| 摘要 |
The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I):;;which penetrate the blood brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system. |
| 主权项 |
1. A compound of formula (I):in free or salt form, wherein:
A1 is CH or N; R1 is C1-6alkyl, C1-6cycloalkyl, or aryl optionally substituted with alkyl, haloalkyl, alkyloxy, or halo group; R2, R3, R4, R5, R6 and R7 are independently hydrogen, halo, C1-4alkyl, C1-4alkyloxy, or trifluoromethyl; or R5 and R6, together with carbon atoms to which they are attached, form a 5 or 6 member hetcyclic ring; Y is —NHCO—, —CONH—, —NHSO2—, —NHCONH—, or —NHCH2—; D is a 5 or 6 member aryl, hetaryl, or hetcyclic ring having at least one N, S, or O ring atom, or a C ring atom forming an oxo (C═O) moiety; provided that D is not a substituted phenyl group if A1=N and R2═R3═R4═R5═R6═H and R7═CH3 and Y═NHCO; and R8 is C0-6alkyl, C3-7cycloalkyl, aryl, hetaryl, hetcyclyl(C0-4alkyl)-, or —C0-6alkyl-N(C0-6 alkyl)(C0-6alkyl), optionally substituted with C1-6alkyl. |
