发明授权
- 专利标题: Trans-2-acylaminocyclohexyloxyacyldipeptides in the form of mixtures of diastereoisomers thereof and in the form of pure diasteredisomers, process for the preparation thereof and pharmaceutical compositions containing the same
- 专利标题(中): 转化-2-氨基甲酰氧基环己基二甲氧基硅烷在其二甲醚混合物形式及其制备方法中的用途及其含有药物组合物的方法
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申请号: US743233申请日: 1991-08-19
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公开(公告)号: US5231216A公开(公告)日: 1993-07-27
- 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
- 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
- 申请人地址: YUX Ljubljana
- 专利权人: Univerza Edvarda Kardelja v Ljubljana
- 当前专利权人: Univerza Edvarda Kardelja v Ljubljana
- 当前专利权人地址: YUX Ljubljana
- 优先权: YUX1546/90 19900809
- 主分类号: C07K1/113
- IPC分类号: C07K1/113 ; A61K38/00 ; C07C231/02 ; C07C233/23 ; C07C237/22 ; C07D265/36 ; C07K1/02 ; C07K1/16 ; C07K5/06 ; C07K5/062
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.
公开/授权文献
- US4604239A Antibiotics 公开/授权日:1986-08-05