| 主权项 |
1. A method of therapeutically treating Alzheimer's disease in a patient in need thereof, wherein therapeutically treating consists of inhibiting the disease in an animal that is experiencing or displaying the pathology or symptomatology of the disease, comprising administering to the patient a therapeutically effective amount of a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein X—Y is selected from the group consisting of
(1) —O—CRARB—,(2) —CRARB—O—,(3) —CRARB—SRC—,(4) —CRARB—NRC—, and(5) —NRC—CRARB—;wherein RA and RB are each independently selected from the group consisting of,
(a) hydrogen, and(b) —C1-6 alkyl, andRC is selected from the group consisting of,
(a) hydrogen,(b) —C(═O)—C1-6 alkyl,(c) —C1-6 alkyl,(d) —C(═O)—CH2—C6H5, and(e) —S(═O)2—C1-6 alkyl; R1 is selected from the group consisting of
(1) hydrogen, and(2) hydroxy, provided that when X—Y is —O—CRARB—, —CRARB—O— or —CRARB—SRC—, then R1 is hydroxy in the isomeric position: R2 is selected from the group consisting of
(1) —C6-10 aryl, and(2) -heteroaryl, which is an aromatic cyclic group, having from five to twelve ring atoms, the ring atoms selected from the group consisting of C, O, N, N→O or S, at least one of which is O, N, N→O or S,wherein the aryl or heteroaryl R2 group is optionally substituted with one or more of the group consisting of
(a) halogen,(b) hydroxy,(c) —NR3R4,(d) —C1-6 alkyl,(e) —O—C1-6 alkyl,(f) —C2-8 alkenyl,(g) —C(═O)—(O)m—R5,(h) —C(═O)—NR5,(i) —S(═O)2—R5,(j) —SR5,(k) —CN;(l) —C6-10 aryl,(m) heteroaryl, which is an aromatic cyclic group, having from five to twelve ring atoms, the ring atoms selected from the group consisting of C, O, N, N→O or S, at least one of which is O, N, N→O or S,(n) Si(R6)3, and(o) ═S,wherein the alkyl, alkenyl, aryl or heteroaryl moiety is optionally substituted with one or more
(a) halogen,(b) hydroxyl,(c) —C1-6 alkyl,(d) —S—R6,(e) —NR8R9, and(f) —O—C1-6 alkyl,wherein the alkyl moiety is optionally substituted with one or more halogen; R3 and R4, or R8 and R9, are independently selected from the group consisting of
(1) hydrogen, and(2) —C1-6 alkyl,wherein the alkyl is optionally substituted with one or more
(a) halogen,(b) hydroxyl,(c) —O—C 1-6 alkyl,(d) —NR10R11, and(e) —C(═O)—(O)n —C 1-6 alkyl,or R3 and R4, or R8 and R9, are linked together with the nitrogen to which they are attached to form a 4-6 membered carbocyclic ring, wherein one or two of the ring carbon atoms is optionally replaced by a nitrogen, oxygen or sulfur, and the ring is optionally substituted with one or more
(a) halogen,(b) hydroxyl,(c) C1-6 alkyl,(d) —O—C 1-6 alkyl, and(e) —C(═O)—(O)n —C1-6 alkyl; R5 is selected from the group consisting of
(1) hydrogen,(2) —C 1-6 alkyl,(3) —C3-8 cycloalkyl,(4) —C2-8 alkenyl, and(5) —C6-10 aryl,wherein the alkyl, cycloalkyl, alkenyl or aryl is optionally substituted with one or more
(a) halogen,(b) hydroxyl,(c) —C 1-6 alkyl,(d) —O—C 1-6 alkyl,(e) —C3-8 cycloalkyl, and(f) —C6-10 aryl; R6 is selected from the group consisting of
(1) hydrogen, and(2) —C 1-6 alkyl; R10 and R11 are independently selected from the group consisting of
(1) hydrogen, and(2) —C 1-6 alkyl,wherein the alkyl is optionally substituted with one or more
(a) halogen,(b) hydroxyl,(c) —O—C1-6 alkyl, and(d) —C(═O)—(O)n —C1-6 alkyl,or R10 and R11 are linked together with the nitrogen to which they are attached to form a 4-6 membered carbocyclic ring, wherein one or two of the ring carbon atoms is optionally replaced by a nitrogen, oxygen or sulfur, and the ring is optionally substituted with one or more
(a) halogen,(b) hydroxyl,(c) C1-6 alkyl,(d) —O—C1-6 alkyl, and(e) —C(═O)—(O)n —C1-6 alkyl; m is 0 or 1; n is 0, 1 or 2. |
