Piperazine substituted aryl benzodiazepines and th

专利名称：Piperazine substituted aryl benzodiazepines

and their use as dopamine receptorantagonists for the treatment of psychoticdisorders

发明人：Thomas Daniel Aicher,Zhaogen Chen,Joseph

Herman Jr Krushinski,Yvan Le Huerou,MartaMaria Pineiro-Nunez,Kevin Michael

Ruley,John Mehnert Schaus,Dennis CharlesThompson,David Edward Tupper,YingChen,Margaret Mary Faul,Vincent PatrickRocco

申请号：US10505805申请日：20030317

公开号：US20050203296A1公开日：20050915

摘要：Described herein are antipyschotic compounds of formula (I) wherein, A is anoptionally benzo-fused five or six member aromatic ring having zero to three heteroatoms independently selected from N, O, and S; Alk is (C) alkylene optionally substitutedwith OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclicheteroaromatic, or bicyclic heteroaromatic; Ris hydrogen or (C) alkyl optionallysubstituted with OH, OR, or OCHCHOH, wherein Ris (C) alkyl; Ris H, (C) alkyl, halogen,fluorinated (C) alkyl, OR, SR, NO, CN, COR, CONRR, SONRR, NRR, NRCOR, NRSOR, oroptionally substituted phenyl, wherein Ris hydrogen, (C) alkyl, fluorinated (C) alkyl,

benzyl, or optionally substituted phenyl, Rand Rare independently hydrogen, (C) alkyl, oroptionally substituted phenyl; Z is one or two substituents independently selected fromhydrogen, halogen, (C) alkyl, fluorinated (C) alkyl, OR, SR, NO, CN, COR, CONRR, SONRR,NRSOR, NRR, or optionally substituted phenyl, wherein Ris hydrogen, (C) alkyl,fluorinated alkyl, benzyl, or optionally substituted phenyl, Rand Rare independentlyhydrogen, (C) alkyl, or optionally substituted phenyl; and salts, solvates, and crystalforms thereof. Also described are the use of the compounds of formula (a) as

antagonists of the dopamine Dreceptor and as agents for the treatment of psychosis andbipolar disorders, and pharmaceutical formulations of the compounds of formula (I). Alsodescribed are compounds useful as intermediates for the synthesis of the compounds offormula (I).

申请人：Thomas Daniel Aicher,Zhaogen Chen,Joseph Herman Jr Krushinski,Yvan LeHuerou,Marta Maria Pineiro-Nunez,Kevin Michael Ruley,John Mehnert Schaus,DennisCharles Thompson,David Edward Tupper,Ying Chen,Margaret Mary Faul,Vincent PatrickRocco

地址：Superior CO US,Noblesville IN US,Brownsburg IN US,Boulder CO US,BrownsburgIN US,Indianapolis IN US,Zionsville IN US,Indianapolis IN US,Reading GB,Thousand OaksCA US,Zionsville IN US,Indianapolis IN US

国籍：US,US,US,US,US,US,US,US,GB,US,US,US

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