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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 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。

10. 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。

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