Aryl piperidinones dihidropiridinonas and as inhibitors MGAT2

2012 
A compound of Formula (I): Formula ** ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt or solvate thereof, wherein: denotes a single or double bond; x and y may both be a single bond; when x is a double bond, then is a simple and R4 and R16 are absent bond; when y is a double bond, then X is a single bond and R5 and R16 are absent; R1 is independently selected from the group consisting of: -CONH (C4-18 alkyl), -CONH-C2-8 haloalkyl, -CONH (CH2) 1-8Ph, C2-8 alkyl -CONHCH2CO, - (CH2) m - (C3-10 carbocycle substituted with 0-2 Rb and 0-2 Rg), - (CH2) m- (5- to 6-membered comprising: carbon atoms and 1-4 heteroatoms selected from N, NR e, O and S, wherein said heteroaryl is substituted with 0-1 Rb and 0-2 Rg) and a hydrocarbon chain substituted with 0-3 Ra C1-12; wherein said hydrocarbon chain may be straight or branched, saturated or unsaturated; R2 is independently selected from the group consisting of: C1-4 alkyl, C3-4 cycloalkyl and C1-4 haloalkyl; R3 is independently selected from the group consisting of: H, F, Cl, CN and C1-4 alkyl; R4 and R5 are independently selected from the group consisting of: H, F, Cl and C1-4 alkyl; when x is a single bond, R3 and R4 may combine with the carbon atom to which they are attached to form a carbocycle of 3 to 6 members; R6 is independently selected from the group consisting of: H, halo, C1-4alkyl, NO2, Rc, alkyl - (CH2) n- (X) t- (CH2) mRC, NH2, -CONH (C1-6 alkyl) , -NHCOX1SO2Rj, -NHCOCH2PO (OEt) 2, -NHCOCORj, - NHCOCH (OH) Rj, -NHCOCH2CORj, -NHCONHRj and -OCONRfRj; X is independently selected from the group consisting of: O, S, NH, CONH and NHCO; X1 is independently a hydrocarbon chain optionally substituted with C1-4 cycloalkyl C1-4 or C3-4 alkyl; when y is a single bond, R5 and R6 may combine with the carbon atom to which they are attached to form a carbocycle of 3 to 6 members; R11, R12, R13, R14 and R15 are independently selected from the group consisting of: H, halo, C1-4 alkyl substituted with 0-2 Ri, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, - (CH2) m-C3-6cycloalkyl, CN, NRfRj, ORj, SRJ, NHCO 2 (C1-4 alkyl), NHSO2 (C1-4 alkyl) and a heterocycle of 4 to 6 membered heterocycle comprising: carbon atoms and 1- 4 heteroatoms selected from N, NR e, O and S; alternatively, R11 and R12, together with the carbon atoms to which they are attached, combine to form a carbocyclic ring of 5 to 6 membered heterocyclic ring or 5 to 6 members comprising carbon atoms and 1-3 heteroatoms selected from N, NR e, O and S; alternatively, R12 and R13, together with the carbon atoms to which they are attached, combine to form a carbocyclic ring of 5 to 6 membered heterocyclic ring or 5 to 6 members comprising carbon atoms and 1-3 heteroatoms selected from N, NR e, O and S; R16 is independently selected from the group consisting of: H and C1-4 alkyl; Ra, at each occurrence, is independently selected from the group consisting of: halo, OH, C1- 6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, N (C1-4alkyl) 2, - (CH2) n - (X) t- (CH2) mRC and - (CH2) n- (CH2O) m- (CH2) NRF; Rb, at each occurrence, is independently selected from the group consisting of: halo, OH, C1-10 alkoxy C1-10 alkyl, C1-10 haloalkyl, C1-10 haloalkoxy, C1-10 alkylthio, C1-10 haloalkylthio , N (C1-4alkyl) 2, -CONH (CH2) 4-20H, -O (CH2) sO (C1-6 alkyl) Rc, - (CH2) n- (X) t- (CH2) mRC and - (CH2) n- (CH2O) m- (CH2) NRF; Rc, at each occurrence, is independently selected from the group consisting of: C3-6 cycloalkyl substituted with 0-2 Rd, C3-6 cycloalkenyl substituted with 0-2 Rd, - (CH2) m- (phenyl substituted with 0 -3 Rd) and a 5- to 6-membered comprising: carbon atoms and 1-4 heteroatoms selected from N, NR e, O and S; wherein said heterocycle is substituted with 0-2 Rd; Rd, at each occurrence, is independently selected from the group consisting of: halo, OH, CN, NO2, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, tetrazolyl, phenyl OBn and substituted with 0-2 RH; Re, at each occurrence, is independently selected from the group consisting of: H, C1-8 alkyl, C1-8 haloalkyl, benzyl optionally substituted with C1-4 alkoxy, CO (C1-4 alkyl) and COBn; Rf, at each occurrence, is independently selected from the group consisting of: H and C1-4 alkyl; Rg, Rh and Ri, each occurrence, are independently selected from the group consisting of: halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl and C1-4 haloalkoxy; Rj, at each occurrence, is independently selected from the group consisting of: C1-4 alkyl, C3-4 cycloalkyl and phenyl; n, at each occurrence, it is independently 0 or 1; m, at each occurrence, is independently 0, 1, 2, 3 or 4; s, at each occurrence, is independently 1, 2 or 3; t, at each occurrence, is independently 0 or 1; provided that the following compound is excluded: ** ** Formula
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