主权项 |
1. A compound of Formula I:or a pharmaceutically acceptable salt thereof, wherein:is: ring a is ring b is Ya1 is CH; Yb1 is N; Yb2 is CH; R1a is independently: H, halogen, or C1-C3-alkyl; R1 is
halogen;Si(CH3)3; orC1-C6-alkyl or C2-C6-alkenyl, optionally substituted with one to four substituents selected from the group consisting of: CN; OH; oxo; NH2; halogen; CO2Rc; CONH2; C1-C3-alkyl; C1-C3-haloalkyl; C1-C3-alkoxyl optionally substituted with OH or fluoro; aryl; Oaryl optionally substituted with halogen; or heterocyclyl; Heterocyclyl is a 4-, 5-, 6-, or 7-membered monocyclic ring or 8-, 9-, 10-, 11-membered bicyclic ring, or 13- or 14-membered tricyclic ring; the monocyclic, bicyclic or tricyclic ring can be saturated, unsaturated or aromatic, containing 1, 2, 3 or 4 heteroatoms selected from O, N or S, the point of attachment of the heterocyclyl can be on the carbon or nitrogen and the heterocyclyl may optionally be substituted with one to four substituents selected from CN; OH; oxo; NH2; halogen; CO(CH2)mCH3, optionally substituted with one or two substituents selected from OH and CO2Rc; C1-C3-alkyl; C2-C4-alkenyl; C1-C3-haloalkyl; C1-C3-alkoxyl optionally substituted with OH; aryl optionally substituted with one or two substituents selected from C1-C3-alkoxyl, halogen, or Oaryl; CH2aryl; OCH2aryl; Oaryl optionally substituted with one or two substituents selected from halogen; (CRaRb)nCO2Rc; (CRaRb)nCONRdRe; (CHRa)nNHCONRdRe; (CHRa)p—C(O)-heterocyclyl; and furyl; or alternatively, 2 substituents which are geminally substituted on a common ring carbon atom of said heterocyclyl may together with the common ring carbon atom form a C3-C6 spirocyclic ring; Aryl is a phenyl or napthyl ring, the aryl may optionally be substituted with one to four substituents selected from halogen, hydroxyl, C1-C3-alkyl, C1-C3-alkoxyl, Oaryl, (CRaRb)nCO2Rc; and (CRaRb)nCONRdRe; R2 is halogen, C1-C3-alkyl, or C1-C3-haloalkyl; R3 is halogen or C1-C3-fluoroalkyl; R4 is H, halogen, or C1-C3-alkyl; Ra and Rb are independently: H, OH, CN, CO2Rc, CONH2, NH2, cyclopropyl, C1-C3-haloalkyl, or C1-C3-alkyl optionally substituted with hydroxyl; Rc is: H; C1-4alkyl; -M-RCH; —(CH2)1-2—Rf; —(CH2)2—O—(CH2)2—Rf; —(CH2)2—Rg, —CHRhOCO2Ri, —CHRiRh, or —(CHRh)sOC(O)Ri; Rd and Re are independently: H, C1-C3-alkoxyl or C1-C6-alkyl, optionally substituted with one, two or three substituents CN; OH; oxo; NH2; halogen; CO2Rc; CONH2; C1-C3-alkoxyl, CO2Rc; aryl, carbocyclyl, or heterocyclyl; or cyclopropyl optionally substituted with phenyl; Rf is —OC(O)Rf1; Rf1 is C1-4alkyl; and Rg is OH, C1-4alkoxyl, NH2, NH(C1-4alkyl) or N(C1-4alkyl)2; Rh is H or C1-4alkyl; and Ri is C1-4alkyl, C3-6cycloalkyl, or phenyl; and, M is a bond or —(CH2)1-3—; RCH is (a) aryl or carbocycle optionally substituted with 1-3 groups independently selected from halo, C1-4alkyl, or C1-4alkoxy; or (b) a 5- to 6-membered monocyclic heterocycle containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein said heterocycle of RCH is optionally substituted with 1 or 2 groups independently selected from the group consisting of oxo and C1-3 alkyl; m is 0, 1, or 2; n is 0, 1, 2, 3 or 4; p is 0 or 1; and s is 1 or 2. |