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1. 发明申请

WO0009483A3 PROCESS AND INTERMEDIATES FOR PRODUCTION OF DONEPEZIL AND RELATED COMPOUNDS 审中-公开
标题翻译：二苯醚及其相关化合物的生产过程和中间体
公开(公告)号：WO0009483A3
公开(公告)日：2001-06-21
申请号：PCT/IL9900436
申请日：1999-08-11
申请人： FINETECH LTD , GUTMAN L ARIE , SHKOLNIK ELEONORA , TISHIN BORIS , NISNEVICH GENADY , ZALTZMAN IGOR
发明人： GUTMAN L ARIE , SHKOLNIK ELEONORA , TISHIN BORIS , NISNEVICH GENADY , ZALTZMAN IGOR
IPC分类号： C07B53/00 , C07B61/00 , C07D211/32 , C07D211/34
CPC分类号： C07D211/32 , C07D211/34
摘要： The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; 4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-( omega -aralkyl)-4-piperidyl; 4-pyridyl; R , R , R and R are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4 or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R , R , R , R and R , m and n are as defined above; R is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents. One of the most potent acetylcholinesterase inhibitors of the class of compounds prepared according to the present invention is donepezil.
摘要翻译：本发明涉及制备式（I）的乙酰胆碱酯酶抑制剂或其盐的新方法，其中：R 1是N-酰基-4-哌啶基; N-烷氧羰基-4-哌啶基; 4-哌啶基; N-烷基-4-哌啶基; N-苄基-4-哌啶基; N-（ω-芳烷基）-4-哌啶基; 4-吡啶基; R 4，R 5，R 6和R 7相同或不同，各自表示氢，直链或支链烷基，芳基，羟基，烷氧基，芳氧基，苄氧基，酰氧基，烷硫基，芳硫基，苄硫基，酰氨基，苯二甲酰亚氨基或卤素; n为1,2或3; m为1,2,3,4或5.该方法包括式（II）化合物或其盐的环化，其中R 1，R 4，R 5，R 6和R 7，m和n如上所定义; R 2选自衍生或未衍生的羧基，氰基，N-取代的氨基羰基或氢; R 3选自衍生化或非衍生的羧基，氰基或N-取代的氨基羰基，任选在酸和/或溶剂的存在下。根据本发明制备的化合物类别中最有效的乙酰胆碱酯酶抑制剂之一是多奈哌齐。

2. 发明申请

WO2002046153A3 PROCESS FOR THE PREPARATION OF ZAFIRLUKAST 审中-公开
公开(公告)号：WO2002046153A3
公开(公告)日：2002-06-13
申请号：PCT/IB2001/002268
申请日：2001-11-30
申请人： ISP FINETECH LTD. , GUTMAN, Arie , NISNEVICH, Gennady , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim
发明人： GUTMAN, Arie , NISNEVICH, Gennady , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim
IPC分类号： C07D209/18
摘要： The present invention provides a novel process for the preparation of alkyl (1-alkylindol-3-ylmethyl)benzoate derivatives which process comprises the steps of: (a) reacting of an alkyl (halomethyl)benzoate with excess of an indole, said indole being unsubstituted at positions 1-, 2- and 3-, under conditions promoting alkylation at the 3-position of the indole to yield a mixture comprising alkyl (indol-3-ylmethyl)benzoate and unreacted starting indole,(b) treating the mixture obtained in step (a) with base to yield a mixture, comprising the salt of (indol-3-ylmethyl)benzoic acid and the unreacted indole, (c) recovering the unreacted indole from the mixture obtained in step (b), and recycling the indole as starting material to step (a), (d) isolating the salt of (indol-3-ylmethyl)benzoic acid and/or acidifying the salt to form (indol-3-ylmethyl)benzoic acid, (e) reacting the (indol-3-ylmethyl)benzoic acid or its salt with alkylating agent in the presence of base to form the desired alkyl (1-alkylindol-3-ylmethyl)benzoate. The above process affords also the preparation of the anti-asthmatic leukotriene antagonist zafirlukast. In such case, methyl 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)benzoate [1a] is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.

3. 发明申请

WO0246153A2 PROCESS FOR THE PREPARATION OF ZAFIRLUKAST 审中-公开
标题翻译：制备ZAFIRLUKAST的方法
公开(公告)号：WO0246153A2
公开(公告)日：2002-06-13
申请号：PCT/IB0102268
申请日：2001-11-30
申请人： ISP FINETECH LTD , GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PONOMAREV VICTOR , SOTRIHIN MAXIM
发明人： GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PONOMAREV VICTOR , SOTRIHIN MAXIM
IPC分类号： C07D209/18 , C07D209/24 , C07D209/00
CPC分类号： C07D209/18 , C07D209/24 , Y02P20/582
摘要： The present invention provides a novel process for the preparation of alkyl (1-alkylindol-3-ylmethyl)benzoate derivatives which process comprises the steps of: (a) reacting of an alkyl (halomethyl)benzoate with excess of an indole, said indole being unsubstituted at positions 1-, 2- and 3-, under conditions promoting alkylation at the 3-position of the indole to yield a mixture comprising alkyl (indol-3-ylmethyl)benzoate and unreacted starting indole,(b) treating the mixture obtained in step (a) with base to yield a mixture, comprising the salt of (indol-3-ylmethyl)benzoic acid and the unreacted indole, (c) recovering the unreacted indole from the mixture obtained in step (b), and recycling the indole as starting material to step (a),(d) isolating the salt of (indol-3-ylmethyl)benzoic acid and/or acidifying the salt to form (indol-3-ylmethyl)benzoic acid, (e) reacting the (indol-3-ylmethyl)benzoic acid or it's salt with alkylating agent in the presence of base to form the desired alkyl (1-alkylindol-3-ylmethyl)benzoate. The above process affords also the preparation of the anti-asthmatic leukotriene antagonist zafirlukast. In such case, methyl 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)benzoate [1a] is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.
摘要翻译：本发明提供了一种制备烷基（1-烷基吲哚-3-基甲基）苯甲酸酯衍生物的新方法，该方法包括以下步骤：（a）使（卤代甲基）烷基烷基酯与过量的吲哚反应，所述吲哚为在吲哚的3位上促进烷基化的条件下，在位置1-，2-和3-未被取代，得到包含烷基（吲哚-3-基甲基）苯甲酸酯和未反应的起始吲哚的混合物，（b）处理得到的混合物在步骤（a）中与碱反应以产生包含（吲哚-3-基甲基）苯甲酸的盐和未反应的吲哚的混合物，（c）从步骤（b）中获得的混合物中回收未反应的吲哚，并将吲哚作为步骤（a）的起始原料，（d）分离（吲哚-3-基甲基）苯甲酸的盐和/或酸化盐以形成（吲哚-3-基甲基）苯甲酸，（e）使吲哚-3-基甲基）苯甲酸或其与烷基化剂的盐在碱的存在下形成所需的烷基（1-alkylindol -3-基甲基）苯甲酸甲酯。上述方法还提供了抗哮喘白三烯拮抗剂扎非司酮的制备。在这种情况下，在该方法的步骤（e）中形成3-甲氧基-4-（1-甲基-5-硝基吲哚-3-基甲基）苯甲酸甲酯[1a]，该化合物随后通过已知方法转化成扎非司酮。

4. 发明申请

WO0155101A2 A NEW PROCESS FOR THE PREPARATION OF LATANOPROST 审中-公开
标题翻译：一种制备LATANOPROST的新工艺
公开(公告)号：WO0155101A2
公开(公告)日：2001-08-02
申请号：PCT/IL0100076
申请日：2001-01-26
申请人： FINETECH LTD , GUTMAN ARIE , NISNEVICH GENNADIY , ETINGER MARINA , ZALTZMAN IGOR , JUDOVICH LEV , PERTSIKOV BORIS
发明人： GUTMAN ARIE , NISNEVICH GENNADIY , ETINGER MARINA , ZALTZMAN IGOR , JUDOVICH LEV , PERTSIKOV BORIS
IPC分类号： C07D307/935 , A61K31/5575 , A61P43/00 , C07B61/00 , C07C405/00 , C07D309/12 , C07D407/12
CPC分类号： C07C405/00
摘要： Disclosed is a novel process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.
摘要翻译：本发明公开了一种制备抗青光眼药物拉坦前列素的新方法，其产率高，产率高，纯度高。还公开了用于上述方法的新型中间体。

5. 发明申请

WO2002085902A1 PROCESS AND INTERMEDIATES FOR PRODUCTION OF CABERGOLINE AND RELATED COMPOUNDS 审中-公开
标题翻译：生产咖啡因及相关化合物的方法和中间体
公开(公告)号：WO2002085902A1
公开(公告)日：2002-10-31
申请号：PCT/IL2001/000344
申请日：2001-04-16
申请人： FINETECH LTD. , GUTMAN, Arie, L. , NISNEVICH, Gennadiy , RUKHMAN, Igor , TISHIN, Boris , VILENSKY, Alex , PERTSIKOV, Boris
发明人： GUTMAN, Arie, L. , NISNEVICH, Gennadiy , RUKHMAN, Igor , TISHIN, Boris , VILENSKY, Alex , PERTSIKOV, Boris
IPC分类号： C07D457/06
CPC分类号： C07D457/06
摘要： A process for preparation of N -(ergoline-8β-carbonyl)ureas of the formula [I] their stereoisomers as well as acid addition salts thereof which process comprises silylating an ergoline -8β-carboxamide of the formula [2], their stereoisomers as well as metal or ammonium salts or acid addition salts thereof and reacting the resultant product with an isocyanates R 1 N=C=O [5] wherein R 1 is selected from alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, and dimethylamino alkyl group -(CH 2 ) n NMe 2 in which n is an integer, R 2 is selected from hydrogen, alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, dimethylamino alkyl group -(CH 2 ) n NMe 2 in which n is an integer, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, thiazolyl or thiadiazolyl , R 3 represents a hydrocarbon group having from 1 to 4 carbon atoms, and R 4 is selected from hydrogen, halogen, methylthio and phenylthio group; followed by desilylation. This novel approach provides an efficient method for preparation of N -(ergoline-8β-carbonyl)ureas of the formula [I] which can be useful as anty-Parkinson drugs and prolactin inhibitors. One of the most potent antiprolactinic agent of the class of compounds prepared according to the present invention is Cabergoline. Silylated ergolines, which are obtained as intermediates in the process of the present invention, are novel compounds and represent a further aspect of the invention.
摘要翻译：制备式[I]的N-（麦角灵-8β-羰基）脲的方法及其酸加成盐，其方法包括使麦角灵-8β-甲酰胺甲硅烷基化式[2]，其立体异构体以及金属或铵盐或其酸加成盐，并使所得产物与异氰酸酯R 1 = C = O [5]反应，其中R 1选自具有 1至4个碳原子，环己基，苯基和二甲基氨基烷基 - （CH 2）n NMe 2，其中n是整数，R 2选自氢，具有1至4个碳原子的烷基，环己基，苯基，二甲基氨基烷基 - （CH 2）n NMe 2，其中n是整数，吡啶基，嘧啶基，吡嗪基，哒嗪基，噻唑基或噻二唑基，R 3表示具有1至4个碳原子的烃基，R 4选自氢，卤素，甲硫基和苯硫基; 然后脱甲硅烷基化。这种新方法提供了一种制备式[I]的N - （麦角灵-8β-羰基）脲的有效方法，其可用作非帕特森帕金森药物和催乳素抑制剂。根据本发明制备的化合物类别中最有效的促乳素剂之一是卡麦角林。在本发明的方法中作为中间体获得的甲硅烷基化的麦角糖是新的化合物，代表本发明的另一方面。

6. 发明申请

WO2002068376A1 PROCESS FOR THE PREPARATION OF RASAGILINE AND ITS SALTS 审中-公开
标题翻译：制备RASAGILINE及其盐的方法
公开(公告)号：WO2002068376A1
公开(公告)日：2002-09-06
申请号：PCT/IB2002/000542
申请日：2002-02-25
申请人： ISP FINETECH LTD. , GUTMAN, Arie, L. , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim , NISNEVICH, Gennady
发明人： GUTMAN, Arie, L. , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim , NISNEVICH, Gennady
IPC分类号： C07C211/42
CPC分类号： C07C209/88 , C07B2200/07 , C07C211/42
摘要： The present invention provides a novel process for the preparation of rasagiline or its salts, in particular rasagiline mesylate, which process comprises the steps of : (a) reacting racemic N-benzyl-1-indanamine with (R,R)-tartaric acid in water; (b) cooling the mixture of step (a) to form a salt of (R)-enantiomerically enriched N-benzyl-1-indanamine with (R,R)-tartaric acid in solid form; (c) separating said precipitated solid obtained in step (b); (d) hydrogenating under catalytic conditions the solid product of step (c), optionally, in the presence of acids, bases or salts; (e) basifying the reaction mixture of step (d) with aqueous base and isolating (R)-enantiomerically enriched 1-indanamine from the obtained mixture; and (f) converting the (R)-enantiomerically enriched 1-indanamine of step (e) to rasagiline or its salts.
摘要翻译：本发明提供了一种制备雷沙吉兰或其盐，特别是甲磺酸雷沙吉兰的新方法，该方法包括以下步骤：（a）使外消旋N-苄基-1-茚胺与（R，R） - 酒石酸反应水; （b）冷却步骤（a）的混合物以形成固体形式的（R） - 对映体富集的N-苄基-1-茚满胺与（R，R） - 酒石酸的盐; （c）分离步骤（b）中获得的沉淀固体; （d）在催化条件下氢化步骤（c）的固体产物，任选地在酸，碱或盐的存在下; （e）将步骤（d）的反应混合物与碱水溶液碱化并从所得混合物中分离（R） - 对映体富集的1-二氮茚; 和（f）将（R） - 对映异构体富集的步骤（e）的1-二胺转化为雷沙吉兰或其盐。

7. 发明申请

WO0238545A3 CRYSTALLINE ETHANOLATE SOLVATE FORM OF ZAFIRLUKAST, PROCESS FOR MANUFACTURE AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译： ZAFIRLUKAST的晶体乙酸盐溶液形式，其制备方法和药物组合物
公开(公告)号：WO0238545A3
公开(公告)日：2002-07-25
申请号：PCT/IL0100982
申请日：2001-10-24
申请人： ISP FINETECH LTD , GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PERTSIKOV BORIS , SOTRIHIN MAXIM , PONOMAREV VICTOR
发明人： GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PERTSIKOV BORIS , SOTRIHIN MAXIM , PONOMAREV VICTOR
IPC分类号： A61P11/06 , C07D209/24 , A61K31/404
CPC分类号： C07D209/24
摘要： A novel, crystalline ethanolate solvate form of zafirlukast is disclosed, as well as methods for preparing it. Pharmaceutical compositions containing this novel form of zafirlukast are also disclosed. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example in the treatment of asthma.
摘要翻译：公开了扎鲁司特的新颖结晶乙醇溶剂化物形式及其制备方法。还公开了含有这种新型扎鲁司特的药物组合物。该组合物可用于治疗涉及白三烯的疾病，例如治疗哮喘。

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