本周共有13篇专利。以中枢神经系统专利为主。如罗氏的 Oxytocin受体激动剂专利和MAP3K12 (DLK)抑制剂专利、杨森的gamma-Secretase 调控剂专利、Lupin Ltd的烟碱酸alpha7正变构调控剂专利；此外Galapagos NV 与上海昀怡和凯惠科技分别公开一片JAK激酶抑制剂专利。
1. CN 103936763标题: Oxazolidone compound, preparing method and application thereof
申请人: 上海药物所、南京长澳医药科技有限公司
优先权日期及相关专利公开号: 2013 CN 10020040
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: 血栓
专利摘要: The present invention relates to the field of a pharmaceutical compound, and more specifically, relates to a new oxazolidone compound, an enantiomer, a diastereoisomer and a raceme thereof, and a mixture thereof, and a pharmaceutically acceptable salt thereof, a preparation method thereof, an application thereof as a bioactive substance in a drug. The compound in the present invention has strong anticoagulant activity, does not affect the activity of thrombin, and can reduce the risk of hemorrhage. A pharmacokinetics experiment shows that the compound in the present invention further has good metabolic characteristics, and has a far better oral bioavailability than a positive contrastive agent rivaroxaban.
备注: 凝血因子Xa抑制剂可以治疗血栓。本发明的化合物可以抑制人源凝血因子Xa (IC50 = 2.25 nM)。
2. WO 2014111380标题: Novel compound useful for the treatment of degenerative and inflammatory diseases
申请人: Galapagos NV
优先权日期及相关专利公开号: 2013 US 753482
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: 过敏、炎症、自身免疫疾病、癌症、移植排异
专利摘要: A novel compound according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
备注: JAK激酶抑制剂，尤其是JAK1抑制剂可用于治疗过敏、炎症、自身免疫疾病、癌症、移植排异、以及与IL-6或干扰素相关的软骨症。本发明的化合物可以抑制JAK1（IC50 = 5.42-12.87 nM, Ki= 9.21 nM），同时对JAK2、JAK3、TYK2具有选择性（IC50 = 16.2-207.5 (Ki= 62.6 nM); 324.2-1315 (Ki= 685 nM) 和461.2-1004 nM (Ki= 336 nM) )。同时可以抑制HeLa细胞 (IC50 = 1650-1661 nM)。
3. WO 2014111356标题: Oxytocin receptor agonists for the treatment of CNS diseases
申请人: 罗氏
优先权日期及相关专利公开号: 2013 EP 151632
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: 孤独症、外伤性应激、抑郁症、失忆、物质滥用、酗酒、药物成瘾、普拉德-威利综合征
专利摘要: The invention relates to the use of a compound of formula I wherein A1 is phenyl or a five or six membered hereroaryl group, containing 1, 2 or 3 heteroatoms, selected from N or S; R1 is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen or cycloalkyl; A2 is phenyl; R2 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, S-lower alkyl substituted by halogen, S(O)2-lower alkyl substituted by halogen; n is 1 or 2; or a to pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawel, drug addiction and for the treatment of Prader-Willi Syndrom.
备注: Oxytocin受体激动剂可以治疗孤独症、外伤性应激、抑郁症、失忆、物质滥用、酗酒、药物成瘾、普拉德-威利综合征。本发明的化合物才对Oxytocin受体的EC50=0.008 mcM.
4. WO 2014111037标题: Five-and-six-membered heterocyclic compound, and preparation method, pharmaceutical composition and use thereof
申请人: 上海昀怡健康管理咨询有限公司、凯惠科技发展(上海)有限公司
优先权日期及相关专利公开号: 2013 CN 10019856
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: 炎症、自身免疫疾病、癌症、感染
专利摘要: A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer.
备注: JAK激酶抑制剂可用于治疗炎症、自身免疫疾病、癌症和感染。本发明的化合物对JAK1、JAK2、JAK3的IC50小于等于 50 nM。
5. WO 2014111465标题: Isomannide derivatives as inhibitors of soluble epoxide hydrolase
申请人: 赛诺菲
优先权日期及相关专利公开号: 2013 EP 305051
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: 高血压
专利摘要: The present invention relates to compounds of the formula (I), wherein R1, R11, R12 and X have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They are highly potent and selective soluble epoxide hydrolase inhibitors and are suitable, for example, for the therapy and prophylaxis of renal failure, diabetic nephropathy, type 2 diabetes mellitus, inflammation or could show beneficial effects in pain, dyslipidemia and atherosclerosis. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
备注: 异甘露醇衍生物可以作为可溶环氧化物酶(sEH)抑制剂用于治疗高血压、炎症、动脉粥样硬化、糖尿病、脂代谢紊乱、慢性阻塞性肺病、肝功能衰竭和关节炎等疾病。本发明的化合物对she酶的IC50 0.001 mcM。
6. WO 2014111496标题: 3-Substituted pyrazoles and use as DLK inhibitors
申请人: 罗氏
优先权日期及相关专利公开号: 2013 US 754501
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: 阿尔兹海默病、帕金森症、肌萎缩性脊髓侧索硬化症
专利摘要: The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. (I) In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.
备注: MAP3K12 (DLK)抑制剂可以治疗神经退行性疾病，如阿尔兹海默病、帕金森症、肌萎缩性脊髓侧索硬化症等。本发明的化合物对DLK的Ki = 0.00017 mcM。
7. WO 2014111028标题: Genistein alkylamine compound, preparation method and use thereof
申请人: 四川大学
优先权日期及相关专利公开号: 2013 CN 10019569
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: 痴呆、阿尔兹海默、多发性硬化症、帕金森症、亨廷顿症
专利摘要: Disclosed in the present invention are a new genistein alkylamine compound (I) and pharmaceutically acceptable salts thereof, and the preparation method and use thereof in the preparation of drugs for the treatment and/or prevention of diseases related to neurodegeneration, comprising but not limited to neurodegenerative diseases such as vascular dementia, Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, HIV related dementia, multiple sclerosis, progressive amyotrophic lateral sclerosis, neuropathic pain and glaucoma, wherein Ar represents any of the structure units as shown in the following (A)-(C), and n=1-2.
备注: 异黄酮可作为乙酰胆碱酯酶抑制剂，用于治疗痴呆、阿尔兹海默、多发性硬化症、帕金森症、亨廷顿症等疾病。本发明的化合物可以选择性的抑制乙酰胆碱酯酶，其IC50 1 mcM。
8. WO 2014111457标题: Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
申请人: 杨森
优先权日期及相关专利公开号: 2013 EP 151654
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
专利摘要: The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
备注: gamma-Secretase 调控剂可以抑制beta-amyloid (Abeta)的产生，可用于治疗阿尔兹海默病。此外也可以治疗脑外伤、中度认知障碍、痴呆、脑淀粉样血管病、唐氏综合症等。本发明的化合物可以降低Abeta42 和Abetatotal肽，IC50分别为0.006和2.09 mcM。
9. WO 2014111839标题: Pyrrole derivatives as alpha 7 nAChR modulators
申请人: Lupin Ltd.
优先权日期及相关专利公开号: 2013 IN 52
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: 注意力缺陷、精神分裂、脑外伤、认知障碍
专利摘要: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as a modulator of nicotinic acetylcholine receptors particularly a7 subtype, its tautomeric forms, its stereoisomers, its pharmaceutically acceptable salts, its pharmaceutical composition, and its combinations with suitable medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer’s disease, mild cognitive impairment, senile dementia, and the like.
备注: 烟碱酸alpha7正变构调控剂可以治疗注意力缺陷、精神分裂、脑外伤、认知障碍等疾病。本发明的化合物可以增加15倍正变构调控剂的活性。
10. WO 2014110705标题: Heterocycle-substituted tetracyclic compounds 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: 2013 CN 38
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: HCV感染
专利摘要: The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A’, R 2 R 3, R 4 and R are as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetracyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.
备注: NS5A抑制剂可以治疗HCV感染。本发明的化合物对基因1a, 基因1a Y93H, 基因1a Q30D, 基因2a和基因2b的EC50分别为 0.0029, 0.0019, 0.007, 0.003 and 0.004nM。
11. WO 2014112798标题: Novel phenylethynyl benzamide glucokinase activator and method for preparing same
申请人: Yuhan Corp.
优先权日期及相关专利公开号: 2013 KR 5076
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: 糖尿病和肥胖
专利摘要: The present invention relates to a novel phenylethynyl benzamide, pharmaceutically acceptable salts thereof, or hydrates or solvates thereof, a method for preparing same, and a pharmaceutical composition containing same. The novel phenylethynyl benzmide, the pharmaceutically acceptable salts thereof, or the hydrates or solvates thereof, according to the present invention, significantly activate glucokinase, and thus can be usefully applied to treatment of diseases transmitted through glucokinase, such as hyperglycemia and diabetes.
备注: 葡糖激酶活化剂可以治疗糖尿病和肥胖。本发明化合物对葡糖激酶的EC50 = 0.006 mcM。
12. US 2014206686标题: Phthalazinones and isoquinolinones as ROCK inhibitors
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2013 US 754007
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、心血管疾病、青光眼、哮喘、勃起功能障碍、自身免疫疾病
专利摘要: The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
备注: ROCK抑制剂，尤其是ROCK 1和ROCK 2,可以治疗癌症、心血管疾病、青光眼、哮喘、勃起功能障碍和自身免疫疾病。本发明的化合物对ROCK1和ROCK2的IC50在 0.1至100 nM之间。
13. WO 2014109414标题: Nitrogen-containing heterocylic compound or salt thereof
申请人: FUJIFILM Corp.
优先权日期及相关专利公开号: 2013 JP 3832
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: A compound represented by general formula [1] or a salt thereof. (In general formula [1], Z1 represents a group such as N or CH; X1 represents a group such as NH; R1 represents a group such as a heteroaryl group; R2, R3, and R4 represent a hydrogen atom, a halogen atom, or a group such as an alkoxy group; and R5 represents a group such as a heteroaryl group.)
备注: PI3K/ERK2抑制剂可以治疗癌症、过敏症、自身免疫疾病、神经退行性疾病、心血管疾病、炎症、内分泌疾病、代谢类疾病和感染。本发明的化合物可以抑制人源 PI3Kalpha 和 Erk2，IC50均小于1 mcM。
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