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61. 发明授权

US5849749A 6-(hydroxymethyl-ethyl)pyridines 失效
标题翻译： 6-（羟甲基 - 乙基）吡啶
公开(公告)号：US5849749A
公开(公告)日：1998-12-15
申请号：US883695
申请日：1997-06-27
申请人： Peter Fey , Rolf Angerbauer , Delf Schmidt , Hilmar Bischoff , Wolfgang Kanhai , Martin Radtke , Wolfgang Karl
发明人： Peter Fey , Rolf Angerbauer , Delf Schmidt , Hilmar Bischoff , Wolfgang Kanhai , Martin Radtke , Wolfgang Karl
IPC分类号： C07D213/30 , A61K31/44 , A61K31/4418 , A61P3/06 , A61P9/10 , C07D213/55 , C07F7/02
CPC分类号： C07D213/55 , Y02P20/55
摘要： The 6-(hydroxymethyl-ethyl)pyridines are prepared by a process in which the 3-hydroxymethylpyridines which are hydroxyl-protected in the 6-position are oxidized to the 3-aldehyde, this is then converted into the corresponding oxoheptenoic acid derivative using a Wittig-Homer reaction, after this the oxo group is reduced to the hydroxyl group and then the isomers are separated by chromatography. The 6-(hydroxymethyl-ethyl)pyridines are suitable as active compounds in medicaments, in particular in medicaments having antiarteriosclerotic activity.
摘要翻译： 6-（羟甲基 - 乙基）吡啶通过其中6-位被羟基保护的3-羟甲基吡啶氧化为3-醛的方法制备，然后将其转化为相应的氧代庚烯酸衍生物，使用维ig - 荷马克反应后，将氧代基还原成羟基，然后通过色谱分离异构体。 6-（羟甲基 - 乙基）吡啶适合作为药物中的活性化合物，特别是具有抗动脉硬化活性的药物。

62. 发明申请

US20140155637A1 CHIRAL SYNTHESIS OF N--1-[2,3-DIHYDROXY-PROPYL]CYCLOPROPANESULFONAMIDES 有权
标题翻译： N-1- [2,3-二羟基丙基]环丙烷磺酰胺的CHIRAL SYNTHESIS
公开(公告)号：US20140155637A1
公开(公告)日：2014-06-05
申请号：US14122568
申请日：2012-05-24
申请人： Peter Fey , Agathe Christine Mayer
发明人： Peter Fey , Agathe Christine Mayer
IPC分类号： C07C303/38 , C07C309/71 , C07D317/24 , C07F7/18 , C07D309/12 , C07D317/18 , C07D303/34
CPC分类号： C07C303/38 , C07B2200/07 , C07C303/40 , C07C309/71 , C07C2601/02 , C07D303/34 , C07D309/12 , C07D317/18 , C07D317/24 , C07F7/1804 , C07C311/28
摘要： The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide.
摘要翻译：本发明涉及制备N- {3,4-二氟-2 - [（2-氟-4-碘苯基）氨基] -6-5甲氧基苯基的（S） - 和（R） - 对映异构体的新型对映选择性方法对于新型中间体化合物，以及所述新型中间体化合物用于制备所述（S） - 和（R） - 对映异构体的用途，所述N-（3） - （2,3-二羟基 - 丙基）环丙烷磺酰胺， 4-二氟-2 - [（2-氟-4-碘苯基）氨基] -6-甲氧基苯基} -1- [2,3-二羟基 - 丙基]环丙烷磺酰胺。

63. 发明授权

US06566523B1 Method for the enantiomer separation of cis-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane 有权
标题翻译：顺式-8-苄基-7,9-二氧代-2,8-二氮杂双环[4.3.0]壬烷的对映异构体分离方法
公开(公告)号：US06566523B1
公开(公告)日：2003-05-20
申请号：US10018110
申请日：2001-12-14
申请人： Peter Fey
发明人： Peter Fey
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07H9/04
摘要： The invention relates to a method for the enantiomer separation of cis-8-benzyl-7,9-dioxo-2,8-diazabicy-clo[4.3.0]nonane (also described below as cis-6-benzyl-5,7-dioxooctahydropyrrolo[3,4-b]pyridine or dioxopyrrolopiperidine). The invention also relates to a method for producing (1S, 6R)- and (1R, 6S)-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane using the above method. The invention further relates to the (−)-2,3:4,6-di-O-isopropylidene-2-keto-L-gulonic acid salts of (1S, 6R)- and (1R, 6S)-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane and to a method for producing the same. Finally, the invention relate to a method for the enantiomer enrichment of (1S, 6R)-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]-nonane.
摘要翻译：本发明涉及顺式-8-苄基-7,9-二氧代-2,8-二氮杂双环[4.3.0]壬烷对映异构体分离方法（下文也描述为顺式-6-苄基-5,7 - 二氧代八氢吡咯并[3,4-b]吡啶或二氧代吡咯并哌啶）。本发明还涉及使用上述方法制备（1S，6R） - 和（1R，6S）-8-苄基-7,9-二氧代-2,8-二氮杂双环[4.3.0]壬烷的方法。本发明进一步涉及（1S，6R） - 和（1R，6S）-8-苄基（ - ） - （ - ） - （2,3,4,6-二-O-异亚丙基-2-酮-L-古洛糖酸盐 -7,9-二氧代-2,8-二氮杂双环[4.3.0]壬烷及其制备方法。最后，本发明涉及（1S，6R）-8-苄基-7,9-二氧代-2,8-二氮杂双环[4.3.0] - 壬烷对映异构体富集的方法。

64. 发明授权

US5952498A Process for the preparation of enantiomerically pure cycloalkano-indol -and azaindol -and pyrimido �1,2a! indolcarboxcyclic acids and their activated derivatives 失效
标题翻译：制备对映异构纯的环烷基 - 吲哚 - 和氮杂吲哚和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法
公开(公告)号：US5952498A
公开(公告)日：1999-09-14
申请号：US829566
申请日：1997-03-31
申请人： Jan-Bernd Lenfers , Peter Fey , Paul Naab , Kai Van Laak
发明人： Jan-Bernd Lenfers , Peter Fey , Paul Naab , Kai Van Laak
IPC分类号： C07C69/612 , C07C69/616 , C07C69/65 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07C69/612 , C07C69/616 , C07C69/65 , C07D487/04
摘要： The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido�1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido�1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.
摘要翻译：本发明涉及制备对映体纯的环烷基吲哚羧酸和氮杂吲哚羧酸和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法和中间体，其特征在于首先用手性醇酯化甲苯基乙酸，然后进行非对映选择性在α-碳原子上进行取代，将该产物在甲苯基中卤化，然后与合适的环亚烷基吲哚，环烷基烷基偶氮或嘧啶并[1,2a]吲哚反应。通过该方法可以高纯度地制备作为有价值药物的中间体的对映体纯的羧酸。

65. 发明授权

US5849924A Highly selective process for the preparation of enantiomerically pure phenyl-substituted 1,4-dihydropyridine-3,5-dicarboxylic acid derivatives 失效
标题翻译：用于制备对映体纯的苯基取代的1,4-二氢吡啶-3,5-二羧酸衍生物的高选择性方法
公开(公告)号：US5849924A
公开(公告)日：1998-12-15
申请号：US896275
申请日：1997-07-16
申请人： Joachim Mittendorf , Peter Fey , Bodo Junge , Johannes Kaulen , Kai van Laak , Heinrich Meier , Rudolf Schohe-Loop
发明人： Joachim Mittendorf , Peter Fey , Bodo Junge , Johannes Kaulen , Kai van Laak , Heinrich Meier , Rudolf Schohe-Loop
IPC分类号： A61K31/4412 , A61P25/28 , C07D207/40 , C07D207/416 , C07D211/80 , C07D211/90 , C07D401/02 , C07D401/06 , C07D401/12 , C07D521/00
CPC分类号： C07D207/416 , C07D211/90 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12
摘要： The present invention relates to a new highly selective process for the preparation of enantiomerically pure halogeno-phenyl-substituted 1,4-dihydropyridine-3,5-dicarboxylic esters of the general formula (I) ##STR1## in which R.sup.1 to R.sup.3 have the meanings given in the description.
摘要翻译：本发明涉及用于制备通式（I）的对映体纯的卤代苯基取代的1,4-二氢吡啶-3,5-二羧酸酯的新的高选择性方法，其中R1至 R3具有说明书中给出的含义。

66. 发明授权

US09328066B2 Chiral synthesis of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides 有权
标题翻译：手性合成N- {3,4-二氟-2 - [（2-氟-4-碘苯基）氨基] -6-甲氧基苯基} -1- [2,3-二羟基 - 丙基]环丙烷磺酰胺
公开(公告)号：US09328066B2
公开(公告)日：2016-05-03
申请号：US14122568
申请日：2012-05-24
申请人： Peter Fey , Agathe Christine Mayer
发明人： Peter Fey , Agathe Christine Mayer
IPC分类号： C07C211/43 , C07D317/10 , C07C303/38 , C07C303/40 , C07C309/71 , C07D309/12 , C07D317/18 , C07F7/18 , C07D303/34 , C07D317/24
CPC分类号： C07C303/38 , C07B2200/07 , C07C303/40 , C07C309/71 , C07C2601/02 , C07D303/34 , C07D309/12 , C07D317/18 , C07D317/24 , C07F7/1804 , C07C311/28
摘要： The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide.
摘要翻译：本发明涉及制备N- {3,4-二氟-2 - [（2-氟-4-碘苯基）氨基] -6-5甲氧基苯基的（S） - 和（R） - 对映异构体的新型对映选择性方法对于新型中间体化合物，以及所述新型中间体化合物用于制备所述（S） - 和（R） - 对映异构体的用途，所述N-（3） - （2,3-二羟基 - 丙基）环丙烷磺酰胺， 4-二氟-2 - [（2-氟-4-碘苯基）氨基] -6-甲氧基苯基} -1- [2,3-二羟基 - 丙基]环丙烷磺酰胺。

67. 发明授权

US06774236B1 Process for the preparation of enantiomerically pure cycloalkano-indol -and azaindol -and pyrimido [1,2A]indolcarbocyclic acids and their activated derivatives 失效
标题翻译：制备对映异构体纯的环烷基 - 吲哚 - 和氮杂吲哚和嘧啶并[1,2A]吲哚羧酸及其活化衍生物的方法
公开(公告)号：US06774236B1
公开(公告)日：2004-08-10
申请号：US09307980
申请日：1999-05-10
申请人： Jan-Bernd Lenfers , Peter Fey , Paul Naab , Kai Van Laak
发明人： Jan-Bernd Lenfers , Peter Fey , Paul Naab , Kai Van Laak
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07C69/612 , C07C69/616 , C07C69/65 , C07D487/04
摘要： The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido[1,2a]indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at &agr;-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido[1,2a]indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.
摘要翻译：本发明涉及制备对映体纯的环烷基吲哚羧酸和氮杂吲哚羧酸和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法和中间体，其特征在于首先用手性醇酯化甲苯基乙酸，然后进行非对映选择性在α-碳原子上进行取代，并将该产物在甲苯基中卤化，然后与适当的环亚烷基吲哚，环烷基烷基偶氮或嘧啶并[1,2a]吲哚反应。通过该方法可以高纯度地制备作为有价值药物的中间体的对映体纯的羧酸。

68. 再颁专利

USRE36607E Pyrrolidine compounds and process of preparing 有权
标题翻译：吡咯烷化合物及其制备方法
公开(公告)号：USRE36607E
公开(公告)日：2000-03-07
申请号：US276220
申请日：1999-03-25
申请人： Joachim Mittendorf , Peter Fey , Bodo Junge , Johannes Kaulen , Kai van Laak , Heinrich Meier , Rudolf Schohe-Loop
发明人： Joachim Mittendorf , Peter Fey , Bodo Junge , Johannes Kaulen , Kai van Laak , Heinrich Meier , Rudolf Schohe-Loop
IPC分类号： A61K31/4412 , A61P25/28 , C07D207/40 , C07D207/416 , C07D211/80 , C07D211/90 , C07D401/02 , C07D401/06 , C07D401/12 , C07D521/00
CPC分类号： C07D207/416 , C07D211/90 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12
摘要： This invention relates to benzolididene compounds of the formula ##STR1## in which R.sup.2 represents the radical ##STR2## in which R.sup.4 and R.sup.5 are identical or different and denote halogen, cyano, ethinyl, trifluoromethoxy, methylthio, nitro, trifluoromethyl or straight-chain or branched alkyl, alkenyl, alkinyl or alkoxy having up to 4 carbon atoms, and one of the substituents optionally represents hydrogen,or a salt thereof.[...]..Iadd., andA represents hydrogen or straight-chain or branched alkyl having up to 8 carbon atoms, or represents phenyl or benzyl which are optionally substituted one to three times by identical or different substituents from the series consisting of hydroxyl, nitro, halogen, cyano, carboxyl, trifluoromethyl, trifluoromethoxy, straight-chain or branched alkoxy having up to 6 carbon atoms or by a group of the formula --NR.sup.6 R.sup.7 or --SO.sub.2 R.sup.8, in whichR.sup.6 and R.sup.7 are identical or different and denote hydrogen, phenyl or straight-chain or branched alkyl having up to 5 carbon atomsandR.sup.8 denotes straight-chain or branched alkyl having up to 4 carbon atoms or phenyl. .Iaddend.
摘要翻译：本发明涉及下式的苯偶姻化合物，其中R 2表示其中R 4和R 5相同或不同并且表示卤素，氰基，乙炔基，三氟甲氧基，甲硫基，硝基，三氟甲基或直链或支链烷基，烯基，炔基或具有至多4个碳原子的烷氧基，其中一个取代基任选代表氢或其盐[和]，A表示氢或具有至多8个碳原子的直链或支链烷基，或表示苯基或苄基，任选地被羟基，硝基，卤素，氰基，羧基，三氟甲基，三氟甲氧基，具有至多6个碳原子的直链或支链烷氧基或通过下式的基团取代的相同或不同的取代基取代一至三次： -NR6R7或-SO2R8，其中R6和R7相同或不同，表示氢，苯基或具有至多5个碳原子的直链或支链烷基，R8表示直链具有至多4个碳原子的直链或支链烷基或苯基。

69. 发明授权

US5700948A Pyrrolidine compounds and process of preparing 失效
标题翻译：吡咯烷化合物及其制备方法
公开(公告)号：US5700948A
公开(公告)日：1997-12-23
申请号：US563725
申请日：1995-11-28
申请人： Joachim Mittendorf , Peter Fey , Bodo Junge , Johannes Kaulen , Kai van Laak , Heinrich Meier , Rudolf Schohe-Loop
发明人： Joachim Mittendorf , Peter Fey , Bodo Junge , Johannes Kaulen , Kai van Laak , Heinrich Meier , Rudolf Schohe-Loop
IPC分类号： A61K31/4412 , A61P25/28 , C07D207/40 , C07D207/416 , C07D211/80 , C07D211/90 , C07D401/02 , C07D401/06 , C07D401/12 , C07D521/00
CPC分类号： C07D207/416 , C07D211/90 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12
摘要： This invention relates to benzolididene compounds of the formula ##STR1## in which R.sup.2 represents the radical ##STR2## in which R.sup.4 and R.sup.5 are identical or different and denote halogen, cyano, ethinyl, trifluoromethoxy, methylthio, nitro, trifluoromethyl or straight-chain or branched alkyl, alkenyl, alkinyl or alkoxy having up to 4 carbon atoms, and one of the substituents optionally represents hydrogen, or a salt thereof.
摘要翻译：本发明涉及式（II）的苯偶姻化合物，其中R 2表示其中R 4和R 5相同或不同并表示卤素，氰基，乙炔基，三氟甲氧基，甲硫基，硝基，三氟甲基或直链的基团具有至多4个碳原子的链或支链烷基，烯基，炔基或烷氧基，其中一个取代基任选代表氢或其盐。

70. 发明授权

US06987185B2 Method for separating methyl 4-(2-chloro-4-fluorophenyl)-2-(3,5-difluoro-2-pyridinyl)-6-methyl-1,4-dihydro-5-pyrimidine-carboxylate-recemate 有权
标题翻译：分离甲基4-（2-氯-4-氟苯基）-2-（3,5-二氟-2-吡啶基）-6-甲基-1,4-二氢-5-嘧啶羧酸甲酯的方法
公开(公告)号：US06987185B2
公开(公告)日：2006-01-17
申请号：US10478602
申请日：2002-05-15
申请人： Siegfried Goldmann , Peter Fey
发明人： Siegfried Goldmann , Peter Fey
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07B2200/07
摘要： The enantiomers of methyl 4-(2-chloro-4-fluorophenyl)-2-(3,5-difluoro-2-pyridinyl)-6-methyl)-1,4-dihydro-5-pyrimidinecarboxylate can be separated with the aid of (−)-camphanic acid.
摘要翻译： 4-（2-氯-4-氟苯基）-2-（3,5-二氟-2-吡啶基）-6-甲基）-1,4-二氢-5-嘧啶甲酸甲酯的对映异构体可以借助于（ - ） - 樟脑酸。

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