1-(5-Methanesulfonyl-pyridin-2-yl)-5-phenoxyamino-3-trifluoromethyl-1H-pyrazole-4-carbonitrile | 519008-30-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-(5-Methanesulfonyl-pyridin-2-yl)-5-phenoxyamino-3-trifluoromethyl-1H-pyrazole-4-carbonitrile
• 英文别名: 1-(5-Methylsulfonylpyridin-2-yl)-5-(phenoxyamino)-3-(trifluoromethyl)pyrazole-4-carbonitrile
• CAS: 519008-30-1
• 化学式: C₁₇H₁₂F₃N₅O₃S
• 分子量: 423.375
• InChiKey: DWTAPVQNORSFRA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  118
• 氢给体数：
  1
• 氢受体数：
  10

文献信息

• Hydrazinyl and nitrogen oxide pyrazoles
  申请人：Pfizer Inc.

  公开号：US20030134850A1

  公开（公告）日：2003-07-17

  The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: 1 wherein the ring of the formula (R 5 )-A-(SO m R 4 ), m, X, R 1 through R 5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

  本发明涉及式I的肼基和氮氧化物吡唑：1其中，式（R5）-A-（SOmR4），m，X，R1至R5的环如规范中所定义，以及包含它们的制药组合物和它们的医药用途。本发明的化合物在哺乳动物中，尤其是人类、狗、猫和家畜动物中，用于治疗或缓解炎症和其他与炎症相关的疾病，如关节炎、结肠癌和阿尔茨海默病。
• Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
  申请人：Huang Q. Charles

  公开号：US20050038056A1

  公开（公告）日：2005-02-17

  GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein n, R 1a , R 1b , R 1c , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

  本发明揭示了一种GnRH受体拮抗剂，可用于治疗男性和女性的各种性激素相关疾病。本发明的化合物具有以下结构：其中n，R1a，R1b，R1c，R2a，R2b，R3，R4，R5，R6和X如此定义，包括立体异构体，前药和其药物学上可接受的盐。本发明还揭示了含有本发明化合物与药物学上可接受的载体组合的组合物，以及与拮抗需要拮抗促性腺激素释放激素的受试者有关的使用方法。
• Sulfonylaryl- and sulfonylheteroaryl-pyrazoles with a hydrazinyl or nitrogen oxide substituent at the 5-position for use as cyclooxygenase inhibitors
  申请人：Pfizer Productors Inc.

  公开号：EP1308158A1

  公开（公告）日：2003-05-07

  The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

  本发明涉及式 I 的肼基和氧化氮吡唑： 其中式(R5)-A-(SOmR4)的环、m、X、R1至R5如说明书中所定义，本发明涉及含有它们的药物组合物及其药用用途。本发明的化合物可用于治疗或缓解哺乳动物（最好是人、狗、猫和家畜）的炎症和其他炎症相关疾病，如关节炎、结肠癌和阿尔茨海默病。
• US6864252B2
  申请人：——

  公开号：US6864252B2

  公开（公告）日：2005-03-08