本周共有12篇专利。默克公开6篇专利，包括MDM2抑制剂、HIV整合酶抑制剂、葡糖激酶抑制剂、syk抑制剂等专利；诺华公开1篇用于治疗COPD的融合蛋白；吉利德公开2篇PI3Kdelta抑制剂专利；辉瑞公开1篇EZH2抑制剂专利。
1. WO 2014097116标题: Stabilized insulin-like growth factor polypeptides
申请人: 诺华
优先权日期及相关专利公开号: 2012 US 738475
相关候选药物类型: 融合蛋白
相关候选药物化学结构:
适应症: 慢性阻塞性肺疾病
专利摘要: This invention is in the field of IGF-1 modifications. In particular, it relates to modified IGF- polypeptides and modified IGF-1 precursor polypeptides wherein the cleavage of E-peptide is prevented. The invention also relates to the use of such polypeptides for treating muscle diseases and disorders.
备注: 包含人类IGF-1蛋白的多肽可用于治疗慢性阻塞性肺病。本发明的融合蛋白由包含G1，P2，E3缺失的重组人源IGF-1和 R37A突变的人类IgG1的Fc域组成。
2. US 2014179680、WO 2014100065标题: Substituted imidazopyridines as HDM2 inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2013 US 777472、2013 US 132946
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 substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
备注: MDM2抑制剂可以用于治疗癌症。本发明的化合物MDM2的IC50小于1 nM。
3. WO 2014100071标题: Substituted pyrrolopyrimidines as HDM2 inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 740255
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 substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
备注: MDM2抑制剂可以用于治疗癌症。本发明的化合物MDM2的IC50小于1 nM。
4. WO 2014099586标题: 4-Pyridinonetriazine derivatives as HIV integrase inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 738112
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: HIV感染
专利摘要: The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R1, R2, R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject.
备注: HIV整合酶抑制剂可以治疗HIV感染。本发明的化合物可以在感染HIV-1的T-lymphoid MT4-GFP细胞中，抑制HIV复制。
5. WO 2014100765、US 2014179673标题: Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors
申请人: 吉利德、Calistoga LLC
优先权日期及相关专利公开号: 2012 US 745429
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: 自身免疫疾病、炎症、癌症
专利摘要: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kd. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kd.
备注: PI3Kdelta抑制剂可以治疗自身免疫疾病、炎症和癌症。本发明的化合物对PI3Kdelta的IC50 100 nM，同时对PI3Kalpha, beta和gamma具有选择性(IC50 > 1 mcM)。
6. WO 2014099578标题: Novel glucokinase activator compounds, compositions containing such compounds, and methods of treatment
申请人: 默克
优先权日期及相关专利公开号: 2012 US 738126
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、肥胖
专利摘要: Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included.
备注: 葡糖激酶（Glucokinase）激活剂可以用于治疗糖尿病和肥胖。本发明的化合物可以激活重组人源肝脏葡糖激酶(EC50 = 1.9 nM; Emax = 624.3%)。
7. WO 2014099584标题: Novel 2-pyridinecarboxamide derivatives, compositions containing such compounds, and methods of treatment
申请人: 默克
优先权日期及相关专利公开号: 2012 US 738146
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、肥胖
专利摘要: Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment.
备注: 葡糖激酶（Glucokinase）激活剂可以用于治疗糖尿病和肥胖。本发明的化合物可以激活重组人源肝脏葡糖激酶（ EC50= 6.2 nM， 与DMSO对照组相比，Emax = 478.6%)。
8. WO 2014096757标题: Pyridazinones as DAAO enzyme inhibitors
申请人: 武田
优先权日期及相关专利公开号: 2012 GB 22711
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: 精神分裂症，认知障碍、疼痛
专利摘要: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
备注: D-氨基酸氧化酶(DAAO)抑制剂可以治疗精神分裂症，认知障碍和疼痛。本发明的化合物可以抑制人源DAAO酶的活性，其IC50=11 nM。
9. WO 2014100314标题: Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 740802
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、癌症
专利摘要: The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript t 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).
备注: Syk抑制剂可以治疗类风湿性关节炎和癌症。本发明的抑制剂可以抑制人类GST和Syk的结合，其IC50值为0.07093 nM。
10. US 2014179667、WO 2014097041
标题: Aryl and heteroaryl fused lactams
申请人: 辉瑞
优先权日期及相关专利公开号: 2012 US 740596、2013 US 132567
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: This invention relates to compounds of general Formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
备注: EZH2抑制剂可以治疗癌症。本发明的化合物可以抑制野生型和Y641N突变的EZH2，,IC50分别小于等于0.00383 和0.00507mcM。
11. WO 2014100767、US 2014179718
标题: Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors
申请人: 吉利德、Calistoga LLC
优先权日期及相关专利公开号: 2013 US 137979
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: 自身免疫疾病、炎症、癌症
专利摘要: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which n, m, R1, R2, and R3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more P13K isoforms, such as PI3K8. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kd.
备注: PI3Kdelta抑制剂可以治疗癌症、炎症和自身免疫疾病。本发明的化合物可以选择性的抑制PI3Kdelta（IC50小于等于1nM）。在人源肝细胞中，显示了良好的代谢稳定性(在1和0.01%的DMSO中， t1/2 > 10或 > 4 h )。
12. WO 2014098831标题: 4,6-Diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 70546
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、唐氏综合症、认知障碍、痴呆、黄斑变性、癌症
专利摘要: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R1 and R2 are independently hydrogen, or -CH3; or R1 and R2 can join together in a ring by adding -(CH2)4-; R3 is hydrogen or C1-C3 alkyl; Y and Z are independently a C6-C10- aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, -C=OC1-4 alkyl, -S02C1-4 alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, benzyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is -NHCO-, or is a single bond; and L and Z together can be absent.
备注: Abeta产物抑制剂可以治疗阿尔兹海默、唐氏综合症、认知障碍、痴呆、黄斑变性和癌症等多种疾病。本发明的化合物可以抑制Abeta42产物，IC50为0.005 mcM。
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