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1. 发明申请

WO2009081087A1 CRYSTALLINE POLYMORPH OF DOXAZOSIN MESYLATE (FORM IV) AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译：二甲氧基硅烷（甲基四）的结晶聚合物及其制备方法
公开(公告)号：WO2009081087A1
公开(公告)日：2009-07-02
申请号：PCT/GB2008/002362
申请日：2008-07-10
申请人： CIPLA LIMITED , CURTIS, Philip, Anthony , KANKAN, Rajendra, Narayanrao , RAO, Dharmaraj, Ramachandra , GANGRADE, Manish, Gopaldas , MUDGAL, Shrikant, Suresh
发明人： KANKAN, Rajendra, Narayanrao , RAO, Dharmaraj, Ramachandra , GANGRADE, Manish, Gopaldas , MUDGAL, Shrikant, Suresh
IPC分类号： C07D405/12 , A61P9/12 , A61P13/08 , A61K31/517
CPC分类号： C07D405/12
摘要： Crystalline Form (IV) of doxazosin mesylate, a process for its preparation and uses thereof.
摘要翻译：甲磺酸多沙唑嗪的结晶形式（IV），其制备方法和用途。

2. 发明申请

WO2008135770A3 PROCESS FOR PREPARING DORZOLAM IDE 审中-公开
标题翻译：制备DORZOLAM IDE的方法
公开(公告)号：WO2008135770A3
公开(公告)日：2009-05-14
申请号：PCT/GB2008001592
申请日：2008-05-07
申请人： CIPLA LTD , CURTIS PHILIP ANTHONY , KANKAN RAJENDRA NARAYANRAO , RAO DHANMARAJ RAMACHANDRA , MUDGAL SHRIKANT SURESH
发明人： KANKAN RAJENDRA NARAYANRAO , RAO DHANMARAJ RAMACHANDRA , MUDGAL SHRIKANT SURESH
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： There is provided a process for preparing dorzolamide and processes for preparing intermediates useful in the preparation of dorzolamide. In particular, there is provided a process for preparing an acetoamido sulfone of formula (viii) comprising oxidation of a hydroxysulfonamide of formula (vii) in the presence of an oxidizing agent selected from the group consisting of: a peracid, tert-butyl hydroperoxide, dimethyl dioxirane, selenium dioxide, m-phenanthroline di-N-oxide, nitric acid and hydrogen peroxide. There is also provided a process for preparing an acetoamidosulfone of formula (ix-a) comprising converting a hydroxysulfone of formula (viii) to the acetoamidosulfone of formula (ix-a) in the presence of acetonitrile and an acid. There is also provided a process for separating the cis- and trans-isomers of dorzolamide from a mixture of the trans-isomer of dorzolamide and the cis-isomer of dorzolamide comprising reacting the mixture of isomers with a carboxylic acid.
摘要翻译：提供了制备多佐胺的方法和制备可用于制备多佐胺的中间体的方法。特别地，提供了制备式（viii）的乙酰胺基砜的方法，包括在选自以下的氧化剂的存在下氧化式（vii）的羟基磺酰胺：过酸，叔丁基过氧化氢，二氧杂环己烷，二氧化硒，间二菲咯啉二-N-氧化物，硝酸和过氧化氢。还提供了制备式（ix-a）的乙酰氨基砜的方法，包括在乙腈和酸存在下将式（Ⅸ）的羟基砜转化成式（ix-a）的乙酰胺基砜。还提供了从多佐胺的反式异构体和多佐胺的顺式异构体的混合物中分离多佐胺的顺式和反式异构体的方法，包括使异构体的混合物与羧酸反应。

3. 发明申请

WO2008135770A2 PROCESS FOR PREPARING DORZOLAM IDE 审中-公开
标题翻译：制备DORZOLAM IDE的方法
公开(公告)号：WO2008135770A2
公开(公告)日：2008-11-13
申请号：PCT/GB2008/001592
申请日：2008-05-07
申请人： CIPLA LIMITED , CURTIS, Philip, Anthony , KANKAN, Rajendra, Narayanrao , RAO, Dhanmaraj, Ramachandra , MUDGAL, Shrikant, Suresh
发明人： KANKAN, Rajendra, Narayanrao , RAO, Dhanmaraj, Ramachandra , MUDGAL, Shrikant, Suresh
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： There is provided a process for preparing dorzolamide and processes for preparing intermediates useful in the preparation of dorzolamide. In particular, there is provided a process for preparing an acetoamido sulfone of formula (viii) comprising oxidation of a hydroxysulfonamide of formula (vii) in the presence of an oxidizing agent selected from the group consisting of: a peracid, tert-butyl hydroperoxide, dimethyl dioxirane, selenium dioxide, m-phenanthroline di-N-oxide, nitric acid and hydrogen peroxide. There is also provided a process for preparing an acetoamidosulfone of formula (ix-a) comprising converting a hydroxysulfone of formula (viii) to the acetoamidosulfone of formula (ix-a) in the presence of acetonitrile and an acid. There is also provided a process for separating the cis- and trans-isomers of dorzolamide from a mixture of the trans-isomer of dorzolamide and the cis-isomer of dorzolamide comprising reacting the mixture of isomers with a carboxylic acid.
摘要翻译：提供了制备多佐胺的方法和制备可用于制备多佐胺的中间体的方法。特别地，提供了制备式（viii）的乙酰胺基砜的方法，包括在选自以下的氧化剂的存在下氧化式（vii）的羟基磺酰胺：过酸，叔丁基过氧化氢，二氧杂环己烷，二氧化硒，间二菲咯啉二-N-氧化物，硝酸和过氧化氢。还提供了制备式（ix-a）的乙酰氨基砜的方法，包括在乙腈和酸存在下将式（Ⅸ）的羟基砜转化成式（ix-a）的乙酰胺基砜。还提供了从多佐胺的反式异构体和多佐胺的顺式异构体的混合物中分离多佐胺的顺式和反式异构体的方法，包括使异构体的混合物与羧酸反应。

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