Patent ID: 8163756
Filing Date: 2012-04-24
Classification: A61P,C07D

Abstract:
1. A compound of the formula wherein A2 is a bicyclic fused heteroaryl selected from the group consisting of and wherein the symbol (**) is the point of attachment to the A1 ring of formula I; and wherein wherein each Z3 and Z5 may be independently attached to either of the rings making up the foregoing bicyclic structures; A1 is R2-substituted monocyclic 5-membered ring heteroaryl; D is a moiety of the formula wherein E1 is phenyl; wherein the symbol (***) is the point of attachment to the Y group of formula I; X1 is selected from the group consisting of O, S, NR3, —C(═O)—, —O—(CH and wherein the carbon atoms of —(CH X2 is a direct bond wherein E1 is directly linked to the Y group of formula I; and wherein the E2 ring is Z5- and/or Z6-substituted pyridinyl, pyrimidinyl; each Z2 is independently and individually selected from the group consisting of hydroxyl, hydroxyC1-C6alkyl, cyano, (R3) wherein the symbol (#) indicates the point of attachment of the Z2 moiety to the A2 ring of formula I; in the event that Z2 contains an alkyl or alkylene moiety, such moieties may be further substituted with one or more C1-C6alkyls; each Z3 is independently and individually selected from the group consisting of H, C1-C6alkyl, hydroxyl, hydroxyC1-C6alkyl, cyano, C1-C6alkoxy, C1-C6alkoxyC1-C6alkyl, halogen, CF wherein the symbol (#) indicates the point of attachment of the Z3 moiety to the A2 ring of formula I; in the event that Z3 contains an alkyl or alkylene moiety, such moieties may be further substituted with one or more C1-C6alkyls; each Z4 is a substituent attached to a ring nitrogen and is independently and individually selected from the group consisting of H, C1-C6alkyl, hydroxyC2-C6alkyl, C1-C6alkoxyC2-C6alkyl, (R4) wherein the symbol (#) indicates the point of attachment of the Z4 moiety to the A2 ring for formula I; in the event that Z4 contains an alkyl or alkylene moiety, such moieties may be further substituted with one or more C1-C6alkyls; each Z5 is independently and individually selected from the group consisting of H, C1-C6alkyl, branched C3-C7alkyl, halogen, fluoroalkyl, cyano, hydroxyl, alkoxy, oxo, aminocarbonyl, carbonylamino, aminosulfonyl, sulfonylamino, —N(R3) each Z6 is independently and individually selected from the group consisting of H, C1-C6alkyl, branched C3-C7alkyl, hydroxyl, C1-C6alkoxy, heteroaryl, heterocyclyl, heteroaryloxy, heterocyclyloxy, arylamino, heteroarylamino, and heterocyclylamino, (R3) each R2 is selected from the group consisting of monocyclic heteroaryl, C1-C6alkyl, branched C3-C7alkyl, R19 substituted C3-C8-carbocyclyl wherein R19 is H or C1-C6alkyl, C1-C6-fluoroalkyl wherein the alkyl group is partially or fully fluorinated, phenyl wherein the phenyl group is optionally substituted by one or more fluorine substituents and chlorine; each R3 is independently and individually selected from the group consisting of H, C1-C6alkyl, branched C3-C7alkyl, C3-C7-carbocyclyl, and phenyl; each R4 is selected from the group consisting of H, C1-C6alkyl, hydroxyC1-C6alkyl, dihydroxyC1-C6alkyl, C1-C6alkoxyC1-C6alkyl, branched C3-C7alkyl, branched hydroxyC1-C6 alkyl, branched C1-C6alkoxyC1-C6alkyl, branched dihydroxyC1-C6alkyl, carbocyclyl, hydroxyl substituted carbocyclyl, alkoxy substituted carbocyclyl, dihydroxy substituted carbocyclyl, phenyl, heteroaryl, heterocyclyl, phenylC1-C6alkyl, heteroarylC1-C6alkyl, and heterocyclylC1-C6alkyl; each R5 is independently and individually selected from the group consisting of and wherein the symbol (##) is the point of attachment to respective R8, R10, Z2, or Z3 moieties containing a R5 moiety; each R6 is independently and individually selected from the group consisting of C1-C6alkyl, branched C3-C7alkyl, carbocyclyl, phenyl, heteroaryl, and heterocyclyl; each R8 is independently and individually selected from the group consisting of C1-C6alkyl, branched C3-C7alkyl, fluoroalkyl wherein the alkyl moiety is partially or fully fluorinated, carbocyclyl, phenyl, phenyC1-C6lalkyl, heteroaryl, heteroarylC1-C6alkyl, heterocyclyl, heterocyclylC1-C6alkyl, OH, C1-C6alkoxy, N(R3) each R10 is independently and individually selected from the group consisting of CO each R13 is independently and individually selected from the group consisting of H, C1-C6alkyl, branched C3-C7alkyl, carbocyclyl, hydroxyC2-C7alkyl, C1-C6alkoxyC2-C7alkyl, (R4) V, V1, and V2 are each independently O or represent two hydrogens connected to the methylene carbon to which the V, V1, or V2 is attached; wherein two R3 or R4 moieties are independently and individually taken from the group consisting of C1-C6alkyl and branched C3-C6alkyl, hydroxyalkyl, and alkoxyalkyl and are attached to the same nitrogen atom, said moieties may cyclize to form a C3-C7 heterocyclyl ring; n is 0-4; p is 1-4; q is 2-6; r is 1; and v is 1 or 2; or a tautomer, diastereomer, geometric isomer, enantiomer, hydrate, or salt of any of the foregoing.