公开(公告)号：US10130621B2

公开(公告)日：2018-11-20

申请号：US14754339

申请日：2015-06-29

申请人： Malle Schmidt ,  Malle Päri ,  Marit Laos ,  Ants Maasalu ,  Kalle Kaljuste

发明人： Malle Schmidt ,  Malle Päri ,  Marit Laos ,  Ants Maasalu ,  Kalle Kaljuste

IPC分类号： A61K31/451 ,  C07D211/52 ,  C07D211/24 ,  C07D211/42 ,  G01N30/88

摘要： This invention provides an isolated compound having the structure: or a salt thereof. 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)-1-propylpiperidine 1-oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridne, 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.

公开(公告)号：US20190030016A1

公开(公告)日：2019-01-31

申请号：US16150977

申请日：2018-10-03

申请人： Malle Schmidt ,  Malle Päri ,  Marit Laos ,  Ants Maasalu ,  Kalle Kaljuste

发明人： Malle Schmidt ,  Malle Päri ,  Marit Laos ,  Ants Maasalu ,  Kalle Kaljuste

IPC分类号： A61K31/451 ,  G01N30/88 ,  C07D211/52 ,  C07D211/42 ,  C07D211/24

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: or a salt thereof.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)-1-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.

公开(公告)号：US20150374677A1

公开(公告)日：2015-12-31

申请号：US14754339

申请日：2015-06-29

申请人： Malle Schmidt ,  Malle Päri ,  Marit Laos ,  Ants Maasalu ,  Kalle Kaljuste

发明人： Malle Schmidt ,  Malle Päri ,  Marit Laos ,  Ants Maasalu ,  Kalle Kaljuste

IPC分类号： A61K31/451 ,  G01N30/74 ,  C07D211/42 ,  C07D211/52 ,  C07D211/24

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: or a salt thereof.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)-1-propylpiperidine 1-oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridne, 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：或其盐。 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）-4-（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物的方法，包括获得一种丙泊德哌啶药物，并将该丙泊德吡啶药物与合适的赋形剂混合，以产生格列方啶药物产品。 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。