公开(公告)号：EP0695308A1

公开(公告)日：1996-02-07

申请号：EP94914681.0

申请日：1994-04-21

申请人： UNIVERZA V LJUBLJANI, FAKULTETA ZA NARAVOSLOVJE IN TEHNOLOGIJO, ODDELEK ZA FARMACIJO ,  LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d., Ljubljana

发明人： KIKELJ, Danijel ,  SUHADOLC, Elizabeta ,  RUTAR, Alenka ,  PECAR, Slavko ,  PUNCUH, Alesa ,  URLEB, Uros ,  LESKOVSEK, Vesna ,  MARC, Gasper ,  SOLLNER, Marija ,  KRBAVCIC, Ales ,  SERSA, Gregor ,  NOVAKOVIC, Srdjan ,  POVSIC, Lucka ,  STALC, Anton

IPC分类号： A61K38 ,  A61P35 ,  A61P37 ,  C07D265 ,  C07D279 ,  C07K5

CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07D265/36 ,  C07D279/16

摘要： Novel heterocyclic acyldipeptides of formula (I) wherein Z represents an oxygen or sulphur atom or a -CH2- group; R1 represents hydrogen, a straight or branched chain 1-4C alkyl, cycloalkyl, cycloalkylalkyl, trifluoromethyl or benzyl group; R2 represents hydrogen, a straight or branched chain 1-4C alkyl, cycloalkyl, alkylcycloalkyl, dialkylaminoalkyl, acylaminoalkyl or benzyl group; R3 represents hydrogen, a straight or branched chain 1-12C alkyl or trifluoromethyl group; R4 and R5, which are identical or different, represent an OR6 or NHR6 group, wherein R6 is hydrogen, a straight or branched chain 1-18C alkyl or benzyl group; Y represents a -CH2-, =CH- or =N- group; A represents a -(CH2)3- group when Y is -CH2-, the two rings being trans-condensed, or a (a) or (b) group, wherein R7 represents H, F, Br, Cl, a straight or branched chain 1-4C alkyl, 1-4C alkoxy, trifluoromethyl, nitro, amino, alkylamino or dialkylamino group, when Y is =CH- or =N-; are prepared by reacting the corresponding heterocyclic carboxylic acid with the corresponding dipeptides using common reagents for the formation of the peptide bond. The heterocyclic acyldipeptides of formula (I) and their pharmaceutically acceptable salts are useful as active compounds in medicaments having immunostimulatory and antitumour activity.

公开(公告)号：EP0695308B1

公开(公告)日：1998-07-01

申请号：EP94914681.5

申请日：1994-04-21

申请人： UNIVERZA V LJUBLJANI, FAKULTETA ZA NARAVOSLOVJE IN TEHNOLOGIJO, ODDELEK ZA FARMACIJO ,  LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d., Ljubljana

发明人： KIKELJ, Danijel ,  SUHADOLC, Elizabeta ,  RUTAR, Alenka ,  PECAR, Slavko ,  PUNCUH, Alesa ,  URLEB, Uros ,  LESKOVSEK, Vesna ,  MARC, Gasper ,  SOLLNER, Marija ,  KRBAVCIC, Ales ,  SERSA, Gregor ,  NOVAKOVIC, Srdjan ,  POVSIC, Lucka ,  STALC, Anton

IPC分类号： C07K5/06 ,  C07D279/16 ,  C07D265/22 ,  A61K38/05

CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07D265/36 ,  C07D279/16