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浮米每周专利快讯：2014年11月（二） 作者：浮米网 来源：浮米网 2014-11-18
1. WO 2014155301 标题: Substituted bicyclic compounds as inhibitors of EZH2 申请人: Piramal Enterprises Ltd. 优先权日期及相关专利公开号: 2013 US 805349 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 provides compounds of formula 1, isotopic forms, stereoisomers or tautomers thereof, or pharmaceutically acceptable salts, solvates, N-oxides, S-oxides and polymorphs thereof, and processes for their preparation. The invention further relates to pharmaceutical compositions containing said compounds and their use in the treatment of diseases or disorders mediated by EZH2 (enhancer of zeste homolog 2), particularly cancer. 备注: EZH2抑制剂可以用于治疗癌症、肺动脉高压、骨髓纤维化、HIV感染和肝纤维化。本发明的化合物对EZH2的IC50为0.001–1 mcM。 2. WO 2014153280 标题: 2-Pyridyl carboxamide-containing spleen tyrosine kinase (Syk) inhibitors 申请人: Merck & Co., Inc. 优先权日期及相关专利公开号: 2013 US 804412 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、哮喘、系统红斑狼疮 专利摘要: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. 备注: Syk抑制剂可以治疗类风湿性关节炎、哮喘和系统红斑狼疮等疾病。本发明的化合物可以抑制重组的人源GST-Syk（IC50小于0.5 nM）。 3. WO 2014146493 标题: Acyclic cyanoethylpyrazolo pyridones as Janus kinase inhibitors 申请人: Merck & Co., Inc. 优先权日期及相关专利公开号: 2013 US 803241 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、炎症、哮喘、自身免疫疾病、阻塞性气道疾病 专利摘要: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. 备注: JAK抑制剂，尤其是JAK1和JAK2抑制剂可以用于治疗癌症、炎症、哮喘、自身免疫疾病和阻塞性气道疾病。本发明的化合物可以抑制Jak1和Jak2(IC50 = 0.04和0.28 nM）。 4. WO 2014150340 标题: S-Imino-S-oxo iminothiadiazine compounds as BACE inhibitors, compositions, and their use 申请人: Merck & Co., Inc. 优先权日期及相关专利公开号: 2013 US 788687 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 专利摘要: In its many embodiments, the present invention provides provides certain S-imino-S-oxo iminothiadiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1, R2, R3, R4, ring A, RA, m, L1, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer’s disease, are also disclosed. 备注: BACE1 和BACE2抑制剂被用于治疗阿尔兹海默。本发明的化合物对BACE1和BACE2的Ki 均小于1nM。 5. WO 2014150344 标题: C2-Azaspiro iminothiazine dioxides as BACE inhibitors 申请人: Merck & Co., Inc. 优先权日期及相关专利公开号: 2013 US 790636 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 专利摘要: In its many embodiments, the present invention provides certain C2-azaspirosubstituted iminothiazine dioxide compounds. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer’s disease, are also disclosed. 备注: BACE1 和BACE2抑制剂被用于治疗阿尔兹海默。本发明的化合物对BACE1和BACE2的Ki 分别为1.4 和0.32 nM。 6. WO 2014146994 标题: Urea derivatives and their use as fatty-acid binding protein (FABP) inhibitors 申请人: F. Hoffmann-La Roche AG 优先权日期及相关专利公开号: 2013 EP 160084 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: 2型糖尿病、动脉粥样硬化、慢性肾病、癌症、非酒精脂肪肝 专利摘要: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, W, A and B are as described herein, compositions including the compounds and methods of using the compounds. 备注: FABP抑制剂，尤其是FABP4抑制剂,可以用于治疗2型糖尿病、动脉粥样硬化、慢性肾病、癌症和非酒精脂肪肝。本发明的化合物可以抑制 FABP4 (IC50 = 0.02 mcM) ，且对FABP5具有选择性 (IC50 > 50 mcM)。 7. WO 2014146995 标题: Urea derivatives and their use as fatty-acid binding protein (FABP) inhibitors 申请人: F. Hoffmann-La Roche AG 优先权日期及相关专利公开号: 2013 EP 160088 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: 2型糖尿病、动脉粥样硬化、慢性肾病、癌症、非酒精脂肪肝 专利摘要: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, W, A and B are as described herein, compositions including the compounds and methods of using the compounds. 备注: FABP抑制剂，尤其是FABP4抑制剂,可以用于治疗2型糖尿病、动脉粥样硬化、慢性肾病、癌症和非酒精脂肪肝。本发明的化合物可以抑制 FABP4 (IC50 = 0.05 mcM) ，且对FABP5具有选择性 (IC50 = 3.79 mcM)。 8. WO 2014152229 标题: Inhibitors of leukotriene A4 hydrolase 申请人: Celtaxsys, Inc. 优先权日期及相关专利公开号: 2013 US 781181 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: 炎症、自身免疫疾病、癌症 专利摘要: The present invention is directed to compounds encompassed by the Formula (I), pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4-h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders. 备注: Leukotriene A4 hydrolase抑制剂可以用于治疗炎症、自身免疫疾病和癌症。本发明的化合物对leukotriene A4 hydrolase的IC50 =57 nM 9. WO 2014152518 标题: Inhibitors of leukotriene A4 hydrolase 申请人: Celtaxsys, Inc. 优先权日期及相关专利公开号: 2013 US 781193 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: 炎症、自身免疫疾病、癌症 专利摘要: The present invention is directed to compounds encompassed by the Formula (I), pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders. 备注: Leukotriene A4 hydrolase抑制剂可以用于治疗炎症、自身免疫疾病和癌症。本发明的化合物对leukotriene A4 hydrolase的IC50 =3.3 nM。 | 
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