本周共11篇专利。默克公布了2篇BTK抑制剂专利；葛兰素史克公开了3篇Lp-PLA2抑制剂专利；波士顿大学公开了1篇HDAC8选择性抑制剂专利；百时美施贵宝和罗氏分别公开了1篇HCV抑制剂专利。
1. WO 2014113932标题: Btk inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2013 CN 70876
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、银屑病关节炎、骨关节炎
专利摘要: The present invention provides Bruton’s Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I) or pharmaceutically acceptable salts thereof. (Formula I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
备注: BTK抑制剂可用于治疗类风湿性关节炎、银屑病关节炎和骨关节炎等疾病。本发明的化合物可以抑制重组BTK的活性 (IC50 = 0.083 nM) 。
2. WO 2014113942标题: Btk inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2013 CN 70898
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、银屑病关节炎、骨关节炎
专利摘要: The present invention provides Bruton’s Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
备注: BTK抑制剂可用于治疗类风湿性关节炎、银屑病关节炎和骨关节炎等疾病。本发明的化合物可以抑制重组BTK的活性(IC50 = 0.33 nM)。
3. WO 2014114578标题: Pyrrolidine derivatives, pharmaceutical compositions and uses thereof
申请人: 勃林格殷格翰
优先权日期及相关专利公开号: 2013 EP 152734
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、肥胖
专利摘要: The invention relates to new pyrrolidine derivatives of the formula (I), to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
备注: ACC2抑制剂可以治疗肥胖和2型糖尿病。本发明的化合物可以抑制人源ACC2的活性 (IC50 = 0.009 mcM)。
4. US 2014213599标题: 2,3-Dihydroimidazol[1,2-c]pyrimidin-5(1H)-one based lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitors
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 CN 70976
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: 动脉粥样硬化、阿尔兹海默疾病
专利摘要: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer’s disease.
备注: Lp-PLA2抑制剂可以治疗动脉粥样硬化和阿尔兹海默疾病。本发明的化合物可以抑制人源Lp-PLA2活性(pIC50 = 10.8)，且对PLA2 VIIB具有选择性 (100倍的选择性)。
5. WO 2014114248标题: Compounds
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 CN 70970
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: 动脉粥样硬化、阿尔兹海默疾病
专利摘要: The present invention relates to novel 3,4-dihydro-1H-pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer’s disease.
备注: Lp-PLA2抑制剂可以治疗动脉粥样硬化和阿尔兹海默疾病。本发明的化合物可以抑制人源Lp-PLA2活性（pIC50 = 9.7）。
6. WO 2014114249标题: Bicyclic pyrimidone compounds as inhibitors of Lp-PLA2
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 CN 70977
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: 动脉粥样硬化、阿尔兹海默疾病
专利摘要: The present invention relates to novel pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer’s disease.
备注: Lp-PLA2抑制剂可以治疗动脉粥样硬化和阿尔兹海默疾病。本发明的化合物可以抑制人源Lp-PLA2活性 (pIC50 = 10.8)，且对PLA2 VIIB具有100倍的选择性。
7. WO 2014116772标题: Squaric derivatives for the treatment of hepatitis C
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2013 US 756557
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: Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
备注: 本发明的化合物可以抑制HCV感染，其对基因1a E1型和基因 E2型的EC50均为0.050 nM。
8. WO 2014114573标题: Antiviral triazole derivatives
申请人: 罗氏
优先权日期及相关专利公开号: 2013 US 755519
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: The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
备注: 苯三唑类化合物可以治疗HCV感染。本发明的化合物可以抑制HCV基因1a和基因1b型(EC50 = 0.019和0.008 mcM)。
9. WO 2014114532标题: Fluoro-[1,3]oxazines as BACE1 inhibitors
申请人: 罗氏
优先权日期及相关专利公开号: 2013 EP 152213
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: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer’s disease.
备注: BACE1抑制剂可以治疗阿尔兹海默疾病。本发明的化合物对BACE1的IC50 为0.002 mcM。
10. WO 2014116962标题: Selective histone deacetylase 8 inhibitors
申请人: 波士顿大学
优先权日期及相关专利公开号: 2013 US 756292
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: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that benefit from inhibition of HDAC8 activity
备注: HDAC抑制剂，尤其是HDAC8抑制剂可以治疗癌症。本发明的化合物对HDAC8的IC50为0.4 nM，且对HDAC6具有选择性 (IC50 > 1000倍).。
11. WO 2014114776标题: Quinoxalinones and dihydroquinoxalinones as respiratory syncytial virus antiviral agents
申请人: 杨森
优先权日期及相关专利公开号: 2013 EP 152915
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: 呼吸道合胞病毒(RSV)感染
专利摘要: Quinoxalinones and dihydroquinoxalinones having inhibitory activity on RSV replication and having the formula (I) including addition salts, and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
备注: 本发明的化合物可以治疗呼吸道合胞病毒(RSV)感染。其可以抑制野生型 rgRSV224 病毒复制(EC50 = 0.0015 mcM)。
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