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浮米每周专利快讯：2014年9月（四） 作者：浮米网 来源：浮米网 2014-09-22 1. US 2014228322 标题: ERK inhibitors and uses thereof 申请人: CelgeneAvilomics Research, Inc. 优先权日期及相关专利公开号: 2013 US 762408 相关候选药物类型: 小分子药物 适应症: 癌症 专利摘要: The present invention provides compounds, compositions thereof, and methods of using the same. 备注: ERK抑制剂，尤其是ERK 1和/或ERK2抑制剂可以治疗癌症。本发明的化合物可以抑制ERK1(IC50≤100 nM)。
2. WO 2014123186 标题: Anti-semaphorin 3A antibody and treatment of Alzheimer’s disease and inflammatory immune diseases using same 申请人: Yokohama City University、Chiome Bioscience Inc. 优先权日期及相关专利公开号: 2013 JP 21309 相关候选药物类型: 抗体 适应症: 阿尔兹海默、癌症、败血症、神经退行性疾病、炎症、凝血障碍 专利摘要: The present invention mainly addresses the problem of providing an antibody against semaphorin 3A protein, said antibody enabling effective prevention and/or treatment of a disease, in which Sema3A protein participates, such as a neurodegenerative disease, autoimmune disease, inflammatory disease, cancer, infectious disease, etc. or disseminated intravascular coagulation syndrome. An anti-Sema3A antibody comprising CDRs having specific amino acid sequences (SEQ ID NOS: 1-6, 60-62, 64-66, 68-70, 72-74, 76-78, 80-82, 84-86 and 88-90) enables effective prevention and/or treatment of a disease, in which Sema3A protein participates, such as a neurodegenerative disease, autoimmune disease, inflammatory disease, cancer, infectious disease, etc. or disseminated intravascular coagulation syndrome and, therefore, remarkably ameliorates symptoms associated with such a disease. 备注: 结合Sema3A的抗体有望用于预防和治疗阿尔兹海默、癌症、败血症、神经退行性疾病、炎症、凝血障碍、感染。本发明提供了人源单克隆IgG1单克隆抗体，其对Sema3A的亲和力为KD=3-4 nM (via Biacore)， IC50=0.101 mcg/L。
3. WO 2014123227 标题: Antibodies to human NRG1 protein 申请人: Medical and Biological Laboratories Co., Ltd. (MBL) 优先权日期及相关专利公开号: 2013 JP 23125 相关候选药物类型: 抗体 适应症: 癌症 专利摘要: The present invention addresses the problem of providing antibodies that specifically recognize isoforms of the human NRG1 protein, and enable signaling involving said isoforms to be suppressed. Furthermore, the present invention has succeeded in obtaining an antibody that binds to the domain of positions 221 to 234 in the human NRG1-a protein, and an antibody that binds to the domain of positions 213 to 239 in the human NRG1-ß1 protein. These antibodies were also found to have inhibitory activity against cleavage of the NRG1 protein, inhibitory activity against the phosphorylation of the ErbB3 protein in cancer cells, and inhibitory activity against the proliferation of cancer in vivo. 备注: 靶向neuregulin-1 (NRG1) alpha或NRG1 beta的抗体可以治疗癌症。本发明的抗体可以靶向NRG1-alpha的胞外域(aa 221-234)。
4. WO 2014123203 标题: Therapeutic agent for diabetes 申请人: Kyoto Pharmaceutical Industries, Ltd. 优先权日期及相关专利公开号: 2013 JP 21833 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、动脉硬化、高血脂、癌症、炎症 专利摘要: Provided is a compound having PTP-1B inhibitory activity that is excellent as a drug, or a pharmaceutically acceptable salt thereof. A compound represented by general formula (I) (in the formula, each symbol means the same as in the specification), or a pharmaceutically acceptable salt thereof. 备注: PTP-1B抑制剂可以治疗糖尿病、肥胖、动脉硬化、高血脂、癌症、炎症和代谢综合征等。本发明的化合物可以抑制PTP-1B（ IC50=0.25 mcM）。
5. WO 2014124208 标题: NSAIDs derivatives and uses thereof 申请人: City University of New York (CUNY) 优先权日期及相关专利公开号: 2013 US 761848 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 discloses novel compounds derived from NSAIDs and pharmaceutically acceptable salts thereof. Other aspects of the invention relate to use of the NSAID derivatives in treating inflammatory diseases and pharmaceutical compositions thereof. Non-steroidal anti-inflammatory drugs (NSAIDs) are prototypical agents for treatment of inflammatory conditions. NSAIDs may also have utility as therapeutic agents against many forms of cancers. However, long-term use of NSAIDs may lead to serious side effects affecting the gastrointestinal and renal systems. 备注: NSAID衍生物可以治疗癌症和炎症。本发明的化合物可以抑制多种肿瘤细胞的活性，如结直肠癌细胞 ( HT-29, HCT-115 and SW480),乳腺癌细胞(MDA-MB-231, SK-BR-3 and MCF-7), 胰腺癌细胞(MIA PaCa-2 and BxPC-3), 肺癌细胞A549, 前列腺癌细胞LNCaP和白血病细胞Jurkat cancer cells (IC50分别为0.082, 0.075, 0.092, 0.180, 0.0098, 0.242, 0.082, 0.075, 0.083, 0.075和0.22 mcM）。
6. WO 2014122480 标题: 16- and 17- deuterated estrogen-3-sulfamates as estrogenic agents 申请人: The University of Bath 优先权日期及相关专利公开号: 2013 GB 2368 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: 避孕、荷尔蒙替代疗法 专利摘要: The present invention relates to novel derivatives of estradiol, in particular to deuterated derivatives of estradiol sulfamates. The present invention also relates to compositions comprising said novel derivatives, as well as to uses of said novel derivatives and compositions comprising said derivatives. 备注: 氘代雌二醇可以用于荷尔蒙替代疗法和避孕。
7. WO 2014121942 标题: Macrocyclicpyridazinone derivatives 申请人: Merck Patent GmbH 优先权日期及相关专利公开号: 2013 EP 154391 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、多发性硬化症、类风湿性关节炎、狼疮肾炎和系统红斑狼疮 专利摘要: The present invention relates to compounds of formula (I) Wherein R1, R2, R3, R4, L and Z have the meaning given in claim 1, and their use in the prophylaxis and treatment of diseases. 备注: IRAK抑制剂，尤其是IRAK-1和/或IRAK-4抑制剂可以治疗癌症、炎症、多发性硬化症、类风湿性关节炎、狼疮肾炎和系统红斑狼疮。本发明的化合物可以抑制 IRAK-1和IRAK-4（IC50均小于 0.1 mcM）。
8. WO 2014124433 标题: 5′-Triphosphate oligoribonucleotides 申请人: McGill University 优先权日期及相关专利公开号: 2013 US 763367 相关候选药物类型: 基因疗法 适应症: 病毒感染 专利摘要: Disclosed are 5′-triposphate oligoribonucleotides, pharmaceutical compositions comprising said 5′-triposphate oligoribonucleotides, and methods of using said 5′-triposphate oligoribonucleotides to treat viral infections. 备注: 包含有寡核苷酸和三磷酸基团的化合物可以用于治疗病毒感染。本发明提供了修饰的短链的RNA寡核苷酸在C57BL / 6小鼠流感模型中有效。
9. WO 2014122303 标题: Glucan synthase inhibitors 申请人: Evolva AG 优先权日期及相关专利公开号: 2013 US 763060 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: 真菌感染 专利摘要: The present invention provides compounds with anti-fungal activity useful for treatment or prevention of fungal infections in human beings or plants. The antifungal compounds are inhibitors of glucan synthase and have the formula (I) (I) wherein Z denotes a mono- or bicyclic aromatic or heteroaromatic ring system; and X1 and X3 are individually selected from the group consisting of -CH and N, wherein at least one of X1 and X3 is N; and X2 is selected from the group consisting of –CH2, -CH-R8 and –(C=O), wherein R8 is C1-3 alkyl; and Y is selected from the group consisting of –(CH2)n-, -(CHR9)-, -(CH2)p-CR10R11- (CH2)q, -(CH2)p-(C=O)-(CH2)q and -(CH2)p-(C=O)-(CH2)q, wherein n is an integer in the range of 1 to 6, p is an integer in the range of 0 to 3 and q is an integer in the range of 1 to 4 and wherein R9 R10 and R11 individually are selected from the group consisting of C1-3-alkyl; and R1 and R5 are individually selected from the group consisting of –H and halogen, wherein at least one of R1 and R5 is halogen; and R2 and R4 is selected from the group consisting of –H and halogen; and R3 is –NH-R6, wherein R6 is selected from the group consisting of –H, alkyl, – (C=O)-R7, -(C=O)-O-R7, – (C=O)-NH2 and –SO2-R7, wherein R7 is selected from the group consisting of –H and alkyl, or a pharmaceutically acceptable salt thereof or a prodrug thereof. 备注: 1, 3-beta-葡聚糖合成酶抑制剂可以治疗真菌感染。本发明的化合物可以抑制1, 3-beta-葡聚糖合成酶，IC50 = 0.86mcM。
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