FIELD: organic chemistry, medicine. SUBSTANCE: invention describes new derivatives of pyridopyrimidine of the formula (A) where means -(CH2)m- (m = 0, 1 or 2); n = 1-3; R1 means hydrogen atom; C1-6-alkyl-group that can be optionally substituted with one of substituents taken from quinolyl or indolyl; phenyl group that can be optionally substituted with at least one C1-6-alkoxy-group; or phenyl-C1-3-alkyl-group that can be optionally substituted with at least one substituent taken from C1-6-alkoxy- and C1-6-alkylthio-group; R2 means hydrogen atom or C1-6-alkyl-group; R3 means phenyl or naphthyl group that can be optionally substituted with at least one substituent taken from C1-6-alkyl, C1-6-alkoxy-, C1-6-alkylenedioxy-group, halogen atom, nitro-, cyano-group, phenyl, C3-7-cycloalkyl; pyridyl that can be optionally substituted with C1-6-alkyl; thienyl that can be optionally substituted with C1-6-alkyl; quinolyl that can be optionally substituted with oxo-group or hydroxyl-group; quinolonyl; benzofuryl or benzothienyl that can be optionally substituted with C1-6-alkyl; R4 means a group -COO-COOR6 where R6 means hydrogen atom; C1-6-alkyl group optionally substituted with at least one substituent taken from C3-7-cycloalkyl-group, quinolyl-group, carboxyl-group, cyano- and phenyl-group; or C3-7-cycloalkyl; or a group -COA-R7R8 where R7 and R8 mean independently hydrogen atom or C1-6-alkyl group; R5 means hydrogen atom; C1-6-alkyl group or phenyl-group that can be optionally substituted with C1-6-alkylenedioxy-group, or its salt. Invention describes also a method of synthesis of compounds of the formula (A), pharmaceutical compositions based on compound of the formula (A) and a method of an antagonistic effect on endothelial receptors in treatment of patients with renal failure, myocardium infarctum, hypertension, cerebral infarctum, angina pectoris, arteriosclerosis, hepatopathy, pulmonary hypertension, bronchial asthma, organohypofunction caused by operation or organ transplantation, New compounds of the formula (A) and pharmocompositions based on said can be used in medicine. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 20 cl, 44 tbl, 46 ex
Authors
Dates
1999-03-20—Published
1993-12-28—Filed