3-(3-chloro-phenyl)-N-(2-thiazol-4-yl-1H-benzoimidazol-5-yl)-butyrarnide | 689297-68-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 3-(3-chloro-phenyl)-N-(2-thiazol-4-yl-1H-benzoimidazol-5-yl)-butyrarnide
• 英文别名: Kv2-IN-A1；3-(3-chlorophenyl)-N-[2-(1,3-thiazol-4-yl)-3H-benzimidazol-5-yl]butanamide
• CAS: 689297-68-5
• 化学式: C₂₀H₁₇ClN₄OS
• 分子量: 396.9
• InChiKey: MRQZOINSVKHDQS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  98.9
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS<br/>[FR] DERIVES DE CARBONYLAMINO-BENZIMIDAZOLE UTILISES COMME MODULATEURS DU RECEPTEUR ANDROGENE
  申请人：MERCK & CO INC

  公开号：WO2004041277A1

  公开（公告）日：2004-05-21

  Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, arthritic condition and joint repair, HIV-wasting, prostate cancer, cancer cachexia, Alzheimer s disease, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

  化学结构式（I）的化合物以组织选择性的方式调节雄激素受体（AR）。它们在男性患者的前列腺或女性患者的子宫中对AR产生拮抗作用，同时在骨骼和/或肌肉组织中作为雄激素受体激动剂，因此这些化合物对于增强肌肉张力和治疗由雄激素缺乏引起或可以通过雄激素治疗改善的疾病具有用处，包括骨质疏松症、骨质疏松、糖皮质激素诱导的骨质疏松症、牙周病、骨折、骨重建手术后的骨损伤、肌肉萎缩、衰弱、皮肤老化、男性性腺功能减退、女性绝经后症状、动脉硬化、高胆固醇血症、高脂血症、肥胖症、再生障碍性贫血和其他造血系统疾病、关节炎和关节修复、HIV消耗综合症、前列腺癌、癌性消瘦、阿尔茨海默病、肌萎缩性疾病、卵巢早衰和自身免疫疾病，可单独使用或与其他活性剂联合使用。
• Carbonylamino-benzimidazole derivatives as androgen receptor modulators
  申请人：Kim Yuntae

  公开号：US20060036098A1

  公开（公告）日：2006-02-16

  Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, arthritic condition and joint repair, HIV-wasting, prostate cancer, cancer cachexia, Alzheimer s disease, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

  化学式（I）的化合物在组织选择性方面是雄激素受体（AR）的调节剂。它们在男性患者的前列腺或女性患者的子宫中作为雄激素受体拮抗剂，同时在骨骼和/或肌肉组织中作为雄激素受体激动剂，因此在增强肌肉张力和治疗由雄激素缺乏引起或可以通过雄激素治疗改善的疾病，包括骨质疏松症、骨质疏松、糖皮质激素诱导的骨质疏松症、牙周疾病、骨折、骨重建手术后的骨损伤、肌无力、衰弱、老化皮肤、男性性腺功能减退症、女性绝经后症状、动脉粥样硬化、高胆固醇血症、高脂血症、肥胖症、再生障碍性贫血和其他造血系统疾病、关节炎和关节修复、艾滋病浪费、前列腺癌、癌症消瘦、阿尔茨海默病、肌萎缩症、早发性卵巢衰竭和自身免疫性疾病方面具有用途，可以单独或与其他活性剂联合使用。
• CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS
  申请人：Merck & Co., Inc.

  公开号：EP1581217A1

  公开（公告）日：2005-10-05
• EP1581217A4
  申请人：——

  公开号：EP1581217A4

  公开（公告）日：2007-07-11
• US7622592B2
  申请人：——

  公开号：US7622592B2

  公开（公告）日：2009-11-24