4-amino-6-(1-isopropyl-7-morpholino-1H-indol-5-yl)-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one | 1610800-29-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 4-amino-6-(1-isopropyl-7-morpholino-1H-indol-5-yl)-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one
• 英文别名: US10174049, Example 24；4-amino-6-(7-morpholin-4-yl-1-propan-2-ylindol-5-yl)-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one
• CAS: 1610800-29-7
• 化学式: C₂₂H₂₆N₆O₃
• 分子量: 422.487
• InChiKey: AYFZEMJCCNOWIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  31
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  98.7
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
  申请人：GlaxoSmithKline LLC

  公开号：US20140148437A1

  公开（公告）日：2014-05-29

  This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy 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 myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.

  这项发明涉及一种新型化合物，它们是酰辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂，以及含有它们的药物组合物，它们的制备方法，以及它们在治疗中的使用，单独或与体重管理疗法或其他降甘油三酯疗法结合，用于预防或治疗与DGAT-1功能障碍相关的疾病，或者调节DGAT-1活性可能具有治疗益处的疾病，包括但不限于肥胖、与肥胖相关的疾病、遗传性（1型、5型高脂血症）和获得性高三酰甘油脂或高脂蛋白血症相关疾病，由脂肪萎缩、甲状腺功能减退、药物（β受体阻滞剂、噻嗪类药物、雌激素、糖皮质激素、移植）和其他因素（怀孕、饮酒）引起，高脂蛋白血症、乳糜微粒血症、血脂异常、非酒精性脂肪肝炎、糖尿病、胰岛素抵抗、代谢综合征、心血管结果、心绞痛、多毛（包括与多毛症相关的综合征）、肾病综合征、纤维化如心肌、肾脏和肝脏纤维化、丙型肝炎病毒感染和痤疮或其他皮肤疾病。
• INTERMEDIATES USED IN THE PRODUCTION OF DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
  申请人：GlaxoSmithKline LLC

  公开号：EP3492474A1

  公开（公告）日：2019-06-05

  This invention relates to intermediates and process involving them for the production of compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1).

  本发明涉及用于生产酰基辅酶 A：二酰甘油酰基转移酶 1（DGAT-1）抑制剂的化合物的中间体及其工艺。
• Compounds as diacylglycerol acyltransferase inhibitors
  申请人：GlaxoSmithKline LLC

  公开号：US10174049B2

  公开（公告）日：2019-01-08

  This invention relates to methods for the preparation of a compound which is an inhibitor of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1).

  本发明涉及一种化合物的制备方法，该化合物是酰基辅酶 A：二酰甘油酰基转移酶 1（DGAT-1）的抑制剂。
• US9738658B2
  申请人：——

  公开号：US9738658B2

  公开（公告）日：2017-08-22
• US9796729B2
  申请人：——

  公开号：US9796729B2

  公开（公告）日：2017-10-24