PYRAZOLOPYRIMIDINES AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS Russian patent published in 1998 - IPC

FIELD: organic chemistry, heterocyclic compounds. SUBSTANCE: invention relates to pyrazolopyrimidines of the general formula (I) and their pharmaceutically acceptable salts where A - a group NR₁R₂ or CR11

R12R₁₁; R₁ - H or C₁-C₆-alkyl that can be free or substituted with some substituents, for example, OH, F, Cl and other, or C₂-C₆--alkenyl, or C₂-C₆--alkynyl; R₂ is C₁-C₆-alkyl that can be free or substituted with some substituents, for example, OH, C₁-C₆-alkoxy and other; or C₂-C₆--alkenyl or C₂-C₆--alkynyl or furanyl; ((C₁-C₄--alkylene)-phenyl that can be substituted with 1 to 3 substituents: Cl, F, C₁-C₄--alkyl and a single substituent: C₁-C₆--alkoxy, CF₃, NO₂, NH₂; or ((C₁-C₄)-alkylene)-heteryl where heteryl - thienyl possibly substituted with Cl, benzothienyl, pyridyl, quinolinyl, furanyl, benzofuranyl, thiazolyl, benzothiazolyl, pyrrolyl, pyrrolidinyl, 1-benzylpiperidinyl, tetrahydropyranyl; or ((C₁-C₄--alkylene)-cyclopropyl; or NR₁R₂ form heteryl taken from a group involving pyrrolinyl possibly substituted with benzyl, pyrrolidinyl possibly substituted with benzyl of OH, pyrrolyl, imidazolyl, thiazolidinyl, thiomorpholinyl; R11 - hydrogen, C₁-C₆--alkyl; R12 is C₁-C₆--alkyl; R₃ - hydrogen, C₁-C₆--alkyl, O-((C₁-C₆--alkyl), S-((C₁-C₄--alkyl); R₄ is C₁-C₆--alkyl or S-(O)_n(C₁-C₆)-alkyl where n = 0-2; R₅ is 2,4,6-substituted phenyl with Cl, C₁-C₆-alkyl, CF₃; R_11/ - H, OH, or COO-((C₁-C₂-alkyl) at condition that a group CR11R12R₁₁ is not alkyl with direct chain; and when R₃ is H then R₄ is not C₁-C₆-alkyl. Synthesized compounds show antagonistic activity with respect to corticotropin releasing factor and can be used for treatment of patients with stress and other sicknesses. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 7 cl, 4 dwg, 5 tbl, 24 ex