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71. 发明授权

US07381537B2 Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease 有权
标题翻译：使用谷氨酰胺酰环化酶抑制剂治疗和预防疾病
公开(公告)号：US07381537B2
公开(公告)日：2008-06-03
申请号：US10839017
申请日：2004-05-05
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre J. Niestroj , Stephan Schilling , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre J. Niestroj , Stephan Schilling , Ulrich Heiser
IPC分类号： C12Q1/34
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译：本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物，这种效应物的筛选方法，以及包含这些效果子的这种效应物和药物组合物的用途，用于治疗可以通过调节QC活性来治疗。优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。

72. 发明授权

US07368421B2 Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis 失效
标题翻译：二肽基肽酶IV抑制剂在多发性硬化症的治疗中的应用
公开(公告)号：US07368421B2
公开(公告)日：2008-05-06
申请号：US10126374
申请日：2002-04-19
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Konrad Glund , Ulrich Heiser , Stephan von Hoersten
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Konrad Glund , Ulrich Heiser , Stephan von Hoersten
IPC分类号： A61K38/00 , A61K38/02 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08 , C07K2/00 , C07K7/04 , C07K5/02 , C07K5/08 , C07K5/10
CPC分类号： C07K7/06 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D277/04 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The present invention provides a new use of DP IV-inhibitors. The compounds of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in treating conditions mediated by DP IV or DP IV-like enzymes, such as immune, autoimmune or central nervous system disorder selected from the group consisting of strokes, tumors, ischemia, Parkinson's disease and migraines. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of multiple sclerosis.
摘要翻译：本发明提供DPIV-抑制剂的新用途。本发明的化合物及其相应的药学上可接受的酸加成盐形式可用于治疗由DP IV或DP IV样酶介导的病症，例如免疫，自身免疫或中枢神经系统疾病，其选自中风，肿瘤，局部缺血，帕金森病和偏头痛。在更优选的实施方案中，本发明的化合物可用于治疗多发性硬化。

73. 发明授权

US07144856B2 Inhibitors of dipeptidyl peptidase I 失效
公开(公告)号：US07144856B2
公开(公告)日：2006-12-05
申请号：US10997821
申请日：2004-11-24
申请人： Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
发明人： Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
IPC分类号： A61K38/05 , C07K5/06
CPC分类号： C07K5/06026 , C07K5/06
摘要： The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I)which can be used in the treatment of malignant cell degeneration, immune diseases impaired wound healing and metabolic diseases of humans and are represented by the general formula and the pharmaceutical salts thereof, in which R is a peptide or a branched or unbranched C1–C9 alkyl chain, a branched or unbranched C2–C9 alkenyl chain, a branched or unbranched C2–C9 alkynyl chain, a C3–C9 cycloalkyl, C4–C9 carbocyclic, C5–C14 aryl, C3–C9 heteroaryl, C3–C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R′ is a branched or unbranched C1–C9 alkyl chain, a branched or unbranched C2–C9 alkenyl chain, a branched or unbranched C2–C9 alkynyl chain, a C3–C9 cycloalkyl, C4–C9 cycloalkenyl, C2–C9 heterocycloalkyl, C3–C9 heterocycloalkenyl, C5–C14 aryl, C3–C9 heteroaryl, C3–C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues may be optionally substituted, or is H.

74. 发明申请

US20060178315A1 Irreversible cysteine protease inhibitors of legumain 失效
标题翻译：不可逆的半胱氨酸蛋白酶抑制剂
公开(公告)号：US20060178315A1
公开(公告)日：2006-08-10
申请号：US10485723
申请日：2002-07-23
申请人： Andre Niestroj , Ulrich Heiser , Bernd Gerhartz , Matthias Hoffmann , Hans-Ulrich Demuth
发明人： Andre Niestroj , Ulrich Heiser , Bernd Gerhartz , Matthias Hoffmann , Hans-Ulrich Demuth
IPC分类号： A61K38/04 , C07K5/04 , C07D403/02
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0806
摘要： Presented are compounds represented by the following general formulas (I) and (II), for inhibiting cysteine protease legumain for modulating associated disease states in subjects.
摘要翻译：提出了由以下通式（I）和（II）表示的化合物，其用于抑制半胱氨酸蛋白酶调节因子用于调节受试者中的相关疾病状态。

75. 发明授权

US06946480B2 Glutaminyl based DPIV inhibitors 失效
标题翻译：基于谷氨酰胺基的DPIV抑制剂
公开(公告)号：US06946480B2
公开(公告)日：2005-09-20
申请号：US10244347
申请日：2002-09-16
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
IPC分类号： C07D295/18 , A61K31/40 , A61K31/426 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , A61P3/04 , A61P3/10 , A61P17/00 , A61P17/02 , A61P19/02 , A61P25/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/04 , C07D277/04 , C07D295/185 , C07K5/083 , C07K5/087 , C07K7/06 , A61K31/425 , C07D207/00
CPC分类号： C07D277/04 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D295/185 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K7/06
摘要： The present invention provides compounds of the formula: wherein X═CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
摘要翻译：本发明提供下式的化合物：其中X-CH 2或S或其药学上可接受的盐可用于治疗由DPIV或DPIV样酶如关节炎，肥胖，免疫和自身免疫介导的病症疾病，同种异体移植，癌症，神经元疾病和皮肤疾病。

76. 发明授权

US06844316B2 Inhibitors of dipeptidyl peptidase I 失效
标题翻译：二肽基肽酶I的抑制剂
公开(公告)号：US06844316B2
公开(公告)日：2005-01-18
申请号：US10236136
申请日：2002-09-06
申请人： Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
发明人： Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
IPC分类号： C07K5/06 , A61K38/05
CPC分类号： C07K5/06026 , C07K5/06
摘要： The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I), which can be used in the treatment of malignant cell degeneration, immune deseases impaired wound healing and metabolic diseases of humans and are represented by the general formula in which R is a peptide or a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 carbocyclic, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R′ is a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 cycloalkenyl, C2-C9 heterocycloalkyl, C3-C9 heterocycloalkenyl, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues may be optionally substituted, or is H.
摘要翻译：本发明涉及半胱氨酸蛋白酶二肽基肽酶I（DPI）的特异性抑制剂，其可用于治疗恶性细胞变性，免疫性疾病受损的伤口愈合和人类的代谢性疾病，并由通式表示，其中R 支链或非支链C 1 -C 9烷基链，支链或非支链C 2 -C 9烯基链，支链或非支链C 2 -C 9炔基链，C 3 -C 9环烷基，C 4 -C 9碳环，C 5 -C 14芳基， C3-C9杂芳基，C3-C9杂环，所有上述残基任选被取代，残基AS-AS是二肽或其模拟物，AS是氨基酸或其模拟肽。氨基酸是与R结合的肽，R'是支链或非支链C1-C9烷基链，支链或非支链C2-C9烯基链，支链或非支链C2-C9炔基链，C3-C9环烷基，C4- C 9环烯基，C 2 -C 9杂环烷基，C 3 -C 9杂环烯基，C 5 -C 14芳基，C 3 -C 9杂芳基，C 3 -C 9杂环基，而杂环烷基，杂环烯基，杂芳基，杂环残基可以具有多达6个杂环原子，或其肽模拟物，所有上述残基可以任选被取代，或者是H.

77. 发明申请

US20050137142A1 Combinations useful for the treatment of neuronal disorders 审中-公开
标题翻译：用于治疗神经元疾病的组合
公开(公告)号：US20050137142A1
公开(公告)日：2005-06-23
申请号：US10976677
申请日：2004-10-29
申请人： Ingo Schulz , Stephan Schilling , Andre Niestroj , Hans-Ulrich Demuth , Steffen Rossner
发明人： Ingo Schulz , Stephan Schilling , Andre Niestroj , Hans-Ulrich Demuth , Steffen Rossner
IPC分类号： A61K31/00 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K38/04
CPC分类号： A61K31/401 , A61K31/00 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K2300/00
摘要： The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, inhibitors of DP IV/DP IV-like enzymes, NPY-receptor ligands, NPY agonists, NPY antagonists, ACE-inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases and inhibitors of neutral endopeptidase, to a mammal in need thereof.
摘要翻译：本发明提供在哺乳动物例如人中治疗神经元疾病的方法，该方法包括施用有效的，无毒的和药学上可接受量的至少一种QC抑制剂，任选地与至少一种选自PEP抑制剂，DP IV / DP IV类酶抑制剂，NPY受体配体，NPY激动剂，NPY拮抗剂，ACE抑制剂，PIMT增强剂，β分泌酶抑制剂，γ分泌酶抑制剂和中性肽链内切酶的抑制剂。

78. 发明申请

US20130116290A1 Use of Dipeptidyl Peptidase IV Effectors for Normalizing the Blood Glucose Level in Mammals 审中-公开
标题翻译：使用二肽基肽酶IV效应物来调节哺乳动物血糖水平
公开(公告)号：US20130116290A1
公开(公告)日：2013-05-09
申请号：US13458484
申请日：2012-04-27
申请人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert P. Pauly , Christopher H.S. McIntosh , Ray A. Pederson
发明人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert P. Pauly , Christopher H.S. McIntosh , Ray A. Pederson
IPC分类号： A61K31/426
CPC分类号： A61K31/426 , A61K9/0019 , A61K9/0053 , A61K31/00 , A61K31/40 , A61K31/401
摘要： The present invention comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to lower elevated post-prandial and basal blood glucose levels in mammalian organisms. The invention further comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to increase the half-life of incretins in vivo.
摘要翻译：本发明包括使用哺乳动物血液中二肽基肽酶（DP IV）的活性降低作用剂和DP IV类似酶活性降低哺乳动物生物体内升高的餐后和基础血糖水平。本发明还包括在哺乳动物的血液中使用二肽基肽酶（DP IV）的活性降低效应物和DP IV-类似酶活性以增加体内胰岛素的半衰期。

79. 发明申请

US20120070444A1 IN VIVO SCREENING MODELS FOR TREATMENT OF isoQC-RELATED DISORDERS 审中-公开
标题翻译：用于治疗等质量相关疾病的生殖器筛查模型
公开(公告)号：US20120070444A1
公开(公告)日：2012-03-22
申请号：US13225033
申请日：2011-09-02
申请人： Sigrid Graubner , Reinhard Sedlmeier , Andreas Becker , Stephan Schilling , Holger Cynis , Hans-Ulrich Demuth
发明人： Sigrid Graubner , Reinhard Sedlmeier , Andreas Becker , Stephan Schilling , Holger Cynis , Hans-Ulrich Demuth
IPC分类号： A61K38/45 , C07K16/00 , A61K49/00 , A01K67/027 , A61P1/04 , A61P25/00 , A61P25/28 , A61P35/00 , A61P31/04 , A61P25/18 , A61P15/00 , A61P29/00 , A61P35/04 , A61P17/06 , A61P11/00 , A61P1/16 , A61P3/00 , A61P5/00 , C12N5/10
CPC分类号： A01K67/0278 , A01K67/0275 , A01K2217/052 , A01K2217/15 , A01K2217/206 , A01K2227/105 , A01K2267/0312 , A01K2267/0318 , C12N9/104 , C12N15/8509 , C12Y203/02005 , G01N33/5088 , G01N2333/9108 , G01N2500/10
摘要： A transgenic non-human animal for overexpressing isoQC, comprising cells containing a DNA transgene encoding human isoQC, characterized in that said human isoQC comprises the amino acid sequence of SEQ ID NO: 1 or an amino acid sequence having at least 75% sequence identity to the amino acid sequence of SEQ ID NO: 1 or a fragment or derivative of the amino acid sequence of SEQ ID NO: 1. Additionally disclosed is a method of screening for biologically active agents that inhibit or promote isoQC.
摘要翻译：一种用于过表达isoQC的转基因非人动物，其包含含有编码人isoQC的DNA转基因的细胞，其特征在于所述人isoQC包含SEQ ID NO：1的氨基酸序列或与SEQ ID NO：1的氨基酸序列具有至少75％ SEQ ID NO：1的氨基酸序列或SEQ ID NO：1的氨基酸序列的片段或衍生物。另外公开了筛选抑制或促进isoQC的生物活性剂的方法。

80. 发明申请

US20110091910A1 NOVEL ASSAY 审中-公开
标题翻译：新的测定
公开(公告)号：US20110091910A1
公开(公告)日：2011-04-21
申请号：US12884403
申请日：2010-09-17
申请人： Martin Kleinschmidt , Claudia Goettlich , Hans-Ulrich Demuth
发明人： Martin Kleinschmidt , Claudia Goettlich , Hans-Ulrich Demuth
IPC分类号： G01N33/566
CPC分类号： G01N33/6896 , G01N2333/4709 , G01N2800/2821
摘要： A novel method for detection of Aβ peptides, in particular in plasma, and to the use of Aβ peptides for diagnosis of Alzheimer's disease.
摘要翻译：一种新的A＆Bgr检测方法肽，特别是血浆中的肽，以及使用A＆bgr; 用于诊断阿尔茨海默氏病的肽。

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