5-acetyl-N-{1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl}-2H-pyrazole-3-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-acetyl-N-{1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl}-2H-pyrazole-3-carboxamide
• 英文别名: 3-acetyl-N-[1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-1H-pyrazole-5-carboxamide
• 化学式: C₁₉H₁₇ClN₆O₂
• 分子量: 396.8
• InChiKey: GMBPVBVTPBWIKC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  117
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] ANDROGEN RECEPTOR MODULATING CARBOXAMIDES<br/>[FR] CARBOXAMIDES MODULANT LES RÉCEPTEURS D'ANDROGÈNES
  申请人：ORION CORP

  公开号：WO2012143599A1

  公开（公告）日：2012-10-26

  Compounds of formula (I) wherein Rx, Rz, R9, R10, R14, R14', R15, R15', A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.

  公式（I）中的化合物，其中Rx、Rz、R9、R10、R14、R14'、R15、R15'、A和B的定义如索赔中所述，并且其药学上可接受的盐和酯已被披露。这些化合物具有作为组织选择性雄激素受体调节剂（SARM）的效用，并且在治疗前列腺癌和其他依赖于雄激素受体的疾病和病症中特别有用，其中需要AR拮抗作用。
• ANDROGEN RECEPTOR MODULATING COMPOUNDS
  申请人：Wohlfahrt Gerd

  公开号：US20120225867A1

  公开（公告）日：2012-09-06

  The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.

  本公开涉及式(I)的化合物及其药学上可接受的盐。本公开还涉及包括式(I)的化合物及其药学上可接受的盐的组合物和治疗方法。
• Androgen receptor modulating compounds
  申请人：ORION CORPORATION

  公开号：US10118933B2

  公开（公告）日：2018-11-06

  The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.

  本公开涉及式（I）化合物及其药学上可接受的盐。本公开还涉及包含式（I）化合物及其药学上可接受的盐的组合物和治疗方法。
• Manufacture of a crystalline pharmaceutical product
  申请人：ORION CORPORATION

  公开号：US11168058B2

  公开（公告）日：2021-11-09

  The present disclosure relates to crystalline particles of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (I) having specific surface area (SSA) in the range from about 8 to about 16 m2/g, preferably from about 10 to about 15 m2/g, and to the method for the preparation of such particles. Compound (I) is a potent androgen receptor (AR) modulator which is useful as a medicament for example in the treatment of prostate cancer.

  本公开涉及N-((S)-1-(3-(3-氯-4-氰基苯基)-1H-吡唑-1-基)-2-丙基)-5-(1-羟乙基)-1H-吡唑-3-甲酰胺(I)的结晶颗粒，其比表面积(SSA)在约8至约16 m2/g之间，优选约10至约15 m2/g，还涉及制备这种颗粒的方法。化合物(I)是一种强效的雄激素受体（AR）调节剂，可用作治疗前列腺癌等疾病的药物。
• ANDROGEN RECEPTOR MODULATING CARBOXAMIDES
  申请人：Orion Corporation

  公开号：EP2699561B1

  公开（公告）日：2015-06-03