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1. 发明专利

JP2008273840A Method for producing benzylamine derivative 审中-公开
标题翻译：生产苯甲酰胺衍生物的方法
公开(公告)号：JP2008273840A
公开(公告)日：2008-11-13
申请号：JP2005205323
申请日：2005-07-14
申请人： Zeria Pharmaceut Co Ltd , ゼリア新薬工業株式会社
发明人： NAGASAWA MASAAKI , MURATA MASAKAZU , KAWASE NOBUO , NAKAO TATSU , NAKANO DAISUKE
IPC分类号： C07D471/10 , C07B61/00 , C07C211/29 , C07C231/02 , C07C231/14 , C07C233/36 , C07C233/78 , C07D211/72
CPC分类号： C07C233/78 , C07D471/10
摘要： PROBLEM TO BE SOLVED: To provide an advantageous method for producing a benzylamine derivative.
SOLUTION: The method for producing a benzylamine derivative represented by formula (21) is characterized by causing a compound represented by formula (15) to react with a compound represented by formula (20). [In the formulae, R
1 and R
2 each represents an alkyl group; R
3 represents an alkyl group that may be substituted with a halogen atom, R
4 represents an aralkyl group, a lower alkyl group, an aryl group, a cycloalkyl group, or an amino group that may be substituted with a phenyl group or a lower alkyl group; and X
1 and X
2 each represents a hydrogen atom or a halogen atom].
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供生产苄胺衍生物的有利方法。解决方案：由式（21）表示的苄胺衍生物的制备方法的特征在于使由式（15）表示的化合物与式（20）表示的化合物反应。 [式中，R 1 和R 2 各自表示烷基; R SP 3表示可以被卤素原子取代的烷基，R 4表示芳烷基，低级烷基，芳基，环烷基或可以被苯基或低级烷基取代的氨基; 和X 1 和X 2 各自表示氢原子或卤素原子]。版权所有（C）2009，JPO＆INPIT

2. 发明专利

JP2006188432A Tetracyclic sulfenamide compound 审中-公开
标题翻译：四氯化硫化合物
公开(公告)号：JP2006188432A
公开(公告)日：2006-07-20
申请号：JP2003046736
申请日：2003-02-25
申请人： Zeria Pharmaceut Co Ltd , ゼリア新薬工業株式会社
发明人： NAGASAWA MASAAKI , ASAMI KAZUYASU , FURUTA SHIGERU , MIURA NAOYOSHI , MORITA HITOSHI
IPC分类号： C07D513/14 , A61K31/549 , A61K31/554 , A61P1/04 , A61P43/00
CPC分类号： C07D513/14 , A61K31/549 , A61K31/554
摘要： PROBLEM TO BE SOLVED: To provide a tetracyclic sulfenamide compound having a proton pump inhibitory activity and useful as a peptic ulcer-treating agent.
SOLUTION: This compound is expressed by formula (I) [wherein, R
1 is a lower alkyl, a lower acyl, cyano, carboxy, hydroxy, a lower alkoxycarbonyl, H or the like; R
2 , R
4 are each a lower alkyl, H or the like; R
3 is a lower alkyl which may have a group selected from a halogen atom, hydroxy, a lower alkyl, a lower alkoxy, furyl, morpholino group, etc.; A is a benzene ring, pyridine ring, thiophene ring or the like; B is a single bond, an amino or a group expressed as NR (wherein, R is a lower alkyl, a lower alkenyl or the like); and Z is a counter anion]. Since the compound has an excellent proton pump inhibitory effect, it is useful as a peptic ulcer-treating agent.
COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供具有质子泵抑制活性的四环亚磺酰胺化合物，可用作消化性溃疡治疗剂。解决方案：该化合物由式（I）表示[其中R 1为低级烷基，低级酰基，氰基，羧基，羟基，低级烷氧基羰基，H等; R 2 ，R 4 分别为低级烷基，H等; R 3是可以具有选自卤素原子，羟基，低级烷基，低级烷氧基，呋喃基，吗啉代基等的基团的低级烷基。 A是苯环，吡啶环，噻吩环等; B是单键，氨基或以NR表示的基团（其中，R为低级烷基，低级烯基等）; Z为抗衡阴离子]。由于该化合物具有优异的质子泵抑制作用，因此可用作消化性溃疡治疗剂。版权所有（C）2006，JPO＆NCIPI

3. 发明专利

JP2008273841A Ethylenediamine derivative and method for producing the same 审中-公开
标题翻译：乙烯二胺衍生物及其生产方法
公开(公告)号：JP2008273841A
公开(公告)日：2008-11-13
申请号：JP2005205324
申请日：2005-07-14
申请人： Zeria Pharmaceut Co Ltd , ゼリア新薬工業株式会社
发明人： NAGASAWA MASAAKI , KAWASE NOBUO , WATANABE TSUYOSHI , KOBAYASHI MINORU
IPC分类号： C07C211/29 , C07B57/00 , C07C45/63 , C07C49/80 , C07C209/62 , C07C213/04 , C07C215/30 , C07D203/08 , C07D301/24 , C07D303/08 , C07F3/02
CPC分类号： C07C45/63 , C07B57/00 , C07C211/29 , C07D203/08 , C07D301/24 , C07D303/08 , C07C49/80
摘要： PROBLEM TO BE SOLVED: To provide an intermediate useful for producing a benzylamine derivative, and a method for producing the intermediate.
SOLUTION: The method for producing an ethylenediamine derivative represented by formula (6) is characterized by reacting an aziridine compound represented by formula (5) with a primary amine. [In the formulae, R
1 represents an alkyl group or an aralkyl group, R
2 represents an alkyl group or an alkenyl group, R
3 represents an alkyl group, an aralkyl group or an aryl group that may contain a substituent, and Ar represents an aryl group that may contain a substituent].
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供可用于生产苄胺衍生物的中间体及其制备方法。解决方案：由式（6）表示的乙二胺衍生物的制备方法的特征在于使由式（5）表示的氮丙啶化合物与伯胺反应。 [式中，R 1表示烷基或芳烷基，R SP 2表示烷基或链烯基，R 3，表示可以含有取代基的烷基，芳烷基或芳基，Ar表示可以含有取代基的芳基。版权所有（C）2009，JPO＆INPIT

4. 发明专利

JP2012250993A Method for producing aminothiazole derivative and production intermediate 有权
标题翻译：生产氨基唑衍生物和生产中间体的方法
公开(公告)号：JP2012250993A
公开(公告)日：2012-12-20
申请号：JP2012200202
申请日：2012-09-12
申请人： Zeria Pharmaceutical Co Ltd , ゼリア新薬工業株式会社
发明人： NAGASAWA MASAAKI , ASAMI KAZUYASU , NAKAO TATSU , TANAKA NOBUYUKI , HAZAMA YOSHIYUKI
IPC分类号： C07D277/20 , A61K31/426 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/14 , C07D277/56
CPC分类号： C07C69/92 , C07C51/347 , C07C51/377 , C07C67/08 , C07C205/60 , C07D277/46 , C07D277/56 , C07C65/05
摘要： PROBLEM TO BE SOLVED: To provide an intermediate important for synthesis of an aminothiazole derivative useful as a medicine.SOLUTION: The intermediate is a compound represented by formula (5a). In the formula, a ring A is a benzene ring or a 6-membered heteroaromatic ring; Ris a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, an amino group, a mono-lower alkylamino group, or a di-lower alkylamino group; and at least one of R, Rand Ris a methoxy group while the rest are each a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, an amino group, a mono-lower alkylamino group, or a di-lower alkylamino group.
摘要翻译：要解决的问题：提供用作合成用作药物的氨基噻唑衍生物的中间体。中间体是由式（5a）表示的化合物。在该式中，环A为苯环或6元杂芳环; R 1是氢原子，低级烷基，卤原子，硝基，氨基，单低级烷基氨基或二低级烷基氨基 ; 并且R 2 ，R 3 和R 4 中的至少一个是甲氧基，其余各自为氢原子，低级烷基，卤素原子，硝基，氨基，单低级烷基氨基或二低级烷基氨基。版权所有（C）2013，JPO＆INPIT

5. 发明专利

JP2012006958A Method for producing amino thiazole derivative, and production intermediate thereof 有权
标题翻译：生产氨基噻唑衍生物的方法及其制备方法
公开(公告)号：JP2012006958A
公开(公告)日：2012-01-12
申请号：JP2011177441
申请日：2011-08-15
申请人： Zeria Pharmaceutical Co Ltd , ゼリア新薬工業株式会社
发明人： NAGASAWA MASAAKI , ASAMI KAZUYASU , NAKAO TATSU , TANAKA NOBUYUKI , HAZAMA YOSHIYUKI
IPC分类号： C07C51/367 , A61K31/426 , A61P1/04 , A61P1/08 , A61P1/14 , C07B61/00 , C07C65/21 , C07C67/00 , C07C67/08 , C07C69/92 , C07C201/14 , C07C205/43 , C07D277/20 , C07D277/56
CPC分类号： C07C69/92 , C07C51/347 , C07C51/377 , C07C67/08 , C07C205/60 , C07D277/46 , C07D277/56 , C07C65/05
摘要： PROBLEM TO BE SOLVED: To provide a selective demethylation method of a methoxy group existing on an ortho position (second position) of aromatic carboxylic acid, and a method for producing a compound via the demethylation method, in which 2-hydroxybenzoic acids are amide-bonded to 2-aminothiazoles having excellent enterokinesis improving action.SOLUTION: This invention relates to a method for producing a compound represented by formula (2a) in which a Lewis acid selected from BF, TiCLand AlClis reacted with a compound represented by formula (1a) in an ester-based, ketone-based or amide-based solvent (with the proviso that, in the case of BF, an alkali metal bromide or an alkali metal iodide is allowed to coexist). The invention also relates to a method for producing an aminothiazole derivative via the method.
摘要翻译：待解决的问题：为了提供存在于芳族羧酸的邻位（第二位置）的甲氧基的选择性脱甲基化方法，以及通过去甲基化方法制备化合物的方法，其中2-羟基苯甲酸酰胺键合到2-氨基噻唑具有优异的肠内营养素改善作用。本发明涉及一种制备式（2a）表示的化合物的方法，其中选自BF 3 ，TiCL 3 的情况下，允许碱金属溴化物或碱金属碘化物共存）。本发明还涉及通过该方法制备氨基噻唑衍生物的方法。版权所有（C）2012，JPO＆INPIT

6. 发明专利

JP2012236863A Method for producing aminothiazole derivative, and production intermediate 有权
标题翻译：生产氨基唑衍生物的方法和生产中间体
公开(公告)号：JP2012236863A
公开(公告)日：2012-12-06
申请号：JP2012200199
申请日：2012-09-12
申请人： Zeria Pharmaceutical Co Ltd , ゼリア新薬工業株式会社
发明人： NAGASAWA MASAAKI , ASAMI KAZUYASU , NAKAO TATSU , TANAKA NOBUYUKI , HAZAMA YOSHIYUKI
IPC分类号： C07C69/92
CPC分类号： C07C69/92 , C07C51/347 , C07C51/377 , C07C67/08 , C07C205/60 , C07D277/46 , C07D277/56 , C07C65/05
摘要： PROBLEM TO BE SOLVED: To provide an intermediate that is important for synthesis of an aminothiazole derivative useful as medicine.SOLUTION: There is provided a compound expressed by formula (3), wherein ring A represents benzene ring or 6-membered aromatic heterocycle; Rrepresents hydrogen atom, lower alkyl, halogen atom, nitro, amino, mono-lower alkylamino or di-lower alkylamino; at least one of R, Rand Ris methoxy, the rest being hydrogen atom, lower alkyl, halogen atom, nitro, amino, mono-lower alkylamino or di-lower alkylamino; Rrepresents hydrogen atom or an electron-withdrawing group.
摘要翻译：要解决的问题：提供对于用作药物的氨基噻唑衍生物的合成重要的中间体。提供由式（3）表示的化合物，其中环A表示苯环或6元芳族杂环; R 1表示氢原子，低级烷基，卤素原子，硝基，氨基，单低级烷基氨基或二低级烷基氨基; R 2 ，R 3 和R 4 中的至少一个是甲氧基其余为氢原子，低级烷基，卤素原子，硝基，氨基，单低级烷基氨基或二低级烷基氨基; R 5 表示氢原子或吸电子基团。版权所有（C）2013，JPO＆INPIT

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