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1. 发明授权

US5814627A 3, 5-disubstituted and 3, 4, 5-trisubstituted 2-isoxazolines and isoxazoles, process for their preparation and their use as pharmaceuticals 失效
标题翻译： 3,5-二取代和3,4,5-三取代的2-异恶唑啉和异恶唑，其制备方法及其作为药物的用途
公开(公告)号：US5814627A
公开(公告)日：1998-09-29
申请号：US704743
申请日：1996-11-19
申请人： Wilfried Schwab , Hiristo Anagnostopulos , Robert Ryder Bartlett , Rudolf Schleyerbach , Klaus Ulrich Weithmann
发明人： Wilfried Schwab , Hiristo Anagnostopulos , Robert Ryder Bartlett , Rudolf Schleyerbach , Klaus Ulrich Weithmann
IPC分类号： A61K31/41 , A61K31/42 , A61K31/423 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , A61P11/00 , A61P29/00 , A61P37/00 , C07C205/51 , C07D261/04 , C07D261/08 , C07D261/18 , C07D261/20 , C07D263/30 , C07D413/04 , C07D413/12 , C07D417/04 , C07F9/653
CPC分类号： C07C205/51 , C07D261/04 , C07D261/08 , C07D261/20 , C07D413/04 , C07D413/12 , C07D417/04 , C07F9/653
摘要： A compound having the formula (I), a physiologically tolerable salt of the compound having the formula (I) and/or a steroisomeric form of the compound having the formula (I), in which one residue R.sup.1 or R.sup.2 stands for the formula (II), are suitable for preparing medicaments for the therapy of inflammations, asthma, rheumatoid diseases and auto-immune diseases.
摘要翻译： PCT No.PCT / EP95 / 00784 Sec。 371日期1996年11月19日 102（e）1996年11月19日PCT PCT 1995年3月3日PCT公布。第WO95 / 24397号公报日期1995年9月14日具有式（I）的化合物，具有式（I）的化合物的生理上可耐受的盐和/或具有式（I）的化合物的立体异构形式，其中一个残基R1或R2 代表式（II），适用于制备用于治疗炎症，哮喘，类风湿病和自身免疫性疾病的药物。

2. 发明授权

US5714514A 2-Cyano-3-mercaptocrotonamides 失效
标题翻译： 2-氰基-3-巯基巴豆酰胺
公开(公告)号：US5714514A
公开(公告)日：1998-02-03
申请号：US715270
申请日：1996-09-16
申请人： Friedrich-Johannes Kammerer , Rudolf Schleyerbach , Werner Thorwart
发明人： Friedrich-Johannes Kammerer , Rudolf Schleyerbach , Werner Thorwart
IPC分类号： C07D521/00 , A61K31/275 , A61P1/00 , A61P1/16 , A61P3/08 , A61P11/00 , A61P17/00 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , C07C319/02 , C07C323/51 , C07C323/60 , C07D295/185 , A61K31/33 , C07C255/33
CPC分类号： C07D295/185 , C07C323/60
摘要： The present invention relates to 2-cyano-3-mercaptocrotonamide derivatives, a process for their preparation, and their use the treatment of immune disorders, carcinomatous disorders, rejection reactions in transplantations and skin disorders or allergy.
摘要翻译：本发明涉及2-氰基-3-巯基巴豆酰胺衍生物，其制备方法及其用途，其用于治疗免疫疾病，癌性疾病，移植排斥反应和皮肤病或变态反应。

3. 发明授权

US4351841A Pharmaceutical preparation and method of treatment 失效
标题翻译：药物制剂及治疗方法
公开(公告)号：US4351841A
公开(公告)日：1982-09-28
申请号：US239986
申请日：1981-03-03
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
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。

4. 发明授权

US6037467A Methods for preparing carbohydrate-containing hydrophilic polymers 失效
标题翻译：制备含碳水化合物的亲水性聚合物的方法
公开(公告)号：US6037467A
公开(公告)日：2000-03-14
申请号：US898464
申请日：1997-07-24
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 , C07H1/00
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。

5. 发明授权

US5308865A 2-cyano-3-hydroxy-enamides 失效
标题翻译： 2-氰基-3-羟基 - 烯酰胺
公开(公告)号：US5308865A
公开(公告)日：1994-05-03
申请号：US1564
申请日：1993-01-06
申请人： Robert R. Bartlett , David P. Kay , Elizabeth A. Kuo , Rudolf Schleyerbach , Wilfried Schwab
发明人： Robert R. Bartlett , David P. Kay , Elizabeth A. Kuo , Rudolf Schleyerbach , Wilfried Schwab
IPC分类号： A61K31/165 , A61K31/275 , A61K31/277 , A61P29/00 , C07C255/19 , C07C255/23 , C07C255/26 , C07C255/60 , C07C255/61 , C07C323/41 , C07C255/36
CPC分类号： C07C255/19 , C07C255/23
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## R.sub.13, R.sub.14 and R.sub.15 are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 3 carbon atoms, n is an integer from 1 to 3, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4 R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, alkylcarbonyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, ##STR3## m is 0, 1, 2 or 3, n is 1, 2 or 3; Hal, Hal.sub.1, Hal.sub.2 and Hal.sub.3 are individually halogen and ##STR4## R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are individually any of the groups defined above for R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 or R.sub.4 and R.sub.5 together form --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable base addition salts having anti-inflammatory activity.
摘要翻译：选自下列化合物的化合物的化合物其中R 1选自下组的化合物：其中R 1选自由下列组成的组：R 1，R 14和R 15分别选自氢，卤素和烷基 1至3个碳原子，n为1至3的整数，R2为氢或1至3个碳原子的烷基，R3，R4 + L，R5，R6和R7分别选自氢，卤素，碳原子数1〜6的烷氧基，碳原子数为2〜6的烷基羰基，碳原子数3〜6的环烷基，（CH 2）m CF 3，O（CH 2）m CF 3，S（CH 2） mCF3， m为0,1,2或3，n为1,2或3; Hal，Hal1，Hal2和Hal3分别为卤素，R8，R9，R10，R11和R12分别是R3，R4，R5，R6和R7中定义的任何基团，R4或R5一起形成-O- CH2-O-及其具有抗炎活性的无毒的药学上可接受的碱加成盐。

6. 发明授权

US4940790A 5-(3-alkyl-5-tert.butyl-4-hydroxyphenyl)-2-amino-6H-1,3,4-thiadiazines 失效
标题翻译： 5-（3-烷基-5-叔丁基-4-羟基苯基）-2-氨基-6H-1,3,4-噻二嗪
公开(公告)号：US4940790A
公开(公告)日：1990-07-10
申请号：US149601
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： A61K31/54 , A61P25/04 , A61P29/00 , A61P43/00 , C07D285/16
CPC分类号： C07D285/16
摘要： Novel 5-(3-alkyl-5-tert.butyl-4-hydroxyphenyl)-2-amino-6H-1,3,4-thiadiazines of the general formula I ##STR1## in which R.sup.1 =C.sub.1 -C.sub.4 -alkyl,R.sup.2 =H or C.sub.1 -C.sub.3 -alkylR.sup.3 and R.sup.4 =independently of one another, optionally substituted and optionally O- or S-interrupted alkyl, alkenyl or alkynyl groups, it being possible for one of the two radicals to also be H,or R.sup.3 +R.sup.4 together with the nitrogen atom to which they are bound, may denote an optionally substituted 4- to 7-membered ring which optionally contains a further heteroatom (O, S or N),and the physiologically acceptable acid-addition salts thereof. The compounds are primarily suitable for prevention and treatment of inflammatory--in particular inflammatory rheumatic--disorders and/or pain.
摘要翻译：通式Ⅰ的新型5-（3-烷基-5-叔丁基-4-羟基苯基）-2-氨基-6H-1,3,4-噻二嗪其中R1 = C1-C4 - 烷基，R 2 = H或C 1 -C 3 - 烷基R 3和R 4彼此独立地是任选取代的，任选地O-或S-间隔的烷基，链烯基或炔基，两个基团之一也可以是 H或R 3 + R 4与它们所连接的氮原子一起可以表示任选取代的4-至7-元环，其任选地含有另外的杂原子（O，S或N）和生理上可接受的酸加成的盐。该化合物主要适用于预防和治疗炎症特别是炎性风湿病和/或疼痛。

7. 发明授权

US5747664A 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
公开(公告)号：US5747664A
公开(公告)日：1998-05-05
申请号：US350740
申请日：1994-12-07
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 , C07C255/17
CPC分类号： A61K31/277 , A61K31/275 , C07C255/23
摘要： 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, auto-immune diseases, and of rejection reactions of the organ recipient to the transplanted organ, is described.
摘要翻译：使用其中R 1为氢原子或（C 1 -C 4） - 烷基，R 2为CN，CX 3，WCX 3，W的式I（I）的N-苯基-2-氰基-3-羟基巴豆酰胺衍生物（CH2）nCX3，NO2，（CH2）nCX3或卤素，其中X为卤素，W为氧或硫原子，n为1至3的整数，R3为（C1-C4） - 烷基，（C3 -C 6） - 环烷基，CN或-CO-R 4，其中R 4为（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，用于治疗风湿性疾病，描述了器官受体对移植器官的免疫疾病和排斥反应。

8. 发明授权

US5268382A Medicaments to combat autoimmune diseases, in particular systemic lupus erythematosus 失效
标题翻译：抵抗自身免疫疾病的药物，特别是系统性红斑狼疮
公开(公告)号：US5268382A
公开(公告)日：1993-12-07
申请号：US870327
申请日：1992-04-17
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
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疾病，特别是系统性红斑狼疮的方法。

9. 发明授权

US4891374A Imidazo- and triazolothiadiazines 失效
标题翻译：咪唑并和三唑并噻二嗪
公开(公告)号：US4891374A
公开(公告)日：1990-01-02
申请号：US149546
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： A61K31/54 , A61P29/00 , A61P37/00 , C07D233/54 , C07D233/84 , C07D233/86 , C07D513/04
CPC分类号： C07D513/04 , C07D233/84 , C07D233/86
摘要： Novel imidazo- and triazolothiadiazines of the general formula I ##STR1## in which R.sup.1 =C.sub.1 -C.sub.4 -alkyl,R.sup.2 =H or C.sub.1 -C.sub.3 -alkyland the structural element --A--B--=--CH.sub.2 --CH.sub.2 --, --CH CH--, --CH.dbd.N--, --CH.sub.2 --CO-- or --CO--CH.sub.2 --,and the physiologically aceptable acid-addition salts thereof, are prepared by reacting 2-halo-1-phenylalkanones of the formula II ##STR2## (meaning of R.sup.1 and R.sup.2 as in formula I, X=halogen) with compounds of the formula III ##STR3## (meaning of --A--B-- as in formula I) and, if appropriate, converting the compounds of the formula I formed into the physiologically acceptable acid-addition salts thereof by means of suitable acids.The compounds of the formula I and the physiologically acceptable acid-addition salts thereof are principally suitable for the prevention and treatment of inflammatory--in particular inflammatory rheumatic--disorders.Some of the intermediates formed during the preparation of the compounds of the formula I are also novel, namely 1-amino-2-mercaptoimidazole ##STR4## and 1-amino-2-thioxo-5-imidazolidinone ##STR5##
摘要翻译：其中R 1 = C 1 -C 4 - 烷基，R 2 = H或C 1 -C 3 - 烷基和结构元素-AB - = - CH 2 -CH 2 - ， - 的通式I（I）的新型咪唑并 - 和三唑并噻二嗪， CH CH - ， - CH = N - ， - CH 2 -CO-或-CO-CH 2 - ，及其生理上可接受的酸加成盐，通过使式II的2-卤代-1-苯基烷基酮（II）（式I中R 1和R 2的含义，X =卤素）与式III化合物（III）（式I中的-AB-的含义）反应，如果合适，将化合物式I通过合适的酸形成生理上可接受的酸加成盐。式I化合物及其生理上可接受的酸加成盐主要适用于预防和治疗炎症特别是炎性风湿病。在制备式I化合物期间形成的一些中间体也是新的，即1-氨基-2-巯基咪唑和1-氨基-2-硫代-5-咪唑啉酮。

10. 发明授权

US5371099A Phenyl carboxamide isoxazoles 失效
标题翻译：苯基甲酰胺异恶唑
公开(公告)号：US5371099A
公开(公告)日：1994-12-06
申请号：US54893
申请日：1993-04-28
申请人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
发明人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
IPC分类号： A61K31/42 , A61P29/00 , C07C235/78 , C07C235/80 , C07C255/60 , C07C323/41 , C07D207/06 , C07D261/18 , C07D295/145 , C07D261/08 , C07D261/12
CPC分类号： C07D295/145 , C07C235/80 , C07C255/60 , C07C323/41 , C07D261/18 , C07C2101/02
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 3 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, R.sub.3 is --COOR.sub.6, R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.4 is selected from the group consisting of halogen, --CN, --NO.sub.2, --SCH.sub.3, alkylcarbonyl of 1 to 6 alkyl carbon atoms, --CX.sub.3, --WCX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --W--(CX.sub.2).sub.n --CX.sub.3, and --W--(CH.sub.2).sub.n --CX.sub.3, X is halogen, W is --O-- or --S--, n is 1, 2 or 3, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms and their salts with non-toxic pharmaceutically acceptable bases with the proviso that if R.sub.2 is alkyl of 1 to 3 carbon atoms, R.sub.1 is hydrogen and R.sub.4 is selected from the group consisting of halogen, --CX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --OCX.sub.3, --O--(CX.sub.2).sub.n --CX.sub.3, and --O--(CH.sub.2).sub.n --CX.sub.3, X is halogen and n is 1, 2 or 3, R.sub.5 cannot be hydrogen having anti-inflammatory activity and their preparation and intermediates.
摘要翻译：选自下式的化合物的化合物其中R 1为氢或1至3个碳原子的烷基，R 2为1至3个碳原子的烷基或3至6个碳原子的环烷基，R 3为 -COOR 6，R 6是氢或1至3个碳原子的烷基，R 4选自卤素，-CN，-NO 2，-SCH 3，1至6个烷基碳原子的烷基羰基，-CX 3，-WCX 3，（CH 2）n -CX 3， - （CX 2）n -CX 3，-W-（CX 2）n -CX 3和-W-（CH 2）n -CX 3，X是卤素，W是-O-或-S-， n为1,2或3，R5选自氢，1至3个碳原子的烷基和3至6个碳原子的环烷基及其与无毒的药学上可接受的碱的盐，条件是如果R2为 1至3个碳原子的烷基，R1是氢，R4选自卤素，-CX3， - （CH2）n -CX3， - （CX2）n -CX3，-OCX3，-O-（CX2） n -CX3和-O-（CH2）n -CX3，X是卤素，n是1,2或3，R5不能是具有抗炎活性的氢及其制备和中间体。

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