3-isopropyl-1-(quinolin-6-yl)-1H-pyrazol-5-amine | 1012879-76-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-isopropyl-1-(quinolin-6-yl)-1H-pyrazol-5-amine
• 英文别名: 5-propan-2-yl-2-quinolin-6-ylpyrazol-3-amine
• CAS: 1012879-76-3
• 化学式: C₁₅H₁₆N₄
• 分子量: 252.319
• InChiKey: CSUAVOBFNFAZIL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  56.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-isopropyl-1-(quinolin-6-yl)-1H-pyrazol-5-amine 、 lithium hexamethyldisilazane 、 异丙烯基氯甲酸酯 以to provide prop-1-en-2-yl 3-isopropyl-1-(quinolin-6-yl)-1H-pyrazol-5-ylcarbamate (0.85 g, 65% yield)的产率得到prop-1-en-2-yl 3-isopropyl-1-(quinolin-6-yl)-1H-pyrazol-5-ylcarbamate
  参考文献：
  名称：

  Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases

  摘要：

  本发明涉及一种新型化合物，可用于治疗增生性疾病和哺乳动物癌症，特别是人类癌症。该发明还涉及调节激酶活性的方法、制药组合物以及使用这些化合物治疗个体的方法。首选的化合物是公式Ia-Iww中列出的活性小分子。

  公开号：

  US08586565B2
• 作为产物：
  描述：

  1-(diphenylmethylene)-2-(quinolin-6-yl)hydrazine 、 3-氧代-4-甲基戊腈 以to provide to 3-isopropyl-1-(quinolin-6-yl)-1H-pyrazol-5-amine的产率得到3-isopropyl-1-(quinolin-6-yl)-1H-pyrazol-5-amine
  参考文献：
  名称：

  Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases

  摘要：

  本发明涉及一种新型化合物，可用于治疗增生性疾病和哺乳动物癌症，特别是人类癌症。该发明还涉及调节激酶活性的方法、制药组合物以及使用这些化合物治疗个体的方法。首选的化合物是公式Ia-Iww中列出的活性小分子。

  公开号：

  US08586565B2

文献信息

• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Flynn L. Daniel

  公开号：US20080090856A1

  公开（公告）日：2008-04-17

  The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.

  本发明涉及一种在治疗高增殖性疾病和哺乳动物癌症，尤其是人类癌症方面有用的新化合物。该发明还涉及调节激酶活性的方法、药物组合物以及治疗个体的方法，包括或使用这些化合物。优选的化合物是在公式Ia-Iww中列出的活性小分子。
• [EN] METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES<br/>[FR] MÉTHODES ET COMPOSITIONS POUVANT ÊTRE UTILISÉES EN VUE DU TRAITEMENT DE MALADIES MYÉLOPROLIFÉRATIVES ET D'AUTRES MALADIES PROLIFÉRATIVES
  申请人：DECIPHERA PHARMACEUTICALS LLC

  公开号：WO2013036232A2

  公开（公告）日：2013-03-14

  Compounds of the present invention find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites secondary sites, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, thyroid cancer, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, i.e. diabetic retinopathy and age-related macular degeneration, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, human inflammation, rheumatoid spondylitis, ostero-arthritis, asthma, gouty arthritis, sepsis, septic shock, endotoxic shock, Gram-negative sepsis, toxic shock syndrome, adult respiratory distress syndrome, stroke, reperfusion injury, neural trauma, neural ischemia, psoriasis, restenosis, chronic obstructive pulmonary disease, bone resorptive diseases, graft-versus-host reaction, Crohn's disease, ulcerative colitis, inflammatory bowel disease, pyresis, and combinations thereof, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, c-KIT kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, VEGFR kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, PDGFR kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, FLT-3 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, TIE-2 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, TRK kinases, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, c-MET kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a HER kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

  本发明的化合物在治疗增生性疾病、哺乳动物癌症，特别是人类癌症方面具有实用性，包括但不限于恶性黑色素瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、宫颈癌、原发肿瘤部位和转移部位的转移、骨髓增生性疾病、慢性髓性白血病、急性淋巴细胞白血病、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、甲状腺癌、眼部疾病，包括各种视网膜病变，如糖尿病性视网膜病变和老年性黄斑变性、类风湿性关节炎、哮喘、慢性阻塞性肺疾病、人类炎症、类风湿脊柱炎、骨关节炎、痛风性关节炎、败血症、脓毒症、内毒素性休克、革兰氏阴性菌感染、毒性休克综合症、成人呼吸窘迫综合症、中风、再灌注损伤、神经创伤、神经缺血、银屑病、再狭窄、慢性阻塞性肺疾病、骨吸收性疾病、移植物抗宿主反应、克罗恩病、溃疡性结肠炎、炎症性肠病、发热和以上疾病的组合，由c-ABL激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，c-KIT激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，VEGFR激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，PDGFR激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，FLT-3激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，TIE-2激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，TRK激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，c-MET激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病，或由HER激酶、其致癌形式、异常融合蛋白和多态形式引起的疾病。
• Kinase inhibitors useful for the treatment of proliferative diseases
  申请人：Flynn L. Daniel

  公开号：US20080114006A1

  公开（公告）日：2008-05-15

  The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

  本发明涉及一种新型激酶抑制剂和调节剂化合物，用于治疗各种疾病。更具体地说，本发明涉及这样的化合物、激酶/化合物加合物、治疗疾病的方法以及合成化合物的方法。优选地，这些化合物对Raf激酶及其疾病多态性的激酶活性调节是有用的。本发明的化合物在哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑色素瘤、结肠直肠癌、卵巢癌、乳头状甲状腺癌、非小细胞肺癌和间皮瘤的治疗中发挥作用。本发明的化合物也在治疗类风湿性关节炎和视网膜病变，包括糖尿病性视网膜神经病变和黄斑变性方面发挥作用。
• Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
  申请人：Deciphera Pharmaceuticals, Inc.

  公开号：US08188113B2

  公开（公告）日：2012-05-29

  The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

  本发明涉及一种新型的二氢吡啶吡嗪基，二氢萘嗪基和相关化合物，这些化合物是激酶抑制剂和调节剂，可用于治疗各种疾病。更具体地说，本发明涉及这些化合物，激酶/化合物加合物，治疗疾病的方法以及合成这些化合物的方法。优选地，这些化合物对Raf激酶及其疾病多态体的激酶活性的调节具有用处。本发明的化合物在哺乳动物癌症治疗中，特别是人类癌症治疗中，包括但不限于恶性黑色素瘤、结肠直肠癌、卵巢癌、乳头状甲状腺癌、非小细胞肺癌和间皮瘤中具有用处。本发明的化合物在类风湿性关节炎和视网膜病变治疗中也具有用处，包括糖尿病性视网膜神经病变和黄斑变性。
• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
  申请人：Flynn Daniel L.

  公开号：US20120289540A1

  公开（公告）日：2012-11-15

  The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

  本发明涉及新型激酶抑制剂和调节剂化合物，可用于治疗各种疾病。更具体地说，本发明涉及这种化合物、激酶/化合物加合物、治疗疾病的方法以及化合物的合成方法。优选地，这些化合物可用于调节Raf激酶及其疾病多态性的激酶活性。本发明的化合物在哺乳动物癌症治疗中特别是人类癌症治疗中，包括但不限于恶性黑色素瘤、结直肠癌、卵巢癌、乳头状甲状腺癌、非小细胞肺癌和间皮瘤等方面有用。本发明的化合物还在类风湿性关节炎和视网膜病变，包括糖尿病视网膜神经病变和黄斑变性的治疗中有用。