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1. 发明授权

US5773447A Compounds for treating disorders of lipid metabolism and their preparation 失效
标题翻译：用于治疗脂质代谢紊乱及其制备的化合物
公开(公告)号：US5773447A
公开(公告)日：1998-06-30
申请号：US874255
申请日：1997-06-13
申请人： Gerhard Rackur , Hans Georg Boger , Norbert Krass , Axel Hoffmann , Michael Leineweber
发明人： Gerhard Rackur , Hans Georg Boger , Norbert Krass , Axel Hoffmann , Michael Leineweber
IPC分类号： A61K31/505 , A61P3/06 , C07D403/04 , C07D403/14 , C07D239/02
CPC分类号： C07D403/04 , C07D403/14
摘要： The present invention relates to tertiary 4-amino-2-ureidopyrimidine-5-carboxamides of formula I: ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.8)-alkyl wherein one or more H are replaced by F; R.sup.2 is selected from the group consisting of F, Cl, Br, H, --O--(C.sub.1 -C.sub.8)-alkyl and (C.sub.1 -C.sub.8)-alkyl, wherein one or more of the H of the alkyls can be replaced by F; R.sup.3 is selected from the group consisting of F, Cl, Br, H, --O--(C.sub.1 -C.sub.4)-alkyl and (C.sub.1 -C.sub.4)-alkyl, wherein one or more of the H of the alkyl can be replaced by F; R.sup.4 is CF.sub.3 or OCF.sub.3 ; and their physiologically tolerable salts. Process for preparing the compounds of formula I are also described. The compounds are suitable for the treatment of disorders of lipid metabolism.
摘要翻译：本发明涉及式I的叔-4-氨基-2-脲基嘧啶-5-甲酰胺：一个或多个H被F取代; R 2选自F，Cl，Br，H，-O-（C 1 -C 8） - 烷基和（C 1 -C 8） - 烷基，其中烷基的H中的一个或多个可以被F ; R 3选自F，Cl，Br，H，-O-（C 1 -C 4） - 烷基和（C 1 -C 4） - 烷基，其中烷基的H中的一个或多个可以被F ; R4是CF3或OCF3; 及其生理上可耐受的盐。还描述了制备式I化合物的方法。该化合物适用于治疗脂质代谢紊乱。

2. 发明授权

US5571816A Pyrimidines 失效
标题翻译：嘧啶类
公开(公告)号：US5571816A
公开(公告)日：1996-11-05
申请号：US515882
申请日：1995-08-16
申请人： Klaus-Dieter Kampe , Ernold Granzer , Michael Leineweber , Gerhard Rackur , Hans G. B oger
发明人： Klaus-Dieter Kampe , Ernold Granzer , Michael Leineweber , Gerhard Rackur , Hans G. B oger
IPC分类号： A61K31/505 , A61P3/06 , C07D233/04 , C07D233/30 , C07D233/36 , C07D233/38 , C07D403/04 , C07D239/48
CPC分类号： C07D403/04 , C07D233/38
摘要： Compounds of the formula I ##STR1## in which R.sup.1 to R.sup.6 have the stated meanings, and the readily water-soluble salts of these compounds, and a process for the preparation thereof are described. The compounds are suitable for the treatment of lipid metabolism disorders which are beneficially influenced by a stimulation of the hepatic LDL receptor.Also described are compounds of the formula II ##STR2## and the salts thereof.
摘要翻译：描述了其中R 1至R 6具有所述含义的式I的化合物及其易溶于水的这些化合物的盐及其制备方法。该化合物适用于治疗受到肝脏LDL受体刺激的有益影响的脂质代谢紊乱。还描述了式II II的化合物及其盐。

3. 发明授权

US4585775A Substituted pyrido (1,2-c)imidazo(1,2-a)benzimidazoles, processes for their preparation, their use and pharmaceutical preparations based on these compounds 失效
标题翻译：取代的吡啶（1,2-c）咪唑并（1,2-a）苯并咪唑，其制备方法及其用途和基于这些化合物的药物制剂
公开(公告)号：US4585775A
公开(公告)日：1986-04-29
申请号：US650106
申请日：1984-09-13
申请人： Volker Hitzel , Gerhard Rackur , Martin Bickel
发明人： Volker Hitzel , Gerhard Rackur , Martin Bickel
IPC分类号： C07D471/10 , A61K31/435 , A61P1/04 , C07D213/38 , C07D213/53 , C07D401/06 , C07D471/14 , A61K31/44 , C07D471/12
CPC分类号： C07D213/53 , C07D213/38 , C07D401/06 , C07D471/14 , Y02P20/55
摘要： The invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen, alkyl, trifluoromethyl, halogen, alkoxycarbonyl, alkoxy or alkanoyl, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, methyl, alkoxy or alkoxyethoxy, and R is hydrogen or a group SR.sup.6, in which R.sup.6 is the lone, unpaired electron of the 12-sulfenyl radical, hydrogen, optionally substituted alkyl, alkenyl, alkynyl, alkanoyl, optionally mono- or poly-substituted benzoyl, fuoryl, phenacyl, phenoxyacetyl, phenylacetyl or another conventional thiol-protective group, and to physiologically acceptable salts thereof, and to processes for their preparation, to their use as a gastric acid secretion inhibitor and to pharmaceutical preparations based on these compounds.
摘要翻译：本发明涉及式（I）的化合物，其中R 1和R 2相同或不同，为氢，烷基，三氟甲基，卤素，烷氧基羰基，烷氧基或烷酰基，R 3，R 4和R 5相同或不同，氢，甲基，烷氧基或烷氧基乙氧基，R是氢或基团SR6，其中R6是12-亚磺酰基的单体不成对电子，氢，任选取代的烷基，烯基，炔基，烷酰基，任选单或多取代苯甲酰基，富酰基，苯甲酰甲基，苯氧基乙酰基，苯乙酰基或另一种常规硫醇保护基，及其生理上可接受的盐，及其制备方法，用作胃酸分泌抑制剂和基于这些化合物的药物制剂。

4. 发明授权

US4305952A 8-Aryl-5,6,7,8-tetrahydropyrazolo(3,4-B)(1,4)-diazepine-1H, 4H-5,7-diones, and medicaments containing these 失效
标题翻译： 8-芳基-5,6,7,8-四氢吡唑并（3,4-B）（1,4） - 二氮杂-1H，4H-5,7-二酮和含有这些
公开(公告)号：US4305952A
公开(公告)日：1981-12-15
申请号：US122692
申请日：1980-02-19
申请人： Gerhard Rackur , Irmgard Hoffmann
发明人： Gerhard Rackur , Irmgard Hoffmann
IPC分类号： A61K31/55 , A61P25/20 , C07D231/38 , C07D231/40 , C07D487/04
CPC分类号： C07D487/04 , C07D231/38 , C07D231/40
摘要： 8-Aryl-5,6,7,8-tetrahydropyrazolo(3,4-b)(1,4)diazepine-1H,4H-5,7-diones of the formula ##STR1## in which R.sub.1 through R.sub.5 are as defined in the specification, and medicaments containing these having an anxiolytic action.
摘要翻译： 8-芳基-5,6,7,8-四氢吡唑并（3,4-b）（1,4）二氮杂-1H，4H-5,7-二酮，其中R1至R5为在本说明书中定义，含有具有抗焦虑作用的药物。

5. 发明授权

US4302468A 4-Aryl-5,6,7,8-tetrahydropyrazolo(3,4-B)-(1,5)diazepine-1H,4H-5,7-diones and medicaments containing same 失效
标题翻译： 4-芳基-5,6,7,8-四氢吡唑并（3,4-B） - （1,5）二氮杂-1H，4H-5,7-二酮和含有它们的药物
公开(公告)号：US4302468A
公开(公告)日：1981-11-24
申请号：US177411
申请日：1980-08-12
申请人： Gerhard Rackur , Irmgard Hoffmann
发明人： Gerhard Rackur , Irmgard Hoffmann
IPC分类号： A61K31/55 , A61P25/20 , C07D231/38 , C07D231/40 , C07D487/04 , A61K31/415
CPC分类号： C07D231/38 , C07D231/40 , C07D487/04
摘要： Compound of the general formula ##STR1## in which R.sub.1 and R.sub.2 are identical or different and represent hydrogen atoms or alkyl groups with 1-6 C atoms, it also being possible for one of the radicals R.sub.1 and R.sub.2 to be, in each case, a benzyl, trifluoromethyl or phenyl group, R.sub.3 denotes a hydrogen atom, an alkyl group which has 1-6 C atoms and is optionally substituted by an aryl group, an alkoxy group with 1-6 C atoms, a trifluoromethyl group, a dialkylamino group with 2-12 C atoms or a cycloalkyl group with 3-6 C atoms, an alkenyl or alkynyl group with 2-6 C atoms, a cycloalkyl group with 3-6 C atoms or a carbalkoxy group with 2-6 C atoms, R.sub.4 is a hydrogen atom and R.sub.5 can be a phenyl group, a phenyl group which is monosubstituted or disubstituted by methyl Cl, Br, F, nitro, cyano and or trifluoromethyl or a pyridyl group and medicaments containing same.
摘要翻译：其中R 1和R 2相同或不同并且表示氢原子或具有1-6个C原子的烷基的通式为“IMAGE”I的化合物，在每一种情况下，基团R 1和R 2之一也可以是苄基，三氟甲基或苯基，R 3表示氢原子，具有1-6个C原子且任选被芳基取代的烷基，具有1-6个C原子的烷氧基，三氟甲基，二烷基氨基具有2-12个碳原子或3-6个碳原子的环烷基，2-6个C原子的烯基或炔基，3-6个碳原子的环烷基或2-6个C原子的烷氧基， R4是氢原子，R5可以是苯基，被C1，Br，F，硝基，氰基和/或三氟甲基或吡啶基甲基单取代或二取代的苯基和含有它们的药物。

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