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1.发明授权4(R)-substituted 6(S)-phenoxymethyl-, 6(S)-.beta.-phenylethyl- and 6(S)-.beta.-styryl-tetrahydropyran-2-ones, a highly stereoselective process for their preparation, pharmaceutical products based on these compounds, and their use 失效4（S） - 苯氧基甲基 - ，6（S） - 苯乙基和6（S） - 苯乙烯基 - 四氢吡喃-2-酮，其立体选择性制备方法，基于药物的 对这些化合物及其用途
公开(公告)号：US4946852A
公开(公告)日：1990-08-07
申请号：US330979
申请日：1989-03-30
申请人： Heiner Jendralla , Gerhard Beck , Gunther Wess , Bela Kerekjarto
发明人： Heiner Jendralla , Gerhard Beck , Gunther Wess , Bela Kerekjarto
IPC分类号： A61K31/365 , A61K31/366 , A61P3/06 , C07D309/30 , C07D309/32
CPC分类号： C07D309/30 , C07D309/32 , Y10S514/824
摘要： 4(R)-Substituted 6(S)-phenyloxymethyl-, 6(S)-.beta.-phenylethyl- and 6(S)-.beta.-styryl-tetrahydropyran-2-ones of the general formula V ##STR1## in which R.sup.7, R.sup.8 and A have the meanings given, and the corresponding open-chain hydroxycarboxylic acids, pharmacologically acceptable salts and esters thereof, processes for the preparation of these compounds, their use as medicaments and pharmaceutical products are described. Novel .alpha.,.beta.-unsaturated lactones for the preparation of the compounds of the formula V are also described.
摘要翻译： 4（R） - 取代的6（S） - 苯氧基甲基 - ，6（S）-β-乙基 - 和6（S）-β-苯乙烯基 - 四氢吡喃-2-酮，其中R 7 R8和A具有所给出的含义，并且描述了相应的开链羟基羧酸，其药理学上可接受的盐和酯，这些化合物的制备方法，它们作为药物和药物的用途。 还描述了用于制备式V化合物的新型α，β-不饱和内酯。
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2.发明授权7(1H-pyrrol-3-YL)-substituted 3,5-dihydroxyhept-6-enoic acids, 7-(1H-pyrrol-3-YL)-substituted 3,5-dihyroxyhept-anoic acids, their corresponding delta-lactones and salts, their use as medicaments and pharmaceutical products and intermediates 失效7（1H-吡咯-3-基） - 取代的3,5-二羟基-6-丁酸，7-（1H-吡咯-3-基） - 取代的3,5-二羟基苯甲酸酐，其相应的三角酸酯 作为药物和药物产品及其中间体使用和销售
公开(公告)号：US5055484A
公开(公告)日：1991-10-08
申请号：US216423
申请日：1988-07-08
IPC分类号： A61K31/40 , A61K31/4025 , A61P3/06 , C07D207/32 , C07D207/337 , C07D207/34 , C07D405/06
CPC分类号： C07D207/337 , C07D405/06
摘要： 7-[1H-pyrrol-3-yl]-substituted 3,5-dihydroxyhept-6-enoic acids, 7-[1H-pyrrol-3-yl]-substituted 3,5-dihydroxyheptanoic acids of the formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the indicated meanings, and the corresponding .delta.-lactones of the formula II ##STR2## processes for the preparation of these compounds, their use as medicaments and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formulae I and II are described.
摘要翻译： 7- [1H-吡咯-3-基] - 取代的3,5-二羟基庚-6-烯酸，式I的7- [1H-吡咯-3-基] - 取代的3,5-二羟基庚酸
其中A，B，R 1，R 2，R 3，R 4和R 5具有指定的含义，并且相应的式II的β-内酯制备这些化合物的方法，它们用作药物和药物产品 被描述。 此外，描述了用于制备式I和II化合物的新中间体。 -
3.发明授权Pyridazine 3,5-dihydroxy carboxylic acids and derivatives thereof, the use thereof for hypercholesterolemia 失效哒嗪3,5-二羟基羧酸及其衍生物，其用于高胆固醇血症
公开(公告)号：US4946841A
公开(公告)日：1990-08-07
申请号：US294096
申请日：1989-01-06
IPC分类号： A61K20060101 , A61K31/50 , A61P3/06 , A61P9/10 , C07C43/23 , C07C45/30 , C07C45/63 , C07C49/04 , C07C49/16 , C07C49/223 , C07C49/567 , C07C49/76 , C07C49/782 , C07C49/80 , C07C49/813 , C07C49/84 , C07D20060101 , C07D237/08 , C07D237/24 , C07D405/06
CPC分类号： C07D405/06 , C07C43/23 , C07C45/305 , C07C45/63 , C07C49/04 , C07C49/16 , C07C49/223 , C07C49/567 , C07C49/76 , C07C49/782 , C07C49/80 , C07C49/813 , C07C49/84 , C07D237/08 , C07D237/24
摘要： New 3,5-dihydroxy carboxylic acids and derivatives thereof, a process for the preparation thereof, the use thereof as pharmaceuticals, pharmaceutical products and intermediates 3,5-Dihydroxy carboxylic acids and derivatives thereof, of the formula I ##STR1## and the corresponding Lactones of the formula II ##STR2## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X-Y have the indicated 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 formulae I and II are described.
摘要翻译： 新的3,5-二羟基羧酸及其衍生物及其衍生物，其制备方法，其作为药物，药物产品和中间体的用途，式I的化合物及其相应的式 其中R1，R2，R3，R4和XY具有指定含义的式II的内酯，制备这些化合物的方法，其作为药物的用途以及药物产品。 此外，描述了用于制备式I和II化合物的新中间体。
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4.发明授权3-Demethylmevalonic acid derivatives, a process for their preparation pharmaceutical products based on these compounds, their use and intermediates 失效3-甲基甲基戊酸衍生物，其制备方法基于这些化合物的药物产品，其用途和中间体
公开(公告)号：US4914127A
公开(公告)日：1990-04-03
申请号：US320924
申请日：1989-03-08
申请人： Gerhard Beck , Bela Kerekjarto , Hans-Hermann Lau , Gunther Wess
发明人： Gerhard Beck , Bela Kerekjarto , Hans-Hermann Lau , Gunther Wess
IPC分类号： C07D409/06 , A61K31/35 , A61K31/351 , A61K31/365 , A61K31/366 , A61K31/38 , A61K31/381 , A61P3/06 , A61P9/10 , C07C51/00 , C07C51/09 , C07C57/30 , C07C57/58 , C07C59/48 , C07C59/54 , C07C59/56 , C07C59/64 , C07C59/72 , C07C67/00 , C07C67/08 , C07C69/66 , C07C69/732 , C07C69/734 , C07D309/10 , C07D309/30 , C07D333/00 , C07D333/16 , C07D333/24 , C07D409/10 , C07F7/18 , C07F9/54
CPC分类号： C07F7/1856 , C07D309/10 , C07D309/30 , C07D409/10 , C07F9/5456 , Y02P20/55
摘要： 3-Demethylmevalonic acid derivatives of the formula I (.delta.-lactone) and Ia (corresponding dihydroxycarboxylic acid derivative) ##STR1## in which A-B, Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the indicated meanings, a process for the preparation of these compounds, their use as medicaments and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I and Ia are described.
摘要翻译： 其中AB，Z，R1，R2，R3和R4具有指定含义的式I的三甲基甲基戊酸衍生物（δ-内酯）和Ia（相应的二羟基羧酸衍生物）IMAGE，其制备方法 描述了它们作为药物和药物用途的用途。 此外，描述了用于制备式I和Ia化合物的新中间体。
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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.
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公开(公告)号：US5143937A
公开(公告)日：1992-09-01
申请号：US480932
申请日：1990-02-16
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。
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7.发明授权
公开(公告)号：US4849444A
公开(公告)日：1989-07-18
申请号：US184963
申请日：1988-04-22
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.
摘要翻译： 式I的化合物，其中R1等于H或（环）烷（en）基，R2等于H或烷基，R3等于烷基，R4 / R5等于H，烷基或酰基，Y相等 至H，烷基，CF 3或Hal，以及其制备方法。 它们是有效的利尿剂和具有降脂作用的抗高血压药物。
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