6-Chloro-1-methyl-1H-indazol-3-amine | 1031927-22-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 6-Chloro-1-methyl-1H-indazol-3-amine
• 英文别名: 6-chloro-1-methylindazol-3-amine
• CAS: 1031927-22-6
• 化学式: C₈H₈ClN₃
• mdl: MFCD09991761
• 分子量: 181.62
• InChiKey: DVNUOUTWILBEAP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  43.8
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  6-Chloro-1-methyl-1H-indazol-3-amine 、 [3-((R)-5-amino-3-methyl-3,6-dihydro-2H-[1,4]oxazin-3-yl)-4-fluoro-phenyl]-(6-chloro-1-methyl-1H-indazol-3-yl)-amine 、 生成 (S)-5-(5-(6-chloro-1-methyl-1H-indazol-3-ylamino)-2-fluorophenyl)-5-methyl-5,6-dihydro-2H-1,4-oxazin-3-amine
  参考文献：
  名称：

  1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS

  摘要：

  本发明涉及具有BACE1和/或BACE2抑制活性的1,4-噁唑烷的公式I，它们的制造，含有它们的制药组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病方面有用。

  公开号：

  US20120184540A1

文献信息

• 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
  申请人：Andreini Matteo

  公开号：US20120184540A1

  公开（公告）日：2012-07-19

  The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4噁嗪，它们的制造，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病等疾病方面是有用的。
• [EN] 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS<br/>[FR] 1,4 OXAZINES UTILISÉS COMME INHIBITEURS DE BACE1 ET/OU BACE2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2012098064A1

  公开（公告）日：2012-07-26

  The present invention relates to 1,4 Oxazines of formula (I): having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明涉及具有BACE1和/或BACE2抑制活性的式(I)的1,4噁嗪，它们的制备，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病方面是有用的。
• COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
  申请人：Ibrahim Prabha N.

  公开号：US20110183988A1

  公开（公告）日：2011-07-28

  Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including melanoma, glioma, glioblastoma, pilocytic astrocytoma, liver cancer, biliary tract cancer, cholangiocarcinoma, colorectal cancer, lung cancer, bladder cancer, gallbladder cancer, breast cancer, pancreatic cancer, thyroid cancer, kidney cancer, ovarian cancer, adrenocortical cancer, prostate cancer, gastrointestinal stromal tumors, medullary thyroid cancer, tumor angiogenesis, acute myeloid leukemia, chronic myelomonocytic leukemia, childhood acute lymphoblastic leukemia, plasma cell leukemia, and multiple myeloma.

  描述了化合物及其盐、制剂、共轭物、衍生物、形式和用途。在某些方面和实施例中，所述的化合物或其盐、制剂、共轭物、衍生物、形式对B-Raf、B-Raf V600E和c-Raf-1蛋白激酶均具有活性。在某些方面和实施例中，所述的化合物在抑制Ras突变细胞系增殖方面具有活性。还描述了使用它们治疗疾病和病况的方法，包括黑色素瘤、胶质瘤、胶质母细胞瘤、毛细胞星形细胞瘤、肝癌、胆管癌、胆管细胞癌、结直肠癌、肺癌、膀胱癌、胆囊癌、乳腺癌、胰腺癌、甲状腺癌、肾癌、卵巢癌、肾上腺皮质癌、前列腺癌、胃肠道间质瘤、髓样甲状腺癌、肿瘤血管生成、急性髓系白血病、慢性髓细胞/单核细胞白血病、儿童急性淋巴细胞白血病、浆细胞白血病和多发性骨髓瘤。
• SOLUBLE GUANYLATE CYCLASE ACTIVATORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2575473B1

  公开（公告）日：2016-01-20
• US9242943B2
  申请人：——

  公开号：US9242943B2

  公开（公告）日：2016-01-26