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1. 发明申请

WO2007137593A1 ESTERS OF (2-HYDROXY-3-OXO-CYCLOPENT-1-ENYL) ACETIC ACID AND THEIR USE FOR PREPARING (-)-R-HOMOCITRIC ACID GAMMA-LACTONE, (+)-S-HOMOCITRIC ACID GAMMA-LACTONE AND THE CORRESPONDING (-)-R-HOMOCITRIC ACID AND (+)-S-HOMOCITRIC ACID SALTS 审中-公开
标题翻译：（2-羟基-3-氧代环丙-1-烯）乙酸酯及其用于制备（ - ） - R-羟基丙酸酯，（+） - S-羟基丙酸酯和对应物的用途（ - ） - R-顺式酸和（+） - S-羟基酸
公开(公告)号：WO2007137593A1
公开(公告)日：2007-12-06
申请号：PCT/EE2007/000009
申请日：2007-05-25
申请人： TALLINN UNIVERSITY OF TECHNOLOGY , AS VÄHIUURINGUTE TEHNOLOOGIA ARENDUSKESKUS , AS PROSYNTEST , LOPP, Margus , PAJU, Anne , EEK, Margus , LAOS, Marit , PEHK, Tõnis , JÄÄLAID, Raissa
发明人： LOPP, Margus , PAJU, Anne , EEK, Margus , LAOS, Marit , PEHK, Tõnis , JÄÄLAID, Raissa
IPC分类号： C07C69/738 , C07D307/33
CPC分类号： C07C69/738 , C07C2601/10 , C07D307/33
摘要： Archiral (2-hydroxy-3-oxo-cyclopent-1-enyl) acetic acid) alkyl, alkylphenyl and phenyl esters, and a simple and efficient method for the synthesis of both enantiomers of homocitric acid gamma-lactone and the corresponding salts from these esters are described. The method is based on asymmetric oxidation of esters, and the steps of basic and acidic hydrolysis and final acidic lactonization of the homocitric acid into homocitric acid gamma-lactone. The homocitric acid salts are obtained after basic treatment of homocitric acid gamma-lactone. The esters, conditions and reagents used in chemical conversion and separating products are important constituents affording efficient and simple method for production of homocitric acid gamma-lactone and homocitric acid salts.
摘要翻译：丙酮（2-羟基-3-氧代 - 环戊-1-烯基）乙酸）烷基，烷基苯基和苯基酯，以及用于合成高柠檬酸γ-内酯和它们的相应盐的两种对映异构体的简单而有效的方法酯描述。该方法基于酯的不对称氧化，以及将高酸性碱性和酸性水解和最终酸性内酯化为高柠檬酸γ-内酯的步骤。在高碱性γ-内酯进行碱处理后得到高氯酸盐。化学转化和分离产物中使用的酯，条件和试剂是提供生产高立高酸γ-内酯和高磷酸盐的有效和简单方法的重要成分。

2. 发明申请

WO2016003919A8 ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE 审中-公开
公开(公告)号：WO2016003919A8
公开(公告)日：2016-01-07
申请号：PCT/US2015/038349
申请日：2015-06-29
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , SCHMIDT, Malle , PÄRI, Malle , LAOS, Marit , MAASALU, Ants , KALJUSTE, Kalle
发明人： SCHMIDT, Malle , PÄRI, Malle , LAOS, Marit , MAASALU, Ants , KALJUSTE, Kalle
IPC分类号： A61K31/451
摘要： This invention provides an isolated compound having the structure: The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1 -propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-l-propylpiperidine 1- oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.

3. 发明申请

WO2016003919A1 ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE 审中-公开
标题翻译：孕激素类似物，其制备和使用
公开(公告)号：WO2016003919A1
公开(公告)日：2016-01-07
申请号：PCT/US2015/038349
申请日：2015-06-29
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , SCHMIDT, Malle , PÄRI, Malle , LAOS, Marit , MAASALU, Ants , KALJUSTE, Kalle
发明人： SCHMIDT, Malle , PÄRI, Malle , LAOS, Marit , MAASALU, Ants , KALJUSTE, Kalle
IPC分类号： A61K31/451
CPC分类号： A61K31/451 , C07D211/24 , C07D211/42 , C07D211/52 , G01N30/88 , G01N2030/8872
摘要： This invention provides an isolated compound having the structure: The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1 -propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-l-propylpiperidine 1- oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.
摘要翻译：本发明提供具有以下结构的分离的化合物：本发明还提供了制备4-（3-（甲基磺酰基）苯基）-1-丙基哌啶-4-醇，1-（3,3-双（3-（甲基磺酰基）苯基）丙基）-4-（3-（甲基磺酰基）苯基）哌啶酮，1,4-双（（3-（1-丙基哌啶-4-基）苯基）磺酰基）丁烷，（3R，4S） - （3-（甲基磺酰基）苯基）-1-丙基哌啶-3-醇，4-（3-（甲基磺酰基）苯基）-1-丙基哌啶1-氧化物，1-（2-甲基戊基）-4-（3- 甲基磺酰基）苯基）哌啶，4-（3-（甲基亚磺酰基）苯基）-1-丙基-1,2,3,6-四氢吡啶和4-（3-（甲基磺酰基）苯基）-1-丙基-1,2 ，3,6四氢吡啶。本发明还提供了一种杂质或其盐作为用于检测药物组合物中微量杂质的参考标准，其包含派多啶或其药学上可接受的盐。本发明进一步提供了一种制备哌多啶药物产品的方法，包括获得一种派多凡定药物，并将该丙泊德吡啶药物与合适的赋形剂混合，从而产生格列方啶药物。本发明还提供了制备格列方啶药物的方法。本发明还提供了分布丙泊德苷药物的方法。

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