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Title:
ESTER PRODRUG OF LEUKOTRIENE ANTAGONIST
Document Type and Number:
Japanese Patent JPH02124869
Kind Code:
A
Abstract:

NEW MATERIAL: A compound of formula I {wherein R1 is an alkyl, an alkoxyl, an alkylthio, an alkinyl, a phenylalyl, a thienylalkyl, a furylalkyl or the like; R2 is H, Br, Cl, CH3, OH or the like; or R1 is H and R2 is R1 except a thienylalkyl; q is 0-2; Y is COR3 or a group of formula II [wherein R3 is amino or OR14 (wherein R14 is H, an alkyl, an aryl or the like); m is 0 or 1; R4 is H, CH3, OH or the like] or the like; R is a group of formula III or IV (wherein n is 0-6; R5 is H, NH2 or the like; and R6 is NH2, SO3H or the like) or the like}.

EXAMPLE: 2-Hydroxy-3-[(2-carboisopropoxyethyl)thio]-3-[2-(8-phenyloctyl) phenyl]propanoic acid.

USE: A leukotriene antagonist.

PREPARATION: An aldehyde of formula V is converted into a methyl 2- hydroxyacetate derivative through the route of trimethylsilyl-protected cyanohydrin, and the product is reacted with thionyl chloride and further reacted with a substituted thiol to obtain a compound of formula I (wherein Y is COR3).


Inventors:
JIYON JIERARUDO GURIISON
RARUFU FUROIDO HOORU
JIYON FUREDERITSUKU NIYUUTON
KIYASURIIN EI FUITSUPUSU
JIYOANNU SUMOORUHIIA
Application Number:
JP24785489A
Publication Date:
May 14, 1990
Filing Date:
September 22, 1989
Export Citation:
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Assignee:
SMITHKLINE BECKMAN CORP
International Classes:
A61K31/19; A61K31/215; A61K31/275; A61K31/415; A61P29/00; A61P37/08; A61P43/00; C07C45/29; C07C45/44; C07C45/56; C07C45/62; C07C45/67; C07C45/68; C07C45/71; A61K31/165; C07C47/542; C07C47/546; C07C47/548; C07C47/55; C07C47/575; C07C255/33; C07C323/25; C07C323/41; C07C323/52; C07C323/56; C07C323/60; C07C323/66; C07C323/67; C07D233/84; C07D233/90; C07D257/04; C07D303/40; C07D303/48; C07D307/38; C07D307/54; C07D309/30; C07D333/24; C07D401/12; (IPC1-7): A61K31/165; A61K31/19; A61K31/215; A61K31/275; A61K31/415; C07C323/25; C07C323/41; C07C323/52; C07D233/84; C07D233/90; C07D257/04; C07D307/54; C07D333/24; C07D401/12
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)



 
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