知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

44 条记录 (耗时 0.049 秒)

    Inhibition of fatty acid synthase as a means to reduce adipocyte mass
    10.
    发明授权
    Inhibition of fatty acid synthase as a means to reduce adipocyte mass 失效
    抑制脂肪酸合酶作为减少脂肪细胞质量的手段

    公开(公告)号：US5981575A

    公开(公告)日：1999-11-09

    申请号：US157

    申请日：1998-01-27

    申请人： Francis P. Kuhajda ,  Gary R. Pasternack ,  Craig A. Townsend ,  Neelakandha S. Mani

    发明人： Francis P. Kuhajda ,  Gary R. Pasternack ,  Craig A. Townsend ,  Neelakandha S. Mani

    IPC分类号： A61K31/00 ,  A61K31/365 ,  A61K31/381 ,  A61K31/4025 ,  A01K31/04

    CPC分类号： A61K31/4025 ,  A61K31/00 ,  A61K31/365 ,  A61K31/381

    摘要： Weight loss was noted in nude mice treated with cerulenin, a non-competitive inhibitor of FAS. Sustained reduction of adipocyte mass in humans without toxicity would significantly impact disease prevention worldwide. Aside from psychological and self-esteem improvement, weight loss via reduction of adipocyte mass may: (1) ameliorate hyperglycemia associated with non-insulin-dependent diabetes mellitus thereby reducing diabetic complications such as arterial disease, blindness, cataracts, etc., (2) reduce hypertension, (3) reduce risk of coronary artery vascular disease and stroke, and (4) reduce the risk of other complications of massive obesity such as osteoarthritis, surgical complications, etc. There is also potential use in livestock and poultry to reduce the saturated fat content of meat products. Therefore FAS inhibitors are disclosed herein as novel agents for weight reduction. A family of compounds (.gamma.-substituted-.alpha.-methylene-.beta.-carboxy-.gamma.-butyrolactones) whose synthesis was based on the cerulenin motif is shown herein to inhibit fatty acid synthesis, inhibit growth in certain susceptible tumor cells, and induce weight loss.

    摘要翻译： PCT No.PCT / US96 / 17678 Sec。 371日期：1998年1月27日 102（e）日期1998年1月27日PCT 1996年11月15日PCT PCT。 第WO97 / 18806号公报 日期1997年5月29日在使用非竞争性FAS抑制剂的木瓜素治疗的裸小鼠中观察到重度损失。 持续减少人体脂肪细胞质量无毒性将严重影响全球疾病预防。 除了心理和自尊心的改善之外，通过减少脂肪细胞质量可以减轻体重：（1）改善与非胰岛素依赖性糖尿病相关的高血糖，从而减少糖尿病并发症，如动脉疾病，失明，白内障等（2 ）降低高血压，（3）降低冠状动脉血管疾病和中风的风险，（4）降低骨质疏松，手术并发症等巨大肥胖的其他并发症的风险。畜禽养殖也有可能减少 肉制品的饱和脂肪含量。 因此，本文公开了FAS抑制剂作为减轻体重的新型药剂。 本文显示了其合成基于苏氨酸基序的化合物（γ-取代-α-亚甲基-β-羧基-γ-丁内酯）家族，以抑制脂肪酸合成，抑制某些易感的肿瘤细胞中的生长，并诱导体重减轻 。