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1. 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。

2. 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。

3. 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.

4. 发明专利

AU2231602A Process for the preparation of zafirlukast 未知
公开(公告)号：AU2231602A
公开(公告)日：2002-06-18
申请号：AU2231602
申请日：2001-11-30
申请人： ISP FINETECH LTD
发明人： GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PONOMAREV VICTOR , SOTRIHIN MAXIM
IPC分类号： C07D209/18 , C07D209/24 , C07D209/00
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 [a]is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.

5. 发明专利

CA2398304A1 A NEW PROCESS FOR THE PREPARATION OF LATANOPROST 未知
公开(公告)号：CA2398304A1
公开(公告)日：2001-08-02
申请号：CA2398304
申请日：2001-01-26
申请人： ISP FINETECH LTD
发明人： GUTMAN ARIE , PERTSIKOV BORIS , JUDOVICH LEV , ETINGER MARINA , NISNEVICH GENNADIY , ZALTZMAN IGOR
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 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.

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