SUBSTITUTED PIPERAZINES, (1,4)-DIAZEPINES AND 2,5- DIAZABICYCLO[2,2,1]HEPTANES AS H1- AND/OR H3-HISTAMINE ANTAGONISTS OR REVERSE H3-HISTAMINE ANTAGONISTS

摘要

FIELD: chemistry. ^ SUBSTANCE: invention relates to the novel piperazine derivatives with the general formula where R1 is benzofuranyl, inolyl or quinolinyl possibly substituted with one or more halogens; trifluoromethyl; -C1-6alkyl, possibly substituted with COOR15; -C1-6alkoxi, possibly substituted with COOR15; C1-6alkenyl; NR15R16; or C1-6alkylthio groups; and where R15 and R16 independently represent hydrogen, C1-6alkyl or C3-8cycloalkyl or can be condensed together with forming the 5-7-membered non-aromatic heterocyclic ring, possibly discontinued by the O or S atoms and possibly substituted with halogen, C1-6alkyl or -C1-6alkylC1-6alkoxi group; Z is the bind or CO; m is 0 or 2; n is 0; r is 0; p is 1; R3 is -(CH2)q-NR11R12, where q is 3; and NR11 R12 is a pirrolidinyl, piperidinyl, azepanyl or azokanyl, possibly substituted with one or more than one C1-6alkyl group; or their pharmaceutically acceptable salts. The pharmaceutical compositions based on the compounds I and their application in production of the pharmaceuticals, are described. ^ EFFECT: compounds can be used in treatment of neurodegenerative disorders including Alzheimer's disease. ^ 10 cl, 503 ex