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11. 发明授权

US09434722B2 Indole amide derivatives and related compounds for use in the treatment of neurodegenerative diseases 有权
标题翻译：吲哚酰胺衍生物和用于治疗神经变性疾病的相关化合物
公开(公告)号：US09434722B2
公开(公告)日：2016-09-06
申请号：US14060563
申请日：2013-10-22
申请人： Katholieke Universiteit Leuven, K.U.Leuven R&D , reMYND
发明人： Gerard Griffioen , Tom Van Dooren , Veronica Rojas De La Parra , Arnaud Marchand , Sara Allasia , Amuri Kilonda , Patrick Chaltin
IPC分类号： C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： A61K31/4045 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/635 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
摘要翻译：本发明提供了新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地，某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症。本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。

12. 发明授权

US09408885B2 Combinations of therapeutic agents for treating melanoma 有权
标题翻译：用于治疗黑色素瘤的治疗剂的组合
公开(公告)号：US09408885B2
公开(公告)日：2016-08-09
申请号：US13689380
申请日：2012-11-29
申请人： VIB VZW , KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D
发明人： Jean-Christophe Marine
IPC分类号： C07K7/00 , A61K38/02 , A61K33/24 , A61K31/496 , A61K31/195 , C12Q1/68 , G01N33/50 , G01N33/574 , A61K45/06 , A61K38/18 , A61K38/30
CPC分类号： A61K38/02 , A61K31/195 , A61K31/496 , A61K33/24 , A61K38/1866 , A61K38/30 , A61K45/06 , C12Q1/6886 , C12Q2600/156 , G01N33/5005 , G01N33/5743 , G01N2800/52
摘要： The present disclosure relates to the field of oncology, more particularly to the field of melanoma. Provided are methods of treating melanoma, particularly advanced cutaneous melanoma, with a combination of pharmaceutical agents comprising MDM4-specific antagonists (such as an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and PI3K-AKT, B-RAF and MEK inhibitors. Further provided are pharmaceutical formulations of MDM4-specific antagonists (be it an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and a pharmaceutical formulation of one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and B-RAF and MEK inhibitors.
摘要翻译：本公开涉及肿瘤学领域，更具体地涉及黑素瘤领域。提供了通过包含MDM4特异性拮抗剂（例如MDM4-p53相互作用的抑制剂或降低MDM4蛋白稳定性的分子）或MDM4-MDM2双重抑制剂（MDM4-MDM2双重抑制剂）的药物组合治疗黑素瘤，特别是晚期皮肤黑色素瘤的方法，即破坏p53和MDM2与p53和MDM4之间的相互作用的分子）和一种或多种化学治疗剂，例如烷化剂（即达卡巴嗪（DITC）或美法仑）），烷化化试剂（即顺铂或卡铂）或有丝分裂抑制剂（紫杉烷多西紫杉醇或紫杉醇）和PI3K-AKT，B-RAF和MEK抑制剂。还提供了MDM4特异性拮抗剂（无论是MDM4-p53相互作用的抑制剂还是降低MDM4蛋白稳定性的分子）或MDM4-MDM2双重抑制剂（即破坏p53和MDM2与p53之间的相互作用的分子）的药物制剂和MDM4）和一种或多种化学治疗剂的药物制剂，例如烷化剂（即达卡巴嗪（DITC）或美法仑）），烷化化试剂（即顺铂或卡铂）或有丝分裂抑制剂（紫杉烷多西紫杉醇或紫杉醇）和B-RAF和MEK抑制剂。

13. 发明授权

US09284271B2 Compounds for the treatment of neurodegenerative diseases 有权
标题翻译：用于治疗神经变性疾病的化合物
公开(公告)号：US09284271B2
公开(公告)日：2016-03-15
申请号：US13993756
申请日：2011-12-13
申请人： Gerard Griffioen , Tom Van Dooren , Verónica Rojas De La Parra , Arnaud Marchand , Sara Alassia , Amuri Kilonda , Patrick Chaltin
发明人： Gerard Griffioen , Tom Van Dooren , Verónica Rojas De La Parra , Arnaud Marchand , Sara Alassia , Amuri Kilonda , Patrick Chaltin
IPC分类号： C07D209/14 , C07D209/18 , C07D401/12 , C07D409/12 , C07D471/04
CPC分类号： C07D209/18 , C07D209/14 , C07D401/12 , C07D409/12 , C07D471/04
摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.
摘要翻译：本发明提供了新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地，某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症。本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。化合物具有式（A1），其中R1，R2，R4，R5，R6，E，n，Y1，Y2，Y3，Y4，Y5，B，R8和m如权利要求中所定义。

14. 发明授权

US09169472B2 Endolysin OBPgpLYS 有权
标题翻译：内溶素OBPgpLYS
公开(公告)号：US09169472B2
公开(公告)日：2015-10-27
申请号：US14475900
申请日：2014-09-03
申请人： LYSANDO AG , KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D
发明人： Yves Briers , Rob Lavigne , Maarten Walmagh , Stefan Miller
IPC分类号： C12N9/26 , C12N15/00 , C12N5/10 , A61K38/46 , C12N9/36 , C07K14/195 , A61K38/00
CPC分类号： C12N9/2462 , A01N43/50 , A23L3/3571 , A61K38/00 , A61K38/47 , C07K7/08 , C07K14/195 , C07K14/21 , C07K14/43518 , C07K2319/21 , C07K2319/55 , C12Q1/04 , C12Q1/34 , C12Y302/01017 , G01N2333/928
摘要： The present invention relates to a polypeptide with an amino acid sequence according to SEQ ID NO: 1 and fragments or derivatives thereof. The present invention further relates to fusion proteins comprising said polypeptide and an additional peptide stretch fused to said polypeptide at the N- or C-terminus. Moreover, the present invention relates to nucleic acid molecules encoding said polypeptide or fusion protein, vectors comprising said nucleic acid molecules and host cells comprising either said nucleic acid molecules or said vectors. In addition, the present invention relates to said polypeptide or fusion protein for use as a medicament, in particular for the treatment or prevention of Gram-negative bacterial infections, as diagnostic means, as cosmetic substance or as sanitizing agent. The present invention also relates to the use of said polypeptide or fusion protein for the treatment or prevention of Gram-negative bacterial contamination of foodstuff, of food processing equipment, of food processing plants, of surfaces coming into contact with foodstuff, of medical devices, of surfaces in hospitals and surgeries. Furthermore, the present invention relates to a pharmaceutical composition comprising said polypeptide or fusion protein.
摘要翻译：本发明涉及具有根据SEQ ID NO：1的氨基酸序列及其片段或衍生物的多肽。本发明还涉及包含所述多肽的融合蛋白和在N-或C-末端与所述多肽融合的另外的肽拉伸。此外，本发明涉及编码所述多肽或融合蛋白的核酸分子，包含所述核酸分子的载体和包含所述核酸分子或所述载体的宿主细胞。此外，本发明涉及用作药物的所述多肽或融合蛋白，特别是用于治疗或预防革兰氏阴性细菌感染，作为诊断手段，作为化妆品或消毒剂。本发明还涉及所述多肽或融合蛋白用于治疗或预防食品的食品加工设备，食品加工厂，与食品接触的表面，医疗器械的革兰氏阴性细菌污染，在医院和手术中的表面。此外，本发明涉及包含所述多肽或融合蛋白的药物组合物。

15. 发明授权

US09042645B2 Feature detection in numeric data 有权
标题翻译：数字数据中的特征检测
公开(公告)号：US09042645B2
公开(公告)日：2015-05-26
申请号：US13896111
申请日：2013-05-16
申请人： IMEC , Katholieke Universiteit Leuven, K.U. LEUVEN R&D
发明人： Pradip Mainali , Gauthier LaFruit
IPC分类号： G06K9/00 , G06K9/46 , G06K9/62
CPC分类号： G06K9/4671 , G06K9/4619 , G06K9/6211
摘要： A method for detecting features in digital numeric data comprises obtaining digital numeric data comprising values corresponding to a plurality of sampling points over a domain space having at least one dimension, computing a plurality of scale-space data comprising filtering said digital numeric data using a filter bank, determining a plurality of feature regions each corresponding to a local extremum in scale and location of the scale-space data; and determining a feature region descriptor for each of said plurality of feature regions. The filter bank is a Cosine Modulated Gaussian filter bank in which the standard deviation parameter of the Gaussian equals 1 π ⁢ ln ⁡ ( 2 ) 2 ⁢ 2 b + 1 2 b - 1 multiplied by the cosine wavelength, in which b is in the range of 0.75 to 1.25, or said filter bank is an Nth-order Gaussian Derivative filter bank with N being in the range of 5 to 20.
摘要翻译：一种用于检测数字数字数据中的特征的方法，包括获得数字数字数据，其包括对应于具有至少一个维度的域空间上的多个采样点的值，计算多个比例空间数据，包括使用滤波器对所述数字数字数据进行滤波确定尺度空间数据的尺度和位置中的局部极值对应的多个特征区域; 以及为所述多个特征区域中的每一个确定特征区域描述符。滤波器组是余弦调制高斯滤波器组，其中高斯的标准偏差参数等于1＆pgr; （2）2 2 b + 1 2 b - 1乘以余弦波长，其中b在0.75到1.25的范围内，或者所述滤波器组是N阶高斯微分滤波器组，N是在5到20的范围内。

16. 发明申请

US20150024469A1 ENDOLYSIN OBPGPLYS 审中-公开
标题翻译：内罗毕OBPGPLYS
公开(公告)号：US20150024469A1
公开(公告)日：2015-01-22
申请号：US14475900
申请日：2014-09-03
申请人： LYSANDO AG , KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D
发明人： Yves BRIERS , Rob LAVIGNE , Maarten WALMAGH , Stefan MILLER
IPC分类号： C12N9/36 , C07K14/195
CPC分类号： C12N9/2462 , A01N43/50 , A23L3/3571 , A61K38/00 , A61K38/47 , C07K7/08 , C07K14/195 , C07K14/21 , C07K14/43518 , C07K2319/21 , C07K2319/55 , C12Q1/04 , C12Q1/34 , C12Y302/01017 , G01N2333/928
摘要： The present invention relates to a polypeptide with an amino acid sequence according to SEQ ID NO: 1 and fragments or derivatives thereof. The present invention further relates to fusion proteins comprising said polypeptide and an additional peptide stretch fused to said polypeptide at the N- or C-terminus. Moreover, the present invention relates to nucleic acid molecules encoding said polypeptide or fusion protein, vectors comprising said nucleic acid molecules and host cells comprising either said nucleic acid molecules or said vectors. In addition, the present invention relates to said polypeptide or fusion protein for use as a medicament, in particular for the treatment or prevention of Gram-negative bacterial infections, as diagnostic means, as cosmetic substance or as sanitizing agent. The present invention also relates to the use of said polypeptide or fusion protein for the treatment or prevention of Gram-negative bacterial contamination of foodstuff, of food processing equipment, of food processing plants, of surfaces coming into contact with foodstuff, of medical devices, of surfaces in hospitals and surgeries. Furthermore, the present invention relates to a pharmaceutical composition comprising said polypeptide or fusion protein.
摘要翻译：本发明涉及具有根据SEQ ID NO：1的氨基酸序列及其片段或衍生物的多肽。本发明还涉及包含所述多肽的融合蛋白和在N-或C-末端与所述多肽融合的另外的肽拉伸。此外，本发明涉及编码所述多肽或融合蛋白的核酸分子，包含所述核酸分子的载体和包含所述核酸分子或所述载体的宿主细胞。此外，本发明涉及用作药物的所述多肽或融合蛋白，特别是用于治疗或预防革兰氏阴性细菌感染，作为诊断手段，作为化妆品或消毒剂。本发明还涉及所述多肽或融合蛋白用于治疗或预防食品的食品加工设备，食品加工厂，与食品接触的表面，医疗器械的革兰氏阴性细菌污染，在医院和手术中的表面。此外，本发明涉及包含所述多肽或融合蛋白的药物组合物。

17. 发明授权

US08906365B2 Antimicrobial agents 有权
标题翻译：抗微生物剂
公开(公告)号：US08906365B2
公开(公告)日：2014-12-09
申请号：US13380312
申请日：2010-06-28
申请人： Rob Lavigne , Stefan Miller , Yves Briers , Guido Volckaert , Maarten Walmagh
发明人： Rob Lavigne , Stefan Miller , Yves Briers , Guido Volckaert , Maarten Walmagh
IPC分类号： C12N9/24 , C07K14/005 , C07K14/47 , C07K19/00 , A61K38/47 , A61L2/00 , C12N15/56 , C12N15/62 , C12N9/50 , C12N15/52 , C12N9/36 , A61K38/00
CPC分类号： A61K38/47 , A61K38/00 , A61L2/00 , C07K14/005 , C07K14/4723 , C07K2319/00 , C07K2319/20 , C12N9/2462 , C12N9/503 , C12N15/52 , C12N15/62 , C12Y302/01017 , Y02A50/475 , Y02A50/478 , Y02A50/479
摘要： The application relates to antimicrobial agents against Gram-negative bacteria, in particular to fusion proteins composed of an enzyme having the activity of degrading the cell wall of Gram-negative bacteria and a peptide stretch fused to the enzyme at the N- or C-terminus, as well as pharmaceutical compositions thereof. Moreover, it relates to nucleic acid molecules encoding such a fusion protein, vectors carrying the nucleic acid molecules and host cells transformed with either the nucleic acid molecules or the vectors. In addition, it relates to such a fusion protein for use as a medicament, in particular for the treatment or prevention of Gram-negative bacterial infections, as diagnostic means or as cosmetic substance. The application also relates to the treatment or prevention of Gram-negative bacterial contamination of foodstuff, of food processing equipment, of food processing plants, of surfaces coming into contact with foodstuff, of medical devices, of surfaces in hospitals and surgeries.
摘要翻译：本申请涉及抗革兰氏阴性细菌的抗微生物剂，特别是由具有降解革兰氏阴性细菌细胞壁的活性的酶和在N-或C-末端与酶融合的肽拉伸组成的融合蛋白，以及其药物组合物。此外，它涉及编码这种融合蛋白的核酸分子，携带核酸分子的载体和用核酸分子或载体转化的宿主细胞。此外，它涉及用作药物，特别是用于治疗或预防革兰氏阴性细菌感染的这种融合蛋白，作为诊断手段或化妆品。该应用还涉及食品加工设备，食品加工厂，与食品接触的表面，医疗器械，医院和手术中的表面的革兰氏阴性细菌污染的治疗或预防。

18. 发明授权

US08810787B2 Single molecule optical spectroscopy in solid-state nanopores in a transmission-based approach 有权
标题翻译：在基于透射的方法中的固态纳米孔中的单分子光谱
公开(公告)号：US08810787B2
公开(公告)日：2014-08-19
申请号：US13133525
申请日：2009-12-09
申请人： Pol Van Dorpe , Iwijn De Vlaminck , Liesbet Lagae , Gustaaf Borghs
发明人： Pol Van Dorpe , Iwijn De Vlaminck , Liesbet Lagae , Gustaaf Borghs
IPC分类号： G01J3/44
CPC分类号： B82Y15/00 , B82Y20/00 , B82Y40/00 , G01N21/554 , G01N21/648 , G01N21/658 , G01N33/48721 , G01N2021/653 , Y10S977/724 , Y10S977/924
摘要： Methods and apparatus in the field of single molecule sensing are described, e.g. for molecular analysis of analytes such as molecular analytes, e.g. nucleic acids, proteins, polypeptides, peptides, lipids and polysaccharides. Molecular spectroscopy on a molecule translocating through a solid-state nanopore is described. Optical spectroscopic signals are enhanced by plasmonic field-confinement and antenna effects and probed in transmission by plasmon-enabled transmission of light through an optical channel that overlaps with the physical channel.
摘要翻译：描述了单分子感测领域的方法和装置，例如用于分析物如分子分析物的分子分析。核酸，蛋白质，多肽，肽，脂质和多糖。描述了通过固态纳米孔易位的分子的分子光谱。光谱信号通过等离激元场约束和天线效应增强，并通过等离子体激发的光透过与物理信道重叠的光信道进行传输。

19. 发明授权

US08741856B2 Avermectins and milbemycins for the treatment, prevention or amelioration of flavivirus infections 失效
标题翻译：阿维菌素和米尔倍霉素用于治疗，预防或改善黄病毒感染
公开(公告)号：US08741856B2
公开(公告)日：2014-06-03
申请号：US13503660
申请日：2010-10-21
申请人： Mario Milani De Mayo De Mari , Eloise Mastrangelo , Martino Bolognesi , Xavier De Lamballerie , Boris Pastorino , Johan Neyts , Suzanne Kaptein
发明人： Mario Milani De Mayo De Mari , Eloise Mastrangelo , Martino Bolognesi , Xavier De Lamballerie , Boris Pastorino , Johan Neyts , Suzanne Kaptein
IPC分类号： A61K31/70
CPC分类号： A61K31/7048 , A61K31/365 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： Avermectin and milbemycin compounds, particularly the substance ivermectin, for preparing an antiviral medicament for the treatment, prevention or amelioration of a Flavivirus infection, such as those caused by YFV (yellow fever virus), DENV (Dengue virus), JEV (Japanese encephalitis virus), TBEV (tick-borne encephalitis virus) or MODV (Modoc virus) are provided. The antiviral compositions of the present invention are suitable for oral administration to a Flavivirus-infected subject or a subject at risk of a infection, such as a human or other mammal.
摘要翻译：阿维菌素和米尔倍霉素化合物，特别是伊维菌素，用于制备用于治疗，预防或改善黄病毒感染的抗病毒药物，例如由YFV（黄热病毒），DENV（登革热病毒），JEV（日本脑炎病毒），TBEV（蜱传脑炎病毒）或MODV（Modoc病毒）。本发明的抗病毒组合物适合于对黄病毒感染的个体或感染风险的受试者例如人或其他哺乳动物进行口服给药。

20. 发明授权

US08618138B2 Indole amide derivatives and related compounds for use in the treatment of neurodegenerative diseases 有权
标题翻译：吲哚酰胺衍生物和用于治疗神经变性疾病的相关化合物
公开(公告)号：US08618138B2
公开(公告)日：2013-12-31
申请号：US13377505
申请日：2010-06-11
申请人： Gerard Griffioen , Tom Van Dooren , Veronica Rojas De La Parra , Arnaud Marchand , Sara Allasia , Amuri Kilonda , Patrick Chaltin
发明人： Gerard Griffioen , Tom Van Dooren , Veronica Rojas De La Parra , Arnaud Marchand , Sara Allasia , Amuri Kilonda , Patrick Chaltin
IPC分类号： A61K31/4439 , A61K31/422 , C07D413/14 , C07D261/18
CPC分类号： A61K31/4045 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/635 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
摘要翻译：本发明提供新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地说是某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症。本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。

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