公开(公告)号：US20030120070A1

公开(公告)日：2003-06-26

申请号：US10334481

申请日：2002-12-30

Applicant: H. Lundbeck A/S

Inventor： Jens Kristian Perregaard ,  Ejner Kund Moltzen

IPC: A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

CPC classification number: C07D401/06 ,  C07D233/32 ,  C07D233/36

Abstract: The present invention relates to a series of 4-phenylpiperazines of formula (I) 1 wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene; R1 is a C3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R2-R5 are optional substituents; R9 and R10 are hydrogen, alkyl or together form an ethylene or propylene bridge, W is O or S; V is O, S, CR6R7, or NR8 wherein R6, R7, and R8 are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R6 and R7 constitute a 3-7 membered spiro ring; Z isnull(CH2)mnull; m being 2 or 3 or Z is nullCHnullCHnull; which show effects on central serotonin 5-HT1A and dopamine D2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders, in particular psychosis.

Abstract translation: 本发明涉及一系列式（I）的4-苯基哌嗪，其中A是亚烷基，亚烯基，亚炔基和C 3-7亚环烷基; R 1是C 3-10烷基，烯基或炔基，环烷基（烯）基，环烷基（烯）基 - 烯（烯/炔）基，三氟甲磺酰基或烷基磺酰基，R 2 -R 5是任选的取代基; R 9和R 10是氢，烷基或一起形成乙烯或丙烯桥，W是O或S; V是O，S，CR 6 R 7或NR 8，其中R 6，R 7和R 8是氢或烷基，烯基，环烷基，环烷基烷基，任选取代的芳烷基或芳基，或R 6和R 7构成3-7元螺环; Z是 - （CH 2）m - ; m为2或3或Z为-CH = CH-; 其显示对中枢5-羟色胺5-HT1A和多巴胺D2受体的作用。 因此，新化合物可用于治疗某些精神病和神经障碍，特别是精神病。