本周共有11篇专利，癌症依然是重点，11篇专利中有4篇涉及癌症，包括拜耳的CDK9/cyclin T1抑制剂，Almirall, SA的PI3K delta抑制剂，University of North Carolina at Chapel Hill的 Mer受体激酶抑制剂和 Astex Therapeutics Ltd.的XIAP抑制剂。除此之外自身免疫疾病（4篇），心血管疾病也备受重视。1. WO 2014064131标题: Inhibitors of Bruton’s tyrosine kinase
申请人: 罗氏
优先权日期及相关专利公开号: 2013 US 831443
相关候选药物化学结构:
适应症: 自身免疫疾病、炎症
专利摘要: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
备注: BTK激酶抑制剂可以治疗自身免疫疾病和炎症。本发明提供的示例性化合物对BTK的IC50为0.00011 mcM。
2. WO 2014064219
标题: 1 H-indole-3-carboxamide derivatives and use thereof as P2Y12 antagonists
申请人: 赛诺菲
优先权日期及相关专利公开号: 2012 EP 306334
相关候选药物化学结构:
适应症: 血栓
专利摘要: The invention relates to compounds corresponding to formula (1): and to the use thereof as P2Y12 receptor antagonists for the treatment of cardiovascular diseases.
备注: P2Y12受体拮抗剂可以治疗血栓、心肌梗塞、中风、短暂脑缺血和心绞痛等疾病。本发明的示例化合物可以抑制血小板聚集，其可以抑制PRP，IC50= 0.025 mcM.
3. WO 2014060493
标题: N-(Pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group
申请人: 拜耳
优先权日期及相关专利公开号: 2012 EP 189129
相关候选药物化学结构:
适应症: 癌症
专利摘要: The present invention relates to N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
备注: CDK9/cyclin T1抑制剂可以治疗肿瘤和心绞痛、心肌衰弱等心血管等疾病及病毒感染等疾病。本发明示例性的化合物可以抑制HIS标记的重组人类CDK9/cyclin T1蛋白，IC50分别为2nM;抑制GST标记的CDK2/cyclin E的IC50=170nM.
4. WO 2014062596
标题: 2′-Methyl substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
申请人: 默克
优先权日期及相关专利公开号: 2012 US 715035
相关候选药物化学结构:
适应症: 丙肝
专利摘要: The present invention relates to 2′-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2′-Methyl Substituted Nucleoside Derivative, and methods of using the 2′-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
备注: NS5B抑制剂可以治疗HCV感染。本发明的示例性化合物可以抑制HCV基因1b型，EC50=0.125 mcM.
5. WO 2014059901
标题: 2′-Cyano substituted nucleoside derivatives and methods of use thereof for treatment of viral diseases
申请人: 默克
优先权日期及相关专利公开号: 2012 US 715024
相关候选药物化学结构:
适应症: 丙肝
专利摘要: Compounds of Formula (I) are disclosed, wherein R1, R2, R3, R4, R5, and R18 are defined herein. The compounds encompassed by Formula (I) include compounds which are HCV NS5B inhibitors and other compounds which can be metabolized in vivo to HCV NS5B inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
备注: NS5B抑制剂可以用于治疗HCV感染。本发明的示例化合物对基因1b型的EC50=33 mcM.
6. WO 2014062667
标题: Phenyl linked quinolinyl modulators of ROR-gamma-t
申请人: 杨森
优先权日期及相关专利公开号: 2013 US 53707
相关候选药物化学结构:
适应症: 自身免疫疾病，哮喘，鼻炎，代谢类疾病
专利摘要: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
备注: 类维生素ROR gamma受体调控剂可以治疗自身免疫疾病，哮喘，鼻炎，代谢类疾病和肿瘤。本发明的示例化合物可以抑制[3H]-25-hydroxycholesterol与RORgamma的结合，IC50=0.0053 mcM.
7. WO 2014062655
标题: Heteroaryl linked quinolinyl modulators of RORgammat
申请人: 杨森
优先权日期及相关专利公开号: 2012 US 714368
相关候选药物化学结构:
适应症: 自身免疫疾病，哮喘，鼻炎，代谢类疾病
专利摘要: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR~ct activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
备注: 类维生素ROR gamma受体调控剂可以治疗自身免疫疾病，哮喘，鼻炎，代谢类疾病和肿瘤。本发明的示例化合物Kd值为0.00072 mcM.
8. WO 2014062963
标题: Methods and compositions relating to anti-IL-21 receptor antibodies
申请人: 安进
优先权日期及相关专利公开号: 2012 US 715156
相关候选药物化学结构:单抗
适应症: AIDS，动脉粥样硬化，多发性硬化症，I型糖尿病，感染
专利摘要: The present invention provides compositions and methods relating to antigen binding proteins against IL-21 receptor.
备注: IL-21R抗体可以治疗AIDS，动脉粥样硬化，多发性硬化症，I型糖尿病，感染，免疫等疾病。本发明提供的人源单克隆lgG2 kappa 抗体靶向IL-21R,其IC50=35 pM.
9. WO 2014060432
标题: Pyrrolotriazinone derivatives as PI3K inhibitors
申请人: Almirall, SA
优先权日期及相关专利公开号: 2012 EP 382399
相关候选药物化学结构:
适应症: 癌症、自身免疫疾病、心血管疾病、神经退行性疾病、炎症
专利摘要: New pyrrolotriazinone derivatives having the chemical structure of formula (I), are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
备注: PI3K delta抑制剂可以用于治疗癌症、自身免疫疾病、心血管疾病、神经退行性疾病、炎症、代谢类疾病、疼痛、移植排异等疾病。本发明示例化合物对重组PI3Kdelta的IC50=0.2 nM.
10. WO 2014062774
标题: Pyrazolopyrimidine compounds for the treatment of cancer
申请人: University of North Carolina at Chapel Hill
优先权日期及相关专利公开号: 2012 US 714841
相关候选药物化学结构:
适应症: 癌症、血栓
专利摘要: Compounds of Formula I are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof.
备注: Mer受体激酶抑制剂可以治疗癌症和血栓。本发明的示例化合物对Mer的IC50小于10 nM.
11. WO 2014060768
标题: Bicyclic heterocycle compounds and their uses in therapy
申请人: Astex Therapeutics Ltd.
优先权日期及相关专利公开号: 2012 US 716089
相关候选药物化学结构:
适应症: 癌症
专利摘要: The invention relates to new bicyclic heterocycle compounds of formula (I): wherein R1 is seected from specific pyrazolyl, imidazolyl, pridinyl and triazolyl groups. The invention also realtes to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
备注: XIAP抑制剂可以治疗癌症。本发明一个示例性化合物可以抑制XIAP的BIR3域和clAP1域，IC50分别为0.04和0.012mcM。
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