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浮米每周专利快讯：2014年3月（一） 已有4人参与
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1. WO 2014023258 标题: Pyrazole carboxamide compounds, compositions and methods of use 申请人: 罗氏；基因泰克 优先权日期及相关专利公开号: 2012 US 682063；2013 US 764930；2013 US 764434 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 专利摘要: Provided herein are compounds of formula (AA): N N H HN O N N R R 6 A (R a ) p, (AA) stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, R a, p, R and R 6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases. 备注: ITK (EMT) 激酶抑制剂可以用于治疗炎症。一个示例性化合物对ITK的活性为Ki小于0.1 nM. 2. WO 2014025854 标题: Piperidine amide derivatives as HIV attachment inhibitors 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2012 US 681306 相关候选药物类型: 小分子药物 相关候选药物化学结构:201403060102 适应症: HIV感染 专利摘要: Compounds of Formula I, including pharmaceutically acceptable salts thereof: formule (I): wherein A is selected from the group consisting of:formule (II) and wherein Z is selected from the group consisting of: formule (III):,, and. are useful as HIV attachment inhibitors. 备注: HIV 粘附抑制剂可以用于治疗HIV感染。一个示例性的化合物在MT-2细胞中对HIV-1的活性为EC50=0.20 nM。 3. WO 2014023815 标题: New antibacterial compounds 申请人: 杨森 优先权日期及相关专利公开号: 2012 EP 180103 相关候选药物类型: 小分子药物 相关候选药物化学结构:201403060103 适应症: 细菌感染 专利摘要: The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds. 备注: 烯酰基 – （酰基载体蛋白）还原酶Fabl抑制剂可以用于治疗细菌感染。一个示例性化合物可以抑制金黄色葡萄球菌ATCC 29213 Fabl，其IC50达到0.407356 mcg/ml。 4. WO 2014024119 标题: Heterocyclic amides as ITK inhibitors 申请人: 格伦马克 优先权日期及相关专利公开号: 2012 IN 2888；2012 IN 2257；2013 IN 762；2012 US 717224；2012 US 696439 相关候选药物类型: 小分子药物 相关候选药物化学结构:201403060104 适应症: 哮喘；慢性阻塞性肺病；特异性皮炎；类风湿性关节炎；过敏性鼻炎 专利摘要: The present invention is directed to heterocyclic amide compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK. 备注: ITK (EMT)抑制剂可以用于治疗哮喘、慢性阻塞性肺疾病、皮炎、类风湿性关节炎、过敏性鼻炎、多发性硬化症、疼痛等疾病。本专利中的提供的部分示例化合物IC50小于50 nM 。 5. WO 2014023367 标题: Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan nuclear receptor RORgamma 申请人: Phenex Pharmaceuticals AG 优先权日期及相关专利公开号: 2012 US 681296；2012 EP 5789 相关候选药物类型: 小分子药物 相关候选药物化学结构:201403060105 适应症: 肌萎缩侧索硬化症；哮喘；I型糖尿病；肠炎；多发性硬化症；银屑病；类风湿性关节炎；脊柱炎 专利摘要: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof. 备注: ROR gamma 受体调控剂可以用于治疗炎症、自身免疫，如肌萎缩性脊髓恻索硬化症、多发性硬化症、牛皮癣、类风湿性关节炎、过敏性湿疹等。一个示例性的化合物在BL-21细胞中显示抑制RORgamma的活性为pIC50为6.3nM。 6. WO 2014023385 标题: Pyridopyrimidine derivatives as protein kinase inhibitors 申请人: 默克 优先权日期及相关专利公开号: 2012 EP 5716 相关候选药物类型: 小分子药物 相关候选药物化学结构:201403060106 适应症: 哮喘；肿瘤；多发性硬化症；类风湿性关节炎；红斑狼疮 专利摘要: Compounds of the formula (I) in which R, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus 备注: Syk激酶抑制剂可以用于多种疾病的治疗，如肿瘤、类风湿性关节炎、红斑狼疮、哮喘、多发性硬化症、糖尿病、唐氏综合症等。一个示例性化合物对Syk的抑制活性为IC500.1 mcM 。 7. WO 2014023673；US 2014044674 标题: Interleukin-10 fusion proteins and uses thereof 申请人: 罗氏 优先权日期及相关专利公开号: 2012 EP 179709 相关候选药物类型: 融合蛋白 适应症: 炎症；肠炎；类风湿性关节炎 专利摘要: The present invention generally relates to fusion proteins of antibodies and interleukin-10 (IL-10). In addition, the present invention relates to polynucleotides encoding such fusion proteins, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the fusion proteins of the invention, and to methods of using them in the treatment of disease. 备注: 由IgG类抗体和IL-10分子组成的融合蛋白可以用于炎症的治疗或预防，特别是炎症性肠疾病和类风湿关节炎的治疗。一个示例性的融合蛋白可以靶向人源FAP。该融合蛋白可以抑制LPS诱导的前炎性细胞活素（IL-6, IL-1beta和TNF-alpha）的产物，其EC50分别为0.054, 0.049和0.017 nM。 8. WO 2014023674 标题: Piperazino[1,2-a]indol-1-ones and [1,4]diazepino[1,2-a]indol-1-one 申请人: 罗氏 优先权日期及相关专利公开号: 2012 EP 179381 相关候选药物类型: 小分子药物 相关候选药物化学结构:201403060108 适应症: 焦虑；阿尔兹海默；抑郁；中风 专利摘要: The present invention relates to compounds of general formula (I), wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or cyano; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is phenyl, benzo[1,3]dioxolyl, 2,3-dihydro-benzofuran-5-yl or a 5- and 6-membered heteroaryl, wherein phenyl and the 5- and 6-membered heteroaryl groups may be substituted by one or more substituents, selected from cyano, nitro, amino and lower di-alkylamino, lower alkyl sulfonyl, lower alkoxy, lower alkoxy substituted by halogen, halogen, lower alkyl, lower alkyl substituted by halogen or lower alkyl substituted by hydroxyl; X is -CH(lower alkyl)-, -CH2-, -CH2CH2- or �CH(lower alkyl)CH2-; R is hydrogen or lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson’s disease, dementia, Alzheimer’s disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington’s disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine. 备注: 神经系统调节类化合物可以用于治疗焦虑、阿尔兹海默、抑郁和中风等疾病。一个示例性的化合物的EC150=0.002 mcM。 9. WO 2014026054 标题: CD20 scFv-ELPs methods and therapeutics 申请人: University of Southern California (USC) 优先权日期及相关专利公开号: 2012 US 682029 相关候选药物类型: 融合蛋白 适应症: 自身免疫；肿瘤 专利摘要: Disclosed herein are recombinant polypeptides comprising an elastin-like peptide (ELP) and a scFv, or a biological equivalent of the scFv. Also disclosed are compositions containing scFv-ELP polypeptides and methods of use. 备注: 包含弹性蛋白样肽（ELP）融合单链抗体（scFv）的重组多肽可以用于治疗癌症和自身免疫类疾病。一个由利妥昔单抗衍生的抗CD20的scFv单链抗体融合ELP(A-192)的融合蛋白scFv-ELPs可以延缓肿瘤生长并延长生存期。 10. WO 2014023814 标题: New antibacterial compounds 申请人: 杨森 优先权日期及相关专利公开号: 2012 EP 180100 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601010 适应症: 细菌感染 专利摘要: The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds. 备注: 烯酰基 – （酰基载体蛋白）还原酶Fabl抑制剂可以用于治疗细菌感染。一个示例性化合物可以抑制金黄色葡萄球菌ATCC 29213 Fabl，其IC50达到0.27 mcg/ml。此外其也对S. aureus ATCC 29213 and S. aureus ATCC 29213具有活性，分别为IC90 = 0.24 和0.21 mcg/ml。 11. WO 2014025708 标题: Compounds that are S1P modulating agents and/or ATX modulating agents 申请人: Biogen Idec Inc. 优先权日期及相关专利公开号: 2012 US 679984 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601011 适应症: 多发性硬化症；疼痛；类风湿性关节炎 专利摘要: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX). 备注: ENPP2抑制剂或SIP调节剂可用于类风湿性关节炎关节炎、多发性硬化症和疼痛、肿瘤、免疫等疾病的治疗。 示例性化合物对ENPP2的IC50小于0.5 mcM。 12. WO 2014025709 标题: Compounds that are S1P modulating agents and/or ATX modulating agents 申请人: Biogen Idec Inc. 优先权日期及相关专利公开号: 2012 US 679992 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601012 适应症: 多发性硬化症；疼痛；类风湿性关节炎 专利摘要: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX). 备注: ENPP2抑制剂或SIP调节剂可用于类风湿性关节炎关节炎、多发性硬化症和疼痛、肿瘤、免疫等疾病的治疗。 示例性化合物对ENPP2的IC50小于0.5 mcM。 13. WO 2014025850 标题: Tricyclic amidine derivatives as HIV attachment inhibitors 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2012 US 681336 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601013 适应症: HIV感染 专利摘要: Compounds of Formula I, including pharmaceutically acceptable salts thereof: (F) wherein A is selected from the group consisting of: (F) and;(F) and wherein Z is: (F) are useful as HIV attachment inhibitors. 备注: HIV 粘附抑制剂可以用于治疗HIV感染。一个示例性的化合物在MT-2细胞中对HIV-1的活性为EC50=1.83nM。 14. WO 2014025852 标题: Tricyclic alkene derivatives as HIV attachment inhibitors 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2012 US 681329 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601014 适应症: HIV感染 专利摘要: Compounds of Formula (I), including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: and wherein Z is: are useful as HIV attachment inhibitors. 备注: HIV 粘附抑制剂可以用于治疗HIV感染。一个示例性的化合物在MT-2细胞中对HIV-1的活性为EC50=0.28 nM。 15. WO 2014022936 标题: Chlamydia antigen compositions and uses thereof 申请人: University of British Columbia 优先权日期及相关专利公开号: 2012 US 680836 相关候选药物类型: 融合蛋白 适应症: 衣原体感染 专利摘要: The present invention provides in part fusion proteins derived from Chlamydia spp. The present invention also provides in part methods for treating or preventing Chlamydia infection using the fusion proteins. 备注: 免疫组合物类的融合蛋白可以作为疫苗，用于衣原体感染的预防和治疗。本专利中，融合蛋白 Chlamydia抗体展示了良好了抗衣原体感染活性。 16. WO 2014022767 标题: Dihydropyridone P1 as factor XIa 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 787081；2012 US 679197 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601016 适应症: 血栓 专利摘要: The present invention provides compounds of Formula (X)  Formula(X), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.备注: 凝血因子XIa和/或激肽释放酶B（血浆激肽释放酶; KLKB1）可以用于治疗血栓。血栓栓塞性病症如不稳定型心绞痛，急性冠状动脉综合征，心房纤维性颤动，心肌梗塞，短暂性缺血发作，中风，动脉粥样硬化，外周阻塞的治疗有用的抑制剂动脉疾病，静脉血栓形成，脑动脉血栓形成，脑，肾和肺栓塞等。本专利中的的示例化合物对凝血因子XIa和KLKB1的 Ki值分别为 0.05和 0.56 nM。 17. WO 2014022766；US 2014038969 标题: Dihydropyridone P1 as factor XIa 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 957609；2012 US 679197；2013 US 786992 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601017 适应症: 血栓 专利摘要: The present invention provides compounds of Formula (VIII): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. 备注: 凝血因子XIa和/或激肽释放酶B（血浆激肽释放酶; KLKB1）可以用于治疗血栓。血栓栓塞性病症如不稳定型心绞痛，急性冠状动脉综合征，心房纤维性颤动，心肌梗塞，短暂性缺血发作，中风，动脉粥样硬化，外周阻塞的治疗有用的抑制剂动脉疾病，静脉血栓形成，脑动脉血栓形成，脑，肾和肺栓塞等。本专利中的的示例化合物对凝血因子XIa和KLKB1的 Ki值分别为 0.25和 0.7 nM。 18. WO 2014022752 标题: Macrocycles as Pim inhibitors 申请人: 安进 优先权日期及相关专利公开号: 2012 US 679521 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601018 适应症: 肿瘤 专利摘要: The invention relates to compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer. 备注: Pim激酶可以用于治疗肿瘤。Pim分为Pim1、Pim2、Pim3等三种亚型。 本专利的化合物对 Pim-1, Pim-2, Pim-1-Mn and Pim-2-Mn的活性分别为IC50 = 0.000209、0.000286、0.0000498和0.0000634 mcM。 19. WO 2014022744 标题: Indole-substituted pyrrolopyrimidinyl inhibitors of Uba6 申请人: Millennium Pharmaceuticals, Inc. 优先权日期及相关专利公开号: 2012 US 679109 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601019 适应症: 肿瘤 专利摘要: Disclosed are chemical entities that inhibit Uba6, each of which is a compound of Formula /: Formula (I) or a pharmaceutically acceptable salt thereof, wherein R*1 is -H or -CH3; and Y is Formula (II) or Formula (III), wherein R2 is -H, -CH3 or C1-4 alkyloxycarbonyl; and RS7.1, RS7.2 and RS8.1 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers. 备注: UBA6酶抑制剂可以用与治疗肿瘤疾病。一个示例性化合物对人源重组his-UBA6酶的IC50小于50nM。 20. EP 2692357；WO 2014020062 标题: Novel anti-Plasmodium parasite antibodies 申请人: Fraunhofer-Gesellschaft zur Foerderung der angewandten Forschung eV 优先权日期及相关专利公开号: 2012 US 679380；2012 EP 179315 相关候选药物类型: 抗体 适应症: 诊断；疟疾 专利摘要: The technology provided herein relates to novel human antibodies against Plasmodium parasites, in particular against the malaria parasite Plasmodium falciparum. The present disclosure pertains to antibodies against merozoite surface protein 10 (MSP10). These antibodies have high affinity e.g. to Plasmodium falciparum schizonts and merozoites, inhibit the reinvasion of merozoites into erythrocytes and thereby neutralize parasitic multiplication. 备注: 人抗体或其抗原可以特异性的结合MSP10，且可以用于疟疾的诊断和治疗。本专利中列举的人单克隆IgG1 kappa抗体展示了对EGF 域1的特异性亲和力。 21. WO 2014022343 标题: 7-Hydroxy-indolinyl antagonists of P2Y1 receptor 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2012 US 678151 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601021 适应症: 血栓 专利摘要: The present invention provides compounds of Formula (I): Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used medicaments. 备注: P2Y1受体拮抗剂可以用于治疗血栓。本专利中列举的化合物在HEK-293细胞中，Ki=11.3nM。 22. WO 2014022253 标题: Amino-heteroaryl 7-hydroxy-spiropiperidine indolinyl antagonists of P2Y1 receptor 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2012 US 678190 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601022 适应症: 血栓 专利摘要: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used as medicaments. 备注: P2Y1受体拮抗剂可以用于治疗血栓。本专利中列举的化合物在HEK-293细胞中，Ki=16 nM。 23. WO 2014021281 标题: Partially saturated nitrogen-containing heterocyclic compound 申请人: Taisho Pharmaceutical Co., Ltd. 优先权日期及相关专利公开号: 2012 JP 168828 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601023 适应症: 贫血 专利摘要: Provided is a compound which is represented by general formula (I’) and has an excellent PHD2-inhibiting activity or a pharmaceutically acceptable salt thereof. (In the general formula (I’), W, Y, R2, R3, R4 and Y4 are as defined in the description.) 备注: 缺氧诱导因子（HIF）脯氨酰羟化酶2（PHD2）抑制剂对贫血症的治疗有效。本专利中的化合物在293FT细胞中可以抑制PHD2，其IC50=14 nM。 24. WO 2014020350 标题: PAR2 receptor antagonists 申请人: Proximagen Ltd. 优先权日期及相关专利公开号: 2012 GB 13700；2013 GB 52069 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601024 适应症: 炎症；肿瘤；特异性皮炎；肠炎；肠易综合征；疼痛；银屑病 专利摘要: Compounds of formula (I) or pharmaceutically acceptable salts, solvates or hydrates thereof wherein P, Q, X, Y, R1, R2, R3, R10, R11, and R12 are as defined in the claims, and the use those compounds in medicine. 备注: PAR2拮抗剂可以用于治疗炎症、肿瘤、疼痛、银屑病等疾病。本专利中的示例化合物对PAR2的IC500.1 mcM。 25. WO 2014022728；US 2014038952 标题: Substituted 5-(quinazolin-2-yl)pyrimidin-2-amine derivatives useful as PI3K/mTOR inhibitors for the treatment of cancer 申请人: Endo Pharmaceuticals Inc. 优先权日期及相关专利公开号: 2013 US 957470；2012 US 678694 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601025 适应症: 肿瘤；炎症 专利摘要: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds of formula (I) and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer. 备注: PI3Kalpha/mTOR(FRAP1)抑制剂可以用于治疗炎症和肿瘤。 本专利中的化合物在H1047R、E545K 和mTOR的IC50均小于50 nM，对 PI3K beta and gamma的IC50均小于500 nM，对PI3Kdelta的IC50 1mcM。 26. US 2014045856；US 2014045857；WO 2014019979 标题: 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes 申请人: 勃林格殷格翰 优先权日期及相关专利公开号: 2012 EP 178713 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601026 适应症: 阿尔兹海默；记忆缺陷 专利摘要: The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention. 备注: PDE2A和/或PDE10A抑制剂可以用于治疗阿尔兹海默和记忆缺陷等精神类疾病。本专利中的一个示例性化合物分别在对PDE2A的IC50 = 0.071mcM，对PD10A的IC50 = 3.01mcM。 27. WO 2014019908 标题: Substituted pyrroles active as kinases inhibitors 申请人: Nerviano Medical Sciences Srl 优先权日期及相关专利公开号: 2012 EP 178946 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601027 适应症: 动脉粥样硬化；肿瘤；免疫；HIV感染；神经退行疾病；前列腺增生；银屑病；中风 专利摘要: The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them. 备注: Janus 激酶抑制剂可以用于治疗肿瘤、动脉粥样硬化、免疫等多种疾病。本专利中提供的示例化合物对Jak1, Jak2 和 Tyk2 的 IC50均为0.001 mcM。 28. WO 2014019023 标题: alpha7 Nicotinic acetylcholine receptor modulators and uses thereof-I 申请人: Bionomics Ltd. 优先权日期及相关专利公开号: 2012 AU 903296；2013 AU 900167 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601028 适应症: 认知障碍；炎症；神经退行性疾病；神经疼痛 专利摘要: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (a7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of a7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases. 备注: alpha7 烟碱乙酰胆碱受体（nAChR的）的调节剂可作为炎症、认知障碍、神经疼痛等疾病的治疗用途。本专利提供的示例化合物对于 alpha7受体具有很好的活性。 29. WO 2014018887 标题: ATX modulating agents 申请人: Biogen Idec Inc. 优先权日期及相关专利公开号: 2012 US 676698 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601029 适应症: 多发性硬化症；慢性疼痛；类风湿性关节炎 专利摘要: Compounds of formula (I) can modulate the activity of autotaxin (ATX). 备注: ENPP2抑制剂或SIP调节剂可用于类风湿性关节炎关节炎、多发性硬化症和疼痛、肿瘤、免疫等疾病的治疗。 示例性化合物对ENPP2的IC50小于100 nM。 30. WO 2014018881 标题: ATX modulating agents 申请人: Biogen Idec Inc. 优先权日期及相关专利公开号: 2012 US 676705 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601030 适应症: 多发性硬化症；慢性疼痛；类风湿性关节炎 专利摘要: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer. 备注: ENPP2抑制剂或SIP调节剂可用于类风湿性关节炎关节炎、多发性硬化症和疼痛、肿瘤、免疫等疾病的治疗。 示例性化合物对ENPP2的IC50小于100 nM。 31. WO 2014018919 标题: Seriniquinones, melanoma-specific anticancer agents 申请人: University of California, Oakland 优先权日期及相关专利公开号: 2012 US 676427 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601031 适应症: 肿瘤 专利摘要: Accordingly, there are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer. 备注: Seriniquinones衍生物可以作为dermcidin抑制剂通过诱导凋亡的机制用于肿瘤，尤其是黑色素瘤和前列腺癌的治疗。本专利中的示例化合物对非小细胞肺癌细胞、肾癌、卵巢癌、前列腺癌、乳腺癌等细胞的抑制活性达到10 mcM。 32. WO 2014016300 标题: Glucagon analogues 申请人: Zealand Pharma A/S 优先权日期及相关专利公开号: 2012 US 674706；2013 DK 360；2013 US 785611 相关候选药物类型: 多肽 相关候选药物化学结构:2014030601032 适应症: 低血糖 专利摘要: The present invention relates to glucagon analogues and their medical use, for example in the treatment of hypoglycaemia. In particular, the present invention relates to stable glucagon analogues suitable for use in a liquid formulation. 备注: GCGR受体激动剂可以用于低血糖、肥胖、高血压、动脉粥样硬化等疾病的治疗。本专利中的示例化合物对人源GCGR的EC50 = 0.15 nM。 33. EP 2689786；WO 2014016312 标题: HPV/CyaA-based chimeric proteins and their uses in the induction of immune responses against HPV infection and HPV-induced disorders 申请人: Genticel SA 优先权日期及相关专利公开号: 2012 EP 305898 相关候选药物类型: 疫苗 相关候选药物化学结构: 适应症: 乳头状瘤病毒感染 专利摘要: The invention relates to a chimeric protein comprising or consisting of, from N-terminal to C-terminal, (a) a N-terminal part of a Bordetella CyaA protein (b) a heterologous polypeptide comprising antigens originating from different HPVs, and (c) a C-terminal part of a Bordetella CyaA protein. The invention also relates to a polynucleotide encoding this chimeric protein. A composition comprising at least one chimeric protein(s) of the invention and the prophylactic and/or therapeutic uses of said composition are also part of the invention. 备注: 有E7蛋白衍生物组成的多肽可以作为疫苗，用于HPV感染的治疗。本专利提供了对HPV感染有效的疫苗。 34. FR 2993562;WO 2014016507 标题: Novel selective compounds inhibiting CYP26A1 useful in cosmetic and pharmaceutical compositions 申请人: Galderma Research & Development, SNC 优先权日期及相关专利公开号: 2012 FR 57128 相关候选药物类型: 小分子药物 相关候选药物化学结构:2014030601034 适应症: 皮肤病 专利摘要: The present invention relates to novel compounds or to any of the salts thereof having the general formula (I), to the pharmaceutical and cosmetic compositions containing said compounds as well as to the use of said compounds and compositions for the treatment of diseases. 备注: 细胞色素 P450 CYP26A1抑制剂可以用于治疗皮肤类疾病。本专利中的一个示例化合物对 CYP26A1的AC50 = 0.19 mcM；对CYP26B1的AC50 = 50.33 mcM。 35. WO 2014016787 标题: Peptide-based compounds and uses thereof to treat beta-amyloid accumulation 申请人: Pharma Bio, LLC. 优先权日期及相关专利公开号: 2012 US 675205 相关候选药物类型: 多肽 相关候选药物化学结构:2014030601035 适应症: 阿尔兹海默 专利摘要: The present application relates to novel peptide-based compounds, optionally comprising an immunoactive built-in adjuvant, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with ß- amyloid accumulation. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: [Ra-NP]m-Lp (I). 备注: 可以抑制β-淀粉样蛋白的多肽可以用作阿尔兹海默、唐氏综合症等疾病的治疗。本专利提供了经修饰的用于抑制β-淀粉样蛋白的多肽结构。 |
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