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    • 2. 发明授权
    • Nitrogen-containing heterocyclic compounds and benamide compounds and drugs containing the same
    • 含氮杂环化合物和苯甲酰胺化合物及含有其的药物
    • US06777414B1
    • 2004-08-17
    • US09958296
    • 2001-10-05
    • Naoto OhkuraYukiko HiraiwaTetsuya MatsushimaKazue SasakiTakehiro YamamotoMasaharu ShiotaniShigeki SuzukiYuuko NakataniChizuko KurodaMieko NagasawaKiyoaki Katano
    • Naoto OhkuraYukiko HiraiwaTetsuya MatsushimaKazue SasakiTakehiro YamamotoMasaharu ShiotaniShigeki SuzukiYuuko NakataniChizuko KurodaMieko NagasawaKiyoaki Katano
    • C07D20946
    • C07D213/40C07D209/46C07D295/155C07D309/04C07D405/04C07D405/12C07D405/14C07D471/04
    • Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases. In formula (I), R1 and R2 represent alkyl, alkoxy, cycloalkyl, phenyl, alkenyl, alkynyl, or a five- or six-membered saturated or unsaturated heterocyclic ring, or R1 and R2, together with a nitrogen atom to which R1 and R2 are attached, may form a ring; R3 and R4 represent a hydrogen atom, alkyl, a halogen atom, hydroxyl, nitrile, alkoxycarbonyl, alkoxy, or carboxyl; or R2 and R3 may be attached to each other to form —(CH2)m—, —N═CH—, —CH═N—, or —(C1-6 alkyl)C═N—; A, D, E, and G each represent a carbon atom, or any one of A, D, E, and G represents a nitrogen atom with the other three each representing a carbon atom; Q represents a nitrogen atom or a carbon atom; Y represents a group represented by formula (II) wherein X represents a hydrogen atom, group —C(═O)N(R5)R6 or group —C(═O)OR7, R8 is absent or represents a bond, an oxygen atom, a sulfur atom, —SO2—, —SO—, —CH2—CH2—, or —CH═CH—, and R9 and R10 represent a hydrogen atom, alkyl, alkoxy, a halogen atom, or hydroxyl; and Z represents —(CH2)n—, —O—(CH2)i—, or —C(═O)NH—(CH2)i—.
    • 公开了在肝脏中具有甘油三酯生物合成抑制活性的由式​​(I)表示的化合物,并且对来自肝脏的含载脂蛋白B的脂蛋白的分泌具有抑制活性,特别是对含有载脂蛋白B的脂蛋白的分泌具有优异的抑制活性。 没有肝脏中脂质积累的副作用,可用于治疗和预防高脂血症和动脉硬化性疾病。 在式(I)中,R 1和R 2表示烷基,烷氧基,环烷基,苯基,烯基,炔基或五元或六元饱和或不饱和杂环,或R 1和R 2, 2>与R 1和R 2连接的氮原子一起形成环; R 3和R 4表示氢原子,烷基,卤素原子,羟基,腈,烷氧基羰基,烷氧基或羧基; 或R 2和R 3可以彼此连接形成 - (CH 2)m - , - N = CH - , - CH = N-或 - (C 1-6烷基)C = N-; A,D,E和G各自表示碳原子,A,D,E和G中的任一个表示氮原子,其余三个表示碳原子; Q表示氮原子或碳原子; Y表示由式(II)表示的基团,其中X表示氢原子,-C(= O)N(R 5)R 6或-C(= O)OR 7, 8>不存在或表示键,氧原子,硫原子,-SO 2 - , - SO - , - CH 2 -CH 2 - 或-CH = CH-,R 9和R 10表示 氢原子,烷基,烷氧基,卤素原子或羟基; 并且Z表示 - (CH 2)n - , - O-(CH 2)i - 或-C(= O)NH-(CH 2)i - 。