Azatyrosine analogues

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546300, A61K 3144, C07D21365

Patent

active

058695079

ABSTRACT:
A novel anti-oncogenic azatyrosine analogues of formula (I) ##STR1## wherein R.sub.1 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, benzyl, or (C.sub.1-6 alkyl)carbonyl; R.sub.2 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, or C.sub.1-6 alkoxyl; and R.sub.3 is CONR.sub.4 R.sub.5, CONHNR.sub.4 R.sub.5, or COOR.sub.6, wherein each R.sub.4 and R.sub.5 independently is a hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, or C.sub.3-6 cycloalkyl, or R.sub.4 and R.sub.5 taken together with the nitrogen attached thereto form a C.sub.3-8 heterocyclic group; R.sub.6 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or benzyl. Also disclosed is a method of preparing such a novel anti-oncogenic azatyrosine analogues, as well as a pharmaceutical composition containing a compound of formula (I).

REFERENCES:
Cooper et al, "A concise synthesis of either, etc" CA 126:75208, 1996.

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