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1. 发明专利

CA2572149A1 PROCESS FOR PRODUCTION OF AZULENE DERIVATIVES AND INTERMEDIATES FOR THE SYNTHESIS OF THE SAME 未知
公开(公告)号：CA2572149A1
公开(公告)日：2006-01-19
申请号：CA2572149
申请日：2005-07-07
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： SUZUKI TAKAYUKI , MIYAFUJI AKIO , TOMIYAMA HIROSHI , YAMASHITA YOHEI , SAKAMOTO KENICHIRO , KOIDE TOKUO , NODA ATSUSHI , NAKAMURA HIROFUMI , YOKOTA MASAYUKI , INAKOSHI MASATOSHI , KAWANO NORIYUKI , MIYATA JUNJI , HAYASHI YASUMASA , OGASAWARA JUNKO , KOBAYASHI YOSHINORI , IMAMURA MASAKAZU , SUGANE TAKASHI
IPC分类号： C07D309/10 , C07C43/225 , C07C49/223 , C07H7/04 , C07H15/04
摘要： A process for producing an azulene derivative useful as a Na + -glucose cotransporter inhibitor, which is high in yield, is simple in operation, is low in cost, is suited for environmental protection, and is advantageous industrially, the process being characterized by reducing and deprotecting at least one compound selected from penta-acyl compounds and tetra-acyl compounds or salts thereof to obtain a C-glycoside compound; and a useful intermediate for synthesis of such an azulene derivative, obtained in the course of the above process.

2. 发明公开

EP1783122A4 PROCESS FOR PRODUCTION OF AZULENE DERIVATIVES AND INTERMEDIATES FOR THE SYNTHESIS OF THE SAME 审中-公开
标题翻译：用于生产甘菊环烃衍生物和中间产品及其合成
公开(公告)号：EP1783122A4
公开(公告)日：2008-12-10
申请号：EP05765585
申请日：2005-07-07
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： TOMIYAMA HIROSHI , YOKOTA MASAYUKI , NODA ATSUSHI , KOBAYASHI Y , OGASAWARA JUNKO , HAYASHI YASUMASA , INAKOSHI MASATOSHI , NAKAMURA HIROFUMI , KOIDE TOKUO , SAKAMOTO KENICHIRO , YAMASHITA YOHEI , MIYAFUJI AKIO , SUZUKI TAKAYUKI , KAWANO NORIYUKI , MIYATA JUNJI , IMAMURA MASAKAZU , SUGANE TAKASHI
IPC分类号： C07D309/10 , C07C43/225 , C07C49/223 , C07H7/04 , C07H15/04
CPC分类号： C07C49/255 , C07C45/48 , C07C45/63 , C07C45/71 , C07C49/245 , C07H7/04 , C07H15/04
摘要： A process for producing azulene derivatives useful as Na+-glucose cotransporter inhibitor easily and simply in high yield at a low cost which is industrially advantageous and excellent in environmental protection, characterized by subjecting at least one compound selected from among specific penta- and tetraacyl precursors of the azulene derivatives and salts of the precursors to reduction and deblocking to obtain a C-glycoside compound; and useful intermediates obtained in the above process.

3. 发明专利

JP2008019168A Process for producing 2-cyano-4-fluoropyrrolidine derivative 审中-公开
标题翻译：生产2-氰基-4-氟代吡咯烷衍生物的方法
公开(公告)号：JP2008019168A
公开(公告)日：2008-01-31
申请号：JP2004307520
申请日：2004-10-22
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： YAMASHITA YOHEI , HAYAKAWA MASAHIKO , NIKAWARA MITSUHIRO
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a new process for producing 4-fluoro-1-(ä[4-methyl-1-(methanesulfonyl)piperidin-4-yl]amino}acetyl)pyrrolidine-2-carbonitrile and to provide an intermediate necessary for the process for production. SOLUTION: A new 2-aminocarbonyl-4-fluoropyrrolidine derivative is represented by formula (I) (wherein, R 1 represents H or a protective group of an amino group). The process for producing the 4-fluoro-1-(ä[4-methyl-1-(methanesulfonyl)piperidin-4-yl]amino}acetyl)pyrrolidine-2-carbonitrile useful as a therapeutic agent and/or a prophylactic agent for type 1 diabetes, type 2 diabetes, insulin-resistant diseases and obesity using the compound is provided. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供一种生产4-氟-1-（ä[4-甲基-1-（甲磺酰基）哌啶-4-基]氨基}乙酰基）吡咯烷-2-甲腈的新方法，提供生产过程所必需的中间体。解决方案：新的2-氨基羰基-4-氟吡咯烷衍生物由式（I）表示（其中R 1表示H或氨基的保护基）。制备可用作治疗剂的4-氟-1-（ä[4-甲基-1-（甲磺酰基）哌啶-4-基]氨基}乙酰基）吡咯烷-2-腈的方法和/或预防剂提供了使用该化合物的1型糖尿病，2型糖尿病，胰岛素抗性疾病和肥胖症。版权所有（C）2008，JPO＆INPIT

4. 发明专利

MX2007000209A PROCESO PARA LA PRODUCCION DE DERIVADOS DE AZULENO E INTERMEDIARIOS PARA LA SINTESIS DE LOS MISMOS. 未知
公开(公告)号：MX2007000209A
公开(公告)日：2007-03-30
申请号：MX2007000209
申请日：2005-07-07
申请人： ASTELLAS PHARMA INC
发明人： SUZUKI TAKAYUKI , KAWANO NORIYUKI , TOMIYAMA HIROSHI , NODA ATSUSHI , KOBAYASHI YOSHINORI , IMAMURA MASAKAZU , SUGANE TAKASHI , YOKOTA MASAYUKI , OGASAWARA JUNKO , HAYASHI YASUMASA , INAKOSHI MASATOSHI , NAKAMURA HIROFUMI , KOIDE TOKUO , SAKAMOTO KENICHIRO , YAMASHITA YOHEI , MIYAFUJI AKIO , MIYATA JUNJI
IPC分类号： C07C49/223 , C07C43/225 , C07D309/10 , C07H7/04 , C07H15/04
摘要： Un procedimiento para la produccion de un derivado de azuleno util como un inhibidor del co-transportador Na+- glucosa, el cual es alto en rendimiento, simple en operacion, de bajo costo, y adecuado para la proteccion ambiental, y es industrialmente ventajoso, el procedimiento esta caracterizado por la reduccion y desproteccion de al menos un compuesto seleccionado de los compuestos de penta-acilo y tetra-acilo o sales de los mismos para obtener un compuesto de C-glicosida; y un intermediario util para la sintesis de dicho derivado de azuleno, obtenido en el curso del procedimiento anterior.

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