申请人:Bongartz Jean-Pierre Andre Marc
公开号:US20100190789A1
公开(公告)日:2010-07-29
The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NR
x
—C(═O)—; —Z
1
—C(O)—; —Z
1
—NR
x
—C(═O)—; —C(═O)—Z
1
—; —NR
x
—C(═O)—Z
1
—; —S(═O)p-; —C(═S)—; —NR
x
—C(═S)—; —Z
1
—C(═S)—; —Z
1
—NR
x
—C(═S)—; —C(═S)—Z1-; NR
x
—C(═S)—Z—; Y represents NR
x
—C(=
0
)-Z
2
—; —NR
x
—C(=
0
)-Z
2
—NR
y
—; —NR
x
—C(=
0
)-Z
2
—NR
y
—C(=
0
)—; —NR
x
—C(=
0
)-Z
2
—NR
y
—C(=
0
)-; O—; —NR
x
—C(=
0
)-Z
2
-
0
-; —NR
x
—C(=
0
)-Z
2
-
0
-C(=
0
)-; —NR
x
—C(=
0
)-Z
2
—C(=
0
)-; —NR
x
—C(=
0
)-Z
2
—C(=
0
)-; —NR
x
—C(=
0
)-
0
-Z
2
—C(=
0
)-; —NR
x
—C(=
0
)-
0
-Z
2
—C(=
0
)-
0
-; —NR
x
—C(═O)—O—Z
2
—O—C(═O)—; —NR
x
—C(═O)—Z
2
—C(═O)—NR
y
—; —NR
x
—C(═O)—Z
2
—NR
y
—C(=
0
)-NR
y
—; —C(═O)—Z
2
—; —C(═O)—Z
2
—O—; —C(=
0
)-NR
x
—Z
2
—; —C(=
0
)-NR
x
—Z
2
-
0
-; —C(=
0
)-NR
x
—Z
2
—C(=
0
)-
0
-; —C(=
0
)-NR
x
—Z
2
-
0
-C(=
0
)-; —C(=
0
)-NR
x
—Z
2
—NR
y
—; —C(=
0
)—NR
x
—Z
2
—NR
y
—C(=
0
)-; —C(=
0
)-NR
x
—Z
2
—NR
y
—C(=
0
)-
0
-; R
1
represents C
1-12
alkyl optionally substituted with cyano, C
1-4
alkyloxy, C
1-4
alkyl-oxyC
1-4
alkyloxy, C
3-6
Cycloalkyl or aryl; C
2-6
alkenyl; C
2-6
alkynyl; C
3-6
cycloalkyl; adamantanyl; aryl
1
; aryl
1
C
1-6
alkyl; Het
1
; or Het
1
C
1-6
alkyl; provided that when Y represents —NR
x
—C(═O)—Z
2
—; —NR
x
—C(=
0
)-Z
2
—NR
y
; —NR
x
—C(═O)—Z
2
—C(═O)—NR
y
—; —C(═O)—Z
2
—; —NR
x
—C(=
0
)-Z
2
—NR
y
—C(=
0
)—NR
y
—; —C(═O)—NR—Z
2
—; —C(═O)—NR—O—Z
2
—; or —C(=
0
)-NR
x
—Z
2
—NR
y
—; then R
1
may also represent hydrogen; R
2
represents hydrogen, C
1-12
alkyl, C
2-6
alkenyl or R
3
; provided that if X represents —O—C(═O)—; the R
2
O represents R
3
; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.