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    2-AZETIDINONE-4-SUBSTITUTED COMPOUND AND ITS PREPARATION
    2.
    发明专利
    2-AZETIDINONE-4-SUBSTITUTED COMPOUND AND ITS PREPARATION 失效

    公开(公告)号：JPS60172996A

    公开(公告)日：1985-09-06

    申请号：JP2765184

    申请日：1984-02-16

    Applicant: YAMANOUCHI PHARMA CO LTD

    Inventor： TAMURA TOSHIYA ,  IWAMOTO HIDENORI ,  YOSHIDA MAKOTO ,  YAMAMOTO MINORU

    IPC: C07K14/575 ,  C07K1/00 ,  C07K1/113 ,  C07K5/02 ,  C07K5/08

    Abstract: NEW MATERIAL:The compound of formula I {R , R and R are H or lower alkyl; R is imidazolyl which may be N-substituted with lower alkyl, aromatic acyl or aryl; n is 0-3; X is methylene, ethylene, O or S; Y is OH, lower alkoxy, aralkoxy or group of formula [-N(R )R ] [R and R are H, (hydroxy) lower alkyl, etc. or together form an N-containing 5-6-membered (hetero)cyclic group]}, and its salt. EXAMPLE:N -[( S )-2-Azetidinone-4-carbonyl]-L-histidyl-DL-( 3,3-dimethyl )prolinamide. USE:An obnubilation-improving agent. PREPARATION:The carboxylic acid (derivative) of formula II [e.g. (S)-2-azetidinone-4-carboxylic acid] is made to react with the amine (derivative) of formula III(His is histidyl) [e.g. L-histidyl-DL-(3,3-dimethyl)prolinamide].

    PYRIDINE DERIVATIVE
    9.
    发明专利
    PYRIDINE DERIVATIVE 失效

    公开(公告)号：JPH0269459A

    公开(公告)日：1990-03-08

    申请号：JP22062488

    申请日：1988-09-02

    Applicant: YAMANOUCHI PHARMA CO LTD

    Inventor： IWAMOTO HIDENORI ,  KOIDE TOKUO ,  MATSUHISA AKIRA ,  IKADAI HIROYUKI

    IPC: C07D211/90 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/451 ,  A61P1/16 ,  C07D213/80

    Abstract: NEW MATERIAL:A compound expressed by formula I (R is lower alkyl; R and R are lower alkyl or either thereof is lower alkyl and the other is benzyl, etc.; R is lower alkyl; R and R are lower alkyl or either thereof is lower alkyl and the other is dilower alkylaminoalkyl; n is 2-5; formula II is dihydropyridine or pyridine ring) or salts thereof. EXAMPLE:Methyl 1-(3-dimethylaminoethyl) 4-(4-methoxyphenyl)-2,6-dimethyl-1,4- dihydropyridine-3,5-dicarboxylate. USE:A preventive and treating agent for hepatopathy. PREPARATION:A substituted benzaldehyde is reacted with an acylacetic acid derivative to provide a compound expressed by formula III, which is then reacted with an aminocrotonic acid derivative expressed by formula IV in a solvent, such as ethanol, to afford the compound expressed by formula I.

    22GUANIDINOTHIAZOLE DERIVATIVE AND ITS PREPARATION
    10.
    发明专利
    22GUANIDINOTHIAZOLE DERIVATIVE AND ITS PREPARATION 失效

    公开(公告)号：JPS5646873A

    公开(公告)日：1981-04-28

    申请号：JP12351279

    申请日：1979-09-26

    Applicant: YAMANOUCHI PHARMA CO LTD

    Inventor： IWAMOTO HIDENORI ,  HIRATA YASUFUMI ,  YANAGISAWA ISAO

    IPC: C07D277/20 ,  C07D277/48

    Abstract: NEW MATERIAL:A 2-guanidinothiazole derivative of formula I (R is H or lower alkyl; m and n are 1-3) or its salt. EXAMPLE:3-(2-Guanidinothiazol-4-ylmethylthio)propionitrile. USE:A synthetic intermediate of a compound having histamine H2 receptor antagonistic activity. PROCESS:The compound of formula I can be prepared by reacting a compound of formula II (R' is lower alkyl) or its salt with stoichiometric or excess amount of an amine of formula R-NH2 in a solvent such as methanol, benzene, etc. at room temperature or an elevated temperature, usually under refluxing or at a higher temperature in a sealed tube.

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