2-Ethoxy-3-(fluoromethyl)-5-nitropyridine

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 2-Ethoxy-3-(fluoromethyl)-5-nitropyridine
• 英文别名: 2-ethoxy-3-(fluoromethyl)-5-nitropyridine
• 化学式: C8H9FN2O3
• 分子量: 200.17
• InChiKey: QIWRXDVFVNLJPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  67.9
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US20150099762A1

  公开（公告）日：2015-04-09

  This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.

  本发明涉及一种新型化合物，其为重排转录因子（RET）激酶抑制剂，包含它们的制药组合物，其制备方法，以及它们在治疗中的应用，单独或联合使用，用于正常化胃肠敏感性、运动性和/或分泌以及腹部疾病或疾病相关的治疗，其中包括但不限于所有分类的肠易激综合症（IBS），包括腹泻型、便秘型或交替排便型，功能性膨胀、功能性便秘、功能性腹泻、未特指的功能性肠道疾病、功能性腹痛综合征、慢性特发性便秘、功能性食管障碍、功能性胃十二指肠障碍、功能性肛门疼痛、炎症性肠病、增殖性疾病，如非小细胞肺癌、肝细胞癌、结肠直肠癌、髓样甲状腺癌、滤泡性甲状腺癌、间叶甲状腺癌、乳头状甲状腺癌、脑肿瘤、腹腔癌、实体瘤、其他肺癌、头颈癌、胶质母细胞瘤、神经母细胞瘤、Von Hippel-Lindau综合症和肾肿瘤、乳腺癌、输卵管癌、卵巢癌、移行细胞癌、前列腺癌、食管和胃食管交界处癌、胆管癌、腺癌以及任何具有增加RET激酶活性的恶性肿瘤。
• US20140275111A1
  申请人：——

  公开号：US20140275111A1

  公开（公告）日：2014-09-18
• US8937071B2
  申请人：——

  公开号：US8937071B2

  公开（公告）日：2015-01-20