主权项 |
1. A compound of Formula Ior a pharmaceutically acceptable salt thereof, wherein:
R is selected from the group consisting of: H, alkyl and hydroxylalkyl; R1 is selected from the group consisting of heterocyclyl, heterocycloalkenyl, aryl and heteroaryl, wherein when said heterocyclyl, heterocycloalkenyl, aryl or heteroaryl has two substituents on adjacent ring atoms, said substituents together with the ring atoms to which they are attached, optionally form a five- or six-membered heterocyclyl, aryl or heteroaryl; R2 is H or alkyl; R3′ is selected from the group consisting of: each R3 independently is selected from the group consisting of —C(═O)—O-alkyl, halo, haloalkyl, —OSi(alkyl)3, —C(═O)—OH, —C(O)NRBRC—C(O)NH-alkyl-NRDRE, —C(O)NH-alkyl-O-alkyl-aryl, —C(O)RF, —C(O)NH—NHRG, —C(O)NH—Oalkyl, —C(O)NH—O-alkyl-cycloalkyl, alkyl, hydroxyl, alkoxy, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl; or wherein two R3 groups together with the carbon atom to which both R3 groups are attached form —C(═O)—; RB and RC are each independently selected from the group consisting of: H, alkyl, cycloalkyl, cycloalkylalkyl-, heteroaryl, aryl, heterocycloalkyl, benzyl, and alkoxy, wherein said alkyl, cycloalkyl, cycloalkylalkyl-, heteroaryl, aryl, heterocycloalkyl, benzyl, and alkoxy groups are optionally substituted with 1 to 3 substitutents independently selected from the group consisting of: —OH, alkyl, alkoxy, hydroxyalkyl-, halo, and —C(O)Oalkyl; RD and RE are each independently selected from the group consisting of: H, alkyl, and —C(O)Oalkyl; RF is a heterocycloalkyl optionally substituted with 1-3 substitutents independently selected from the group consisting of: —OH, halo, —C(O)Oalkyl, —C(O)NH-alkyl, —C(O)alkyl, alkyl, —C(O)Ocycloalkyl, —O—Si(alkyl)2 (wherein each alkyl is independently selected), and —C(O)Oheterocycloalkyl; RG is selected from the group consisting of: H, alkyl, and —C(═S)—NH-alkyl; each m independently is 0, 1, 2 or 3; n independently is 1; Each R4 is independently selected from the group consisting of: H, alkyl, cycloalkyl, aryl, heteroaryl, —SO2-aryl, —C(O)—O-alkyl, —C(O)—O-alkylaryl, and —(CR5R6)pR7, wherein p is 1 or 2; wherein when said R4 cycloalkyl has two substituents on adjacent carbon atoms, said substituents together with the carbon atoms to which they are attached, optionally form a five- or six-membered ring selected from the group consisting of heterocyclyl, aryl and heteroaryl; R4′ is selected from the group consisting of H and alkyl; Ra is alkyl; R5 and R6 independently are selected from the group consisting of H, D, halo, —OH, —C(O)NRHR2, —C(O)—O-alkyl, and alkyl; or wherein one —CR5R6— is —C(═O)—; RH is selected from the group consisting of H and alkyl; and R7 is selected from the group consisting of H, —O-alkyl-aryl, aryl and heteroaryl, wherein when said aryl or heteroaryl has two substituents on adjacent carbon atoms, said substituents together with the carbon atoms to which they are attached, optionally form a five- or six-membered ring selected from the group consisting of cycloalkylheterocyclyl, aryl or heteroaryl. |