BONGARTZ, JEAN-PIERRE ANDRE MARC,柏葛兹,柏葛茲,LINDERS, JOANNES THEODORUS MARIA,林德斯,MEERPOEL, LIEVEN,梅波尔,梅波爾,VAN LOMMEN, GUY ROSALIA EUGEEN,范罗曼,范羅曼,COESEMANS, ERWIN,寇曼斯,BRAEKEN, MIRIELLE,布雷肯,BUY
申请号：
TW097121020
公开号：
TWI438197B
申请日:
2008.06.06
申请国别(地区):
TW
年份:
2014
代理人:
摘要：
The invention relates to a DGAT inhibitor of formulaincluding 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 -O-C(=O)-； -C(=O)-C(=O)-； -NRx-C(=O)-； -Z-C(=O)-； -Z-NRx-C(=O)-； -C(=O)-Z-； -NRx-C(=O)-Z-； -C(=S)-； -NRx-C(=S)-； -Z-C(=S)-； -Z-NRx-C(=S)-； -C(=S)-Z-； -NRx-C(=S)-Z-； Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl； wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted； and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl； Y represents -C(=O)-NRx- or -NRx-C(=O)-； R1represents adamantanyl, C3-6cycloalkyl； aryl1or Het1； R2represents C3－6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted； R7represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl； provided that the following compoundsare excluded； aN-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, as a DGAT inhibitor, of said compounds.本發明係有關一種下式之DGAT抑制劑包括其任何立體化學異構形式，其中A係表示CH或N；當A係表示碳原子時，虛線係表示視情況存在之鍵結；X係表示－O－C(＝O)－；－C(＝O)－C(＝O)－；－NRx－C(＝O)－；－Z－C(＝O)－；－Z－NRx－C(＝O)－；－C(＝O)－Z－；－NRx－C(＝O)－Z－；－C(＝S)－；－NRx－C(＝S)－；－Z－C(＝S)－；－Z－NRx－C(＝S)－；－C(＝S)－Z－；－NRx－C(＝S)－Z－；Z係表示選自以下之二價基團：C1－6烷二基、C2－6烯二基或C2－6炔二基；其中該C1－6烷二基、C2－6烯二基或C2－6炔二基各可視情況經取代；且其中連接於C1－6烷二基中同一碳原子的兩氫原子可視情況由C1－6烷二基置換；Y係表示－C(＝O)－NRx
