主权项 |
1. A compound of Formula (I) or (II): wherein: ring A is a 5- or 6-membered heteroaryl group; the dashed lines are optional double bonds. X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; R1 is —R5R6, where R5 is a covalent bond, C1 to C3 alkyl or a linker group, for example, sulfonamide, ether, ester, amine, amide, etc., and R6 is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcycloalkyl, alkylheterocycloalkyl, alkylaryl, alkylheteroaryl or alkyl, and wherein R6 is optionally substituted one, two or three times with independently selected polar groups; R1 is —R5R6A, where R5 is a covalent bond, C1 to C3 alkyl or a linker group, for example, sulfonamide, ether, ester, amine, amide, etc., and R6A is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcycloalkyl, alkylheterocycloalkyl, alkylaryl, alkylheteroaryl or alkyl, and wherein R6A is optionally substituted one, two or three times with independently selected polar groups selected from the group consisting of halo, hydroxy, alkoxy, carboxy, nitro, cyano, amino primary, secondary and tertiary; amido, ureido, sulfinyl, sulfhydryl, silyl, S-sulfonamido, N-sulfonamido, C-carboxy, O-carboxy, C-amido, N-amido, sulfonyl, N-tert-butoxycarbonyl, phosphono, morpholino, piperazinyl, tetrazolo, alcohol, thiol, polyethylene glycol, polyol including sugar, aminosugar, uronic acid; carboxamide, hydrazide, N-hydroxycarboxamide, urea, metal chelates including macrocyclic ligand or crown ether metal chelates; the polar group can be an ionic group for example, anionic and cationic groups; for example, carboxylate, sulfonate, phosphate, amine, N-oxide, and ammonium including quaternized heterocyclic amines such as imidazolium and pyridinium groups; uronic acids, carboxylic acid, sulfonic acid, amine, and moieties such as guanidinium, phosphoric acid, phosphoric acid, phosphatidyl choline, phosphonium, borate, and sulfate; R2 is —R7′R8′, where R7′ is a covalent bond or C1 to C3 alkyl and R8′ is cycloalkyl, heterocycloalkyl, aryl, heteroaryl or alkyl, and wherein R8 is optionally substituted one, two or three times with independently selected polar groups; R3 is hydrogen; R4 is H, loweralkyl, halo, or loweralkoxy; R7 is alkyl, arylalkyl, cycloalkylalkyl, alkylheterocycloalkyl, heteroarylalkyl, and alkoxyalkyl, each of which is optionally substituted one, two or three times with independently selected polar groups; R8 is alkyl, arylalkyl, cycloalkylalkyl, alkylheterocycloalkyl, heteroarylalkyl, and alkoxyalkyl, preferably alkyl or cycloalkyl, each of which is optionally substituted one, two or three times with independently selected polar groups; or a pharmaceutically acceptable composition, salt, isotopic analog, or prodrug thereof. |