Piperazinilcarbonilquinolinas e - isoquinolinas, a process for their preparation, Pharmaceutical Preparations Containing them, their use for preparing a Drug, Selective antagonists of the 5-ht2a receptor comprising these compounds and the use of these antagonists in the

摘要

The e-isoquinolinas e-isoquinolinas formula (1),Among them, R1 is a phenyl or nafile radical substance, not replaced or replaced by R3 and / or R4, or a het1; R2 is a quinine or isoquinine radical substance, not replaced or replaced by R5 and / or R6; R3 and R4 are independent,H Hal A OA OH o CN R5 y R6 son cada uno independientemente entre sH. Cn, acilo, Hal, a, OA, O H, CONH2, conha o con2; het1 is an unsaturated, single ring or double ring acyclic ring system, which has not been replaced or replaced by Hal, a, OA or oh. It contains 1, 2 or 3 same or different heteroatoms, such as nitrogen, oxygen and sulfur; a is C1-6 tar; Alq is C1-6 tar; Hal This is f, Cl, Br or I; and acceptable salts and solutions for medicinal use. These compounds are selective antagonists of 5-htma receptor, which have clinical antipsychotic activity with little or no side effects. The process of compounding formula compound (1) is also introduced,Drug formulations containing these compounds, selective antagonism of 5-htma receptors, and use of these compounds as 5-htma antagonists for the treatment of psychosis, schizophrenia, depression, neurological disorders, and memory disorders, Parkinson's disease, lateral amoebae disease, Alzheimer's disease, Huntington's disease, appetite disorders, anorexia nervosa, premarital syndrome and / or obsessive-compulsive disorder have positive effects: