Patent ID: 6531475
Filing Date: 2003-03-11
Classification: A61P,C07D

Abstract:
A compound having the following structure: or a stereoisomer or pharmaceutically acceptable salt thereof,wherein:n is 1; A is nitrogen; C is nitrogen, carbon or CH; B is nitrogen or CR3; with the provisos that A, B and C are not all nitrogen; and either Aâ€”B or Bâ€”C is a double bond; X is nitrogen or CRq; Rq is hydrogen, alkyl or halo; Ar is substituted aryl or substituted heteroaryl; R is an optional substituent which, at each occurrence, is independently alkyl, alkylidenyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, wherein m is 0, 1, 2 or 3 and represents the number of R substituents; R1 is â€”C(H)0,1(R4)(R5) or â€”SO2R5; R2 is hydrogen, alkyl, haloalkyl or cyano R3 is hydrogen, alkyl or haloalkyl; R4 is hydrogen, oxo, alkyl, substituted alkyl,alkylidenyl or halo; and R5 is a radical of the formula â€”Yâ€”Zâ€”R6, wherein Y is an alkanediyl, substituted alkanediyl, or a direct bond, Z is NH, â€”N(R7), O, S, SO2, C(&boxH;O), C(&boxH;O)O, OC(&boxH;O), NHC(&boxH;O), C(&boxH;O)NH, NH(SO2), (SO2)NH, NR8C(&boxH;O)O, or a direct bond; R6 is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocyclealkyl, or substituted heterocyclealkyl; R7 and R8 are alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocyclealkyl, or substituted heterocyclealkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached form a heterocycle ring or substituted heterocycle ring; or R4 and R5 taken together with the carbon atom to which they are attached form cycloalkyl, substituted cycloalkyl, cycloalkylcycloalkyl, substituted cycloalkylcycloalkyl, cycloalkylaryl, substituted cycloalkylaryl, cycloalkylheterocycle, or substituted cycloalkylheterocycle; and wherein:heterocycle is, at each occurrence, independently heteroaryl, morpholinyl, pyrrolidinonyl, pyrrolidinyl, piperidinyl, hydantoinyl, valerolactamyl, oxiranyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydropyridinyl, tetrahydrothienyl, tetrahydropyrimidinyl or tetrahydrothiopyranyl; and heteroaryl is, at each occurrence, independently furyl, benzofuranyl, thiophenyl, benzothiophenyl, pyrrolyl, indolyl, isoindolyl, azaindolyl, pyridyl, quinolinyl, isoquinolinyl, oxazolyl, isooxazolyl, benzoxazolyl, pyrazolyl, imidazolyl, benzimidazolyl, thiazolyl, benzothiazolyl, isothiazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, cinnolinyl, phthalazinyl or quinazolinyl.