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1. 发明授权

US07084250B2 Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides 有权
标题翻译：制备乙酰基 - 脒基苯丙氨酰 - 环己基甘氨酰 - 吡啶并氨酰胺的方法
公开(公告)号：US07084250B2
公开(公告)日：2006-08-01
申请号：US10869076
申请日：2004-06-17
申请人： Gerhard Breipohl , Wolfgang Holla , Heiner Jendralla , Gerhard Beck
发明人： Gerhard Breipohl , Wolfgang Holla , Heiner Jendralla , Gerhard Beck
IPC分类号： C07K5/08
CPC分类号： C07K5/0821 , C07K5/06139
摘要： The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, in which the anions X are physiologically acceptable anions, and their analogs, which are effective inhibitors of the blood coagulation factor Xa and which can be used, for example, for preventing thromboses. The process according to the invention comprises the coupling of 2-[2-acetylamino-3-(4-amidinophenyl)propionylamino]-2-cyclohexylacetic acid, which is obtained from 2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid by asymmetric hydrogenation and conversion of the cyano group into the amidine, or a salt thereof, with a 3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof. The invention furthermore provides starting materials and intermediates for this process, processes for their preparation and acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-pyridinio)alaninamide as ditosylate salt.
摘要翻译：本发明涉及一种制备式I的乙酰基 - 脒基苯脒基 - 环己基甘氨酰 - 吡啶并吡喃酰胺的方法，其中阴离子X是生理上可接受的阴离子，以及它们的类似物，它们是凝血因子Xa的有效抑制剂，可用于例如用于预防血栓形成。根据本发明的方法包括2- [2-乙酰氨基-3-（4-脒基苯基）丙酰基氨基] -2-环己基乙酸的偶联，其由2- [2-乙酰氨基-3-（4-氰基苯基）丙烯酰氨基] -2-环己基乙酸，通过不对称氢化，并将氰基转化为脒或其盐与3-（2-氨基-2-氨基甲酰基乙基）-1-甲基吡啶鎓盐或其盐。本发明还提供了该方法的起始原料和中间体，其制备方法和乙酰基 - （S）-4-脒基苯基丙氨酰 - （S） - 环己基甘氨酰 - （S） - （1-甲基-3-吡啶鎓）丙烯酰胺作为二甲苯磺酸盐。

2. 发明授权

US5684185A Process for the stereoselective synthesis of 3-substituted 2-sulfonylmethylpropionic acids, and intermediate products 失效
标题翻译：用于立体选择性合成3-取代的2-磺酰基甲基丙酸和中间产物的方法
公开(公告)号：US5684185A
公开(公告)日：1997-11-04
申请号：US411832
申请日：1995-03-30
申请人： Gerhard Beck , Joachim-Heiner Jendralla , Bernhard Kammermeier
发明人： Gerhard Beck , Joachim-Heiner Jendralla , Bernhard Kammermeier
IPC分类号： C07B53/00 , C07C315/00 , C07C315/02 , C07C315/04 , C07C317/44 , C07C319/14 , C07C323/51 , C07C323/52 , C07C323/56
CPC分类号： C07C323/56 , C07C315/02 , C07C315/04 , C07C317/44 , C07C323/52
摘要： Compounds of the formula I ##STR1## can be prepared in a multi-day process starting from the compounds of the formulae II and III R.sup.1 --SH, II ##STR2## where the substituents R.sup.1, R.sup.2 and R.sup.3 have the meanings given.
摘要翻译： PCT No.PCT / EP93 / 02674 371日期1995年3月30日 102（e）1995年3月30日PCT PCT 1993年9月30日PCT公布。出版物WO94 / 07850 日期1994年4月14日，式Ⅰ的化合物I可以从式II和III化合物R1-SH，II，III，其中取代基R 1，R 2和R 3在多天的方法中制备具有给定的意义。

3. 发明授权

US5399722A Process for preparing tert-butyl (3R,5S)-6-hydroxy-3,5--O--isopropylidene-3,5-dihydroxyhexanoate 失效
标题翻译：（3R，5S）-6-羟基-3,5-O-异亚丙基-3,5-二羟基己酸叔丁酯的方法
公开(公告)号：US5399722A
公开(公告)日：1995-03-21
申请号：US83488
申请日：1993-06-30
申请人： Gerhard Beck , Joachim-Heiner Jendralla , Kurt Kesseler
发明人： Gerhard Beck , Joachim-Heiner Jendralla , Kurt Kesseler
IPC分类号： C07D319/06
CPC分类号： C07D319/06 , Y02P20/55
摘要： A novel process is described for preparing tert-butyl (3R, 5S ) 6-hydroxy-3,5-O-isopropylidene-3,5-dihydroxyhexanoate of the formula I ##STR1## which is a valuable structural element for preparing inhibitors of HMG-CoA reductase.
摘要翻译：描述了用于制备式I的（3R，5S）6-羟基-3,5-O-异亚丙基-3,5-二羟基己酸叔丁酯的新方法，其是用于制备式I的抑制剂的有价值的结构元件 HMG-CoA还原酶。

4. 发明授权

US5055484A 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
标题翻译： 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
申请人： Heiner Jendralla , Gerhard Beck , Ekkehard Baader , Bela Kerekjarto
发明人： Heiner Jendralla , Gerhard Beck , Ekkehard Baader , Bela Kerekjarto
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。

5. 发明授权

US5294724A 4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters and a process for their preparation 失效
标题翻译： 4-羟基四氢吡喃-2-酮和相应的二羟基羧酸衍生物，盐和酯及其制备方法
公开(公告)号：US5294724A
公开(公告)日：1994-03-15
申请号：US578240
申请日：1990-09-06
申请人： Heiner Jendralla , Gunther Wess , Kurt Kesseler , Gerhard Beck
发明人： Heiner Jendralla , Gunther Wess , Kurt Kesseler , Gerhard Beck
IPC分类号： C07D319/06 , A61K31/35 , A61K31/357 , A61K31/365 , A61K31/366 , A61P3/06 , A61P9/10 , A61P43/00 , C07C1/24 , C07C17/12 , C07C17/26 , C07C39/08 , C07C43/23 , C07C45/46 , C07C46/04 , C07C50/24 , C07C69/712 , C07C323/20 , C07C331/10 , C07D309/30 , C07C69/612 , C07C321/04 , C07C321/26
CPC分类号： C07C17/12 , C07C1/24 , C07C17/263 , C07C17/2632 , C07C323/20 , C07C331/10 , C07C45/46 , C07C46/04 , C07C50/24 , C07C69/712 , C07D309/30 , C07C2101/02
摘要： 4-Hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, process for their preparation, their use as pharmaceuticals, and pharmaceutical preparations and precursors.Compounds of the formula I ##STR1## and the corresponding open-chain dihydroxycarboxylic acids of the formula II ##STR2## in which X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings indicated, and also their pharmacologically tolerable salts with bases and their pharmacologically tolerable esters, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. In addition, compounds of the formula III ##STR3## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and Y have the meanings indicated are described.
摘要翻译： 4-羟基四氢吡喃-2-酮和相应的二羟基羧酸衍生物，盐和酯，其制备方法，它们作为药物的用途，以及药物制剂和前体。其中X，Y，R 1，R 2，R 3，R 4和R 5具有所示含义的式I化合物（*化学结构*）I和相应的式II（* CHEMICAL STRUCTURE *）II的开链二羟基羧酸，以及它们与碱的药理学上可耐受的盐及其药理学上可耐受的酯，这些化合物的制备方法，它们作为药物和药物制剂的用途。另外，描述了其中R 1，R 2，R 3，R 4，R 5，X和Y具有所述含义的式III化合物（*化学结构*）III。

6. 发明授权

US5166171A 6-phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiphenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, and in treating hypercholesterolemia 失效
标题翻译： 6-苯氧基甲基-4-羟基四氢吡喃-2-酮和6-硫代氧甲基-4-羟基四氢吡喃-2-酮及相应的二羟基羧酸衍生物，盐和酯，以及治疗高胆固醇血症
公开(公告)号：US5166171A
公开(公告)日：1992-11-24
申请号：US680613
申请日：1991-04-02
申请人： Heiner Jendralla , Gunther Wess , Wilhelm Bartmann , Gerhard Beck
发明人： Heiner Jendralla , Gunther Wess , Wilhelm Bartmann , Gerhard Beck
IPC分类号： C07C59/68 , C07C323/09 , C07D309/30
CPC分类号： C07C59/68 , C07C323/09 , C07D309/30 , Y10S514/824
摘要： 6-Phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiophenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, processes for the preparation of these compounds, their use as pharmaceuticals, pharmaceutical preparations and novel phenols and thiophenols Compounds of the general formula I ##STR1## and the corresponding open-chain dihydroxycarboxylic acids of the formula II ##STR2## in which X, Y and Z have the meanings given, and pharmacologically tolerated salts thereof with bases and pharmacologically tolerated esters thereof, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. Novel phenols and thiophenols of the formula III ##STR3## in which X, Y and Z have the meanings given, are also described.
摘要翻译： 6-苯氧基甲基-4-羟基四氢吡喃-2-酮和6-噻吩氧基甲基-4-羟基四氢吡喃-2-酮以及相应的二羟基羧酸衍生物，盐和酯，用于制备这些化合物的方法，它们作为药物，药物制剂和新型酚类和噻吩类化合物通式Ⅰ的化合物及其相应的式Ⅱ的开环二羟基羧酸，其中X，Y和Z具有给定的含义，其药理学上可容许的盐与碱和描述了其药理学耐受的酯，制备这些化合物的方法，它们作为药物和药物制剂的用途。还描述了其中X，Y和Z具有给定的含义的式III“III”的新型酚类和噻吩类。

7. 发明授权

US4946852A 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
标题翻译： 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。

8. 发明授权

US4946841A Pyridazine 3,5-dihydroxy carboxylic acids and derivatives thereof, the use thereof for hypercholesterolemia 失效
标题翻译：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
申请人： Ekkehard Baader , Heiner Jendralla , Bela Kerekjarto , Gerhard Beck
发明人： Ekkehard Baader , Heiner Jendralla , Bela Kerekjarto , Gerhard Beck
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。

9. 发明授权

US6018053A Process for the preparation of chiral, nonracemic (4-aryl-2,5-dioxoimidazolidin-1-yl) acetic acids 失效
标题翻译：手性，非糖化（4-芳基-2,5-二氧代咪唑烷-1-基）乙酸的制备方法
公开(公告)号：US6018053A
公开(公告)日：2000-01-25
申请号：US879289
申请日：1997-06-19
申请人： Wolfgang Holla , Gerhard Beck , Bernhard Kammermeier , Berndt Kulitzscher , Jurgen Michalowsky
发明人： Wolfgang Holla , Gerhard Beck , Bernhard Kammermeier , Berndt Kulitzscher , Jurgen Michalowsky
IPC分类号： A61K31/415 , A61K31/4166 , A61P7/02 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/78 , C07D233/80
CPC分类号： C07D233/76
摘要： The present invention relates to a process for the preparation of chiral, nonracemic compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings indicated in claim 1 and which are useful intermediates for the preparation of pharmaceutical active compounds in which, for resolution, a salt is formed from the racemic compound of the formula I and a chiral, nonracemic amino compound. It furthermore relates to compounds of the formula I and esters thereof.
摘要翻译：本发明涉及制备式I的手性，非微量化合物的方法，其中R 1和R 2具有权利要求1所示的含义，并且它们是制备药物活性化合物的有用的中间体，其中为了拆分，盐由式I的外消旋化合物和手性，非糖化的氨基化合物形成。此外，它还涉及式I的化合物及其酯。

10. 发明授权

US5861304A Process for the enzymatic separation of enantiomers of rac-2-oxotricyclo�2.2.1.0 3,5! heptane-7-carboxylic acid and of rac-2-oxotricyclo�2.2.1.0 3,5! heptane-7-carboxylic esters 失效
标题翻译：使用来自念珠菌的脂肪酶分离外消旋-2-氧杂环己烷-2,2.0.0,3H庚烷-7-羧酸酯的方法
公开(公告)号：US5861304A
公开(公告)日：1999-01-19
申请号：US932933
申请日：1997-09-17
申请人： Wolfgang Holla , Gerhard Beck
发明人： Wolfgang Holla , Gerhard Beck
IPC分类号： C07C69/757 , C12P15/00 , C12P41/00 , C12R1/07 , C12R1/38 , C12R1/66 , C12R1/72 , C12R1/785 , C12R1/845
CPC分类号： C12P41/005 , C12P15/00 , Y10S435/921
摘要： Process for the resolution of rac-2-oxotricyclo�2.2.1.0.sup.3,5 !heptane-7-carboxylic acid esters using lipase from candida.Compounds of the formula I ##STR1## in which R.sup.1 has the meanings mentioned, may be obtained in isomerically pure form from enantiomer mixtures or racemic mixtures by reacting the compound of the formula I in the presence of a lipase or esterase from porcine liver, porcine pancreas, bovine pancreas or from microorganisms such as Candida, Pseudomonas, Mucor, Rhizopus and Aspergillus, or proteases from Bacillus in the presence of water and, if desired, a cosolvent and separating from one another the esters and acids present in the solution obtained.
摘要翻译：使用来自念珠菌的脂肪酶拆分外消旋-2-氧代三环[2.2.1.03,5]庚烷-7-羧酸酯的方法。通过在来自猪的脂肪酶或酯酶的存在下使式I化合物与对映体混合物或外消旋混合物以异构体纯的形式获得其中R 1具有所述含义的式I的化合物（I）肝，猪胰腺，牛胰腺或来自诸如假丝酵母属，假单胞菌属，毛霉属，根霉属和曲霉属的微生物或来自芽孢杆菌的蛋白酶，并且如果需要，共溶剂并且彼此分离存在于溶液得到。

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