Patent ID: 6514982
Filing Date: 2003-02-04
Classification: A61P,C07D

Abstract:
A compound having the following structure: or a stereoisomer or pharmaceutically acceptable salt thereof, wherein:n is 1; A is carbon or CH; B is nitrogen or CR3; C is nitrogen, carbon or CH; with the provisos that at least one of B and C is nitrogen, and either Aâ€”B or Bâ€”C is a double bond; X is nitrogen or CH; Ar is substituted aryl or substituted heteroaryl; R is an optional substituent which, at each occurrence, is independently alkyl, alkylidenyl, arylalkyl 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 or alkyl; R3 is hydrogen, alkyl or haloalkyl; R4 is hydrogen, keto, 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 the same or different and independently 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 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.