Amide or urea containing benzothiazole inhibitors of endothelial lipase

摘要

The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.;

主权项

1. A compound of Formula (I):or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein:
R1 is independently selected from the group consisting of: phenyl and a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-4 heteroatoms selected from N, NRc, O, and S(O)p; wherein each phenyl and heteroaryl are substituted with 0-3 Ra; R2 is, independently at each occurrence, selected from the group consisting of: halogen, OH, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, CN, NH2, NO2, NH(C1-4 alkyl), N(C1-4 alkyl)2, CO2H, CO2(C1-4 alkyl), and CONH2; R3 is independently selected from the group consisting of: C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy, —(CH2)mCHF2, —(CH2)mCF3, —(CH2)m—(C3-6 carbocycle substituted with 0-3 Rb), —(CH2)m-(pyridyl substituted with 0-2 Rb), —NH(C1-4 alkyl), —NHCH2CO2(C1-4 alkyl), —NH(4-halo-Ph), 4-CF3-Ph, —NHBn, and R4 independently selected from the group consisting of: R5 is independently selected from the group consisting of: NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, NHCO(C1-4 alkyl), NHCO2(C1-4 alkyl), NHCONH(C1-4 alkyl), SO2OH, SO2(4-halo-Ph), SO2NH2, SO2NHCH2CF3, SO2NHPh, NHSO2NH2, NHSO2(C1-4 alkyl), SO2NHSO2(CH2)2-3CF3, N(C1-4 alkyl)SO2NH2, N(CO2C1-4 alkyl)SO2(C1-4 alkyl), and R6 is independently selected from the group consisting of: Ra is, independently at each occurrence, selected from the group consisting of: halogen, C1-6 alkyl substituted with 0-1 OH, C1-4 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, OH, CN, NO2, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, CO2H, CO2(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), SO2NH2, SO2N(C1-4 alkyl)2, CONH(CH2)1-3CF3, pyrazolyl, Rb is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, OH, CN, NH2, NO2, NH(C1-4 alkyl), N(C1-4 allyl)2, CO2H, CO2(C1-4 alkyl), SO2(C1-4 alkyl), SO2NH2, CONH2, and CONH(C1-4 alkyl); Rc is, independently at each occurrence, selected from the group consisting of: H, C1-6 alkyl, CO(C1-4 alkyl), CO2(C1-4 alkyl), COBn, CO2Bn,  pyrimidinyl and —(CH2)t—(C3-6 carbocycle substituted with 0-2 Re); Re is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, and C1-4 haloalkoxy; m and t are, independently at each occurrence, selected from 0, 1, 2, and 3; and p is, independently at each occurrence, selected from 0, 1, and 2; and s is, independently at each occurrence, selected from 1, 2, and 3.