FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of N-(3-piperidinylcarbonyl)-beta-alanine of the general formula (I) where R1 means piperidinyl that can has amino-protective group; R2 means carboxy- or esterified carboxy-group; A1 means C1-C6-alkylene, C1-C6-alkanyl-idene; A2 means C1-C6-alkylene; A3 means C1-C6-alkylene that can has a single suitable substituent taken among the group including C1-C6-alkyl, C2-C6-alkenyl, C1-C6-alkynyl, cyano-, amino- -group, protected aminoacyl-group, C1-C6-alkylsulfonylamino- -C1-C6-alkyl, phenyl, phenyl-C1-C6-alkynyl, phenyl-C1-C6alkyl substituted with from 1 to 4 C1-C6-alkoxy-groups, halogen-C1-C6- alkyl, C1-C6-alkylenedioxy, C1-C6-alkyl substituted with unsaturated condensed 5-6-membered heterocyclic group containing from 1 to 4 nitrogen atoms, phenylsulfonyl-C1-C6- -alkyl and unsaturated 5-6-membered heterocyclic group containing from 1 to 4 nitrogen atoms;
is the group
where
means piperidyl, tetrahydroquinolyl, pyrrolidinyl or morpholinyl; X means O or NH; Y means NH; Z means the group (a)
where R3 is hydrogen atom or C1-C6-alkyl; l = 0 or 1; m = 0 or 1; n = 0 or 1, or its pharmaceutically acceptable salt. Novel compounds are antagonists of glyco-protein IIb/IIIa, inhibitors of platelet aggregation and inhibitors of binding fibrinogen with platelets. Invention describes also method of synthesis of proposed compounds, pharmaceutical preparation containing this compound and method of prophylaxis and/or treatment of patients or animals with diseases given in the description of invention. EFFECT: new compounds indicated above, improved method of synthesis, valuable medicinal properties. 32 cl, 1 tbl, 44 ex
Authors
Dates
2000-12-27—Published
1994-09-21—Filed