4-phenyl-4-heteroarylpiperidine derivatives

A compound of the formula

• wherein X and Y are nitrogen with the proviso that the ring containing X and Y must be aromatic;
• ( )n means (CH2)n and n is zero or one;
• R1 is hydrogen, (C0-C8)alkoxy-(C0-C8)alkyl-, wherein the total number of carbon atoms in said (C0-C8)alkoxy-(C0-C8)alkyl- is eight or less, aryl, aryl-(C1-C8)alkyl-, heteroaryl, heteroaryl-(C1-C8)alkyl-, heterocyclic, heterocyclic-(C1-C8)alkyl, (C3-C7)cycloalkyl-, or (C3-C7)cycloalkyl-(C1-C8)alkyl, wherein said aryl and the aryl moiety of said aryl-(C1-C8)alkyl- are selected, independently, from phenyl and naphthyl, and wherein said heteroaryl and the heteroaryl moiety of said heteroaryl-(C1-C8)alkyl- are selected, independently, from pyrazinyl, benzofuranyl, quinolyl, isoquinolyl, benzothienyl, isobenzoflryl, pyrazolyl, indolyl, isoindolyl, benzimidazolyl, purinyl, carbazolyl, 1,2,5-thiadiazolyl, quinazolinyl, pyridazinyl, cinnolinyl, phthalazinyl, quinoxalinyl, xanthinyl, hypoxanthinyl, pteridinyl, 5-azacytidinyl, 5-azauracilyl, triazolopyridinyl, imidazolopyridinyl, pyrrolopyrimidinyl, pyrazolopyrimidinyl, oxazolyl, oxadiazolyl, isoxazolyl, thiazolyl, isothiazolyl, furanyl, pyrrolyl, tetrazolyl, triazolyl, thienyl, imidazolyl, pyridinyl, and pyrimidinyl;
• and wherein said heterocyclic and the heterocyclic moiety of said heterocyclic-(C1-C8)alkyl- are selected from saturated or unsaturated nonaromatic monocyclic or bicyclic ring systems, wherein said monocyclic ring systems contain from four to seven ring carbon atoms, from one to three of which may optionally be replaced with O, N or S, and wherein said bicyclic ring systems contain from seven to twelve ring carbon atoms, from one to four of which may optionally be replaced with O, N or S;
• and wherein any of the aryl, heteroaryl or heterocyclic moieties of R1 may optionally be substituted with from one to three substituents, preferably with one or two substituents, independently selected from halo, (C1-C6)alkyl optionally substituted with from one to seven fluorine atoms, phenyl, benzyl, hydroxy, acetyl, amino, cyano, nitro, (C1-C6)alkoxy, (C1-C6)akylamino and 2amino, and wherein any of the alkyl moieties in R1 may optionally be substituted with from one to seven fluorine atoms;
• R2 is hydrogen, aryl, halo, heteroaryl, heterocyclic, SO2R4, COR4, CONR5R6, COOR4, or C(OH)R5R6 wherein each of R4, R5 and R6 is defined, independently, as R1 is defined above, or R5 and R6, together with the carbon or nitrogen to which they are both attached, form a three to seven membered saturated ring containing from zero to three heterocarbons selected, independently, from O, N and S, and wherein said aryl, heteroaryl, and heterocyclic are defined as such terms are defined above in the definition of R1, and wherein any of the aryl, heteroaryl and heterocyclic moieties of R2 may optionally be substituted with from one to three substituents, independently selected from halo, (C1-C6)alkyl optionally substituted with from one to seven fluorine atoms, phenyl, benzyl, hydroxy, acetyl, amino, cyano, nitro, (C1-C6)alkoxy optionally substituted with from one to seven fluorine atoms, (C1-C6)alkylamino and 2amino;
• R3 is hydroxy, —(C1-C6)alkyl-OH, —(C1-C6)alkyl-(C1-C6)alkoxy, NHSO2R7, C(OH)R7R8, halo, or heteroaryl as defined for R1 above or CONHR7, wherein R7 and R8 are the same or different and are selected from hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy and (C1-C4)alkoxy-(C1-C4)alkyl having in said (C1-C4)alkoxy-(C1-C4)alkyl a total of 4 or less carbon atoms, and wherein any of the alkyl moieties of R7 and R8 may optionally be substituted with from one to seven fluorine atoms;
• and
• Z1 is hydrogen, halo or (C1-C5)alkyl;
• with the proviso that there are no two adjacent ring oxygen atoms and no ring oxygen atom adjacent to either a ring nitrogen atom or a ring sulfur atom in any of the heterocyclic or heteroaryl moieties of formula I;
• and the pharmaceutically acceptable salts of such compounds.