9-[4-[4-(2-benzothiazol-2-yl-benzoylamino)piperidin-1-yl]butyl]-9H-fluorene-9-carboxylic acid-(2,2,2-trifluoroethyl)amide

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: 9-[4-[4-(2-benzothiazol-2-yl-benzoylamino)piperidin-1-yl]butyl]-9H-fluorene-9-carboxylic acid-(2,2,2-trifluoroethyl)amide
• 英文别名: 9-[4-[4-[[2-(2-Benzothiazolyl)benzoyl]amino]-1-piperidinyl]butyl]-N-(2,2,2-trifluoroethyl)-9H-fluorene-9-carboxamide；9-[4-[4-[[2-(1,3-benzothiazol-2-yl)benzoyl]amino]piperidin-1-yl]butyl]-N-(2,2,2-trifluoroethyl)fluorene-9-carboxamide
• 化学式: C₃₉H₃₇F₃N₄O₂S
• 分子量: 682.81
• InChiKey: JMZYIYGMXMSLEH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.2
• 重原子数：
  49
• 可旋转键数：
  10
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  103
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• Malonamic acids and derivatives thereof as thyroid receptor ligands
  申请人：——

  公开号：US20010051657A1

  公开（公告）日：2001-12-13

  The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula 1, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders. 1

  本发明涉及新型甲状腺受体配体，更具体地涉及Formula 1的马隆酰胺酸及其衍生物，可用于治疗肥胖、超重症、高脂血症、青光眼、心律失常、皮肤疾病、甲状腺疾病、甲状腺功能减退、甲状腺癌及相关疾病，如糖尿病、动脉粥样硬化、高血压、冠心病、充血性心力衰竭、高胆固醇血症、抑郁症、骨质疏松症和脱发。本发明还提供了用于治疗此类疾病和疾病的方法、药物组合物和试剂盒。
• Indole carboxylic acids as thyroid receptor ligands
  申请人：——

  公开号：US20030078289A1

  公开（公告）日：2003-04-24

  A compound of the formula 1 wherein W, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 13 are as defined herein, useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss.

  一种化合物的公式1，其中W，R1，R2，R3，R4，R5，R6，R7，R8和R13如本文所定义，在治疗肥胖、超重症、高脂血症、青光眼、心律失常、皮肤疾病、甲状腺疾病、甲状腺功能减退症、甲状腺癌及相关疾病和疾病（如糖尿病、动脉粥样硬化、高血压、冠心病、充血性心力衰竭、高胆固醇血症、抑郁症、骨质疏松症和脱发）的治疗中有用。
• Tetrazole compounds as thyroid receptor ligands
  申请人：——

  公开号：US20020006946A1

  公开（公告）日：2002-01-17

  The present invention relates to tetrazole compounds of Formula I, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, and pharmaceutically acceptable salts of the prodrugs. 1 The invention also relates to compositions comprising the tetrazole compounds and to methods of treating obesity, diabetes, atherosclerosis, hypertension, coronary heart disease, hypercholesterolemia, hyperlipidemia, thyroid disease, thyroid cancer, hypothyroidism, depression, glaucoma, cardiac arrhythmias, congestive heart failure, and osteoporosis using the tetrazole compounds.

  本发明涉及公式I的四唑化合物、立体异构体、药用可接受的盐及其前药，以及前药的药用可接受的盐。该发明还涉及包含四唑化合物的组合物，以及使用四唑化合物治疗肥胖、糖尿病、动脉粥样硬化、高血压、冠心病、高胆固醇血症、高脂血症、甲状腺疾病、甲状腺癌、甲状腺功能减退症、抑郁症、青光眼、心律失常、充血性心力衰竭和骨质疏松症的方法。
• Thyroid receptor ligands
  申请人：——

  公开号：US20010051645A1

  公开（公告）日：2001-12-13

  The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands. 1 The invention further provides pharmaceutical compositions and kits comprising such compounds and methods of treating obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer, diabetes, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesterolemia, depression, and osteoporosis using such compounds.

  该发明提供了化合物的噻唑烷二酮，噁唑烷二酮和三唑酮的化合物（I）的公式，这些化合物是甲状腺受体配体。该发明还提供了包含这些化合物的药物组合物和试剂盒，以及使用这些化合物治疗肥胖，超重症，高脂血症，青光眼，心律失常，皮肤疾病，甲状腺疾病，甲状腺功能减退症，甲状腺癌，糖尿病，动脉粥样硬化，高血压，冠心病，充血性心力衰竭，高胆固醇血症，抑郁症和骨质疏松症的方法。
• [EN] MALONAMIC ACIDS AND DERIVATIVES THEREOF AS THYROID RECEPTOR LIGANDS<br/>[FR] ACIDES MALONAMIQUES ET LEURS DERIVES EN TANT QUE LIGANDS DU RECEPTEUR DE THYROIDE
  申请人：PFIZER PROD INC

  公开号：WO2001072692A1

  公开（公告）日：2001-10-04

  The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula (I), which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression and osteoporosis. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.

  本发明涉及新型甲状腺受体配体，更具体地涉及公式（I）的马隆酰胺酸及其衍生物，可用于治疗肥胖、超重、高脂血症、青光眼、心律失常、皮肤疾病、甲状腺疾病、甲状腺功能减退、甲状腺癌及相关疾病和疾病，如糖尿病、动脉硬化、高血压、冠心病、充血性心力衰竭、高胆固醇血症、抑郁症和骨质疏松症。本发明还提供了治疗这些疾病和疾病的方法、制药组合物和工具包。