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浮米每周专利快讯：2015年5月
1. WO 2015069512 标题: Pyrido[2,3-d]pyrimidin-4-one compounds as tankyrase inhibitors 申请人: 礼来 优先权日期及相关专利公开号: 2013 US 901023 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: Pyrido[2,3-d]pyrimidin-4-one compounds, formulations containing those compounds, and their use as tankyrase 1 and 2 inhibitors Formula (I). 备注: TNKS1和TNKS2是治疗肿瘤的有效靶点。示例化合物对人TNKS1和TNKS2抑制活性分别为IC50 = 19.1和13.7 nM，选择性较高。在小鼠模型中显示出抑癌活性。 2. WO 2015069441 标题: Pyrazolo-, imidazolo- and pyrrolo-pyridine or -pyrimidine derivatives as inhibitors of Bruton’s kinase (Btk) 申请人: Medivation Technologies, Inc. 优先权日期及相关专利公开号: 2013 IN 4713 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、风湿性关节炎 专利摘要: The present application discloses compounds that are inhibitors of Btk, compounds that are inhibitors of PI3Kd, and compounds that are dual inhibitors of both Btk and PI3Kd. Also described are methods for synthesizing such inhibitors and methods for using such inhibitors for the treatment of diseases wherein inhibition of Btk and PI3Kd provides a therapeutic benefit to a patient having the disease. 备注: BTK和PI3Kdelta的双抑制剂可用于治疗癌症、风湿性关节炎和其他自身免疫性疾病。示例化合物对BTK和PI3Kdelta的抑制活性分别为IC50 = 0.167和0.0100 mcM，且选择性较高。 3. WO 2015067923 标题: NMDA antagonist prodrugs 申请人: 阿斯利康 优先权日期及相关专利公开号: 2013 US 899903 相关候选药物类型: 小分子药物、前药 相关候选药物化学结构: 适应症: 燥郁症、抑郁、癫痫、强迫性精神障碍 专利摘要: Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them. 备注: Lanicemine前药作为NMDA拮抗剂，用于治疗抑郁、疼痛、瑞特综合征、癫痫等。示例化合物在肠液、肝S9段、血液中转化为自由态Lanicemine。 4. WO 2015069593 标题: Substituted pyridine derivatives useful as GSK-3 inhibitors 申请人: Bristol-Myers Squibb 优先权日期及相关专利公开号: 2013 US 900547 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: 阿尔兹海默型痴呆 专利摘要: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. 备注: GSK-3是治疗阿尔兹海默病的有效靶点。示例化合物对GSK-3β和GSK-3α的有效抑制活性分别为IC50 = 0.15 and 0.10 nM 5. US 2015133447/WO 2015067770 标题: Triazolopyrazine derivatives as BRD4 inhibitors 申请人: 勃林格殷格翰 优先权日期及相关专利公开号: 2013 EP 192002 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 present invention encompasses compounds of general formula (I), wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament. 备注: 溴区包含蛋白4（Brd4，HUNK1)抑制剂对治疗癌症有效。示例化合物抑制四乙酰化组蛋白H4与GST-Brd4-BD1溴区的相互作用，活性为IC50 = 9 nM。
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