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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

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。

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. 发明专利

AU1265902A Crystalline ethanolate solvate form of zafirlukast, process for manufacture and pharmaceutical compositions thereof 未知
公开(公告)号：AU1265902A
公开(公告)日：2002-05-21
申请号：AU1265902
申请日：2001-10-24
申请人： ISP FINETECH LTD
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
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.

6. 发明专利

IL121288A Process and a novel intermediate for the preparation of flecainide 未知
公开(公告)号：IL121288A
公开(公告)日：2000-10-31
申请号：IL12128897
申请日：1997-07-11
申请人： FINETECH LTD
发明人： GUTMAN ARIE L , NISNEVICH GENADY , SHKOLNIK ELEONORA , ZALTZMAN IGOR
IPC分类号： C07C255/14 , C07D211/26 , C07D213/40 , C07B43/08
摘要： The invention relates to processes for the preparation of compounds of the formulawherein R is a 2-piperidyl or 2-pyridyl radical, and pharmaceutically acceptable salts thereof, the process comprising the steps of:a) reacting 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid or a salt thereof with a haloacetonitrile to form a cyanomethyl ester of formulab) reacting the ester with an amine of the formula RCH2NH2, where R is as defined above.

7. 发明专利

AU2878101A A new process for the preparation of latanoprost 未知
公开(公告)号：AU2878101A
公开(公告)日：2001-08-07
申请号：AU2878101
申请日：2001-01-26
申请人： FINETECH LTD
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 , A61K31/557
摘要： Disclosed is a 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.

8. 发明专利

AU7546398A Preparation of alkyl 4,5-dihydro-gamma,5-dioxo-2-aryl-4-oxazolebutanoates 未知
公开(公告)号：AU7546398A
公开(公告)日：1998-12-30
申请号：AU7546398
申请日：1998-05-29
申请人： FINETECH LTD
发明人： GUTMAN ARIE L , NISNEVICH GENADY , SHKOLNIK ELEONORA , ZALTZMAN IGOR , PERTSIKOV BORIS , TISHIN BORIS , SOTRIKHIN MAXIM
IPC分类号： C07D263/42

9. 发明专利

AU3986700A Polyaldimines of oligomeric aminobenzoic acid derivatives, and their use for preparation of moisture-curable, storage-stable, one-part polyreas 未知
公开(公告)号：AU3986700A
公开(公告)日：2000-11-10
申请号：AU3986700
申请日：2000-04-23
申请人： FINETECH LTD , KUZNETSOV VLADIMIR
发明人： GUTMAN ARIE , NISNEVICH GENNADIY , ZALTZMAN IGOR , JUDOVICH LEV
IPC分类号： C07D307/52 , C07C251/24 , C07D213/53 , C08G18/32 , C08G18/50 , C09J175/02 , C09D175/02
摘要： The invention relates to polyaldimines of formula [1] and their use within moisture curable one part polyurea compositions.wherein j is an integer of 3 to 30 and R2 is unsubstituted homocyclic or heterocyclic aryl radical or alkyl, alkoxy, alkylthio or halogen substituted homocyclic or heterocyclic aryl radical.

10. 发明专利

AU5191099A Novel process and intermediates for production of donepezil and related compounds 未知
公开(公告)号：AU5191099A
公开(公告)日：2000-03-06
申请号：AU5191099
申请日：1999-08-11
申请人： FINETECH LTD
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 , C07D211/00
摘要： The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R1 is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-(omega-aralkyl)-4-piperidyl; 4-pyridyl; R4, R5, R6, and R7 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 R1, R4, R5, R6 and R7, m and n are as defined above; R2 is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R3 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.

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