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US 6,683,091 B2Granted
Gamma Secretase inhibitors
AssigneeSchering Corporation
InventorsTheodoros Asberom, Henry S. Guzik, Hubert B. Josien, Dmitri A Pissarnitski
Life of this patent
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Abstract
This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, —(CR32)1-4X(CO)Y; each R3A is independently H or alkyl; X is —O—, —NH, or —N-alkyl; and Y is —NR6R7, or —N(R3)(CH2)2-6NR6R7. Also disclosed is a method of treating Alzheimer's Disease.
Claims15
A compound of the formula:
- or a pharmaceutically acceptable salt or solvate thereof, wherein:
- (A) R1 is selected from:
- (1) unsubstituted aryl;
- (2) aryl substituted with one or more (e.g., 1-3) R5 groups;
- (3) heteroaryl;
- or
- (4) heteroaryl substituted with one or more (e.g., 1-3) R5 groups;
- (B) R2 is selected from:
- (1) alkyl,
- (2) —X(CO)Y;
- (3) —(CR3)1-4X(CO)Y;
- or
- (4) any of the groups for R1,
- (C) Each R3 is independently selected from:
- (1) H, or
- (2) alkyl;
- (D) Each R3A is independently selected from:
- (1) H;
- or
- (2) alkyl;
- (E) R4 is independently selected from:
- (1) halogen;
- (2) —CF3;
- (3) —OH;
- (4) —Oalkyl;
- (5) —OCF3;
- (6) —CN;
- (7) —NH2;
- (8) —CO2alkyl;
- (9) —CONR6R7;
- (10) -alkylene-NR6R7;
- (11) —NR6COalkyl;
- (12) —NR6COaryl;
- (13) —NR6COheteroaryl;
- or
- (14) —NR6CONR6R7;
- (F) R5 is independently selected from:
- (1) halogen;
- (2) —CF3;
- (3) —OH;
- (4) —Oalkyl;
- (5) —OCF3;
- (6) —CN;
- (7) —NH2;
- (8) —CO2alkyl;
- (9) —CONR6R7;
- (10) alkylene-NR6R7;
- (11) —NR6COalkyl;
- (12) —NR6COaryl;
- (13) —NR6COheteroaryl;
- (14) —NR6CONR6R7;
- (G) X is selected from:
- (1) —O—;
- (2) —NH;
- (3) —N-alkyl;
- or
- (H) Y is selected from:
- (1) —NR6R7;
- or
- (2) —N(R3)(CH2)2-6NR6R7;
- (I) R6 and R7 are independently selected from:
- (1) H;
- (2) alkyl;
- (3) cycloalkyl,
- (4) -arylalkyl;
- (5) -heteroarylalkyl;
- (6)
- (7)
- (J) R6 and R7 taken together with the nitrogen atom to which they are bound form a heterocycloalkyl group selected from:
- (K) Each R8 is independently selected from:
- (1) alkyl;
- or (2) alkyl substituted with 1 to 4 hydroxy groups;
- (L) Each R9 is independently selected from:
- (1) H;
- (2) alkyl;
- (3) alkyl substituted with 1 to 4 hydroxy groups;
- (4) cycloalkyl;
- (5) cycloalkyl substituted with 1 to 4 hydroxy groups;
- (6) -arylalkyl;
- (7) -heteroarylalkyl;
- (8) —COOalkyl;
- or
- (9) any of the groups for R1;
- (M) Each R10 is independently selected from:
- (1) H;
- or
- (2) alkyl;
- (N) m is 0 to 3, and n is 0 to 3, such that m+n is 1, 2, 3 or 4;
- (O) p is 0 to 4;
- (P) r is 0 to 4;
- (Q) s is 0 to 3;
- and
- (R) with the proviso that compounds of formula 1.0 do not include:
- (S) and with the further proviso that when n=0 and m=2, R2 is not alkyl, dialkyl or alkenyl.
91 more elements
Dependencies are inferred from the claim text.