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11. 发明申请

US20070112217A1 Methods for isolating propargylated aminoindans 失效
标题翻译：分离炔丙基化氨基酸的方法
公开(公告)号：US20070112217A1
公开(公告)日：2007-05-17
申请号：US11600561
申请日：2006-11-15
申请人： Anton Frenkel , Ramy Lidor-Hadas , Eduard Gurevich , Gsan Attili
发明人： Anton Frenkel , Ramy Lidor-Hadas , Eduard Gurevich , Gsan Attili
IPC分类号： C07C209/84
CPC分类号： C07C209/86 , C07C209/84 , C07C2602/08 , C07C211/42
摘要： Disclosed is a process for isolating from a reaction mixture a salt of a mono-propargylated aminoindan having the structure wherein R1 is H, hydroxyl, alkoxy or wherein Y is O or S; R2 and R3 is each, independently, C1-8 alkyl, C6-12 aryl, C6-12 aralkyl, each optionally halo substituted, or hydrogen; where the reaction mixture further comprises a solvent, a primary aminoindan having the structure wherein R1 is defined as above, and a tertiary aminoindan having the structure the process comprising d) adding an acid to the reaction mixture; e) crystallizing the mono-propargylated aminoindan under conditions suitable for the formation of a crystalline salt of the mono-propargylated aminoindan; and f) recovering the crystalline salt of the mono-propargylated aminoindan, wherein the process is performed without addition of an organic solvent. Also disclosed are the crystalline diastereomeric salts produced by the process and pharmaceutical compositions containing the salts.
摘要翻译：公开了一种从反应混合物中分离具有其中R 1为H，羟基，烷氧基或其中Y为O或S的结构的单炔丙基化氨基茚满的盐的方法; R 2和R 3各自独立地为C 1-8烷基，C 6-12芳基， C 6-12芳烷基，各自任选被卤素取代，或氢; 其中反应混合物还包含溶剂，具有如上定义的R 1'的结构的伯氨基茚满和具有以下方法的结构的叔氨基茚满：d）向反应混合物中加入酸; e）在适合形成单炔丙基化氨基茚满的结晶盐的条件下，使单炔丙基化氨基茚满结晶; 和f）回收单炔丙基化氨基茚满的结晶盐，其中在不加入有机溶剂的情况下进行该方法。还公开了通过该方法产生的结晶非对映体盐和含有该盐的药物组合物。

12. 发明授权

US09233927B2 Crystals of laquinimod sodium and improved process for the manufacture thereof 有权
标题翻译：拉喹莫德钠晶体及其制备方法
公开(公告)号：US09233927B2
公开(公告)日：2016-01-12
申请号：US14214191
申请日：2014-03-14
申请人： Anton Frenkel , Avital Laxer
发明人： Anton Frenkel , Avital Laxer
IPC分类号： C07D215/56
CPC分类号： C07D215/56 , A61K31/47 , C07B2200/13 , G01N30/06 , G01N33/15
摘要： The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroqunoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; or f) an amount of methyl 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate (MCQME) in the mixture is no more than 0.12% relative to the amount of laquinimod sodium as measured by HPLC.
摘要翻译：本发明提供结晶laquinimod钠颗粒的混合物，其中（i）拉喹莫德钠颗粒的总体积的90％或更多具有40微米或更小的尺寸或（ii）总量的50％或更多拉喹莫德钠颗粒的体积量具有15微米或更小的尺寸，并且其中：a）混合物的堆积密度为0.2g / mL至0.4g / mL; b）混合物的密度为0.40g / mL至0.7g / mL; c）混合物中重金属的量相对于拉喹莫德钠的重量计不超过0.002％重金属; d）混合物中5-氯-4-羟基-1-甲基-2-氧代-1,2-二氢喹啉（MCQ）的量相对于通过HPLC测定的拉喹莫德钠的量不超过0.15％; e）混合物中5-氯-4-羟基-1-甲基-2-氧代-1,2-二氢喹啉-3-羧酸（MCQCA）的量相对于拉喹莫德钠的量不超过0.15％通过HPLC测量; 或f）混合物中5-氯-4-羟基-1-甲基-2-氧代-1,2-二氢喹啉-3-羧酸甲酯（MCQME）的量相对于拉喹莫德的量不超过0.12％通过HPLC测量的钠。

13. 发明申请

US20140128430A1 AMINE SALTS OF LAQUINIMOD 有权
标题翻译： LAQUINIMOD的胺盐
公开(公告)号：US20140128430A1
公开(公告)日：2014-05-08
申请号：US14068599
申请日：2013-10-31
申请人： Anton Frenkel , Avital Laxer , Judith Aronheim
发明人： Anton Frenkel , Avital Laxer , Judith Aronheim
IPC分类号： C07D215/56 , C07C229/26 , C07C215/08 , C07C215/10
CPC分类号： C07D215/56 , C07C215/08 , C07C215/10 , C07C215/40 , C07C229/26
摘要： The subject invention provides a Laquinimod amine salt, which is laquinimod meglumine, laquinimod choline hydroxide, laquinimod L-lysine or laquinimod monoethanolamine.
摘要翻译：本发明提供了拉喹莫德胺盐，其为拉喹莫德葡甲胺，拉喹莫德胆碱氢氧化物，拉喹莫德L-赖氨酸或拉喹莫德单乙醇胺。

14. 发明授权

US08614252B2 Crystalline solid rasagiline base 失效
标题翻译：结晶固体雷沙吉兰碱
公开(公告)号：US08614252B2
公开(公告)日：2013-12-24
申请号：US12655827
申请日：2010-01-08
申请人： Anton Frenkel , Tamas Koltai
发明人： Anton Frenkel , Tamas Koltai
IPC分类号： A01N33/02 , A61K31/135 , C07C211/00
CPC分类号： C07C209/82 , C07B2200/13 , C07C211/42 , C07C2602/08
摘要： The subject invention provides crystalline R(+)-N-propargyl-1-aminoindan, pharmaceutical compositions and methods of manufacture thereof.
摘要翻译：本发明提供结晶R（+） - N-炔丙基-1-氨基茚满，其药物组合物及其制备方法。

15. 发明授权

US08334409B2 Process for purifying rasagiline base 失效
标题翻译：雷沙吉兰碱的纯化方法
公开(公告)号：US08334409B2
公开(公告)日：2012-12-18
申请号：US12456642
申请日：2009-06-19
申请人： Anton Frenkel
发明人： Anton Frenkel
IPC分类号： C07C211/00
CPC分类号： C07C209/84 , C07C2602/08 , C07C211/42
摘要： Disclosed is crystalline R(+)-N-propargyl-1-aminoindan and racemic N-propargyl-1-aminoindan characterized by colorless crystals a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is pure liquid R(+)-N-propargyl-1-aminoindan and a pharmaceutical composition comprising the same, and the process for the manufacture thereof.
摘要翻译：公开了结晶的R（+） - N-炔丙基-1-氨基茚满和外消旋的N-炔丙基-1-氨基茚满，其特征在于无色晶体，其包含其的药物组合物及其制备方法和验证方法。还公开了纯液体R（+） - N-炔丙基-1-氨基茚满和包含其的药物组合物及其制备方法。

16. 发明申请

US20120101168A1 DEUTERIUM ENRICHED RASAGILINE 审中-公开
标题翻译：卓越的RASAGILINE
公开(公告)号：US20120101168A1
公开(公告)日：2012-04-26
申请号：US13281054
申请日：2011-10-25
申请人： Eliezer Bahar , Anton Frenkel , Victor Piryatinsky
发明人： Eliezer Bahar , Anton Frenkel , Victor Piryatinsky
IPC分类号： A61K31/135 , C07C309/04 , C07C209/14 , A61P25/28 , A61P25/16 , C07C211/42 , C07C309/29
CPC分类号： C07C211/42 , A61K31/135 , C07B59/001 , C07B2200/05 , C07C209/68 , C07C2602/08 , A61K2300/00
摘要： The subject invention provides deuterated rasagiline, its salts and uses.
摘要翻译：本发明提供氘代雷沙吉兰及其盐和用途。

17. 发明申请

US20120100189A1 DELAYED RELEASE RASAGILINE MALATE FORMULATION 审中-公开
标题翻译：延迟释放RASAGILINE MALATE配方
公开(公告)号：US20120100189A1
公开(公告)日：2012-04-26
申请号：US13336609
申请日：2011-12-23
申请人： Muhammad Safadi , Daniella Licht , Rachel Cohen , Anton Frenkel , Marina Zholkovsky
发明人： Muhammad Safadi , Daniella Licht , Rachel Cohen , Anton Frenkel , Marina Zholkovsky
IPC分类号： A61K9/00 , A61P25/16 , A61K31/135
CPC分类号： A61K9/2893 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/2846 , A61K9/2886 , A61K31/135 , C07C59/265 , C07C211/42 , C07C2602/08
摘要： Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.
摘要翻译：公开了旨在延迟雷沙吉兰释放同时保持特定药代动力学性质的制剂。

18. 发明申请

US20110152381A1 3-KETO-N-PROPARGYL-1-AMINOINDAN 审中-公开
公开(公告)号：US20110152381A1
公开(公告)日：2011-06-23
申请号：US12974769
申请日：2010-12-21
申请人： Anton Frenkel , Ramy Lidor-Hadas , Eliezer Bahar
发明人： Anton Frenkel , Ramy Lidor-Hadas , Eliezer Bahar
IPC分类号： A61K31/135 , C07C225/20 , C07C221/00 , A61P25/16 , A61P25/00
CPC分类号： A61K31/135 , C07C221/00 , C07C225/20 , C07C2602/08
摘要： The subject invention provides a pharmaceutical composition containing N-propargyl-1(R)-aminoindan or a pharmaceutically acceptable salt thereof, and a compound of 3-keto-N-propargyl-1-aminoindan or a salt thereof.
摘要翻译：本发明提供含有N-炔丙基-1（R） - 氨基茚满或其药学上可接受的盐和3-酮-N-炔丙基-1-氨基茚满的化合物或其盐的药物组合物。

19. 发明授权

US06696600B2 L-DOPA ethyl ester salts and uses thereof 失效
标题翻译： L-DOPA乙酯盐及其用途
公开(公告)号：US06696600B2
公开(公告)日：2004-02-24
申请号：US10292028
申请日：2002-11-12
申请人： Anton Frenkel , Ramy Lidor-Hadas
发明人： Anton Frenkel , Ramy Lidor-Hadas
IPC分类号： C07C22900
CPC分类号： A61K31/216 , C07C229/36
摘要： The present invention provides non-hygroscopic, crystalline salts of levodopa ethyl ester (LDEE), wherein the salt is the octanoate salt, the myristate salt, the succinate salt, the succinate dihydrate salt, the fumarate salt or the fumarate dihydrate salt of levodopa ethyl ester. The subject invention also encompasses compositions comprising a levodopa ethyl ester salt and a carrier and processes for making these compositions. In addition, the subject invention concerns pharmaceutical compositions comprising a levodopa ethyl ester salt and a pharmaceutically acceptable carrier, as well as processes for making these pharmaceutical compositions. Furthermore, the subject invention includes methods of treating a subject afflicted with Parkinson's disease, senile dementia, dementia of the Alzheimer's type, a memory disorder, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, brain ischemia, a head trauma injury, a spinal trauma injury, schizophrenia, an attention deficit disorder, multiple sclerosis and seizures by the administration of levodopa ethyl ester salts.
摘要翻译：本发明提供了左旋多巴乙酯（LDEE）的非吸湿结晶盐，其中盐是辛酸盐，肉豆蔻酸盐，琥珀酸盐，琥珀酸盐二水合物盐，左旋多巴乙基的富马酸盐或富马酸盐二水合盐酯。本发明还包括含有左旋多巴乙酯盐和载体的组合物和制备这些组合物的方法。此外，本发明涉及包含左旋多巴乙酯盐和药学上可接受的载体的药物组合物以及制备这些药物组合物的方法。此外，本发明包括治疗患有帕金森病，老年痴呆，阿尔茨海默氏型痴呆，记忆障碍，抑郁症，多动症综合征，情感性疾病，神经变性疾病，神经毒性损伤，脑缺血，脑损伤，脊髓损伤，精神分裂症，注意力缺陷障碍，多发性硬化和通过施用左旋多巴乙酯盐的癫痫发作。

20. 发明申请

US20170327464A1 CRYSTALS OF LAQUINIMOD SODIUM AND IMPROVED PROCESS FOR THE MANUFACTURE THEREOF 审中-公开
公开(公告)号：US20170327464A1
公开(公告)日：2017-11-16
申请号：US15666259
申请日：2017-08-01
申请人： Anton Frenkel , Avital Laxer
发明人： Anton Frenkel , Avital Laxer
IPC分类号： C07D215/56
CPC分类号： C07D215/56 , A61K31/47 , C07B2200/13 , G01N30/06 , G01N33/15
摘要： The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; or f) an amount of methyl 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate (MCQME) in the mixture is no more than 0.12% relative to the amount of laquinimod sodium as measured by HPLC.

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