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Invention Publication
CN101678013A 哌啶/哌嗪衍生物 有权

哌啶/哌嗪衍生物
Abstract:
本发明涉及式(I)的DGAT抑制剂，包括其任何立体化学异构形式、N-氧化物、可药用盐或溶剂化物，其中A代表CH或N；虚线在A代表碳原子时表示一个任选的键；X代表-O-C(＝O)-，-C(＝O)-C(＝O)-，-NR x -C(＝O)-，-Z-C(＝O)-，-Z-NR x -C(＝O)-，-C(＝O)-Z-，-NR x -C(＝O)-Z-，-C(＝S)-，-NR x -C(＝S)-，-Z-C(＝S)-，-Z-NR x -C(＝S)-，-C(＝S)-Z-，-NR x -C(＝S)-Z-；Z代表选自C 1-6 链烷二基、C 2-6 链烯二基或C 2-6 链炔二基的二价基团，其中该C 1-6 链烷二基、C 2-6 链烯二基或C 2-6 链炔二基均可任选地被取代，并且连接在C 1-6 链烷二基中同一碳原子上的两个氢原子可以任选地被C 1-6 链烷二基代替；Y代表-C(＝O)-NR x -或-NR x -C(＝O)-；R 1 代表金刚烷基，C 3-6 环烷基，芳基 1 或Het 1 ；R 2 代表C 3-6 环烷基，苯基，萘基，2，3-二氢-1，4-苯并二氧杂环己烯基，1，3-苯并二氧杂环戊烯基，2，3-二氢苯并呋喃基，或含1或2个N原子的6元芳族杂环，其中该C 3-6 环烷基、苯基、萘基、2，3-二氢-1，4-苯并二氧杂环己烯基、1，3-苯并二氧杂环戊烯基或杂环可任选地被取代；R 7 代表氢，卤素，C 1-4 烷基，被羟基取代的C 1-4 烷基；条件是以下化合物(A)，(B)被排除在外。本发明还涉及制备此类化合物的方法，含有该化合物的药物组合物，以及该化合物作为药物和DGAT抑制剂的用途。
Abstract(English):

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 -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)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents 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; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (A), (B) are excluded. 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. The formula (I) is shown in the description.

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