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1. 发明授权

US06221866B1 Indanyl-substituted benzenecarboxamides, processes for their preparation, their use as a medicament, and pharmaceutical formulations containing them 失效
标题翻译：茚满基取代的苯甲酰胺，其制备方法，它们作为药物的用途，以及含有它们的药物制剂
公开(公告)号：US06221866B1
公开(公告)日：2001-04-24
申请号：US09603436
申请日：2000-06-23
申请人： Joachim Brendel , Uwe Gerlach , Hans Ulrich Stilz , Hans-Jochen Lang
发明人： Joachim Brendel , Uwe Gerlach , Hans Ulrich Stilz , Hans-Jochen Lang
IPC分类号： A61K31535
CPC分类号： C07D295/26 , C07C311/16 , C07C311/20 , C07C311/21 , C07C311/26 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D217/02
摘要： in which R(1) to R(8) have the meanings stated in the claims, act on the Kv1.5 potassium channel, and inhibit a potassium current, referred to as “ultra-rapidly activating delayed rectifier,” in the human atrium. They are therefore very particularly suitable as novel antiarrhythmic active substances, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g., atrial fibrillation or atrial flutter.
摘要翻译：其中R（1）至R（8）具有权利要求中所述的含义，作用于Kv1.5钾通道，并抑制在人心房中称为“超快速活化延迟整流剂”的钾电流。因此，它们特别适合作为新型抗心律失常活性物质，特别是用于治疗和预防房性心律失常，例如房颤或心房颤动。

2. 发明授权

US06759424B2 Imidazolidine derivatives, their preparation, their use, and pharmaceutical preparations comprising them 有权
标题翻译：咪唑烷衍生物，其制备方法，用途及包含它们的药物制剂
公开(公告)号：US06759424B2
公开(公告)日：2004-07-06
申请号：US10147921
申请日：2002-05-20
申请人： Volkmar Wehner , Hans Ulrich Stilz , Wolfgang Schmidt , Dirk Seiffge
发明人： Volkmar Wehner , Hans Ulrich Stilz , Wolfgang Schmidt , Dirk Seiffge
IPC分类号： C07D23302
CPC分类号： C07K5/1024 , A61K38/00 , C07K5/0202 , C07K5/0812 , C07K5/0821 , C07K5/1016 , C07K5/1027 , Y02A50/411
摘要： The present invention relates to novel imidazolidine derivatives of the formula I, in which B, E, W, Z, R, R0, R2, R3, e and h have the meanings indicated in the application. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use in the therapy and prophylaxis of the disease states mentioned and pharmaceutical preparations which contain compounds of the formula I.
摘要翻译：本发明涉及式I的新型咪唑烷衍生物，其中B，E，W，Z，R，R 0，R 2，R 3，e和h具有本申请中指出的含义。式I的化合物是有价值的药物活性化合物，其适用于例如治疗和预防炎症性疾病，例如类风湿性关节炎或过敏性疾病。式I的化合物是属于整联蛋白组的粘附受体VLA-4的白细胞和/或拮抗剂的粘附和迁移的抑制剂。它们通常适用于治疗或预防由不良程度的白细胞粘附和/或白细胞迁移或与之相关的疾病或其中基于VLA- 4受体与其配体发挥作用。本发明还涉及制备式I化合物的方法，它们在治疗和预防所述疾病状态中的用途以及含有式I化合物的药物制剂。

3. 发明授权

US06399620B1 Cycloalkyl derivatives as inhibitors of bone resporption and vitronectin receptor antagonists 有权
标题翻译：环烷基衍生物作为骨吸收抑制剂和玻连蛋白受体拮抗剂
公开(公告)号：US06399620B1
公开(公告)日：2002-06-04
申请号：US09606080
申请日：2000-06-29
申请人： Volkmar Wehner , Jochen Knolle , Hans Ulrich Stilz , Jean-Francois Gourvest , Denis Carniato , Thomas Richard Gadek , Robert McDowell , Robert Maurice Pitti , Sarah Catherine Bodary
发明人： Volkmar Wehner , Jochen Knolle , Hans Ulrich Stilz , Jean-Francois Gourvest , Denis Carniato , Thomas Richard Gadek , Robert McDowell , Robert Maurice Pitti , Sarah Catherine Bodary
IPC分类号： A61K31505
CPC分类号： C07C277/08 , C07C279/20 , C07C2603/74 , C07D233/48 , C07D239/16 , C07C279/22
摘要： There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要翻译：描述了式（I）的环烷基衍生物，其中R 1，Y，A，B，D，E，F和G具有本文所指的含义，它们的制备及其作为药物的用途。根据本发明的化合物可用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

4. 发明授权

US06387895B1 Vitronectin receptor antagonists, their preparation and their use 有权
标题翻译： Vitronectin受体拮抗剂，其制备及其应用
公开(公告)号：US06387895B1
公开(公告)日：2002-05-14
申请号：US09777011
申请日：2001-02-06
申请人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
发明人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
IPC分类号： A61K31551
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要翻译：本发明涉及式Iin的化合物，其中A，B，D，E，F和G具有专利权利要求中给出的含义，其制备和用作药物。本发明的化合物用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

5. 发明授权

US07348333B2 Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists 有权
标题翻译：环烷基衍生物作为骨吸收抑制剂和玻连蛋白受体拮抗剂
公开(公告)号：US07348333B2
公开(公告)日：2008-03-25
申请号：US10141986
申请日：2002-05-10
申请人： Volkmar Wehner , Jochen Knolle , Hans Ulrich Stilz , Jean-Francois Gourvest , Denis Carniato , Thomas Richard Gadek , Robert McDowell , Robert Maurice Pitti , Sarah Catherine Bodary
发明人： Volkmar Wehner , Jochen Knolle , Hans Ulrich Stilz , Jean-Francois Gourvest , Denis Carniato , Thomas Richard Gadek , Robert McDowell , Robert Maurice Pitti , Sarah Catherine Bodary
IPC分类号： A61P9/00 , A61K31/517 , A61K31/44 , C07D403/00 , C07D257/00
CPC分类号： C07C277/08 , C07C279/20 , C07C2603/74 , C07D233/48 , C07D239/16 , C07C279/22
摘要： There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要翻译：描述式（I）的环烷基衍生物<？in-line-formula description =“In-line Formulas”end =“lead”？> R 1 -YABDEFG（I）<αin 其中R 1，Y，A，B，D，E，F和G具有本文所示的含义，-line-formula description =“In-line Formulas”end =“tail”？> 他们的准备和用作药物。根据本发明的化合物可以用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

6. 发明授权

US07342029B2 Substituted indoles 有权
标题翻译：取代的吲哚
公开(公告)号：US07342029B2
公开(公告)日：2008-03-11
申请号：US11187396
申请日：2005-07-22
申请人： Olaf Ritzeler , Hans Ulrich Stilz , Bernhard Neises , Gerhard Jaehne , Joerg Habermann
发明人： Olaf Ritzeler , Hans Ulrich Stilz , Bernhard Neises , Gerhard Jaehne , Joerg Habermann
IPC分类号： A61K31/44 , A61K31/405 , C07D209/04
CPC分类号： C07D401/04 , C07D209/08 , C07D401/14
摘要： Compounds of the formula I are suitable for preparing pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
摘要翻译：式I化合物适用于制备用于预防和治疗其中涉及NFκB活性升高的病症的药物。

7. 发明授权

US06838439B2 Heterocytes as inhibitors of leucocyte adhesion and as VLA-4 antagonists 失效
标题翻译：杂种细胞作为白细胞粘附的抑制剂和VLA-4拮抗剂
公开(公告)号：US06838439B2
公开(公告)日：2005-01-04
申请号：US09995631
申请日：2001-11-29
申请人： Hans Ulrich Stilz , Volkmar Wehner , Christoph Huls , Dirk Seiffge
发明人： Hans Ulrich Stilz , Volkmar Wehner , Christoph Huls , Dirk Seiffge
IPC分类号： C07D277/20 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/54 , C07D233/72 , C07D277/34 , C07K5/06 , C07K5/078 , C07K5/097 , C07K5/107 , C07K5/11 , C07K5/117
CPC分类号： C07K5/1016 , A61K38/00 , C07K5/1019 , Y02A50/411
摘要： The present invention relates to compounds of the formula I which are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention also relates to processes for the preparation of formula I, pharmaceutical compositions containing compounds of formula I, and the treatment or prophylaxis of various diseases caused by or are associated with excess leucocyte adhesion and/or leucocyte migration, as well as diseases associated with cell-cell or cell-matrix interactions, which on interactions of VLA-4 receptors with their ligands play a part of, for example, inflammatory processes, rheumatoid arthritis or allergic disorders.

8. 发明授权

US06521654B2 Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations including them 有权
标题翻译：取代的咪唑烷衍生物，其制备方法，用途及包括它们在内的药物制剂
公开(公告)号：US06521654B2
公开(公告)日：2003-02-18
申请号：US09952028
申请日：2001-09-14
申请人： Volkmar Wehner , Hans Ulrich Stilz , Wolfgang Schmidt , Dirk Seiffge
发明人： Volkmar Wehner , Hans Ulrich Stilz , Wolfgang Schmidt , Dirk Seiffge
IPC分类号： A61K314166
CPC分类号： C07K5/0202 , C07K5/1016
摘要： Substituted imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations which contain compounds of the formula I.
摘要翻译：取代的式I的咪唑烷衍生物，其中B，E，W，Y，R，R 2，R 3，R 30，e和h具有权利要求中所示的含义。式I的化合物是有价值的药物活性化合物，其适用于例如治疗和预防炎症性疾病，例如类风湿性关节炎或过敏性疾病。式I的化合物是属于整联蛋白组的粘附受体VLA-4的白细胞和/或拮抗剂的粘附和迁移的抑制剂。它们通常适用于治疗或预防由不良程度的白细胞粘附和/或白细胞迁移或与之相关的疾病或其中基于VLA- 4受体与其配体发挥作用。本发明还涉及制备式I化合物，其用途，特别是作为药物活性化合物的方法和含有式I化合物的药物制剂。

9. 发明授权

US06207663B1 Vitronectin receptor antagonists, their preparation and use 有权
标题翻译： Vitronectin受体拮抗剂，其制备和用途
公开(公告)号：US06207663B1
公开(公告)日：2001-03-27
申请号：US09412331
申请日：1999-10-05
申请人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel LeFrancois , Thomas Richard Gadek , Robert McDowell
发明人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel LeFrancois , Thomas Richard Gadek , Robert McDowell
IPC分类号： A61K3155
CPC分类号： C07D487/04
摘要： Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要翻译：玻连蛋白受体拮抗剂及其制备及其用途本发明涉及式Iin的化合物，其中A，B，D，E，F和G具有专利权利要求中给出的含义，其制备及其作为药物的用途。本发明的化合物用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

10. 发明授权

US6034238A Heterocyclic compounds, their preparation and their use as leucocyte adhesion inhibitors and VLA-4-antagonists 有权
标题翻译：杂环化合物，它们的制备及其作为白细胞粘附抑制剂和VLA-4-拮抗剂的用途
公开(公告)号：US6034238A
公开(公告)日：2000-03-07
申请号：US158772
申请日：1998-09-23
申请人： Volkmar Wehner , Hans Ulrich Stilz , Wolfgang Schmidt , Dirk Seiffge
发明人： Volkmar Wehner , Hans Ulrich Stilz , Wolfgang Schmidt , Dirk Seiffge
IPC分类号： C07D233/76 , A61K31/00 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/42 , A61K31/425 , A61K38/00 , A61K38/05 , A61K38/06 , A61P1/00 , A61P3/00 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/08 , A61P17/00 , A61P25/00 , A61P27/00 , A61P27/14 , A61P29/00 , A61P35/00 , A61P35/04 , C07D233/02 , C07D233/84 , C07D233/86 , C07D263/34 , C07D277/32 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/078 , C07K5/097 , C07K5/117 , C07D413/00 , C07D233/40 , A61K31/535
CPC分类号： C07K5/0202 , C07K5/1024 , A61K38/00
摘要： Compounds of the formula I, ##STR1## in which B, E, W, Y, Z, R, R.sup.2, R.sup.2a, R.sup.2b, R.sup.3, g and h have the meanings indicated in the specifications. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use in the therapy and prophylaxis of the disease states mentioned and pharmaceutical preparations which contain the compounds of the formula I.
摘要翻译：其中B，E，W，Y，Z，R，R 2，R 2a，R 2b，R 3，g和h具有说明书中所示含义的式I化合物。式I的化合物是有价值的药物活性化合物，其适用于例如治疗和预防炎症性疾病，例如类风湿性关节炎或过敏性疾病。式I的化合物是属于整联蛋白组的粘附受体VLA-4的白细胞和/或拮抗剂的粘附和迁移的抑制剂。它们通常适用于治疗或预防由白细胞粘附和/或白细胞迁移的不期望程度或与之相关的疾病引起的疾病，或其中以基于VLA的相互作用为基础的细胞 - 细胞或细胞 - 基质相互作用 4受体与其配体发挥作用。本发明还涉及制备式I化合物的方法，它们在治疗和预防所述疾病状态中的用途以及含有式I化合物的药物制剂。

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