(2S)-N-[(1S)-2-Amino-1-methyl-2-oxoethyl]-2-(4-{[4-(trifluoromethyl)-1,3-oxazol-2-yl]amino} phenyl) propanamide | 1217896-28-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (2S)-N-[(1S)-2-Amino-1-methyl-2-oxoethyl]-2-(4-{[4-(trifluoromethyl)-1,3-oxazol-2-yl]amino} phenyl) propanamide
• 英文别名: (2S)-N-[(2S)-1-amino-1-oxopropan-2-yl]-2-[4-[[4-(trifluoromethyl)-1,3-oxazol-2-yl]amino]phenyl]propanamide
• CAS: 1217896-28-0
• 化学式: C₁₆H₁₇F₃N₄O₃
• 分子量: 370.331
• InChiKey: MKZYVOPIEKSBNO-IUCAKERBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  110
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• 2-aryl-propionic acids and derivatives and pharmaceutical compositions containing them
  申请人：Dompe' S.P.A.

  公开号：EP2166006A1

  公开（公告）日：2010-03-24

  The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single enantiomer (S) and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pcmphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion.

  本发明涉及(R,S) 2-芳基丙酸及其衍生物，它们的单对映体(S)，以及含有它们的药物组合物，用于预防和治疗由于在炎症部位过度招募多形核中性粒细胞（PMN白细胞）而导致的组织损伤。 本发明提供了用于治疗短暂性脑缺血、水疱性天疱疮、类风湿关节炎、特发性纤维化、肾小球肾炎以及缺血再灌注引起的损伤的化合物。
• 2-Aryl-Propionic Acids and Derivatives and Pharmaceutical Compositions Containing Them
  申请人：Allegretti Marcello

  公开号：US20110207785A1

  公开（公告）日：2011-08-25

  The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single enantiomer (S) and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PIvTN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion. (Formula (I)

  本发明涉及(R,S) 2-芳基丙酸及其衍生物，它们的单对映体(S)，以及含有它们的制药组合物，用于预防和治疗由于在炎症部位极化中性粒细胞（PIvTN白细胞）的过度招募而导致的组织损伤。本发明提供了用于治疗短暂性脑缺血、天疱疮、类风湿性关节炎、特发性纤维化、肾小球肾炎以及缺血再灌注引起的损伤的化合物。（公式（I））
• Method for treating cancer using chemokine antagonists
  申请人：Syntrix Biosystems Inc.

  公开号：US10660909B2

  公开（公告）日：2020-05-26

  What is described is a method for treating cancer in a patient in need of such treatment through the use of an antagonist to CXCR1 and/or CXCR2 receptors by administering a therapeutically effective amount of an antagonist of CXCR1 and/or CXCR2, or pharmaceutical compositions thereof, either alone as monotherapy, or in combination with at least one other anticancer therapy.

  所描述的是一种通过使用 CXCR1 和/或 CXCR2 受体拮抗剂治疗需要此类治疗的患者癌症的方法，其方法是施用治疗有效量的 CXCR1 和/或 CXCR2 拮抗剂或其药物组合物，既可单独作为单一疗法，也可与至少一种其他抗癌疗法联合使用。
• 2-ARYL-PROPIONIC ACIDS AND DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：Dompé S.p.A.

  公开号：EP2346841B1

  公开（公告）日：2015-01-14
• METHOD FOR TREATING CANCER USING CHEMOKINE ANTAGONISTS
  申请人：Syntrix Biosystems Inc.

  公开号：US20180177808A1

  公开（公告）日：2018-06-28

  What is described is a method for treating cancer in a patient in need of such treatment through the use of an antagonist to CXCR1 and/or CXCR2 receptors by administering a therapeutically effective amount of an antagonist of CXCR1 and/or CXCR2, or pharmaceutical compositions thereof, either alone as monotherapy, or in combination with at least one other anticancer therapy.