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浮米每周专利快讯：2014年10月（三）作者：浮米网 来源：浮米网 2014-10-14
本周共有10篇专利。其中罗氏公开Cannabinoid CB2受体激动剂、BTK抑制剂、苯三唑类化合物等三篇专利；拜耳公开TTK抑制剂用于治疗癌症；辉瑞公开JAK抑制剂用于治疗类风湿关节炎等疾病。诺华公开针对IDH突变的抑制剂，用于治疗癌症。
1. WO 2014135507
标题: Novel pyrazol derivatives
申请机构: 罗氏
优先权日期及相关专利公开号: 2013 EP 158233
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: 糖尿病视网膜病变、视网膜静脉阻塞、疼痛、炎症、动脉粥样硬化、再灌注损伤、癌症
专利摘要: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
备注: Cannabinoid CB2受体激动剂糖尿病视网膜病变、视网膜静脉阻塞、疼痛、炎症、动脉粥样硬化、再灌注损伤和癌症。本发明的化合物对CB2受体的EC50 = 0.0004 mcM，且对CB1受体具有选择性 (EC50 > 10 mcM) 。
2. WO 2014135470
标题: Inhibitors of Bruton’s tyrosine kinase
申请机构: 罗氏
优先权日期及相关专利公开号: 2013 US 772948
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: 哮喘、类风湿性关节炎
专利摘要: This application discloses compounds according to generic Formula I: (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抑制剂可以治疗自身免疫和炎症。本发明的化合物对BTK的IC50 =0.013 mcM。
3. WO 2014135495
标题: Antiviral compounds
申请机构: 罗氏
优先权日期及相关专利公开号: 2013 US 773221
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(EC50 = 0.001)和HCV基因1b型 (EC50=0.014 mcM)。
4. WO 2014141153
标题: 3-Pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
申请机构: 诺华
优先权日期及相关专利公开号: 2013 US 782211
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 invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are described herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant I DH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
备注: 突变的IDH抑制剂可以治疗癌症。本发明的化合物可以抑制突变的IDH1(R132H)，IC50 =0.00845 mcM。
5. US 2014243312
标题: Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of Janus-related kinases (JAK)
申请机构: 辉瑞
优先权日期及相关专利公开号: 2013 US 767947
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、阿尔兹海默、牛皮癣、移植排异、癌症、肠炎和慢性阻塞性肺病
专利摘要: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.
备注: JAK抑制剂，尤其是JAK1，可用于治疗类风湿性关节炎、阿尔兹海默、牛皮癣、移植排异、癌症、肠炎和慢性阻塞性肺病等。本发明的化合物可以抑制JAK1的活性(IC50 = 4.6 nM)，同时对Jak2、Jak3和Tyk2 酶具有选择性(IC50 = 512, > 10000和546 nM)。
6. WO 2014134774
标题: Compounds inhibiting leucine-rich repeat kinase enzyme activity
申请机构: 默克
优先权日期及相关专利公开号: 2013 CN 72130
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: 帕金森综合症
专利摘要: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson’s Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
备注: LRRK2抑制剂可以治疗帕金森症。本发明的化合物可以抑制LRRK2的活性，其IC50=0.45 nM。
7. WO 2014131739
标题: Substituted imidazopyridazines
申请机构: 拜耳
优先权日期及相关专利公开号: 2013 EP 198930
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 relates to substituted imidazopyridazine compounds, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
备注: 双特异蛋白激酶TTK (MPS1; MPS1L1)抑制剂可以治疗癌症。本发明的化合物可以抑制Mps-1(IC50 = 0.97 nM)。
8. WO 2014143666
标题: HDAC inhibitors
申请机构: BioMarin Pharmaceutical Inc.
优先权日期及相关专利公开号: 2013 US 863235
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: 亨廷顿症、佛里德里希失调症、肌萎缩性脊髓侧索硬化症、阿尔兹海默、癌症、炎症
专利摘要: Disclosed herein are compounds of formula (I), and methods of inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I).
备注: HDAC抑制剂，尤其是HDAC1, HDAC2和HDAC3可用于治疗亨廷顿症、佛里德里希失调症、肌萎缩性脊髓侧索硬化症、阿尔兹海默、癌症、炎症。本发明的化合物对HDAC 1、HDAC 2和HDAC3的IC50 1 mcM。
9. US 2014256945
标题: Phosphonic acid compounds as sphingosine-1-phosphate receptor modulators
申请机构: Allergan, Inc.
优先权日期及相关专利公开号: 2013 US 774521
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: 疼痛、眼疾、免疫抑制、过敏症、自身免疫疾病、炎症和癌症
专利摘要: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
备注: S1P1受体配体可以用于治疗疼痛、眼疾、免疫抑制、过敏症、自身免疫疾病、炎症和癌症。本发明的化合物对S1P1的EC50=1.9 nM。
10. WO 2014141065
标题: Azetidine amide derivatives as orexin receptor antagonists
申请机构: Actelion Pharmaceuticals Ltd.
优先权日期及相关专利公开号: 2013 EP 158791
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: 物质滥用、焦虑、睡眠，情绪和认知障碍
专利摘要: The present invention relates to azetidine amide derivatives derivatives of formula (I) wherein rings A1 A2 and A3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to pharmaceutical compositions containing one or more compounds of formula (I), and to their use as pharmaceuticals, especially to their use as orexin receptor antagonists.
备注: Orexin OX-2受体拮抗剂可以治疗物质滥用、焦虑、睡眠，情绪和认知障碍等疾病。 本发明的化合物对OX-2 受体的IC50=0.6 nM，且对 OX-1受体具有选择性(IC50 = 178 nM)。
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