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浮米每周专利快讯：2015年3月（一） 作者：浮米网 来源：浮米网 2015-03-17
1. WO 2015019365 标题: N-Cyanomethylamides as inhibitors of Janus kinase 申请人: Cadila Healthcare Ltd. (d/b/a Zydus Cadila) 相关候选药物类型: 小分子化合物 相关候选药物化学结构: 适应症: 癌症、过敏、炎症、自身免疫性疾病、移植排斥反应 专利摘要: The present invention relates to compounds of general formula (1) that are inhibitors of Janus Kinase (JAK), a family of tyrosine kinases that are involved in inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound of the invention inhibits JAK1 and/or JAK2 and/or JAK3 sub families. The present invention also provides methods for the production of the compounds of the invention, pharmaceutical compositions comprising the compounds of the invention, their tautomeric forms, and their pharmaceutically acceptable salts. 备注: Jak抑制剂可以治疗癌症、过敏、炎症、自身免疫性疾病和移植排斥反应等疾病。本发明的化合物对 Jak1, Jak2和Jak3的IC50分别为12, 8 and 48 nM。 2. 标题: Compounds and compositions as inhibitors of MEK 申请人: 诺华 相关候选药物类型: 小分子化合物 相关候选药物化学结构: 专利摘要: The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer. 备注: MEK抑制剂可以用于治疗癌症。本发明的化合物可以抑制BRAF-MEK-ERK信号通路(IC50 = 0.005 mcM)。 3. 标题: Compounds and compositions as inhibitors of MEK 申请人: 诺华 相关候选药物类型: 小分子化合物 相关候选药物化学结构: 专利摘要: The present invention relates to compounds of formula I: in which n, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer and 10 inflammation. 备注: MEK抑制剂可以用于治疗癌症。本发明的化合物可以抑制BRAF-MEK-ERK信号通路(IC50 = 0.0023 mcM)。 4. WO 2015022663 标题: Compounds and compositions as inhibitors of MEK 申请人: 诺华 相关候选药物类型: 小分子化合物 相关候选药物化学结构: 适应症: 癌症 专利摘要: The present invention relates to compounds of formula I: in which n, Y, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer and inflammation. 备注: MEK抑制剂可以用于治疗癌症。本发明的化合物可以抑制BRAF-MEK-ERK信号通路(IC50 =0.01 mcM). 5. WO 2015023915 标题: Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof 申请人: Constellation Pharmaceuticals, Inc. 相关候选药物类型: 小分子化合物 相关候选药物化学结构: 适应症: 癌症 专利摘要: Agents of formulas (l)/(ll)/(lll) for modulating methyl modifying enzymes, compositions and uses thereof are provided herein. 备注: EZH2抑制剂可用于治疗肿瘤疾病。本发明的化合物可以抑制野生型和Y641N突变型EZH2(IC50均小于100 nM)。同时对HeLa细胞的EC50 400 nM。 6. WO 2015025018 标题: New bis-amido pyridines 申请人: 勃林格殷格翰 相关候选药物类型: 小分子化合物 相关候选药物化学结构: 适应症: 癌症 专利摘要: This invention relates to bis-amidopyridinesof general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification. 备注: SMAC类似物可以作为XIAP抑制剂，以用于肿瘤疾病的治疗，本发明的化合物可以抑制SMAC肽和XIAP或IAP2的结合，其IC50=10和1 nM。 7. WO 2015025019 标题: New 6-alkynyl pyridine 申请人: 勃林格殷格翰 相关候选药物类型: 小分子化合物 适应症: 癌症 专利摘要: This invention relates to 6-alkynyl-pyridine of general formula (I), their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification. 备注: SMAC类似物可以作为XIAP抑制剂，以用于肿瘤疾病的治疗，本发明的化合物可以抑制SMAC肽和XIAP或IAP2的结合，其IC50=10和1 nM。 8. EP 2837626 标题: Indolinone derivatives as GRK5 modulators 申请人: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften eV 相关候选药物类型: 小分子化合物 适应症: 癌症、2型糖尿病 专利摘要: The present invention relates to benzopyrrolidone derivatives of formula (I) and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of metabolic diseases and cancer, and pharmaceutical compositions containing at least one of said benzopyrrolidone derivatives and/or pharmaceutically acceptable salts thereof. Metabolic diseases include diabetes, obesity and impaired adipogenesis. Furthermore, the present invention relates to the use of said benzoypyrrolidone derivatives as GRK5 inhibitors, thereby regulating the glucose dependent insulin production and/or release. 备注: GRK5抑制剂可以用于治疗2型糖尿病和癌症。本发明的化合物可以抑制GRK5，IC50在0.1~1.0 mcM 。 9. WO 2015014815 标题: Thieno[3,2-d]pyrimidines derivatives for the treatment of viral infections 申请人: 杨森 相关候选药物类型: 小分子化合物 相关候选药物化学结构: 适应症: 病毒感染、免疫疾病、炎症 专利摘要: This invention relates to thieno[3,2-d]pyrimidinesderivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections. 备注: TLR7/TLR8激动剂可以用于治疗病毒感染、免疫疾病和炎症。本发明的化合物可以激活TLR8（LEC=0.03 mcM)，且对TLR7 (LEC = 0.5 mcM) 具有选择性。
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