公开(公告)号：US5514654A

公开(公告)日：1996-05-07

申请号：US245810

申请日：1994-05-18

申请人： Slavko Pecar ,  Marija Sollner ,  Uros Urleb ,  Danijel Kikelj ,  Gasper Marc ,  Ales Krbavcic ,  Vlado Kotnik ,  Branka Wraber-Herzog ,  Sasa Simcic ,  Alojz Ihan ,  Lidija Klamfer ,  Lucka Povsic ,  Zdravko Kopitar ,  Anton Stalc

发明人： Slavko Pecar ,  Marija Sollner ,  Uros Urleb ,  Danijel Kikelj ,  Gasper Marc ,  Ales Krbavcic ,  Vlado Kotnik ,  Branka Wraber-Herzog ,  Sasa Simcic ,  Alojz Ihan ,  Lidija Klamfer ,  Lucka Povsic ,  Zdravko Kopitar ,  Anton Stalc

IPC分类号： A61K38/00 ,  A61P17/00 ,  A61P37/00 ,  C07K1/00 ,  C07K1/113 ,  C07K5/06 ,  C07K5/062 ,  A61K38/14 ,  C07K9/00 ,  C08L37/00

CPC分类号： C07K5/06026 ,  A61K38/00 ,  Y10S436/823 ,  Y10S436/826

摘要： N-acyldipeptides of formula I ##STR1## wherein R represents a rest of formula ##STR2## and R.sub.4, Y, m, n and Z have the meaning as defined in the description, R.sub.1 represents hydrogen, a 1-10 C. alkyl, an optionally substituted methyl or benzyl,R.sub.2 represents a --CO--A group,wherein A has the meanings as defined in the description,R.sub.3 represents a --(CH.sub.2).sub.p --CO--W group,wherein p and W have the meaning as defined in the description.

摘要翻译： 式I的N-酰基二肽其中R表示式的其余部分，且R 4，Y，m，n和Z具有如说明书中所定义的含义，R 1表示氢，1-10C烷基 ，任选取代的甲基或苄基，R 2表示-CO-A基团，其中A具有如说明书中定义的含义，R 3表示 - （CH 2）p -CO-W基团，其中p和W具有如 在说明书中定义。

公开(公告)号：US5231216A

公开(公告)日：1993-07-27

申请号：US743233

申请日：1991-08-19

申请人： Slavko Pecar ,  Danijel Kikelj ,  Uros Urleb ,  Marija Sollner ,  Gasper Marc ,  Ales Krbavcic ,  Vlado Kotnik ,  Branka Wraber-Herzog ,  Sasa Simcie ,  Alojz Than ,  Lidija Klamfer ,  Lucka Povsic ,  Zdravko Kopitar ,  Anton Stalc

发明人： Slavko Pecar ,  Danijel Kikelj ,  Uros Urleb ,  Marija Sollner ,  Gasper Marc ,  Ales Krbavcic ,  Vlado Kotnik ,  Branka Wraber-Herzog ,  Sasa Simcie ,  Alojz Than ,  Lidija Klamfer ,  Lucka Povsic ,  Zdravko Kopitar ,  Anton Stalc

IPC分类号： C07K1/113 ,  A61K38/00 ,  C07C231/02 ,  C07C233/23 ,  C07C237/22 ,  C07D265/36 ,  C07K1/02 ,  C07K1/16 ,  C07K5/06 ,  C07K5/062

CPC分类号： C07K5/06026 ,  C07C233/23 ,  C07D265/36 ,  A61K38/00 ,  C07C2101/14

摘要： There are described novel trans-2-acylaminocyclohexyloxyacyldipeptides of formula I ##STR1## wherein R.sub.1 represents --CO--R.sub.6, --SO.sub.2 --R.sub.7 or ##STR2## R.sub.6 is C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.18 alkoxy, R.sub.7 is C.sub.1 -C.sub.18 alkyl or an optionally substituted phenyl group,Y is .dbd.O, .dbd.S or .dbd.NH;R.sub.2 =R.sub.3 and represent --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 represents --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, a straight or branched chain C.sub.1 -C.sub.18 alkyl group or benzyl group;R.sub.5 represents --OR.sub.9 or --NHR.sub.9,and novel (1R,2R)- and (1S,2S)-trans-2-acylaminocyclohexyloxyacetyldipeptides of the formulas Ia and Ib ##STR3## wherein R.sub.1 is --CO--R.sub.6, R.sub.6 is C.sub.1 -C.sub.18 alkyl,R.sub.2 is --H,R.sub.3 is --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 is --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, C.sub.1 -C.sub.18 alkyl or benzyl,R.sub.5 is --OR.sub.9 or --NHR.sub.9Compounds of formula I, Ia and Ib and the pharmaceutically acceptable alkali salts thereof show immunomodulatory and antitumour activities and can be used in the preparation of medicaments.