Piperazine substituted aryl benzodiazepines and their use as...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C540S557000

Reexamination Certificate

active

10505805

ABSTRACT:
Described herein are antipyschotic compounds of formula (I)wherein,A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S;Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F;Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic;R1is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH,wherein R3is (C1-2) alkyl;R2is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl,whereinR4is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl,R5and R6are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl;Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R7, NR8R9, or optionally substituted phenyl,whereinR7is hydrogen, (C1-6) alkyl, fluorinated alkyl, or optionally substituted phenyl,R8and R9are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl;and salts, solvates, and crystal forms thereof.Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2receptor and as agents for the treatment of psychosis and bipolar disorder, and pharmaceutical formulations of the compounds of formula (I).

REFERENCES:
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patent: 4087421 (1978-05-01), Safir et al.
patent: 0 054 416 (1982-06-01), None
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patent: WO 96 18629 (1996-06-01), None
G.M. Singerman,The Chemistry of Pyrazine and its Derivatives. IX The Pyrazylethylation of Amines, J. Het. Chem., vol. 1, 1964, pp. 151-152.
J. K. Chakrabarti,Effects of Conformationally Restricted 4-Piperazinyl-10H- thienobenzodiazepine Neuroleptics on Central Dopaminergic and Cholinergic Systems, Journal of Medicinal Chemistry, Ameritcan Chemical Society, Washington, US, vol. 25, No. 10, Oct. 1, 1982, pp. 1133-1140.

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