Pyridyl derivatives and their use as mGlu5 antagonists

Details Pyridyl derivatives and their use as mGlu5 antagonists Pyridyl derivatives and their use as mGlu5 antagonists

2011-03-29

2011-03-29

Andres, Janet L (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S348000, C546S287000, C546S315000, C546S345000

Reexamination Certificate

active

07915424

ABSTRACT:
The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor. As such the compounds may be useful for treatment or prevention of disorders remedied by antagonism of the mGlu5 receptor, wherein Ar is phenyl or napthyl each of which may be substituted by one or more C1-C4alkyl, C1-C4alkoxy, C1-C5acyl, halo, amino, nitro, cyano, hydroxy, C1-C5acylamino, C1-C4alkylsulfonylamino, mono-, di- or trifluorinated C1-C3alkyl, substituents which may be the same or different and may bear a CONH2, CONHCH3, CON(CH3)2, CO2H, CO2CH3, OCF3, CH2NHCOCH3, CH2NH2, CH2N(CH3)2, CH2CN, CH2OH, CH2NHSO2CH3, CH2N(CH3)(CH2)2CN, CH2N(CH3)CH(CH3)2, CH2NHCH(CH3)2, CH2NH(CH2)2CH3, CH2NHCO2R4, CH2NHCH2CH3, CH2NHCH3NHCOC(CH3)2, or N(S(O)2CH3)2substituent; R1is hydrogen, halo, R4, CN, C(NOH)R3, C(NO—R4)R3, (CH)2CO2R4, (CH2)nOR3, COR3, CF3, SR4, S(O)R4, S(O)2R4, COCH2CO2R3, NHSO2R4, NHCOR3, C(NOR3)NH2, CH2OCOR3, (CH2)nNH2, CON(CH3)2(CH2)nNHCO2R4, CO2R3, CONH2, CSNH2, C(NH)NHOR3, (CH2)nN(CH3)2, or CONHNHCOR3; R2is 1,2-ethenediyl or 1,2-ethynediyl; R3is hydrogen or C1-C4alkyl; R4is C1-C4alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof, or an N-oxide thereof.

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