上周共有11项专利公布，例如3、葛兰素史克的EZH2抑制剂，化合物对EZH2的IC50=3nM；9、浙江医药有限公司、上海生物医药创新中心等的细菌感染药物，化合物对万古霉素抵抗的肠球菌和肺炎链球菌的MIC值分别为 0.25和0.031mcg/ml。1. WO 2014106762标题: 4-Pyrimidinylamino-benzenesulfonamide derivatives and their use for the inhibition of polo-like kinase 1 (PLK1) for the treatment of cancer and their use for the treatment of bacterial infections
申请人: Vichem Chemie Research Ltd.
优先权日期及相关专利公开号: 2013 HU 7
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、肺结核
专利摘要: The present invention relates to 4-pyrimidinylamino-benzenesulfonamide derivatives of general formula (I) and pharmaceutically acceptable salts, solvates, hydrates, regioisomeric and polymorphic forms thereof, processes for manufacturing of them, the use of them, as well as pharmaceutical compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the inhibition of polo-like kinases (PLKs) and the treatment of cancer. Said 4-pyrimidinylamino-benzenesulfonamide compounds have been also identified as new drug candidates for the prevention and/or treatment of infectious diseases like bacterial diseases e.g. tuberculosis, including the currently multidrug-resistant tuberculosis (MDR-TB), extensively drug-resistant tuberculosis (XDR-TB) as well as for preventing tuberculosis.?
备注: PLK1抑制剂可以治疗癌症和肺结核。本发明的化合物对PLK1的IC50=1.456 mcM.
2. WO 2014106612标题: Aminopyridine derived compounds as LRRK2 inhibitors
申请人: 灵北
优先权日期及相关专利公开号: 2013 US 748142
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、痴呆、肠炎、帕金森综合症
专利摘要: The present invention is directed to aminopyridine derived compounds of formula (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such a Lewy body dementia, Parkinson’s disease or cancer.
备注: LRRK2抑制剂可以治疗癌症、痴呆、肠炎、帕金森综合症等疾病。本发明的化合物可以抑制野生型和G2019S突变的LRRK2，IC50分别为93nM和86 nM。
3. WO 2014107277标题: Enhancer of Zeste Homolog 2 inhibitors
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 US 777443
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 novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. Epigenetic modifications play an important role in the regulation of many cellular processes including cell proliferation, differentiation, and cell survival. Global epigenetic modifications are common in cancer, and include global changes in DNA and/or histone methylation, dysregulation of non-coding RNAs and nucleosome remodeling leading to aberrant activation or inactivation of oncogenes, tumor suppressors and signaling pathways.
备注: EZH2抑制剂可以治疗增生性疾病，尤其是癌症。本发明的化合物对EZH2的IC50=3 Nm
4. WO 2014106606标题: Nove phenyl/pyridine series substitued by hydroxyethylamino for the treatment of cancer
申请人: 罗氏
优先权日期及相关专利公开号: 2013 CN 70044
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 provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and W are as described herein, compositions including the compounds and methods of using the compounds.
备注: CDK8/cyclin C抑制剂可以治疗癌症，尤其是胃癌和结直肠癌。本发明的化合物对CDK8/cyclin C的IC50=0.0004 mcM。
5. WO 2014106800标题: Substituted 2-amino pyrimidine derivatives as kinase inhibitors
申请人: Aurigene Discovery Technologies Ltd.
优先权日期及相关专利公开号: 2013 IN 39
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
专利摘要: The present invention provides novel substituted 2-amino pyrimidine derivatives kinase enzyme inhibitor compounds of formula (1), which may be therapeutically useful kinase inhibitor, more particularly PI3K inhibitors. Formula (1) in which A, R1, R2 R3. R4, Q and ‘n’ have the same meanings given in the specification, and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting kinase enzyme, more particularly PI3K enzyme. The present invention also provides methods for synthesizing and administering the kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
备注: PI3Kdelta和PI3Kgamma抑制剂可以治疗炎症和癌症。本发明的化合物对PI3Kgamma和PI3Kdelta 的IC50分别小于20 nM。
6. US 2014187571标题: 7,8-Cyclicmorphinan analogs
申请人: Purdue Pharma LP
优先权日期及相关专利公开号: 2013 US 138380
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
专利摘要: The application is directed to compounds of Formula (I), and pharmaceutically acceptable salts and solvates thereof, wherein Cy, R1-R3, R4A, and R4B are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
备注: 阿片生物碱可以作为阿片受体激动剂，可以用于治疗疼痛、便秘、腹泻、瘙痒、戒酒和戒毒用药。本发明的化合物对mu-阿片受体的Ki = 30 nM。
7. US 2014187573标题: Substituted morphinans and the use thereof
申请人: Purdue Pharma LP
优先权日期及相关专利公开号: 2012 US 746878
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
专利摘要: The application is directed to compounds of Formula (I), and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
备注: 阿片生物碱可以作为阿片受体激动剂，可以用于治疗疼痛、便秘、腹泻、瘙痒、戒酒和戒毒用药。本发明的化合物对mu-阿片受体的EC50 = 14.2 nM。
8. WO 2014104279标题: Substituted spiropyrido[1,2-a]pyrazine derivative and medicinal use thereof as HIV integrase inhibitor
申请人: Japan Tobacco Inc. (JT)
优先权日期及相关专利公开号: 2012 US 746457
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: Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof which are useful as an anti-HIV agent. The invention relates to a compound represented by general formula [I] or [II] or a pharmaceutically acceptable salt thereof [in the formulae, the symbols have the same meanings as in the description].
备注: HIV整合酶抑制剂可以治疗HIV感染。本发明的化合物对 HIV-1 NL4-3 strain 的 EC50=0.7 nM。
9. CN 103897040标题: Glycopeptide compound or pharmaceutical salt thereof and method for preparing same, and pharmaceutical compositions and applications thereof
申请人: 浙江医药有限公司、上海生物医药创新中心、中国医药工业研究院
优先权日期及相关专利公开号: 2012 CN 10581733
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: 细菌感染
专利摘要: The present invention provides a glycopeptide compound or a pharmaceutical salt thereof, as shown in Formula (I) or (II), and a method for preparing same, and pharmaceutical compositions and applications thereof. The glycopeptide compound of the present invention has in-vitro antibacterial activity.
备注: 糖肽类可以治疗细菌感染。本发明的化合物对万古霉素抵抗的肠球菌和肺炎链球菌的MIC值分别为 0.25和0.031mcg/ml。
10. WO 2014101113标题: Piperazine-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A antagonist properties
申请人: 默克
优先权日期及相关专利公开号: 2012 CN 87851
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: Parkinson’s disease
专利摘要: Disclosed are compounds of Formula A: (structurally represented) where “RG1″, “RG2a”, “RG4″, “RG5″, “MG1″, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
备注: 腺苷A2A拮抗剂可以治疗帕金森综合症。本发明的化合物对A2A受体展示了良好的亲和力，EC50 = 0.8983 nM。
11. WO 2014105662标题: Glycosidase inhibitors and uses thereof
申请人: 默克
优先权日期及相关专利公开号: 2012 CN 87286
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、青光眼、帕金森、精神分裂症、神经损伤、癌症
专利摘要: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
备注: O-GlcNAcase抑制剂可以治疗阿尔兹海默、青光眼、帕金森、精神分裂症、神经损伤和癌症。本发明的化合物可以抑制O-GlcNAcaseKi = 0.075 nM。
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