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    1.
    发明专利
    失效

    公开(公告)号：JPH05294929A

    公开(公告)日：1993-11-09

    申请号：JP28722891

    申请日：1991-10-08

    Applicant: UBE INDUSTRIES

    Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  TAKAMURA SHINJI ,  YAMANO KAYOKO ,  FUJIWARA HIROSHI

    IPC: A61K31/445 ,  A61K31/4465 ,  A61P11/00 ,  A61P17/00 ,  A61P37/08 ,  A61P43/00 ,  C07D211/46

    Abstract: PURPOSE:To obtain a new piperidine derivative having strong anti-histamine activity and antiallergic activity and useful as an anti-histamic agent reduced in action enhancing sleepiness. CONSTITUTION:The objective compound of formula I [Ar and Ar are phenyl which may have substituent groups (halogen, NO2, lower alkoxy, lower alkyl or halo-lower alkyl); A is 2-6C linear alkylene or branched linear alkylene having >=2C main chain or alkenylene; B is lower alkyl, OH, lower alkoxy, phenoxy, NH2, lower alkylamino or anilino) or a compound of formula II (Ar and Ar are pyridyl and further, Ar is phenyl which have a substituent group other than halogen; B is above-mentioned B or phenyl which may be substituted with a lower alkyl) or its pharmaceutically permissible acid addition salt, e.g. 4-[4-(diphenylmethoxy)-1-piperidyl]butanoic acid ethyl fumaric acid salt. This compound can readily be produced from a compound of formula III and a compound of formula IV (W is eliminable group).

    XANTHINE DERIVATIVE
    3.
    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).

    5-FLUOROURACIL DERIVATIVE
    4.
    发明专利
    5-FLUOROURACIL DERIVATIVE 失效

    公开(公告)号：JPH0338573A

    公开(公告)日：1991-02-19

    申请号：JP17312289

    申请日：1989-07-06

    Applicant: UBE INDUSTRIES

    Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  KAKU YOSHIO ,  HORIMI IICHIRO

    IPC: C07D239/553 ,  A61K31/505 ,  A61P35/00

    Abstract: NEW MATERIAL:A 1-carbamoyl-5-fluorouracil derivative expressed by formula I [x is 4-12C alkylene or cycloalkylene: R1 is acyl; R2 is H, 1-13C alkyl, aralkyl, (halogen-substituted)-lower-alkenyl or phenyl which may have a substituent group (lower alkyl, lower alkenyl or halogen); (n) is 0-8]. EXAMPLE:1-[6-[N-(2-n-Propyl-n-pentanoyl)glycyl]amino-n hexylcarbamoyl]-5- fluorouracil. USE:An antitumor agent reduced in side effects and having strong antitumor activity. PREPARATION:5-Fluorouracil is reacted with phosgene to give 1-chlorocarbonyl 5-fluorouracil expressed by formula II, which is then reacted with a compound expressed by formula V and obtained by subjecting a compound expressed by formula III to condensation through dehydration with a compound expressed by formula IV to provide the compound expressed by formula I.

    5-FLUOROURIDINE AND 2'-DEOXY-5-FLUOROURIDINE DERIVATIVE
    6.
    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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