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1. 发明专利

JP2011084579A Process for producing solifenacin or salt of the same 有权
标题翻译：生产固体或其盐的方法
公开(公告)号：JP2011084579A
公开(公告)日：2011-04-28
申请号：JP2011014815
申请日：2011-01-27
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： C07D453/02 , A61K31/4725 , A61P13/10 , A61P43/00
CPC分类号： C07D453/02 , A61K31/4725 , C07D217/06
摘要： PROBLEM TO BE SOLVED: To provide a novel process for producing solifenacin or its salt that is useful as a medicine, especially a therapeutic agent and/or preventive agent for urinary diseases, such as frequent urination and involuntary urination. SOLUTION: In particular, there are provided (1) a process for producing solifenacin from 2-(imidazolylcarbonyl)-1-phenyltetrahydroisoquinoline as a production starting material; (2) a process for producing solifenacin succinate from quinuclidinyl (1RS)-phenyltetrahydroisoquinolinecarboxylate as a production starting material; (3) a process for producing solifenacin from a lower-alkylquinuclidinyl carbonate as a production starting material; and (4) a process for producing solifenacin, comprising causing an alkali metal lower alkoxide to act on a secondary lower alkyl or tertiary lower alkyl phenyltetrahydroisoquinolinecarboxylate as a production starting material. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供可用作药物，特别是尿路疾病的治疗剂和/或预防剂例如频尿和非自愿排尿的新型的索非那新或其盐的制备方法。具体地，提供（1）从2-（咪唑基羰基）-1-苯基四氢异喹啉生产索非那新的方法作为生产起始原料; （2）从奎宁环基（1RS） - 苯基四氢异喹啉羧酸盐作为生产起始原料生产索非那新琥珀酸盐的方法; （3）从作为生产起始原料的低级烷基奎宁环碳酸酯制造索非那新的方法; （4）一种制备索非那新的方法，包括使碱金属低级醇盐作为生产起始原料作用于仲低级烷基或叔低级烷基苯基四氢异喹啉羧酸盐。版权所有（C）2011，JPO＆INPIT

2. 发明公开

EP1714965A4 COMPOSITION CONTAINING SOLIFENACIN SUCCINATE 审中-公开
标题翻译：琥珀酸索利那新成分含
公开(公告)号：EP1714965A4
公开(公告)日：2007-12-19
申请号：EP05709799
申请日：2005-02-07
申请人： ASTELLAS PHARMA INC
发明人： ISHII YUSUKE , TAKAOKA KOUJI , INAKOSHI MASATOSHI , NAKAGAWA SHUICHI , NAGATA KOJI , YORIMOTO NAOKI , TAKEUCHI MAKOTO , YONETOKU YASUHIRO
IPC分类号： C07D453/02 , A61K31/439 , A61P1/12 , A61P13/02 , A61P27/08
CPC分类号： C07D453/02
摘要： A composition comprising solifenacin succinate with the content of impurities reduced, which can be used as a pharmaceutical primary material. This composition comprising solifenacin succinate is especially featured by reduction of the content of optical isomers thereof as compared with the conventional compositions containing solifenacin acid adduct salts and can be used in the production of pharmaceutical products containing solifenacin succinate. There is further provided a process for easily producing this composition comprising solifenacin succinate.

3. 发明专利

CA2564757A1 PROCESS FOR PRODUCING SOLIFENACIN OR ITS SALT 未知
公开(公告)号：CA2564757A1
公开(公告)日：2005-11-10
申请号：CA2564757
申请日：2005-04-25
申请人： ASTELLAS PHARMA INC
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： C07D453/02
摘要： A novel process for producing solifenacin or its salt that is useful as a medicine, especially a therapeutic agent and/or preventive agent for urinary diseases, such as frequent urination and involuntary urination. In particula r, there are provided (1) a process for producing solifenacin from 2- (imidazolylcarbonyl)-1-phenyltetrahydroisoquinoline as a production starting material; (2) a process for producing solifenacin succinate from quinuclidin yl (1RS)-phenyltetrahydroisoquinolinecarboxylate as a production starting material; (3) a process for producing solifenacin from a lower- alkylquinuclidinyl carbonate as a production starting material; and (4) a process for producing solifenacin, comprising causing an alkali metal lower alkoxide to act on a secondary lower alkyl or tertiary lower alkyl phenyltetrahydroisoquinolinecarboxylate as a production starting material.

4. 发明专利

CA2558877A1 COMPOSITION CONTAINING SOLIFENACIN SUCCINATE 未知
公开(公告)号：CA2558877A1
公开(公告)日：2005-08-18
申请号：CA2558877
申请日：2005-02-07
申请人： ASTELLAS PHARMA INC
发明人： YORIMOTO NAOKI , TAKAOKA KOUJI , ISHII YUSUKE , INAKOSHI MASATOSHI , YONETOKU YASUHIRO , TAKEUCHI MAKOTO , NAGATA KOJI , NAKAGAWA SHUICHI
IPC分类号： C07D453/02 , A61K31/439 , A61P1/12 , A61P13/02 , A61P27/08
摘要： A composition comprising solifenacin succinate with the content of impuritie s reduced, which can be used as a pharmaceutical primary material. This composition comprising solifenacin succinate is especially featured by reduction of the content of optical isomers thereof as compared with the conventional compositions containing solifenacin acid adduct salts and can b e used in the production of pharmaceutical products containing solifenacin succinate. There is further provided a process for easily producing this composition comprising solifenacin succinate.

5. 发明公开

EP1757604A4 PROCESS FOR PRODUCING SOLIFENACIN OR ITS SALT 失效
标题翻译：用于生产索利那新或其盐
公开(公告)号：EP1757604A4
公开(公告)日：2010-04-28
申请号：EP05734743
申请日：2005-04-25
申请人： ASTELLAS PHARMA INC
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： C07D453/02 , A61K31/4725
CPC分类号： C07D453/02 , A61K31/4725 , C07D217/06

6. 发明专利

ES2393540T3 Síntesis de monosuccinato de solifenacina 未知
公开(公告)号：ES2393540T3
公开(公告)日：2012-12-26
申请号：ES10191324
申请日：2005-04-25
申请人： ASTELLAS PHARMA INC
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： C07D453/02 , A61K31/4725 , C07B57/00
摘要： Un método para producir succinato de solifenacina, que comprende permitir que reaccione ácido succínico con un compuesto representado por una fórmula (II) [en la fórmula, la estereoquímica de la posición 1 de la tetrahidroisoquinolina sustituida con fenilo es una mezcla de la forma (R) y la forma (S) ], en el que el compuesto representado por la fórmula (II) es (3R) -quinuclidin-3-il éster del ácido (1RS) -1-fenil-1, 2, 3, 4tetrahidroisoquinolin-2-carboxílico.

7. 发明专利

ES2385892T3 Proceso para producir solifenacina o su sal 未知
公开(公告)号：ES2385892T3
公开(公告)日：2012-08-02
申请号：ES05734743
申请日：2005-04-25
申请人： ASTELLAS PHARMA INC
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： C07D453/02 , A61K31/4725
摘要： Un método para producir solifenacina, o una sal farmacéuticamente aceptable de la misma, que comprendepermitir que un compuesto representado por una fórmula (I)[en la fórmula, Lv representa 1H-imidazol-1-ilo] y (R)-quinuclidin-3-ol experimentan condensación.

8. 发明专利

CA2564757C METHOD FOR PRODUCING SOLIFENACIN OR SALTS THEREOF 未知
公开(公告)号：CA2564757C
公开(公告)日：2011-08-02
申请号：CA2564757
申请日：2005-04-25
申请人： ASTELLAS PHARMA INC
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： C07D453/02
摘要： There is provided a novel method for producing solifenacin or a salt thereof which is useful as a medicine, particularly a therapeutic agent and/or a preventive agent for a urinary organ system disease such as pollakiuria or urinary incontinence. Illustratively, there are provided (1) a method for producing solifenacin in which 2-(1H-imidazolylcarbonyl)-1-phenyltetrahydroisoquinoline is used as the starting material, (2) a method for producing solifenacin succinate in which (1RS)-phenyltetrahydroisoquinoline-carboxylic acid quinuclidinyl ester is used as the starting material, (3) a method for producing solifenacin in which a lower alkyl quinuclidinyl carbonate is used as the starting material and (4) a method for producing solifenacin in which phenyltetrahydroisoquinoline-carboxylic acid secondary lower alkyl or tertiary lower alkyl ester is used as the starting material and allowed to react with an alkali metal lower alkoxide.

9. 发明专利

CA2692561A1 METHOD FOR PRODUCING SOLIFENACIN OR SALTS THEREOF 未知
公开(公告)号：CA2692561A1
公开(公告)日：2005-11-10
申请号：CA2692561
申请日：2005-04-25
申请人： ASTELLAS PHARMA INC
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： C07D453/02 , A61K31/4725
摘要： There is provided a novel method for producing solifenacin or a salt thereof which is useful as a medicine, particularly a therapeutic agent and/or a preventive agent for a urinary organ system disease such as pollakiuria or urinary incontinence. Illustratively, there are provided (1) a method for producing solifenacin in which 2-(1H-imidazolylcarbonyl)-1-phenyltetrahydroisoquinoline is used as the starting material, (2) a method for producing solifenacin succinate in which (1RS)-phenyltetrahydroisoquinoline-carboxylic acid quinuclidinyl ester is used as the starting material, (3) a method for producing solifenacin in which a lower alkyl quinuclidinyl carbonate is used as the starting material and (4) a method for producing solifenacin in which phenyltetrahydroisoquinoline-carboxylic acid secondary lower alkyl or tertiary lower alkyl ester is used as the starting material and allowed to react with an alkali metal lower alkoxide.

10. 发明专利

CA2560080A1 SOLIFENACIN-CONTAINING COMPOSITION 未知
公开(公告)号：CA2560080A1
公开(公告)日：2005-09-22
申请号：CA2560080
申请日：2005-03-11
申请人： ASTELLAS PHARMA INC
发明人： INAKOSHI MASATOSHI , ISHII YUSUKE
IPC分类号： A61K31/435 , C07D453/02
摘要： A novel process for producing a composition containing either solifenacin or a salt thereof; and a composition containing either solifenacin or a salt thereof obtained by the production process, which contains a solifenacin compound having an optionally substituted lower alkyl bonded to the 2-positi on of the quinuclidine. The composition contains solifenacin in a high purity, and contains, only in an extremely small amount, unexpected compounds which are peculiar to the production process. It hence has extremely preferable properties required of ingredients for medicines.

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