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浮米每周专利快讯：2014年12月（四） 作者：浮米网 来源：浮米网 2014-12-25
1. WO 2014187932 标题: Pyridone derivatives for the treatment of viral infections and further diseases 申请人: Janssen R&D Ireland 优先权日期及相关专利公开号: 2013 EP 169076 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: 病毒感染、免疫疾病和炎症 专利摘要: This invention relates to pyridone derivatives, processes for their preparation, phamaceutical compositions, and their use in therapy. 备注: TLR7和TLR8激动剂可用于治疗病毒感染、免疫疾病和炎症。本发明的化合物可以激活TLR7和TLR8 （LEC= 0.9和2.7 mcM。 2. WO 2014188211 标题: Heterocyclic derivates 申请人: Kalvista Pharmaceuticals Ltd. 优先权日期及相关专利公开号: 2013 US 826596 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: 血管性视网膜病 专利摘要: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R5, R6, R7, A, B,W, X, Y and Z are as defined herein. 备注: KLKB1抑制剂可以治疗血管性视网膜病、心肌病、糖尿病、炎症性肠病、肾病、神经病变、胰腺炎、关节炎和癌症等。本发明的化合物可以抑制KLKB1，IC50 = 1.89 nM, 且对KLK1（IC50 = 8860 nM)Factor XIIa (IC50 > 10000 nM)具有选择性。 3. CN 104163851 标题: Fluorinated alpha-keto amide and HCV NS3/4A serine protease inhibitor containing said component 申请人: Beijing Xintianyu Technology Development Co., Ltd. 优先权日期及相关专利公开号: 2013 CN 10186244 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: 丙肝 专利摘要: A novel fluorinated HCV NS3/4A serine protease inhibitor, salt thereof, stereoisomer thereof, and preparation method thereof, as shown below in (1), and at least containing as an active ingredient a pharmaceutical formulation of the inhibitor, salt thereof, or stereoisomer thereof, and application in the prevention and treatment of the disease hepatitis C. R1, R2, and R3 are as defined in the description. Not only does the inhibitor not undergo epimerization, but inhibition of HCT activity is also improved. 备注: HCV NS3 NS4A 蛋白抑制剂可以治疗HCV感染。本发明的化合物可以抑制HCV复制(IC50 = 0.19 mcM)。 4. WO 2014187343 标题: Benzofuran derivative, preparation method therefor, and medical application thereof 申请人: Sichuan Haisco Pharmaceutical Co., Ltd. 优先权日期及相关专利公开号: 2013 CN 10192084 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: II型糖尿病 专利摘要: Disclosed are a benzofuran derivative, a preparation method therefor, and a medical application thereof, specifically relating to a compound represented by general formula (I), a stereoisomer thereof, a hydrate thereof, a solvate thereof, an eutecticum thereof, a pharmaceutically accepted salt or prodrug thereof, a preparation method therefor, a pharmaceutical composition comprising the benzofuran derivative, and a medical application of the compound or pharmaceutical composition, especially as a GPR40 receptor (G-protein coupled receptor) agonist, wherein definitions of substituent groups in general formula (I) are the same as definitions in the specification. 备注: GPR40激动剂可以治疗糖尿病，对II型糖尿病尤其有效。本发明的化合物对GPR40的EC50=17.36 nM。 5. WO 2014187365 标题: Oxabicyclo derivatives, preparation method and use thereof 申请人: Sichuan Haisco Pharmaceutical Co., Ltd. 优先权日期及相关专利公开号: 2013 CN 10198829 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: II型糖尿病 专利摘要: The present invention relates to a oxabicyclo derivative, preparation method and use thereof, specifically to oxabicyclo derivatives shown by general formula (I) or hydrates, solvates, stereoisomers thereof, pharmaceutically acceptable salts, co-crystals, prodrugs, preparation methods, pharmaceutical compositions comprising the derivatives and pharmaceutical uses for preparing sodium-dependent glucose transporter (SGLT) inhibitors, and the definition of each substituent in general formula (I) is the same as that in description. 备注: SGLT-2抑制剂可用于治疗II型糖尿病及其他代谢类疾病，如肥胖、高脂血症、动脉粥样硬化、高血压、糖尿病肾病、神经病变、视网膜病变等。本发明的化合物可以抑制SGLT-2 (IC50 = 1.3 nM)，且对SGLT-1具有选择性(IC50 = 1096 nM)。 6. WO 2014190949 标题: Quadri-fused cyclic anaplastic lymphoma kinase inhibitor 申请人: XuanZhu Pharma Co., Ltd. 优先权日期及相关专利公开号: 2013 CN 10214667 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: 癌症 专利摘要: Provided are the compounds as shown by formula (I) or the stereoisomers thereof, or the pharmaceutically acceptable salts, esters, or solvates thereof, wherein A1, A2, A3, M, Y, X, R3, R5, R6, R7, Q and n are as defined in the description, the preparation method of these compounds, pharmaceutical preparations and pharmaceutical compositions containing these compounds, and the use of the compounds or the stereoisomers thereof, or the pharmaceutically acceptable salts, esters, or solvates thereof in the preparation of drugs for the treatment and/or prevention of diseases associated with cancers mediated by ALK. 备注: ALK抑制剂可用于治疗癌症。本发明的化合物可以抑制ALK，IC50=1.3 nM。 7. WO 2014193696 标题: Benzimidazole carboxylic acid derivatives, compositions, and methods of use as aurora kinase inhibitors 申请人: TransTech Pharma, LLC 优先权日期及相关专利公开号: 2013 US 828040 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: 癌症 专利摘要: The invention provides benzimidazole carboxylic acid derivatives that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods of treatment using the compounds of the present invention or pharmaceutical compositions comprising compounds of the present invention. 备注: Aurora激酶抑制剂前药可用于治疗癌症。本发明中Aurora A抑制剂的IC50 = 6.1 nM。 8. WO 2014187262 标题: Bruton’s tyrosine kinase inhibitor 申请人: Jiangsu Simcere Pharmaceutical R&D Co., Ltd. 优先权日期及相关专利公开号: 2013 CN 10192167 相关候选药物类型: 小分子药物 相关候选药物化学结构:
适应症: 类风湿性关节炎 专利摘要: Provided are a 2-phenyl-isoquinoline-1-ketone derivative having a structure of formula (I), and uses thereof. The compound has good inhibitory effect on Bruton’s tyrosine kinase activity, and the median inhibition concentration of the compound is generally below 10-7 mol.L-1. The compound having the structure of formula (I) and prepared in an embodiment of the present invention has clear anti-inflammatory activity on different animal models. 备注: BTK抑制剂对类风湿性关节炎有效。本发明的化合物对BTK的IC50=18.73 nM。
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