Patent ID: 7947692

Claim:
A compound of the formula wherein X is N, R 1 is C 1-4 alkoxy, R 2 is hydrogen, hydroxy, C, 1-2 alkoxy or C 1-2 alkylthio, R 3 is hydrogen or C 1-3 alkyl, R 4 is C 1-4 alkyl substituted with aryl, aroyl, aryloxy, arylsulfonyl, aralkylamino, or aroylamino, or R 3 and R 4 together with the urea nitrogen to which they are attached form a 5 to 6 membered heterocyclic ring of the formula wherein R 3 and R 4 are both CH 2 or one is CH 2 and the other is a methylene mono-substituted with lower alkyl, Ya is a saturated or partially unsaturated alkyl segment of 2 to 3 ring carbons which is substituted with an aromatic substituent selected from the group consisting of aryl, aralkyl, aralkyloxy, aroyl, aryloxy, arylsulfonyl, aralkylamino, aryloxyalkyl, aryloxyalkylamino and aroylamino, and Ya may additionally have 0, 1 or 2 non-aromatic substituents selected from hydroxy, amino, lower alkylamino, lower alkanoylamino, oxo, cyano, carboxy, hydroxyalkylamino, carbamoyl and lower alkylcarbamoyl, or R 3 and R 4 together with the urea nitrogen to which they are attached form a 5 to 6 membered heterocyclic ring of the formula wherein R 3 and R 4 are both CH 2 or one is CH 2 and the other is a methylene mono-substituted with lower alkyl, Yh is a saturated heteroalkyl segment of 2 to 3 ring atoms one of which is a heteroatom, and Yh is substituted with one aromatic group which in the case of a carbon ring atom is selected from the group consisting of aryl, aralkyl, aroyl, aryloxy, arylsulfonyl, aralkylamino, aryloxyalkyl, aryloxyalkylamino and aroylamino or, in the case of nitrogen, is selected from the group consisting of aryl, aralkyl, aroyl, arylhydroxymethylalkyl, arylcarboxymethylalkyl, arylalkoxymethylalkyl, arylsulfonyl, aryloxyalkyl, arylaminoalkyl and aroylaminoalkyl, or R 3 and R 4 together with the urea nitrogen to which they are attached form a piperidinyl or pyrrolidinyl which is benz-fused to unsubstituted or mono- di- or tri-substituted phenyl, or R 3 and R 4 together with the urea nitrogen to which they are attached form a piperidinyl which is spiro-fused to a 5 to 6 membered saturated heterocyclic ring containing from 1 or 2 heteroatoms which heterocyclic ring is bound or benz-fused to an unsubstituted or mono- di- or tri-substituted phenyl, and said heterocyclic ring may additionally have 0, 1 or 2 non-aromatic substituents selected from lower alkyl, oxo, acyl and lower alkylsulfonyl, or R 3 and R 4 together with the urea nitrogen to which they are attached form a 5-substituted 2,5-diaza-[2.2.1]-bicycloheptane or 5-substituted 2,5-diaza-[3.3.0]-bicyclooctane wherein the 5-substituent is selected from the group consisting of aryl, aralkyl, aryloxy, aralkylamino, aryloxyalkylamino, aroylamino, aroyl, arylsulfonyl, aryloxyalkyl, and arylhydroxymethylalkyl, arylcarboxymethylalkyl, arylalkoxymethylalkyl, or the pharmaceutically acceptable salts or esters thereof.