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    • 1. 发明申请
    • NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
    • 新型化合物作为二乙酰胆碱酯酶抑制剂
    • WO2014074761A3
    • 2014-10-23
    • PCT/US2013069024
    • 2013-11-08
    • GLAXOSMITHKLINE LLC
    • CHEUNG MUITANGIRALA RAGHURAM S
    • A61K31/501
    • C07D213/72A61K31/122A61K31/50C07D213/74C07D237/20C07D277/42C07D401/12C07D405/12C07D417/12
    • This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyl transferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with other triglyceride lowering therapies for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.
    • 本发明涉及作为酰基辅酶A:二酰基甘油酰基转移酶1(DGAT-1)的抑制剂的新化合物,含有它们的药物组合物,其制备方法及其在治疗中的用途,单独或与其它甘油三酯组合 降低用于预防或治疗与DGAT-1功能障碍有关的疾病或DGAT-1活性调节可能具有治疗益处的疗法,包括但不限于肥胖症,肥胖相关疾病,遗传(1型,5型高脂血症)和获得性形式 高甘油三酯血症或高脂蛋白血症相关疾病,由但不限于脂肪营养不良,甲状腺功能减退,药物(β受体阻滞剂,噻嗪类,雌激素,糖皮质激素,移植物)等因素(怀孕,酒精摄入),高脂蛋白血症,乳糜微粒血症,血脂异常,非酒精性脂肪性肝炎 ,糖尿病,胰岛素抵抗,代谢综合征,心血管结局,心绞痛,过量的h 空气生长(包括与多毛症相关的综合征),肾病综合征,纤维化如心肌炎,肾和肝纤维化,丙型肝炎病毒感染和痤疮或其他皮肤病。