4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophene-methyl) piperazines
申请人:H. Lundbeck A/S
公开号:US06218394B1
公开(公告)日:2001-04-17
4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I)
wherein one of X and Y is CH2, and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute a 3-7-membered ring; R8 is hydrogen or alkyl; have effects at central serotonergic receptors and are therefore useful in the treatment of certain psychic and neurologic disorders.
通用式(I)的4-芳基-1-(茚甲基、二氢苯并呋喃甲基或二氢苯并噻吩甲基)哌啶、-四氢吡啶或-哌嗪化合物,其中X和Y中的一个是CH2,另一个是CH2、O或S;Z是N、C、CH或COH;Ar是可选择取代的芳基基团;R1是氢、烷基、环烷基、环烷基烷基、芳基、芳基烷基、酰基、硫酰基、烷基磺酰基、三氟甲基磺酰基、芳基磺酰基、一个基团R9VCO—其中V是O或S,R9是烷基或芳基,或一个基团R10R11NCO—或R10R11NCS—其中R10和R11是氢、烷基或芳基,或R10和R11连接形成环;R2是氢、烷基、环烷基或环烷基烷基;或R1和R2连接形成环;R3-R5是氢、卤素、烷基、烷基羰基、苯基羰基、烷氧基、烷硫基、羟基、烷基磺酰基、氰基、三氟甲基、环烷基、环烷基烷基或硝基;R6和R7是氢或烷基,或它们连接形成一个3-7成员环;R8是氢或烷基;在中枢5-羟色胺受体具有作用,因此在治疗某些精神和神经疾病方面是有用的。