| 主权项 |
1. A compound of Formula I or Formula II or a pharmaceutically acceptable salt thereof, wherein:
R1 is selected from the group consisting of:(1) C2-8alkyl,(2) C2-8alkenyl,(3) C2-8alkynyl,(4) C3-6cycloalkyl-(CH2)p—, wherein p is 1, 2, 3 or 4, and(5) benzyl, wherein groups (1) to (5) above are optionally substituted with 1 to 3 Ra groups;each Ra and R2 is independently selected from the group consisting of: halo, OH, C1-4alkyl, C1-4alkoxy, CF3, —OCF3 and —CN;Y is selected from the group consisting of: H, halo, CN, C1-4alkyl, C2-4alkenyl and CH3—S(O)q—, wherein said C1-4alkyl and C2-4alkenyl are optionally substituted with hydroxy, oxo and one or more fluoro groups as allowed by valence;X is C(R8) or N, or the N-oxide thereof;R3 is selected from H or halogen;R4 and R5 are independently selected from H and C1-4alkyl, optionally substituted with hydroxy, or R4 and R5 may be joined together to form carbonyl;R6 is selected from the group consisting of H, —C(O)—R9 and —S(O)r—R9, andR7 is H or C1-4alkyl,or R6 and R7 and the nitrogen atom to which they are attached may be joined together to form a 5- membered non-aromatic ring optionally containing one or two additional heteroatoms selected from N, S or O, said ring optionally substituted with one or two oxo groups and one to three substituents independently selected from halo, CN, R9, —O—R9, —C(O)—R9—C(O)—O—R9 and —S(O)t—R9,or R6 and R7 and the nitrogen atom to which they are attached may be joined together to form a 6-membered non-aromatic ring optionally containing one or two additional heteroatoms selected from N or S, said ring optionally substituted with one or two oxo groups and one to three substituents independently selected from halo, CN, R9, —O—R9, —C(O)—R9—C(O)—O—R9 and —S(O)t—R9,or R6 and R7 and the nitrogen atom to which they are attached are joined together to form morpholine which is optionally substituted with one to three substituents independently selected from halo, CN, R9, —O—R9, —C(O)—R9, —C(O)—O—R9 and —S(O)t—R9,or R6 and R7 and the nitrogen atom to which they are attached may be joined together to form azide;R8 is selected from H and C1-4alkyl;each R9 independently represents: (1) H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-10cycloalkyl, C3-10cycloalkylC1-4alkyl, C3-10cycloalkenyl or C3-10cycloalkenylC1-4alkyl, any of which except H optionally bear OH, CN, CF3 and C1-4alkoxy and up to 5 halogen atoms; (2) phenyl, benzyl or heteroaryl, optionally bridged with a methylene, any of which optionally bear up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, C1-4alkyl, C1-4hydroxyalkyl, C3-6cycloalkyl, phenyl, heteroaryl, C1-4alkoxy, acetyl, amino, carbamoyl, CO2—C1-4alkyl, C1-4alkylamino and di(C1-4alkyl)amino; and (3) Het, optionally bridged with a methylene and said Het optionally bearing up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, C1-4alkyl, C1-4hydroxyalkyl, C3-6cycloalkyl, phenyl, heteroaryl, C1-4alkoxy, acetyl, amino, carbamoyl, CO2—C1-4alkyl, C1-4alkylamino and di(C1-4alkyl)amino;each “heteroaryl” independently defined as 5- or 6-membered aromatic monocyclic or 9- or 10-membered aromatic bicyclic ring systems, in which at least one ring atom is selected from N or N-oxide, O and S;each “Het” independently defined as nonaromatic or partially aromatic mono- or bicyclic heterocyclic systems of up to 10 ring atoms, in which at least one ring atom is selected from N, O and S, where the sulfur atom may be in the form of the S-oxide or S,S-dioxide; andq, r and t are independently 0, 1 or 2. |
