1,2-Benzoxazole;1,3-thiazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并异恶唑
• 英文名称: 1,2-Benzoxazole;1,3-thiazole
• 英文别名: 1,2-benzoxazole;1,3-thiazole
• 化学式: C10H8N2OS
• 分子量: 204.25
• InChiKey: DTVSMNPZZCMFNT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.97
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.2
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] INHIBITORS OF HEPATOCYTE GROWTH FACTOR [HGF] AND MACROPHAGE STIMULATING PROTEIN [MSP] MATURATION<br/>[FR] INHIBITEURS DE MATURATION DU FACTEUR DE CROISSANCE HÉPATOCYTAIRE (HGF] ET DE LA PROTÉINE DE STIMULATION DES MACROPHAGES [MSP]
  申请人：SOUTHERN RES INST

  公开号：WO2015184222A1

  公开（公告）日：2015-12-03

  Provided are certain cyclic urea compounds that are capable of inhibiting certain serine proteases, and especially the serine proteases matriptase, hepsin and hepatocyte growth factor activator (HGFA) involved in the maturation of hepatocyte growth factor (HGF) and macrophage stimulating protein (MSP), and novel precursors thereof. Compounds of the present disclosure can be used to treat a number of disorders caused by or associated with abnormal matriptase, hepsin and HGFA protease activity by inhibiting the proteolytic cleavage of pro-HGF to mature HGF and pro-MSP to mature MSP caused by these enzymes. Compounds of the present disclosure can be used to treat disorders including precancerous conditions and cancer including metastatic disease, prevention and reversion of cancer resistance, and the inhibition of cancer stem cells. The compounds of this invention are applicable to the treatment of cancers of many tissue types including solid and liquid tumors.

  提供了一些能够抑制特定丝氨酸蛋白酶的环脲化合物，尤其是涉及肝细胞生长因子（HGF）和巨噬细胞刺激蛋白（MSP）成熟的丝氨酸蛋白酶matriptase、hepsin和肝细胞生长因子激活酶（HGFA），以及其新颖前体。本公开的化合物可用于治疗由或与异常matriptase、hepsin和HGFA蛋白酶活性相关的多种疾病，通过抑制这些酶引起的pro-HGF到成熟HGF和pro-MSP到成熟MSP的蛋白水解裂解。本公开的化合物可用于治疗包括癌前病变和癌症（包括转移性疾病、预防和逆转癌症耐药性以及抑制癌干细胞）在内的多种疾病。本发明的化合物适用于治疗多种组织类型的癌症，包括实体肿瘤和液体肿瘤。
• TRIAZOLOPYRIDAZINE COMPOUNDS, USE AS INHIBITORS OF THE KINASE LRRK2, AND METHODS FOR PREPARATION THEREOF
  申请人：Southern Research Institute

  公开号：EP2844660A1

  公开（公告）日：2015-03-11
• [EN] TRIAZOLOPYRIDAZINE COMPOUNDS, USE AS INHIBITORS OF THE KINASE LRRK2, AND METHODS FOR PREPARATION THEREOF<br/>[FR] COMPOSÉS DE TRIAZOLOPYRIDAZINE, UTILISATION COMME INHIBITEURS DE LA KINASE LRRK2, ET PROCÉDÉS POUR LEUR PRÉPARATION
  申请人：SOUTHERN RES INST

  公开号：WO2013166276A1

  公开（公告）日：2013-11-07

  The present invention provides novel LRRK2 kinase inhibitors and methods of treating disease states using these inhibitors. Certain triazolopyridazine compounds have been discovered according to the present disclosure that inhibit LRRK2, and therefore find utility in the treatment of a number of disorders neurodegenerative diseases such as Parkinson's disease; precancerous conditions and cancer; autoimmune disorders such as Crohn's disease, rheumatoid arthritis and psoriasis; and leprosy.