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31 条记录 (耗时 0.02 秒)

    Methods for isolating propargylated aminoindans
    6.
    发明授权
    Methods for isolating propargylated aminoindans 失效
    分离炔丙基化氨基酸的方法

    公开(公告)号：US07491847B2

    公开(公告)日：2009-02-17

    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： C07C211/42 ,  C07C271/44 ,  A61K31/21 ,  A61K31/135

    CPC分类号： C07C209/86 ,  C07C209/84 ,  C07C2602/08 ,  C07C211/42

    摘要： A process for isolating from a reaction mixture a salt of a mono-propargylated aminoindan, a process for isolating from a reaction mixture a crystalline diastereomeric salt of a mono-propargylated aminoindan, and a process for isolating from a reaction mixture a salt of enantiomerically pure N-propargyl-1-aminoindan or a salt of enantiomerically pure 6-(N-methyl, N-ethyl-carbamoyloxy)-N′-propargyl-1-aminoindan. The corresponding products are also disclosed.

    摘要翻译： 从反应混合物中分离单炔丙基化氨基茚满盐的方法，从反应混合物中分离出单炔丙基化氨基茚满的结晶非对映体盐的方法和从反应混合物中分离出对映异构体纯的盐的方法 N-炔丙基-1-氨基茚满或对映体纯的6-（N-甲基，N-乙基 - 氨基甲酰氧基）-N'-炔丙基-1-氨基茚满的盐。 相应的产品也被披露。

    Methods for isolating propargylated aminoindans
    7.
    发明申请
    Methods for isolating propargylated aminoindans 失效
    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。

    L-DOPA ethyl ester salts and uses thereof
    8.
    发明授权
    L-DOPA ethyl ester salts and uses thereof 失效
    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。