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公开(公告)号：US11320438B2
公开(公告)日：2022-05-03
申请号：US15772030
申请日：2016-10-31
发明人： Sasa Koncarevic , Karsten Kuhn , Peter Schulz-Knappe , Ian Hugo Pike , Christiane Opitz , Michael Platten
IPC分类号： G01N33/68 , G01N33/532
摘要： Tryptophan degradation is a key metabolic pathway controlling immune reactions and evidence suggests that during cancer progression generation of tryptophan metabolites may be fundamental for immune escape promoting the malignant phenotype of cancer cells in an autocrine fashion. The present invention relates to methods of measuring mass tag labelled tryptophan and metabolites thereof and methods using the labelled molecules for monitoring in a subject the effectiveness of a treatment and of disease recurrence after treatment, for stratifying patients and for diagnosing suppression of an immune response in a subject.
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公开(公告)号：US10527629B2
公开(公告)日：2020-01-07
申请号：US15318247
申请日：2015-06-12
IPC分类号： G01N33/00 , G01N33/68 , C12Q1/6872 , C07B59/00 , C07K5/02
摘要： The present invention relates to a set of two or more mass labels. Each mass label comprises: X-L-M-Re; X is a reporter moiety having exact mass; L is a bond cleavable by collision in a mass spectrometer; M is a mass modifier; Re is a) a reactive functionality for attaching the mass label to an analyte or b) the analyte. Each mass label in the set has the same integer mass; wherein the set comprises two or more subsets of mass labels, each subset comprising one or more mass labels; wherein, when the subset comprises two or more mass labels, the exact mass of the reporter moiety X of each mass label in the subset is different from the exact mass of the reporter moiety X of the mass labels in the same subset and in all other subsets; each mass label is distinguishable by mass spectrometry.
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公开(公告)号：US20180364244A1
公开(公告)日：2018-12-20
申请号：US16061177
申请日：2016-12-09
IPC分类号： G01N33/58 , C07D207/46 , G01N33/532 , G01N33/68
摘要： The present invention relates to a set of two or more mass labels, wherein each mass label comprises the formula: X-L-M-Re wherein X is a reporter moiety having an exact mass, L is a bond cleavable by collision in a mass spectrometer, M is a mass modifier, and Re is a) a reactive functionality for attaching the mass label to an analyte or b) the analyte, wherein each mass label in the set has an integer mass, wherein each mass label in the set has the same integer mass, and wherein the set comprises two or more subsets of mass labels, each subset comprising one, two or more mass labels, and wherein, when the subset comprises two or more mass labels, the exact mass of the reporter moiety X of each mass label in the subset is different from the exact mass of the reporter moiety X of the mass labels in the same subset and in all other subsets, and wherein each mass label is distinguishable by mass spectrometry.
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公开(公告)号：US20150065392A1
公开(公告)日：2015-03-05
申请号：US14485994
申请日：2014-09-15
发明人： Christian Baumann , Stefan Kienle , Karsten Kuhn , Harald Legner
IPC分类号： G01N33/74 , C07D211/14 , G01N33/58 , C07D401/12
CPC分类号： G01N33/743 , C07B59/002 , C07D211/14 , C07D401/12 , G01N33/58 , G01N2458/15 , G01N2560/00 , Y10T436/196666 , Y10T436/200833 , Y10T436/24
摘要： A reactive mass label for labelling a biological molecule for detection by mass spectrometry includes the following structure: X-L-M-S-Re, wherein X is a mass marker moiety, L is a cleavable linker, M is a mass normalization moiety, and S is a mass series modifying group including the following group: wherein J is C═O, K is NH, and n is 2 or J and K are both CH2 and n is 1, m is at least 1; and Re is a reactive functionality for attaching the reactive mass label to a biological molecule.
摘要翻译： 用于通过质谱法标记用于检测的生物分子的反应性质量标签包括以下结构：XLMS-Re，其中X是质量标记物部分，L是可切割接头，M是质量归一化部分，S是质量序列 包括以下基团的改性基团：其中J为C = O，K为NH，n为2或J和K均为CH 2且n为1，m为至少1; 并且Re是用于将反应性质量标签附着到生物分子的反应性官能团。
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公开(公告)号：US20180362416A1
公开(公告)日：2018-12-20
申请号：US16061136
申请日：2016-12-09
IPC分类号： C07B59/00 , C07D403/12 , G01N33/58
摘要： The present invention relates to a set of two or more mass labels, wherein each mass label comprises the formula: X-L-M-Re wherein X is a reporter moiety having an exact mass, L is a bond cleavable by collision in a mass spectrometer, M is a mass modifier, and Re is a) a reactive functionality for attaching the mass label to an analyte or b) the analyte, wherein each mass label in the set has an integer mass, wherein each mass label in the set has the same integer mass, and wherein the set comprises two or more subsets of mass labels, each subset comprising one, two or more mass labels, and wherein, when the subset comprises two or more mass labels, the exact mass of the reporter moiety X of each mass label in the subset is different from the exact mass of the reporter moiety X of the mass labels in the same subset and in all other subsets, and wherein each mass label is distinguishable by mass spectrometry.
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公开(公告)号：US20180246118A1
公开(公告)日：2018-08-30
申请号：US15772030
申请日：2016-10-31
发明人： Sasa Koncarevic , Karsten Kuhn , Peter Schulz-Knappe , Ian Hugo Pike , Christiane Opitz , Michael Platten
IPC分类号： G01N33/68 , G01N33/532
CPC分类号： G01N33/6848 , G01N33/532 , G01N2458/15
摘要： Tryptophan degradation is a key metabolic pathway controlling immune reactions and evidence suggests that during cancer progression generation of tryptophan metabolites may be fundamental for immune escape promoting the malignant phenotype of cancer cells in an autocrine fashion. The present invention relates to methods of measuring mass tag labelled tryptophan and metabolites thereof and methods using the labelled molecules for monitoring in a subject the effectiveness of a treatment and of disease recurrence after treatment, for stratifying patients and for diagnosing suppression of an immune response in a subject.
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公开(公告)号：US20180140585A1
公开(公告)日：2018-05-24
申请号：US15577522
申请日：2016-05-27
IPC分类号： A61K31/437 , A61K31/13 , A61K31/445 , A61K31/55 , A61K31/57 , C07K14/47 , C12N9/16 , G01N33/68 , A61P25/28
CPC分类号： A61K31/437 , A61K31/13 , A61K31/445 , A61K31/55 , A61K31/57 , A61P25/28 , C07K14/4711 , C12N9/16 , G01N33/6896 , G01N2800/2821 , G01N2800/50 , G01N2800/56 , A61K2300/00
摘要： The invention relates to panels of biomarkers including proteins phosphatase 1 regulatory subunit 14A and/or 2′,3′-cyclic-nucleotide 3′-phosphodiesterase and/or phosphorylated tau or fragments thereof and methods using thereof for diagnosing, staging, treating and assessing the response of a treatment for a neurocognitive disorder characterised by tau toxicity, in particular for Alzheimer's disease. The present invention shows that the biomarkers disclosed herein are elevated in the brain of subjects with an advanced stage of a neurocognitive disorder (Braak stage V/VI) and/or are regulated in the CSF of AD subjects in comparison to cognitively affected non-AD controls; and/or regulated in response to two casein kinase 1 delta inhibitors.
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公开(公告)号：US20170146544A1
公开(公告)日：2017-05-25
申请号：US15412555
申请日：2017-01-23
发明人： PETER SCHULZ-KNAPPE , Ian Pike , Karsten Kuhn
CPC分类号： G01N33/58 , G01N1/28 , G01N33/6848 , G01N33/6851 , G01N33/96 , G01N2001/2893 , G01N2333/4703 , G01N2333/765 , G01N2333/775 , G01N2458/15 , G01N2560/00 , G01N2570/00 , H01J49/0009 , Y10T436/105831
摘要： Provided is a method of assaying for an analyte, including combining a test sample having the analyte, with a calibration sample having at least two different aliquots of the analyte, each aliquot having a different known quantity of the analyte. The test sample and each aliquot are differentially labeled with one or more isobaric mass labels each with a mass spectrometrically distinct mass marker group, such that the test sample and each aliquot of the calibration sample can be distinguished by mass spectrometry. The method further includes determining by mass spectrometry the quantity of analyte in the test sample and in each aliquot, and calibrating the quantity of analyte in the test sample against known and determined quantities of analytes in the aliquots.
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9.发明申请CASEIN KINASE 1delta (CK 1delta) INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES SUCH AS TAUOPATHIES 审中-公开CASEIN KINASE 1Delta（CK 1delta）抑制剂及其在治疗神经病变性疾病如TAUOPATHIES中的应用公开(公告)号：US20160354375A1
公开(公告)日：2016-12-08
申请号：US15171582
申请日：2016-06-02
IPC分类号： A61K31/517 , A61K31/444 , A61K31/506
CPC分类号： A61K31/517 , A61K31/397 , A61K31/4045 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/55 , C07D209/42 , C07D277/68 , C07D401/04 , C07D401/12 , C07D403/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D413/06 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/14 , C07D495/14
摘要： The invention relates to pharmaceutical compositions comprising casein kinase 1 delta (CK1δ) and to the use of said inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.
摘要翻译： 本发明涉及包含酪蛋白激酶1δ（CK1δ）的药物组合物以及所述抑制剂在治疗神经变性疾病如阿尔茨海默氏病中的用途。
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公开(公告)号：US20150209368A1
公开(公告)日：2015-07-30
申请号：US14677273
申请日：2015-04-02
IPC分类号： A61K31/55 , A61K31/4192 , A61K31/397 , A61K31/53 , A61K31/437 , A61K31/506 , A61K31/4439 , A61K31/519
CPC分类号： A61K31/517 , A61K31/397 , A61K31/4045 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/55 , C07D209/42 , C07D277/68 , C07D401/04 , C07D401/12 , C07D403/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D413/06 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/14 , C07D495/14
摘要： The invention relates to pharmaceutical compositions having casein kinase 1 delta (CK1δ) inhibitors and to the use of the inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.
摘要翻译： 本发明涉及具有酪蛋白激酶1δ（CK1δ）抑制剂的药物组合物以及抑制剂用于治疗神经变性疾病如阿尔茨海默病的用途。
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