1-((4-fluorophenyl)(methyl)carbamoyl)cyclopropane-1-carboxylic acid | 918642-72-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-((4-fluorophenyl)(methyl)carbamoyl)cyclopropane-1-carboxylic acid
• 英文别名: 1-((4-Fluorophenyl)(methyl)carbamoyl)cyclopropanecarboxylic acid；1-[(4-fluorophenyl)-methylcarbamoyl]cyclopropane-1-carboxylic acid
• CAS: 918642-72-5
• 化学式: C₁₂H₁₂FNO₃
• 分子量: 237.231
• InChiKey: ZMZIFNJZAFDVFO-UHFFFAOYSA-N

物化性质

• 沸点：
  410.5±30.0 °C(Predicted)
• 密度：
  1.435±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  57.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-((4-fluorophenyl)(methyl)carbamoyl)cyclopropane-1-carboxylic acid 在 氯化亚砜 作用下， 以 二氯甲烷 为溶剂， 6.0~85.0 ℃ 、101.33 kPa 条件下， 反应 24.0h， 生成 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)-1-N'-methylcyclopropane-1,1-dicarboxamide hydrochloride
  参考文献：
  名称：

  WO2020154610A5

  摘要：

  公开号：

  WO2020154610A5
• 作为产物：
  描述：

  4-氟-N-甲基苯胺 在 lithium hydroxide monohydrate 、 水 、 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 反应 23.0h， 生成 1-((4-fluorophenyl)(methyl)carbamoyl)cyclopropane-1-carboxylic acid
  参考文献：
  名称：

  [EN] COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS
  [FR] COMPOSÉS POUR LE TRAITEMENT DE TROUBLES DÉPENDANT DE LA KINASE

  摘要：

  本文揭示了一种Formula (I)的化合物，它们可以抑制、调节和/或调控酪氨酸激酶受体，特别是与细胞活动变化相关的Axl和Mer信号转导途径，包含这些化合物的组合物，使用这些化合物治疗激酶依赖性疾病和病况的方法，以及制备这些化合物的方法。

  公开号：

  WO2020247418A1

文献信息

• [EN] CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES<br/>[FR] AMIDES DE CYCLOPROPANE ET ANALOGUES PRÉSENTANT DES ACTIVITÉS ANTICANCÉREUSES ET ANTIPROLIFÉRATIVES
  申请人：DECIPHERA PHARMACEUTICALS LLC

  公开号：WO2010051373A1

  公开（公告）日：2010-05-06

  Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.

  本发明的化合物在治疗哺乳动物癌症，尤其是人类癌症方面具有实用性，包括但不限于恶性黑色素瘤、实体肿瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、肝癌、宫颈癌、原发肿瘤部位的转移、骨髓增生性疾病、慢性髓细胞白血病、白血病、乳头状甲状腺癌、非小细胞肺癌、间皮瘤、高嗜酸性综合征、胃肠道间质瘤、结肠癌、由高增殖导致失明的眼部疾病，包括各种视网膜病变、糖尿病视网膜病变、类风湿性关节炎、哮喘、慢性阻塞性肺病、肥大细胞增多症、肥大细胞白血病，以及由PDGFR-α激酶、PDGFR-β激酶、c-KIT激酶、cFMS激酶、c-MET激酶和致癌形式、异常融合蛋白和任何上述激酶的多态体引起的疾病。
• Inhibitors of VEGF receptor and HGF receptor signaling
  申请人：Saavedra Mario Oscar

  公开号：US20070004675A1

  公开（公告）日：2007-01-04

  The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions

  该发明涉及抑制VEGF受体信号和HGF受体信号。该发明提供了抑制VEGF受体信号和HGF受体信号的化合物和方法。该发明还提供了治疗细胞增殖性疾病和病况的组合物和方法。
• CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
  申请人：Flynn Daniel L.

  公开号：US20100120806A1

  公开（公告）日：2010-05-13

  Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.

  本发明的化合物在哺乳动物癌症治疗中具有实用性，特别是人类癌症，包括但不限于恶性黑色素瘤、实体肿瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、肝癌、宫颈癌、原发肿瘤部位的转移、骨髓增生性疾病、慢性髓性白血病、白血病、乳头状甲状腺癌、非小细胞肺癌、间皮瘤、高嗜酸性综合症、胃肠道间质瘤、结肠癌、眼部疾病，其特征为细胞过度增殖导致失明，包括各种视网膜病变、糖尿病视网膜病变、类风湿性关节炎、哮喘、慢性阻塞性肺疾病、肥大细胞增多症、肥大细胞白血病以及由PDGFR-α激酶、PDGFR-β激酶、c-KIT激酶、cFMS激酶、c-MET激酶和任何上述激酶的癌变形式、异常融合蛋白和多态性引起的疾病。
• N-acyl ureas exhibiting anti-cancer and anti-proliferative activities
  申请人：Deciphera Pharmaceuticals, LLC

  公开号：US08278331B2

  公开（公告）日：2012-10-02

  Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.

  本发明的化合物在哺乳动物癌症的治疗中具有实用性，特别是人类癌症，包括但不限于恶性黑色素瘤、实体肿瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、肝癌、宫颈癌、原发性肿瘤部位的转移、骨髓增生性疾病、慢性髓细胞白血病、白血病、乳头状甲状腺癌、非小细胞肺癌、间皮瘤、高嗜酸性综合征、胃肠间质肿瘤、结肠癌、眼部疾病，其特征为过度增殖导致失明，包括各种视网膜病变、糖尿病视网膜病变、类风湿性关节炎、哮喘、慢性阻塞性肺疾病、肥大细胞增多症、肥大细胞白血病，以及由PDGFR-α激酶、PDGFR-β激酶、c-KIT激酶、cFMS激酶、c-MET激酶和任何上述激酶的癌变形式、异常融合蛋白和多态性引起的疾病。
• INHIBITORS OF VEGF RECEPTOR AND HGF RECEPTOR SIGNALING
  申请人：Saavedra Oscar Mario

  公开号：US20120083482A1

  公开（公告）日：2012-04-05

  The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A 1 is sulfur, A 3 is CH, A 2 is CH, D is heterocycle, Z is oxygen, SO 0-2 or NR, Ar is phenyl and G is not a ring, and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

  本发明涉及抑制VEGF受体信号和HGF受体信号的技术。本发明提供了通式（A）的化合物，其中A1为硫，A3为CH，A2为CH，D为杂环，Z为氧，SO0-2或NR，Ar为苯基，G不是环，并提供了抑制VEGF受体信号和HGF受体信号的方法。本发明还提供了治疗细胞增殖性疾病和病情的组合物和方法。