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1. 发明授权

US06573277B2 Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids 失效
标题翻译：环状和杂环N-取代的α-亚氨基肟基和羧酸
公开(公告)号：US06573277B2
公开(公告)日：2003-06-03
申请号：US09780514
申请日：2001-02-12
申请人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase , Eckart Bartnik , Klaus-Ulrich Weithmann
发明人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase , Eckart Bartnik , Klaus-Ulrich Weithmann
IPC分类号： A61K314709
CPC分类号： C07D405/12 , C07D209/42 , C07D217/26 , C07D471/04 , C07D491/04
摘要： Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.
摘要翻译：式I化合物适用于制备用于治疗病症的药物，其中包括增加基质降解金属蛋白酶的活性。

2. 发明授权

US06207672B1 Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and carboxyclic acids 有权
标题翻译：环状和杂环N-取代的α-亚氨基肟酸和羧基酸
公开(公告)号：US06207672B1
公开(公告)日：2001-03-27
申请号：US09068497
申请日：1999-03-09
申请人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase , Eckart Bartnik , Klaus-Ulrich Weithmann
发明人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase , Eckart Bartnik , Klaus-Ulrich Weithmann
IPC分类号： A61K31472
CPC分类号： C07D405/12 , C07D209/42 , C07D217/26 , C07D471/04 , C07D491/04
摘要： Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.
摘要翻译：式I化合物适用于制备用于治疗病症的药物，其中包括增加基质降解金属蛋白酶的活性。

3. 发明授权

US06180334B2 Artificial recombinant substrate (rAGG 1) and native aggrecan to determine the proteolytic activity of ‘aggrecanase’ in cell culture systems 有权
标题翻译：人工重组底物（rAGG 1）和天然聚集蛋白聚糖来确定细胞培养系统中“聚集蛋白聚糖酶”的蛋白水解活性
公开(公告)号：US06180334B2
公开(公告)日：2001-01-30
申请号：US09176228
申请日：1998-10-21
申请人： Eckart Bartnik , Bernd Eidenmueller , Frank Buettner , Bruce Caterson , Clare Hughes
发明人： Eckart Bartnik , Bernd Eidenmueller , Frank Buettner , Bruce Caterson , Clare Hughes
IPC分类号： C12Q100
CPC分类号： C40B40/02 , C07K14/4725 , C07K2319/00 , C07K2319/02 , C12N9/6421 , C12N15/1037 , C12Q1/37 , G01N33/573
摘要： The invention relates to novel recombinant substrates for aggrecanase. In one embodiment, this substrate comprises the signal sequence of CD5, the FLAG-epitope for M1 monoclonal antibody detection, the interglobular domain of human aggrecan, the hinge region of human IgG1, the CH2 region of human IgG1 and the CH3 region of human IgG1. DNA sequences encoding the recombinant substrate are also provided, as are vectors and host cells containing said DNA. Various methods are provided for: monitoring aggrecanase activity, detecting new enzymatic cleavage sites, purifying aggrecanase chromatographically, and cloning the aggrecanase cDNA, screening for aggrecanase inhibitors; and for monitoring the onset or progression of osteoarthritis. A diagnostic aid containing the recombinant substrate is also provided.
摘要翻译：本发明涉及用于聚集蛋白聚糖蛋白聚糖酶的新型重组底物。在一个实施方案中，该底物包含CD5的信号序列，用于M1单克隆抗体检测的FLAG表位，人聚集蛋白聚糖的小球结构域，人IgG1的铰链区，人IgG1的CH2区和人IgG1的CH3区。还提供了编码重组底物的DNA序列，载体和含有所述DNA的宿主细胞也是如此。提供了多种方法：监测聚集蛋白聚糖酶活性，检测新的酶裂解位点，纯化聚蛋白聚糖蛋白酶，色谱纯化，克隆聚蛋白聚糖酶cDNA，筛选聚集蛋白聚糖酶抑制剂; 并监测骨关节炎的发病或发展。还提供了含有重组基质的诊断助剂。

4. 发明授权

US5872209A Artificial recombinant substrate (rAGG 1) and native aggrecan to determine the proteolytic activity of `aggrecanase` in cell culture systems 失效
标题翻译：人工重组底物（rAGG 1）和天然聚集蛋白聚糖来确定细胞培养系统中“聚集蛋白聚糖蛋白酶”的蛋白水解活性
公开(公告)号：US5872209A
公开(公告)日：1999-02-16
申请号：US784512
申请日：1997-01-17
申请人： Eckart Bartnik , Bernd Eidenmueller , Frank Buettner , Bruce Caterson , Clare Hughes
发明人： Eckart Bartnik , Bernd Eidenmueller , Frank Buettner , Bruce Caterson , Clare Hughes
IPC分类号： C07K14/47 , C07K16/40 , C12N5/10 , C12N9/64 , C12N15/09 , C12N15/10 , C12N15/12 , C12P21/02 , C12Q1/37 , C12R1/91 , C40B40/02 , G01N33/573 , A61K38/00 , A61K38/17 , C12P21/06
CPC分类号： C40B40/02 , C07K14/4725 , C12N15/1037 , C12N9/6421 , C12Q1/37 , G01N33/573 , C07K2319/00 , C07K2319/02
摘要： The invention relates to novel recombinant substrates for aggrecanase. In one embodiment, this substrate comprises the signal sequence of CD5, the FLAG-epitope for M1 monoclonal antibody detection, the interglobular domain of human aggrecan, the hinge region of human IgG1, the CH2 region of human IgG1 and the CH3 region of human IgG1. DNA sequences encoding the recombinant substrate are also provided, as are vectors and host cells containing said DNA. Various methods are provided for: monitoring aggrecanase activity, detecting new enzymatic cleavage sites, purifying aggrecanase chromatographically, and cloning the aggrecanase cDNA, screening for aggrecanase inhibitors; and for monitoring the onset or progression of osteoarthritis. A diagnostic aid containing the recombinant substrate is also provided.
摘要翻译：本发明涉及用于聚集蛋白聚糖蛋白聚糖酶的新型重组底物。在一个实施方案中，该底物包含CD5的信号序列，用于M1单克隆抗体检测的FLAG表位，人聚集蛋白聚糖的小球结构域，人IgG1的铰链区，人IgG1的CH2区和人IgG1的CH3区。还提供了编码重组底物的DNA序列，载体和含有所述DNA的宿主细胞也是如此。提供了多种方法：监测聚集蛋白聚糖酶活性，检测新的酶切位点，纯化聚蛋白聚糖蛋白聚糖酶色谱，克隆聚蛋白聚糖蛋白聚糖酶cDNA，筛选聚集蛋白聚糖酶抑制剂; 并监测骨关节炎的发病或发展。还提供了含有重组基质的诊断助剂。

5. 发明授权

US5817742A Polymer-conjugated malonic acid derivatives and their use as medicaments and diagnostic agents 失效
标题翻译：聚合物共轭丙二酸衍生物及其作为药物和诊断剂的用途
公开(公告)号：US5817742A
公开(公告)日：1998-10-06
申请号：US718524
申请日：1996-09-11
申请人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Wolfgang Schmidt , Brigitte Horsch
发明人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Wolfgang Schmidt , Brigitte Horsch
IPC分类号： A61K31/785 , A61K31/70 , A61K31/7028 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P43/00 , C07H3/04 , C07H3/06 , C07H15/04 , C07H15/207 , C07H17/04 , C08G69/10 , C08G69/48 , C08G73/06 , C08G73/10
CPC分类号： C07H3/04 , C07H15/207 , C07H17/04 , C07H3/06 , C08G73/0611
摘要： Polymer-based polyvalent malonic acid derivatives having anti-adhesive properties are described. The compounds comprise a polyamino acid linked to a group of formula (I). In formula (I), R.sup.1 and R.sup.2 together form a six-membered carbocylic or heterocyclic ring, containing at least one substituent selected from R.sup.4, R.sup.5, and R.sup.6. R.sup.3 is H, (CH.sub.2) .sub.m X or CH.sub.2 O(CH.sub.2).sup.m X.sup.1. The polyamino acid and the group of formula II are linked via R.sup.4, R.sup.5, or R.sup.6, or optionally via a spacer of formula --�Q.sup.1 --(CH.sub.2).sub.p --Q.sup.2 --!.sub.r. A and B independently are O, S, NH, HN--CO, OC--NH, O--CO, OC--O, NH--CO--O, --O--CO--NH, S--CO, SC--O, O--CS--S, S--CS--OS, NH--CS--S, S--CS--NH, or CH.sub.2. Z is a pyranose, furanose, open-chain polyalcohol or Y--X.sup.6. Y is --O--(CX.sup.2,X.sup.3).sub.n, -(CX.sup.2,X.sup.3).sub.n, --CH.sub.2 --(CX.sup.2,X.sup.3).sub.n or a saturated or unsaturated six-membered carbo- or heterocyclic group having at least one substituent R.sup.9, or a combination of the chain --O--(CX.sup.2,X.sup.3).sub.n, or -(CX.sup.2,X.sup.3).sub.n, and the carbocyclic or heterocyclic group, in which R.sup.4, R.sup.5, and R.sup.6 independently are H, OH, --O--(CH.sub.2) .sub.q X.sup.4, --CH.sub.2 O(CH.sub.2) .sub.q X.sup.5, or HNC(O)CH.sub.3, and X, X.sup.1, X.sup.2, and X.sup.3 independently are H, NH.sub.2, COOH, OH, CH.sub.2 OH, CH.sub.2 NH.sub.2, C.sub.1 -C.sub.20 -alkyl, or C.sub.6 -C.sub.10 -aryl, X.sup.4 and X.sup.5 independently are --NH-- or --O--, and X.sup.6 is OH or --C(R.sup.3) (COOH).sub.2. m, n, and q independently can be 1-20. In the linker, Q.sup.1 is CH.sub.2 or --CO--, Q.sup.2 is --NH-- or --CO--NH--, p is 1-6, and r is 0 or 1. Methods of preparing the compounds, and their use as medicaments or diagnostic agents also are disclosed. ##STR1##
摘要翻译： PCT No.PCT / EP95 / 00844 Sec。 371日期：1996年9月11日 102（e）1996年9月11日PCT PCT 1995年3月7日PCT公布。公开号WO95 / 24437 日期1995年9月14日描述了具有防粘性的聚合物多价丙二酸衍生物。化合物包含与式（I）的基团连接的聚氨基酸。在式（I）中，R 1和R 2一起形成含有至少一个选自R4，R5和R6的取代基的六元碳环或杂环。 R3是H，（CH2）mX或CH2O（CH2）mX1。聚氨基酸和式II基团通过R4，R5或R6连接，或任选地经由式[Q1-（CH2）p-Q2-] r的间隔基连接。 A和B分别是O，S，NH，HN-CO，OC-NH，O-CO，OC-O，NH-CO-O，-O-CO-NH，S-CO，SC-O， CS-S，S-CS-OS，NH-CS-S，S-CS-NH或CH 2。 Z是吡喃糖，呋喃糖，开链多元醇或Y-X6。 Y是-O-（CX2，X3）n， - （CX2，X3）n，-CH2-（CX2，X3）n或具有至少一个取代基R9的饱和或不饱和六元碳 - 或杂环基，或链-O-（CX2，X3）n或 - （CX2，X3）n和碳环或杂环基团的组合，其中R4，R5和R6独立地为H，OH，-O-（CH2 ）qX4，-CH2O（CH2）qX5或HNC（O）CH3，X，X1，X2和X3独立地为H，NH2，COOH，OH，CH2OH，CH2NH2，C1-C20-烷基或C6-C10 芳基，X 4和X 5独立地是-NH-或-O-，X 6是OH或-C（R 3）（COOH）2。 m，n和q独立地可以是1-20。在接头中，Q1是CH2或-CO-，Q2是-NH-或-CO-NH-，p是1-6，r是0或1.制备化合物的方法及其用作药物或诊断代理商也被披露。

6. 发明授权

US5693621A Malonic acid derivatives having antiadhesive properties 失效
标题翻译：具有抗粘附性的丙二酸衍生物
公开(公告)号：US5693621A
公开(公告)日：1997-12-02
申请号：US403525
申请日：1995-03-13
申请人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Dirk Seiffge
发明人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Dirk Seiffge
IPC分类号： C07H15/04 , A61K31/70 , A61K31/7028 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P43/00 , C07H3/04 , C07H3/06 , C07H15/207 , C07H17/04 , A61K31/19 , C07C55/00 , C07H15/00
CPC分类号： C07H15/207 , C07H17/04 , C07H3/04 , C07H3/06
摘要： The invention relates to malonic acid derivatives, which inhibit the binding of selectin to carbohydrate ligands, and pharmaceutical compositions and diagnostic agents containing these derivatives, and methods for using these pharmaceutical compositions and diagnostic agents.
摘要翻译：本发明涉及抑制选择蛋白与碳水化合物配体的结合的丙二酸衍生物以及含有这些衍生物的药物组合物和诊断剂，以及使用这些药物组合物和诊断剂的方法。

7. 发明申请

US20050037965A1 Use of PAK inhibitor for the treatment of a joint disease 有权
标题翻译：使用PAK抑制剂治疗关节疾病
公开(公告)号：US20050037965A1
公开(公告)日：2005-02-17
申请号：US10893025
申请日：2004-07-16
申请人： Sebastian Barradeau , Eckart Bartnik , Joerg Czech , Andreas Klatt , Ekkehard Leberer , Thomas Leeuw
发明人： Sebastian Barradeau , Eckart Bartnik , Joerg Czech , Andreas Klatt , Ekkehard Leberer , Thomas Leeuw
IPC分类号： A61K38/17 , A61K48/00 , C07K16/44
CPC分类号： A61K38/17 , C07K16/44 , Y10T436/143333
摘要： The invention refers to the use of a p21-activated kinase (PAK) inhibitor for the treatment of a joint disease such as osteoarthritis or rheumatoid arthritis or for the treatment of a joint pain and the use of PAK as a target protein for the discovery of a PAK inhibitor as a medicament for the treatment of a joint disease.
摘要翻译：本发明涉及使用p21激活的激酶（PAK）抑制剂来治疗关节疾病如骨关节炎或类风湿性关节炎或用于治疗关节疼痛，以及使用PAK作为靶蛋白来发现 PAK抑制剂作为治疗关节疾病的药物。

8. 发明授权

US6136790A Carbohydrate mimetics having antiadhesive properties 失效
标题翻译：具有抗粘附性的碳水化合物模拟物
公开(公告)号：US6136790A
公开(公告)日：2000-10-24
申请号：US999957
申请日：1997-07-28
申请人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Dirk Seiffge
发明人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Dirk Seiffge
IPC分类号： A61K31/785 , A61K31/70 , A61K31/7028 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P43/00 , C07H3/04 , C07H3/06 , C07H15/04 , C07H15/207 , C07H17/04 , C08G69/10 , C08G69/48 , C08G73/06 , C08G73/10 , C07H15/00
CPC分类号： C07H3/04 , C07H15/207 , C07H17/04 , C07H3/06 , C08G73/0611
摘要： The invention relates to carbohydrate mimetics, which inhibit the binding of selectin to carbohydrate ligands, of the formula I ##STR1## excluding the compounds sialyl-Lewis-X and -A and their derivatives which, instead of an N-acetyl group, carry the substituents N.sub.3, NH.sub.2 or OH or which, instead of fucose, carry glycerol,and pharmaceutical compositions and diagnostic agents containing these derivatives, and methods for using these pharmaceutical compositions and diagnostic agents.
摘要翻译：本发明涉及抑制选择蛋白与碳水化合物配体结合的碳水化合物模拟物，其不包括化合物唾液酸基-LX-X和-A及其衍生物，其代替N-乙酰基携带取代基N 3， NH 2或OH，或代替岩藻糖携带甘油，以及含有这些衍生物的药物组合物和诊断剂，以及使用这些药物组合物和诊断剂的方法。

9. 发明授权

US5811405A Multiply fucosylated dicarboxylic acids possessing antiadhesive properties 失效
标题翻译：具有抗粘附性的倍增岩藻糖化二羧酸
公开(公告)号：US5811405A
公开(公告)日：1998-09-22
申请号：US788269
申请日：1997-01-24
申请人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Christoph Huls , Dirk Seiffge
发明人： Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Christoph Huls , Dirk Seiffge
IPC分类号： C07H15/04 , A61K31/70 , A61K31/7028 , A61K31/715 , A61K49/00 , A61P9/00 , A61P9/08 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/06 , A61P43/00 , C07C55/02 , C07C55/22 , C07C55/24 , C07C55/26 , C07C59/235 , C07C217/08 , C07C219/06 , C07C229/24 , C07H3/04 , C07H3/06 , C08B37/00 , C07H1/00
CPC分类号： C07H3/06 , C07H3/04
摘要： The invention relates to multiply fucosylated dicarboxylic acid derivatives possessing antiadhesive properties, to a process for preparing them, to their use, and to pharmaceuticals and diagnostic agents which are prepared from these derivatives. These multiply fucosylated dicarboxylic acid derivatives are suitable for preparing pharmaceuticals or diagnostic agents for diseases which are associated with an excessive, selectin receptor-mediated cell adhesion in the tissue which is affected by the disease.
摘要翻译：本发明涉及具有抗粘附性的多重岩藻糖基化二羧酸衍生物，其制备方法及其应用，以及由这些衍生物制备的药物和诊断剂。这些多重岩藻糖基化二羧酸衍生物适用于制备与受该疾病影响的组织中过度选择素受体介导的细胞粘附相关的疾病的药物或诊断剂。

10. 发明申请

US20090104279A1 USE OF PAK INHIBITOR FOR THE TREATMENT OF A JOINT DISEASE 有权
标题翻译： PAK抑制剂用于治疗联合疾病的使用
公开(公告)号：US20090104279A1
公开(公告)日：2009-04-23
申请号：US12055511
申请日：2008-03-26
申请人： Sebastian BARRADEAU , Eckart BARTNIK , Joerg CZECH , Andreas R. Klatt , Ekkehard LEBERER , Thomas LEEUW
发明人： Sebastian BARRADEAU , Eckart BARTNIK , Joerg CZECH , Andreas R. Klatt , Ekkehard LEBERER , Thomas LEEUW
IPC分类号： A61K35/12 , C12Q1/48 , G01N33/50 , C40B30/00 , G01N33/53 , G01N33/536
CPC分类号： A61K38/17 , C07K16/44 , Y10T436/143333
摘要： The invention refers to the use of a p21-activated kinase (PAK) inhibitor as a target protein for the discovery of a PAK inhibitor as a medicament for the treatment of a joint disease.
摘要翻译：本发明涉及使用p21激活的激酶（PAK）抑制剂作为靶蛋白，用于发现PAK抑制剂作为治疗关节疾病的药物。

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