| 摘要 |
Piperidine and piperazine derivatives (I), and salts and solvates of (I), some of which are new, are used as medicaments with a 5-HT2A receptor antagonist effect. Use of piperidine and piperazine derivatives of formula (I), and salts and solvates of (I), as medicaments with a 5-HT2A receptor antagonist effect, is new: [Image] R1>, R2>Het1>, or phenyl or naphthyl (both optionally substituted by R3>, R4> and/or R5>); R3>, R4>, R5>halo, A, OA, OH, CN, NH2, NHA, NA2, NHAc, Ac, SA, SOA, SO2A or phenyl; X : CH or N; Y : SO2 (when X is N), or S, SO or SO2 (when X is CH); A : 1-6C alkyl; Alk : 1-6C alkylene; halo : F, Cl, Br or I; Het1>an unsaturated heterocyclic ring system which (i) contains 1-3 N, O or S atoms and (ii) is optionally substituted by 1-3 halo, A, CN, OA or OH; and Ac : acyl. An independent claim is included for compounds of formula (I) in which Het1> is not 2,1,3-benzoxadiazolyl or 2,1,3-benzothiazolyl. - ACTIVITY : Cerebroprotective; neuroprotective; anxiolytic; antidepressant; antipsychotic; anabolic; hypotensive; antispasmodic; antiparkinsonian; nootropic; antimigraine; antiaddictive; ophthalmological. - MECHANISM OF ACTION : Serotonin 5-HT2A receptor antagonist. |
