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1. 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。

2. 发明授权

US5430110A Polyvinylamine derivatives having hydrophilic centers, processes for their preparation and the use of the compounds as a medicament, active compound carrier and foodstuff auxiliary 失效
标题翻译：具有亲水中心的聚乙烯胺衍生物，其制备方法和化合物作为药物的用途，活性化合物载体和食品助剂
公开(公告)号：US5430110A
公开(公告)日：1995-07-04
申请号：US95623
申请日：1993-07-21
申请人： Michael Ahlers , Heiner Glombik , Susanne Grabley , Ernold Granzer , Stefan Mullner , Axel Walch , Guan-Yu Xu
发明人： Michael Ahlers , Heiner Glombik , Susanne Grabley , Ernold Granzer , Stefan Mullner , Axel Walch , Guan-Yu Xu
IPC分类号： A23L33/00 , A61K31/785 , A61K47/30 , A61P3/06 , A61P3/12 , C08F8/12 , C08F26/00 , C08F226/02 , C08F8/30
CPC分类号： C08F8/12
摘要： Polyvinylamine derivatives having hydrophilic centers, processes for their preparation and the use of the compounds as a medicament, active compound carrier and foodstuff auxiliary.Polyvinylamine derivatives containing hydrophilic centers, of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X, w, x, y and z have the meanings given, and a process for their preparation, and the use of these compounds as medicaments, active compound carriers and foodstuff auxiliaries are described. Highly pure polyvinylamines having the recurring unit of the formula Ia ##STR2## the preparation of which is likewise described, are used in particular as starting substances for the preparation.
摘要翻译：具有亲水中心的聚乙烯胺衍生物，其制备方法和化合物作为药物的用途，活性化合物载体和食品助剂。含有亲水中心的聚乙烯胺衍生物，其中R 1，R 2，R 3，X，W，x，y和z具有给定的含义的式I（I）及其制备方法，以及这些描述了作为药物的化合物，活性化合物载体和食品助剂。具有式Ia（Ia）的重复单元的高纯度聚乙烯胺其制备同样被描述，特别是用作制备的起始物质。

3. 发明授权

US4929643A Benzenesulfonamide derivatives and a process for the preparation thereof 失效
标题翻译：苯磺酰胺衍生物及其制备方法
公开(公告)号：US4929643A
公开(公告)日：1990-05-29
申请号：US345168
申请日：1989-05-01
申请人： Hans-Jochen Lang , Max Hropot , Ernold Granzer , Bela Kerekjarto
发明人： Hans-Jochen Lang , Max Hropot , Ernold Granzer , Bela Kerekjarto
IPC分类号： C07D207/27 , C07D207/26 , C07D207/273
CPC分类号： C07D207/273
摘要： Compounds of the formula I ##STR1## with R.sup.1 equal to H or (cyclo)alk(en)yl, R.sup.2 equal to H or alkyl, R.sup.3 equal to alkyl, R.sup.4 /R.sup.5 equal to H, alkyl or acyl, and Y equal to H, alkyl, CF.sub.3 or Hal, are described, as are processes for the preparation thereof.They are effective diuretics and antihypertensive agents with a lipid-lowering action.

4. 发明授权

US4238626A 4-Phenoxy-phenoxy-alkane-carboxylic acid derivatives and process for their manufacture 失效
标题翻译： 4-苯氧基 - 苯氧基 - 烷烃 - 羧酸衍生物及其制备方法
公开(公告)号：US4238626A
公开(公告)日：1980-12-09
申请号：US905049
申请日：1978-05-11
申请人： Helmut Nahm , Ernold Granzer
发明人： Helmut Nahm , Ernold Granzer
IPC分类号： A61K31/19 , C07C37/05 , C07C43/263 , C07C43/29 , C07C51/09 , C07C59/68 , C07C59/70 , C07C69/712 , C07C69/736
CPC分类号： C07C323/00 , C07C51/09 , C07C59/68
摘要： Novel 4-phenoxy-phenoxy-alkane-carboxylic acid derivatives of the formula I ##STR1## in which R.sub.1 stands for hydrogen, methylthio, cyclopentyl, cyclohexyl, phenyl, methylcyclohexyl, ethylcyclohexyl, or R.sub.1 and R.sub.3 together stand for a --CH.dbd.CH--CH.dbd.CH-- bridge or--unless at least one of the substituents R.sub.2 to R.sub.8 stands for hydrogen, or if R.sub.9 stands for a radical having at least 2 carbon atoms--for chlorine,R.sub.2 and R.sub.3, independent of one another, each stands for hydrogen, chlorine or alkyl of 1 to 4 carbon atoms,R.sub.4 stands for hydrogen, chlorine, alkyl of 1 to 4 carbon atoms, cyclopentyl, cyclohexyl, methylcyclohexyl or R.sub.3 and R.sub.4 together stand for a --CH.dbd.CH--CH.dbd.CH-- bridge,R.sub.5, R.sub.6 and R.sub.7, independent of one another, each stands for hydrogen or alkyl of 1 to 4 carbon atoms,R.sub.8 stands for hydrogen, alkyl of 1 to 4 carbon atoms or allyl,R.sub.9 stands for alkyl of 1 to 10 carbon atoms or phenyl andX stands for hydrogen, the cation of a physiologically acceptable inorganic or organic base of a hydrocarbon radical of 1 to 10 carbon atoms, having a strong action on the lipide and cholesterine metabolism and a process for their manufacture.
摘要翻译： R1代表氢，甲硫基，环戊基，环己基，苯基，甲基环己基，乙基环己基或R 1和R 3的新的4-苯氧基 - 苯氧基 - 烷 - 羧酸衍生物，其中R1代表氢，甲基， -CH = CH-桥或 - 除非取代基R2至R8中的至少一个代表氢，或者如果R9表示具有至少2个碳原子的基团，则对于氯，R 2和R 3彼此独立地，各自独立地对于氢，氯或1至4个碳原子的烷基，R4代表氢，氯，1至4个碳原子的烷基，环戊基，环己基，甲基环己基或R3和R4一起代表-CH = CH-CH = CH- 桥，R5，R6和R7彼此独立，各代表氢或1-4个碳原子的烷基，R8代表氢，1-4个碳原子的烷基或烯丙基，R9代表1-10个碳原子的烷基原子或苯基，X代表氢，生理上可接受的无机或有机碱的烃的阳离子具有1至10个碳原子的基团，对脂质和胆固醇代谢具有强烈的作用及其制造方法。

5. 发明授权

US4056629A Pharmacologically active O-acyl-2,3-diaryl-3-halogeno-acryl-aldoximes 失效
标题翻译：药理活性的O-酰基-2,3-二芳基-3-卤代丙烯酰基肟
公开(公告)号：US4056629A
公开(公告)日：1977-11-01
申请号：US716277
申请日：1976-08-20
申请人： Wilhelm Bartmann , Gerhard Beck , Ernold Granzer , Josef Musil , Hermann Teufel
发明人： Wilhelm Bartmann , Gerhard Beck , Ernold Granzer , Josef Musil , Hermann Teufel
IPC分类号： A61K20060101 , A61K31/15 , A61K31/215 , A61K31/27 , C07C20060101
CPC分类号： C07D417/04
摘要： A medicament consisting of or containing an O-acyl-2,3-diaryl-3-halogeno-acrylaldoxime of the formula I ##STR1## in which X represents a chlorine or bromine atom, R stands for an alkyl, alkenyl, alkoxy, alkenoxy or alkylamino group having from 1 to 12 carbon atoms each, or for an aryl, aryloxy, arylalkyl, arylalkoxy, arylamino or arylalkylamino group substituted optionally by 1 or 2 alkyl groups each having from 1 to 6 carbon atoms, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different, each representing a hydrogen atom, a halogen atom or an alkyl or alkoxy group having each from 1 to 6 carbon atoms, a process for preparing them and a method for the treatment of disorders of the purine metabolism.
摘要翻译：由式I（I）的O-酰基-2,3-二芳基-3-卤代 - 丙烯醛肟组成或含有其中X表示氯或溴原子的药物，R代表烷基，烯基，或具有1至12个碳原子的芳基，芳氧基，芳基烷基，芳基烷氧基，芳基氨基或芳基烷基氨基，任选地被1或2个具有1至6个碳原子的烷基取代的烷氧基，链烯氧基或烷基氨基， R2，R3和R4相同或不同，各自表示氢原子，卤素原子或具有1至6个碳原子的烷基或烷氧基，其制备方法和治疗嘌呤病症的方法代谢。

6. 发明授权

US4001431A Derivatives of the 1,2-diarylethylene- and pharmaceutical compositions thereof 失效
标题翻译：其1,2-二氨基乙烯和其药物组合物的衍生物
公开(公告)号：US4001431A
公开(公告)日：1977-01-04
申请号：US556221
申请日：1975-03-07
申请人： Hermann Teufel , Wilhelm Bartmann , Ernold Granzer , Josef Musil
发明人： Hermann Teufel , Wilhelm Bartmann , Ernold Granzer , Josef Musil
IPC分类号： C07C251/32 , A61K20060101 , A61K31/00 , A61K31/11 , A61K31/15 , A61K31/275 , C07C20060101 , C07C47/38 , C07C67/00 , C07C253/00 , C07C255/34 , C07C255/35 , C07C255/53 , C07C131/00
CPC分类号： C07C255/00
摘要： The invention relates to derivatives of 1,2-diarylethylene and to a process for their preparation. The compounds have valuable pharmaceutical properties and may be used as medicaments.

7. 发明授权

US5795899A Soluble salts of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl) pyrimidine-5-carboxylic acid N-methyl-N-(3-trifluoromethylphenyl)-amide, a process for the preparation thereof, the use thereof as pharmaceuticals and starting materials 失效
标题翻译： 4-氨基-2-（4,4-二甲基咪唑烷-2-酮-1-基）嘧啶-5-甲酸N-甲基-N-（3-三氟甲基苯基） - 酰胺的可溶性盐，其制备方法，其作为药物和起始材料的用途
公开(公告)号：US5795899A
公开(公告)日：1998-08-18
申请号：US394521
申请日：1995-02-23
申请人： Klaus-Dieter Kampe , Ernold Granzer , Michael Leineweber , Manfred Huttinger
发明人： Klaus-Dieter Kampe , Ernold Granzer , Michael Leineweber , Manfred Huttinger
IPC分类号： A61K31/505 , A61K31/506 , A61P3/00 , A61P3/06 , C07D233/36 , C07D233/38 , C07D403/04 , C07D403/02
CPC分类号： C07D403/04 , C07D233/38
摘要： Soluble salts of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl)pyrimidine-5-carboxylic acid N-methyl-N-(3-trifluoromethylphenyl)amide, a process for the preparation thereof, the use thereof as pharmaceuticals and starting materials. Salts, which are soluble and freely soluble in water, of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl)pyrimidine-5-carboxylic acid N-methyl-N-(3-trifluoromethylphenyl)-amide 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 stimulation of the hepatic LDL receptor. Also described are the compounds of the formula IV ##STR1## and the salts thereof.
摘要翻译： 4-氨基-2-（4,4-二甲基咪唑烷-2-酮-1-基）嘧啶-5-甲酸N-甲基-N-（3-三氟甲基苯基）酰胺的可溶性盐，其制备方法，其作为药物和原料的用途。 4-氨基-2-（4,4-二甲基咪唑烷-2-酮-1-基）嘧啶-5-甲酸N-甲基-N-（3-三氟甲基苯基）嘧啶-5-羧酸的水溶性和易溶于水的盐， - 酰胺及其制备方法。该化合物适用于治疗有益于肝LDL受体刺激影响的脂质代谢紊乱。还描述了式IV的化合物及其盐。

8. 发明授权

US5292898A Process for the stereoselective preparation of 5-substituted delta-lactones and use thereof 失效
标题翻译： 5-取代的δ-内酯的立体选择性制备方法及其用途
公开(公告)号：US5292898A
公开(公告)日：1994-03-08
申请号：US937718
申请日：1992-09-01
申请人： Peter Hammann , Susanne Grabley , Ernold Granzer , Yvonne Romeyke
发明人： Peter Hammann , Susanne Grabley , Ernold Granzer , Yvonne Romeyke
IPC分类号： C07C31/22 , C07C33/02 , C07C45/51 , C07C49/24 , C07D309/30 , C07D309/10
CPC分类号： C07D309/30 , C07C31/22 , C07C33/02 , C07C45/513 , C07C49/24
摘要： A process for the stereoselective preparation of 5-substituted .delta.-lactones of the formulae Ia, Ib, Ic and Id ##STR1## in which R.sup.1 is a straight-chain or branched alkyl or alkenyl group or methylhydroxy, novel 5-substituted .delta.-lactones and novel intermediates, and use thereof as pharmaceuticals having cholesterol synthesis-inhibiting action, fragrances and flavorings is described.
摘要翻译：用于立体选择性制备式Ia，Ib，Ic和Id的5-取代的δ-内酯的方法，其中R 1是直链或支链烷基或烯基或甲基羟基，新的5-取代描述了作为具有胆固醇合成抑制作用的药物，香料和调味剂的用途。

9. 发明授权

US5143937A Benzenesulfonamides and a process for their preparation 失效
标题翻译：苯并呋喃类及其制备方法
公开(公告)号：US5143937A
公开(公告)日：1992-09-01
申请号：US480932
申请日：1990-02-16
申请人： Hans-Jochen Lang , Ernold Granzer , Bela Kerekjarto
发明人： Hans-Jochen Lang , Ernold Granzer , Bela Kerekjarto
IPC分类号： A61K31/18 , A61P3/06 , C07C303/38 , C07C311/21 , C07C311/29 , C07C311/44 , C07C317/10 , C07C317/14 , C07C323/67
CPC分类号： C07C323/67 , C07C311/21 , C07C311/29 , C07C317/14 , Y10S514/824 , Y10S514/869
摘要： Compounds of the formula I ##STR1## where R.sup.1 to R.sup.5 have the meaning indicated, a process for their preparation and their use as medicaments are described. They are effective lipid-lowering agents with antioxidative properties from the benzenesulfonamide series. They do not have hypotensive and diuretic properties.
摘要翻译：描述了其中R1至R5具有所示含义的式I的化合物，其制备方法及其作为药物的用途。它们是来自苯磺酰胺系列的具有抗氧化性质的有效降脂剂。他们没有低血压和利尿性质。

10. 发明授权

US5091386A 7-substituted derivatives of 3,5-dihydroxyhept-6-ynoic acids and corresponding lactones and their use as hypercholeserolemics 失效
标题翻译： 3,5-二羟基-6-氰基酸和相应乳液的7-取代衍生物及其作为高效液相色谱
公开(公告)号：US5091386A
公开(公告)日：1992-02-25
申请号：US411003
申请日：1989-09-22
申请人： Kurt Kesseler , Wilhelm Bartmann , Gunther Wess , Ernold Granzer
发明人： Kurt Kesseler , Wilhelm Bartmann , Gunther Wess , Ernold Granzer
IPC分类号： A61K31/215 , A61K31/34 , A61K31/35 , A61K31/351 , A61K31/365 , A61K31/366 , A61K31/38 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4418 , A61K31/443 , A61K31/496 , A61K31/50 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07C33/48 , C07C45/30 , C07C47/24 , C07C51/367 , C07C59/42 , C07C59/46 , C07C59/48 , C07C59/56 , C07C67/31 , C07C69/732 , C07C69/734 , C07D207/32 , C07D207/333 , C07D207/337 , C07D213/48 , C07D213/55 , C07D213/62 , C07D213/63 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D261/08 , C07D275/02 , C07D309/30 , C07D405/06
CPC分类号： C07D207/333 , C07C33/486 , C07C45/305 , C07C47/24 , C07C59/56 , C07D207/337 , C07D213/48 , C07D213/55 , C07D237/08 , C07D239/26 , C07D309/30 , C07D405/06
摘要： 7-Substituted 3,5-dihydroxyhept-6-ynoic acids and the derivatives thereof of the formula I ##STR1## as well as the corresponding lactones of the formula II ##STR2## in which R and R.degree. have the specified meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I or formula II are described.
摘要翻译： 7-取代的3,5-二羟基庚基-6-炔酸及其式I的衍生物，其中R和R DEG具有特定含义，式II的相应内酯，描述了这些化合物的制备方法，其作为药物和药物的用途被描述。此外，描述了用于制备式I或式II化合物的新中间体。

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