.sub.2, (CH.sub.2).sub.n CX.sub.3, or halogen, in which X is halogen, W is an oxygen or sulfur atom and n is an integer from 1 to 3, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, CN or --CO--R.sup.4, in which R.sup.4 is (C.sub.1 -C.sub.4)-alkyl or (C.sub.3 -C.sub.6)-cycloalkyl, and/or their physiologically tolerable salts, for the treatment of rheumatic diseases, autoimmune diseases, and of rejection reactions of the organ recipient to the transplanted organ, is described.
摘要翻译： N-苯基-2-氰基-3-羟基巴豆酰胺衍生物及其作为具有免疫调节性的药物的用途。使用式I C 1 -C 4） - 烷基，R 2的N-苯基-2-氰基-3-羟基巴豆酰胺衍生物是CN，CX3，WCX3，W（CH2）nCX3，NO2，（CH2）nCX3或卤素，其中X是卤素，W是氧或硫原子，n是1-3的整数，R3是（C1-C4） - 烷基，（C3-C6） - 环烷基，CN或-CO-R4，其中 R4是用于治疗风湿性疾病，自身免疫疾病和器官受体对移植器官的排斥反应的（C 1 -C 4） - 烷基或（C 3 -C 6） - 环烷基和/或其生理上可耐受的盐，是描述。

14. 发明授权

US5679709A Medicaments to combat autoimmune diseases 失效
标题翻译：抵抗自身免疫性疾病的药物
公开(公告)号：US5679709A
公开(公告)日：1997-10-21
申请号：US478847
申请日：1995-06-07
申请人： Robert R. Bartlett , Rudolf Schleyerbach , Friedrich-Johannes Kammerer
发明人： Robert R. Bartlett , Rudolf Schleyerbach , Friedrich-Johannes Kammerer
IPC分类号： A61K31/275 , A61K31/42 , C07C255/23 , A61K31/16
CPC分类号： C07C255/23 , A61K31/275 , A61K31/42
摘要： A pharmaceutical composition for use in the treatment of chronic Graft-versus-host diseases as well as autoimmune diseases, in particular for the treatment of systemic lupus erythematosus containing as an active ingredient at least one compound of the formula 1 or 2 ##STR1## the latter being present per se or in the form of a physiologically tolerable salt. The invention also relates to a dosage unit form of said pharmaceutical composition and a method of treating chronic Graft-versus host diseases as well as autoimmune diseases, in particular systemic lupus erythematosus.
摘要翻译：一种用于治疗慢性移植物抗宿主病以及自身免疫疾病的药物组合物，特别是用于治疗系统性红斑狼疮的系统性红斑狼疮，所述系统性红斑狼疮含有至少一种式1或2化合物作为活性成分。后者本身存在或以生理上可耐受的盐的形式存在。本发明还涉及所述药物组合物的剂量单位形式和治疗慢性移植物抗宿主病以及自身免疫性疾病，特别是系统性红斑狼疮的方法。

15. 发明授权

US5470843A Carbohydrate-containing polymers, their preparation and use 失效
标题翻译：含碳水化合物的聚合物，其制备和用途
公开(公告)号：US5470843A
公开(公告)日：1995-11-28
申请号：US165805
申请日：1993-12-13
申请人： Wilhelm Stahl , Michael Ahlers , Axel Walch , Eckhart Bartnik , Gerhard Kretzschmar , Susanne Grabley , Rudolf Schleyerbach
发明人： Wilhelm Stahl , Michael Ahlers , Axel Walch , Eckhart Bartnik , Gerhard Kretzschmar , Susanne Grabley , Rudolf Schleyerbach
IPC分类号： A61K31/715 , A61K31/765 , A61K31/785 , A61K31/80 , A61K47/48 , A61K49/00 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P43/00 , C07H15/04 , C07H15/203 , C08B37/00 , C08G63/00 , C08G63/06 , C08G64/00 , C08G64/42 , C08G65/16 , C08G67/04 , C08G69/00 , C08G69/10 , C08G73/16 , A61K31/735
CPC分类号： C07H15/203 , A61K47/48207 , A61K47/48315 , C07H15/04
摘要： Carbohydrate-containing polymers which can have an HLB* of from about 10 to about 20 are disclosed. The compounds comprise a hydrophilic polymer portion, a carbohydrate portion comprising from 1 to about 20 naturally occurring, identical or different, monosaccharide units, at least one bifunctional spacer coupling the carbohydrate portion to the hydrophilic polymer portion, and a potentiator moiety. The potentiator moiety can be is a crosslinking moiety located within the hydrophilic polymer or a hydrophobic, hydrophilic or ionic moiety. Processes for the preparation and use of such polymers are also disclosed.
摘要翻译：公开了可以具有约10至约20的HLB *的含碳水化合物的聚合物。所述化合物包括亲水性聚合物部分，包含1至约20个天然存在的，相同或不同的单糖单元的碳水化合物部分，将碳水化合物部分与亲水性聚合物部分偶联的至少一个双功能间隔基和增强剂部分。增效剂部分可以是位于亲水性聚合物内的交联部分或疏水的，亲水的或离子的部分。还公开了制备和使用这些聚合物的方法。

16. 发明授权

US4965276A Medicaments to combat chronic graft-versus-host diseases 失效
标题翻译：抵抗慢性移植物抗宿主病的药物
公开(公告)号：US4965276A
公开(公告)日：1990-10-23
申请号：US911328
申请日：1986-09-25
申请人： Robert R. Bartlett , Rudolf Schleyerbach , Friedrich-Johannes Kammerer
发明人： Robert R. Bartlett , Rudolf Schleyerbach , Friedrich-Johannes Kammerer
IPC分类号： A61K31/275 , A61K31/42 , A61K31/425 , A61P37/00 , A61P37/02 , A61P37/04 , A61P37/06 , C07C255/23 , C07C255/24 , C07D261/18
CPC分类号： C07C255/23 , A61K31/275 , A61K31/42
摘要： A pharmaceutical composition for use in the treatment of chronic Graft-versus-host diseases as well as autoimmune diseases, in particular for the treatment of systemic lupus erythematosus containing as an active ingredient at least one compound of the formulae 1 or 2 ##STR1## the latter being present per se or in the form of a physiologically tolerable salt.The invention also relates to a dosage unit form of said pharmaceutical composition and a method of treating chronic Graft-versus host diseases as well as autoimmune diseases, in particular systemic lupus erythematosus.
摘要翻译：一种用于治疗慢性移植物抗宿主病以及自身免疫疾病的药物组合物，特别是用于治疗系统性红斑狼疮的系统性红斑狼疮，所述系统性红斑狼疮含有至少一种式1或2化合物作为活性成分。后者本身存在或以生理上可耐受的盐的形式存在。本发明还涉及所述药物组合物的剂量单位形式和治疗慢性移植物抗宿主病以及自身免疫性疾病，特别是系统性红斑狼疮的方法。

17. 发明授权

US4908364A Substituted 3-phenyl-7H-thiazol[3,2-b][1,2,4]-triazin-7-ones 失效
标题翻译：取代的3-苯基-7H-噻唑并[3,2-b] [1,2,4] - 三嗪-7-酮
公开(公告)号：US4908364A
公开(公告)日：1990-03-13
申请号：US149603
申请日：1988-01-28
申请人： Werner Thorwart , Ulrich Gebert , Rudolf Schleyerbach , Robert R. Bartlett
发明人： Werner Thorwart , Ulrich Gebert , Rudolf Schleyerbach , Robert R. Bartlett
IPC分类号： A61K31/53 , A61P29/00 , C07D253/06 , C07D253/075 , C07D285/16 , C07D513/04
CPC分类号： C07D253/075 , C07D285/16 , C07D513/04
摘要： Novel substituted 3-phenyl-7H-thiazolo[3,2-b][1,2,4]-triazin-7-ones of the formula I are disclosed ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meaning recited in the specification. The compounds are suitable for prevention and treatment of inflammatory disorders.
摘要翻译：公开了式（I）的新型取代的3-苯基-7H-噻唑并[3,2-b] [1,2,4] - 三嗪-7-酮，其中R 1，R 2和R 3具有在说明书中叙述的含义。该化合物适用于预防和治疗炎症性疾病。

18. 发明授权

US4636513A Isoxazole derivatives and medicaments containing these compounds 失效
标题翻译：异恶唑衍生物和含有这些化合物的药物
公开(公告)号：US4636513A
公开(公告)日：1987-01-13
申请号：US702312
申请日：1985-02-15
申请人： Friedrich-Johannes Kammerer , Rudolf Schleyerbach
发明人： Friedrich-Johannes Kammerer , Rudolf Schleyerbach
IPC分类号： C07D261/10 , A61K31/42 , A61K31/445 , A61K31/535 , A61K31/5377 , A61K31/54 , A61P25/04 , A61P29/00 , C07D261/18 , C07D413/06
CPC分类号： C07D413/06 , C07D261/18
摘要： 4-Isoxazolecarboxylic acid amides of the general formula I ##STR1## in which R denotes hydrogen, alkyl with up to 4 carbon atoms or halogenoalkyl with up to 2 carbon atoms andW denotes a direct bond, CH.sub.2, CH--CH.sub.3, CH--C.sub.2 H.sub.5, CHOH, O or S,processes for their preparation, medicaments which contain these compounds and the use of the compounds for the treatment of pain and/or fever.
摘要翻译：其中R表示氢，具有至多4个碳原子的烷基或具有至多2个碳原子的卤代烷基的通式I（I）的4-异恶唑羧酸酰胺，W表示直接键，CH 2，CH-CH 3， CH-C2H5，CHOH，O或S，其制备方法，含有这些化合物的药物和该化合物用于治疗疼痛和/或发烧的用途。

19. 发明授权

US4284786A 5-Methylisoxazole-4-carboxylic-(4-trifluoromethyl)-anilide 失效
标题翻译： 5-甲基异恶唑-4-羧酸（4-三氟甲基） - 苯胺
公开(公告)号：US4284786A
公开(公告)日：1981-08-18
申请号：US103551
申请日：1979-12-13
申请人： Friedrich-Johannes Kammerer , Rudolf Schleyerbach
发明人： Friedrich-Johannes Kammerer , Rudolf Schleyerbach
IPC分类号： A61K31/42 , A61P25/00 , A61P29/00 , A61P37/08 , C07D261/18 , C07D261/12
CPC分类号： C07D261/18 , Y10S514/825 , Y10S514/903 , Y10S514/916
摘要： 5-Methylisoxazole-4-carboxylic acid-(4-trifluoromethyl)-anilide and a process for its preparation is described. The compound has an antirheumatic, antiphlogistic, antipyretic and analgesic action, and can be used for the treatment of multiple sclerosis.
摘要翻译：描述了5-甲基异恶唑-4-羧酸 - （4-三氟甲基） - 苯胺及其制备方法。该化合物具有抗风湿，消炎，解热镇痛作用，可用于治疗多发性硬化。

20. 发明授权

US3931141A Novel heptapeptides having gastrin activity 失效
标题翻译：具有胃泌素活性的新型七肽
公开(公告)号：US3931141A
公开(公告)日：1976-01-06
申请号：US416012
申请日：1973-11-15
申请人： Hans Wissmann , Rolf Geiger , Rudolf Schleyerbach
发明人： Hans Wissmann , Rolf Geiger , Rudolf Schleyerbach
IPC分类号： C07K1/113 , A61K38/00 , A61P1/00 , A61P5/00 , C07K7/06 , C07K14/595 , C07C103/52 , A61K37/00
CPC分类号： C07K14/595 , A61K38/00 , Y02P20/55
摘要： Heptapeptides of the general formulaHOOC--(CH.sub.2).sub.3 --CO--Ala--Tyr--Gly--Trp--X--Asp--Phe--NH.sub.2in which X represents leucine or methionine, and process for preparing them by reacting tert.butyl-protected heptapeptides with glutaric acid anhydride and subsequently splitting off the protective groups with the aid of trifluoroacetic acid.
摘要翻译：通式为HOOC-（CH2）3-CO-Ala-Tyr-Gly-Trp-X-Asp-Phe-NH2的肽，其中X表示亮氨酸或甲硫氨酸，以及通过叔丁基保护的七肽用戊二酸酐，然后借助三氟乙酸分离保护基团。

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