US 8,541,427 B2 · Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use

A compound, or a deuterate thereof, or a tautomer of said compound or said deuterate, or a pharmaceutically acceptable salt of said compound, said deuterate, or said tautomer, said compound having the structural Formula (II-A):

wherein R2, R3, R4, R5, R8, R7, and R8 are each selected independently and wherein:
R2 is selected from hydrogen, fluorine, chlorine, and cyano;
R3 is selected from hydrogen, fluorine, chlorine, and cyano;
R4 is selected from hydrogen, fluorine, chlorine, and cyano;
R5 is selected from hydrogen, fluorine, and chlorine;
R6 is selected from lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, and lower alkyl-OH;
R7 is selected from fluorine and chlorine;
and
R8 is selected from lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, cycloalkyl, -alkyl-cycloalkyl, —O-cycloalkyl, and —O-alkyl-cycloalkyl.

6 more elements

A compound, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer, said compound having the structural Formula (II-AA):

wherein:
R2 is selected from hydrogen, fluorine, chlorine, and cyano;
R3 is selected from hydrogen, fluorine, chlorine, and cyano;
R4 is selected from hydrogen, fluorine, chlorine, and cyano;
and
R5 is selected from hydrogen, fluorine, and chlorine.

3 more elements

A compound, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer, said compound having the structural Formula (II-AB):

wherein each variable is selected independently of the others and wherein:
the moiety
shown in (II-AB) is selected from the group consisting of
either R2 is F and R3 is H or R2 is H and R3 is F.

1 more element

A compound, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer, said compound being selected from:

Ex
No.
Compound
1
2
3
4
5
6
7
8
9
10
11
12
13
14
15
16
17
18
19
20
21
22
23
24
25
26
27
28
29
30
31
32
33
34
35
36
37
38
39
40
41
42
43

43 more elements

A compound, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer, said compound having a structure selected from:

Ex
No.
Compound
1
2
8
9
10
15
16
17
18
19
20
31
35
38
39

15 more elements

A compound, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer, said compound having the following structure:

A deuterated compound, or a tautomer thereof, or a pharmaceutically acceptable salt of said deuterated compound or said tautomer, said deuterated compound having the following structure:

Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use

Life of this patent

Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use

Life of this patent

Abstract

Claims21