tert-butyl 4'-((2,3-dimethyl-5-((2-oxo-2-phenylethyl)carbamoyl)-1H-indol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylate | 1415256-63-1

• 分子结构分类: 有机化合物
• 英文名称: tert-butyl 4'-((2,3-dimethyl-5-((2-oxo-2-phenylethyl)carbamoyl)-1H-indol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylate
• 英文别名: Tert-butyl 2-[4-[[2,3-dimethyl-5-(phenacylcarbamoyl)indol-1-yl]methyl]phenyl]benzoate
• CAS: 1415256-63-1
• 化学式: C₃₇H₃₆N₂O₄
• 分子量: 572.704
• InChiKey: NVANOIVLCZTEJI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.5
• 重原子数：
  43
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  77.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] PPARG MODULATORS FOR TREATMENT OF OSTEOPOROSIS<br/>[FR] MODULATEURS DE PPARG POUR LE TRAITEMENT DE L'OSTÉOPOROSE
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2015161108A1

  公开（公告）日：2015-10-22

  The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.

  本发明提供了一种治疗进行性骨病的方法，如骨质疏松症、佩吉特病、多发性骨髓瘤或甲状旁腺功能亢进症，包括向患有该病的患者施用有效量的非激动剂PPARG调节剂。
• N-BIPHENYLMETHYLINDOLE MODULATORS OF PPARG
  申请人：Kamenecka Theodore Mark

  公开号：US20120309757A1

  公开（公告）日：2012-12-06

  The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.

  该发明提供了与PPARG（PPARγ）结合亲和力高的分子实体，抑制激酶介导的，例如cdk5介导的PPARG磷酸化，但不对PPARG产生激动作用。该发明的化合物可用于治疗患有PPARG起作用的疾病的患者，如糖尿病、胰岛素抵抗、糖耐量受损、糖尿病前期、高血糖、高胰岛素血症、肥胖或炎症。在使用该发明的化合物治疗这些疾病的方法中，该化合物可以避免在接受该化合物的患者中产生明显体重增加、水肿、骨生长或形成受损、心肌肥大或上述任何组合的副作用。该发明还提供了化合物的制备方法、用于评估该发明的化合物作为非激动性PPARG结合化合物的生物测定方法，以及制药组合物。
• PPARG modulators for treatment of osteoporosis
  申请人：The Scripps Research Institute

  公开号：US10016394B2

  公开（公告）日：2018-07-10

  The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.

  本发明提供了治疗进行性骨病（如骨质疏松症、帕吉特氏病、多发性骨髓瘤或甲状旁腺功能亢进症）的方法，包括向患病患者施用有效量的非拮抗剂 PPARG 调节剂。
• PPARG modulators for the treatment of osteoporosis
  申请人：The Scripps Research Institute

  公开号：US10744117B2

  公开（公告）日：2020-08-18

  The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.

  本发明提供了治疗进行性骨病（如骨质疏松症、帕吉特氏病、多发性骨髓瘤或甲状旁腺功能亢进症）的方法，包括向患病患者施用有效量的非拮抗剂 PPARG 调节剂。
• PPARG MODULATORS FOR TREATMENT OF OSTEOPOROSIS
  申请人：The Scripps Research Institute

  公开号：US20170035730A1

  公开（公告）日：2017-02-09

  The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.