Eli Lilly and Company

Yvan LeHuerou

John M Schaus

Thomas Daniel Aicher

David Edward Tupper

Vincent Patrick Rocco

Patrick Gianpietro Spinazze

Zhaogen Chen

Marta Maria Pineiro-Nunez

Fionna Mitchell Martin

Kevin Michael Ruley

Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C) alkylene or hydroxy substituted (C) alkylene; X is oxygen or sulfur; Ris hydrogen, (C) fluroalkyl, (C) cycloalkyl, or (C) alkyl, wherein the (C) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCHCHOH, or &#x2014;CN; Ris H, halogen, (C) fluoroalkyl, (C) cycloalkyl, OR, SR, NO, CN, COR, C(O)OR, CONRR, NRR, SONRR, NRCOR, NRSOR, optionally substituted aromatic, or (C) alkyl, wherein (C) alkyl is unsubstituted or substituted with a hydroxy group; Ris hydrogen (C) fluoroalkyl, (C) alkenyl, Ar, (C)alkyl-Ar, or (C) alkyl wherein (C) alkyly is unsubstituted or substituted with a phenyl; Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic, Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Zand Zare independently selected from hydrogen, halogen, (C) alkyl, (C) fluoroalkyl, OR, SR, NO, CN, COR, CONRR, NRR, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I) 

Piperazine substituted aryl benzodiazepines

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Boulder, CO, United States of America

Yvan LeHuerou