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    XANTHINE DERIVATIVE
    23.
    发明专利
    XANTHINE DERIVATIVE 失效

    公开(公告)号：JPS6413090A

    公开(公告)日：1989-01-17

    申请号：JP16767887

    申请日：1987-07-07

    Applicant: UBE INDUSTRIES

    Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  KUROKI YOSHIAKI ,  TAKAMURA SHINJI

    IPC: C07D473/06 ,  A61K31/52 ,  A61K31/522 ,  A61P43/00

    Abstract: NEW MATERIAL:A compound expressed by formula I [Ar and Ar represent (substituted) phenyl or pyridyl; Z represents -O- or -NH-; A represents C2-6 (substituted) alkylene; B represents formulae II and III (R1-R4 represent C1-4 alkyl or lower alkenyl); m is 0 or 1, provided that at least one of Ar and Ar is pyridyl when m is 0] and acid addition salt thereof. EXAMPLE:7-[2-[4-[[(4-Chlorophenyl)-2-pyridyl] methoxy]-1-piperidino]-1-ethyl] theophylline. USE:An antihistamine agent. PREPARATION:A piperidine derivative expressed by formula IV (X represents halogen atom) is reacted with a compound expressed by the formula X-A-B to afford a compound expressed by formula I (group A is alkylene).

    OPTICALLY ACTIVE PIPERIDINE DERIVATIVE AND ITS PRODUCTION
    27.
    发明专利
    OPTICALLY ACTIVE PIPERIDINE DERIVATIVE AND ITS PRODUCTION 失效

    公开(公告)号：JPH10182635A

    公开(公告)日：1998-07-07

    申请号：JP34798596

    申请日：1996-12-26

    Applicant: UBE INDUSTRIES

    Inventor： KITA JUNICHIRO ,  TAKAMURA SHINJI

    IPC: C07D401/12 ,  A61K31/4427 ,  A61K31/445 ,  A61P37/08 ,  A61P43/00 ,  C07B57/00

    Abstract: PROBLEM TO BE SOLVED: To produce a diasteremoer salt useful as an intermediate for syntheses of pharmaceuticals having antihistaminic and antiallergic activities by optically resolving a specific piperazine derivative by using L(+)-tartaric acid. SOLUTION: This diastereomer, which consists of (S)-(-)-4-[(4-chlorophenyl)(2- pyridyl)methoxyl]piperidine.L(+)-tartarate of formula I, is obtained by making a racemic modification of formula II react with L(+)-tartaric acid, and fractivonally crystallizing the formed salt. Furthermore, by treating this diastereomer slat with an alkali to decompose, (S)-(-)-4-[(4-chlorophenyl)(2- pyrizyl)methoxyl]piperidine can be obtained.

    5-FLUOROURIDINE AND 2'-DEOXY-5-FLUOROURIDINE DERIVATIVE
    28.
    发明专利
    5-FLUOROURIDINE AND 2'-DEOXY-5-FLUOROURIDINE DERIVATIVE 失效

    公开(公告)号：JPH032193A

    公开(公告)日：1991-01-08

    申请号：JP13480689

    申请日：1989-05-30

    Applicant: UBE INDUSTRIES

    Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  KAKU YOSHIO ,  SAKAMOTO OSAMI

    IPC: C07H19/067 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P35/00 ,  C07H19/073

    Abstract: NEW MATERIAL:A compound of formula I {R is H or OR ; R to R are each H or of formula II [R is acyl; R is H, 1-13C alkyl, cycloalkyl, aralkyl, (halogen-substituted) lower alkenyl or (substituted)phenyl; n is 0-6], where, at least one of R to R being of formula II and R and R are not H at the same time.} EXAMPLE:2',3',5'-tris-O-[N-(2-n-propyl-n-pentanoyl)glycyl]-5-fluorouri dine. USE:Antineoplastic agents. Low toxic. PREPARATION:A 5-fluorouridine of formula III (R is H or OH) or 2'-deoxy-5- fluorouridine is put to ester condensation with a compound of formula IV in a solvent such as dichloromethane in the presence of a base such as a trialkylamine and a condensation agent such as p-toluenesulfonyl chloride.

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