181 results about "D2 dopamine receptors" patented technology

Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and / or Ib:In certain embodiments, the heteroaryl amide analogues are agonists and / or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.

Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.

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;R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH,wherein R3 is (C1-2) alkyl;R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl,whereinR4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl,R5 and R6 are 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,whereinR7 is hydrogen, (C1-6) alkyl, fluorinated alkyl, or optionally substituted phenyl,R8 and R9 are 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 D2 receptor and as agents for the treatment of psychosis and bipolar disorder, and pharmaceutical formulations of the compounds of formula (I).