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1. 发明授权

US08039481B2 Tetrahydrofuran derivatives for use as inhibitors of matrix metalloproteinases 有权
标题翻译：用作基质金属蛋白酶抑制剂的四氢呋喃衍生物
公开(公告)号：US08039481B2
公开(公告)日：2011-10-18
申请号：US11777324
申请日：2007-07-13
申请人： Manfred Schudok , Hans Matter , Armin Hofmeister
发明人： Manfred Schudok , Hans Matter , Armin Hofmeister
IPC分类号： A61K31/4355 , C07D471/04
CPC分类号： C07D491/04
摘要： The present invention includes novel derivatives of bicyclic tetrahydrofuran imino acids of formula I, processes for their preparation, and uses thereof as medicaments. The compounds are suitable for use in the therapy and prophylaxis of diseases which are associated with an increased matrix metalloproteinase activity.
摘要翻译：本发明包括式I的双环四氢呋喃亚氨基酸的新衍生物，其制备方法及其作为药物的用途。该化合物适合用于治疗和预防与增加的基质金属蛋白酶活性有关的疾病。

2. 发明申请

US20100099663A1 4-TRIFLUOROMETHOXYPHENOXYBENZOL-4'-SULFONIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF IN MEDICAMENTS 审中-公开
标题翻译： 4-三氟甲氧基苯甲基-4'-磺酸，用于生产和在医药中使用的方法
公开(公告)号：US20100099663A1
公开(公告)日：2010-04-22
申请号：US12643162
申请日：2009-12-21
申请人： Manfred SCHUDOK , Armin HOFMEISTER
发明人： Manfred SCHUDOK , Armin HOFMEISTER
IPC分类号： A61K31/55 , C07D217/22 , A61K31/47 , C07D471/02 , A61K31/4353 , C07D223/16 , A61P43/00
CPC分类号： C07D217/26 , C07D223/16 , C07D493/04
摘要： The present invention is directed to a compound of formula I, wherein R1, R2, R3, X, A, m and n are as herein defined, the process for its preparation and its use thereof as a medicament.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，X，A，m和n如本文所定义，其制备方法及其作为药物的用途。

3. 发明授权

US07160903B2 Sulfonylaminocarboxylic acids 有权
标题翻译：磺酰氨基羧酸
公开(公告)号：US07160903B2
公开(公告)日：2007-01-09
申请号：US10170870
申请日：2002-06-13
申请人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase
发明人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase
IPC分类号： A61K31/381 , C07D409/04 , C07C311/19
CPC分类号： C07D213/42 , C07C311/19 , C07C311/29 , C07C311/44 , C07C317/48 , C07C323/59 , C07C381/10 , C07D203/24 , C07D207/16 , C07D209/08 , C07D209/20 , C07D211/96 , C07D213/75 , C07D233/64 , C07D235/16 , C07D249/06 , C07D317/60 , C07D333/24 , C07D409/04 , C07D413/04 , C07F9/301
摘要： Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
摘要翻译：式（I）化合物适用于生产用于预防和治疗病症的药物，其中涉及基质降解金属蛋白酶活性增加。

4. 发明授权

US06706715B2 Urea derivatives with antiproteolytic activity 有权
标题翻译：具有抗蛋白水解活性的尿素衍生物
公开(公告)号：US06706715B2
公开(公告)日：2004-03-16
申请号：US10183848
申请日：2002-06-26
申请人： Manfred Schudok , Otmar Klingler , Hans-Peter Nestler , Hans Matter , Herman Schreuder , Hauke Szillat
发明人： Manfred Schudok , Otmar Klingler , Hans-Peter Nestler , Hans Matter , Herman Schreuder , Hauke Szillat
IPC分类号： A61K314425
CPC分类号： C07C275/42 , C07C2601/14 , C07D333/38
摘要： The present invention relates to compounds of the formula I, in which R1, R2, R4, R5, D1, D2, X1, X2, X3, A and B have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 4，R 5，D 1，D 2，X 1，X 2，X 3，A和B具有所指定的含义在权利要求中。式I的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病和再狭窄。它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件下使用。本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

5. 发明授权

US06500803B1 Factor VIIa inhibitors 有权
标题翻译：因子VIIa抑制剂
公开(公告)号：US06500803B1
公开(公告)日：2002-12-31
申请号：US09588651
申请日：2000-06-07
申请人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
发明人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
IPC分类号： A61K3805
CPC分类号： C07K5/06086 , A61K38/00
摘要： The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式Ⅰ化合物，其中R1，R2，R91，R92，R93，R94，R95，R96，R97，r，s和t具有权利要求中所示的含义。式I化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

6. 发明授权

US6159995A Substituted diaminocarboxylic acids 失效
标题翻译：取代的二氨基羧酸
公开(公告)号：US6159995A
公开(公告)日：2000-12-12
申请号：US74587
申请日：1998-05-08
申请人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase , Bernhard Neises , Gunter Billen
发明人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase , Bernhard Neises , Gunter Billen
IPC分类号： C07D295/18 , A61K31/195 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/48 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61P1/02 , A61P9/10 , A61P19/00 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07C311/13 , C07C311/19 , C07C311/22 , C07C311/29 , C07C323/59 , C07D207/16 , C07D207/34 , C07D207/38 , C07D209/46 , C07D209/48 , C07D213/81 , C07D213/82 , C07D215/14 , C07D233/54 , C07D233/61 , C07D233/64 , C07D233/74 , C07D235/08 , C07D241/24 , C07D249/08 , C07D249/12 , C07D261/10 , C07D275/04 , C07D277/06 , C07D277/28 , C07D307/24 , C07D307/54 , C07D307/58 , C07D307/68 , C07D333/22 , C07D333/24 , C07D333/38 , C07D401/12 , A61K31/55 , A61K31/495 , A61K31/505 , A61K31/54 , C07D207/18 , C07D207/30 , C07D207/40 , C07D209/02 , C07D209/36 , C07D235/04 , C07D243/00 , C07D277/62 , C07D403/02 , C07D417/00 , C07D513/00
CPC分类号： C07C323/59 , C07C311/19 , C07C311/29 , C07C2601/02 , C07C2601/04 , C07C2603/74
摘要： Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
摘要翻译：式（I）化合物适用于生产用于预防和治疗病症的药物，其中涉及基质降解性金属蛋白酶活性增加。

7. 发明申请

US20090275523A1 Spirocyclic nitriles as protease inhibitors 有权
标题翻译：螺环腈作为蛋白酶抑制剂
公开(公告)号：US20090275523A1
公开(公告)日：2009-11-05
申请号：US12277880
申请日：2008-11-25
申请人： Manfred Schudok , Michael Wagner , Armin Bauer , Anna Kohlmann
发明人： Manfred Schudok , Michael Wagner , Armin Bauer , Anna Kohlmann
IPC分类号： A61K38/05 , C07D221/20 , C07D471/10 , C07C255/29 , C07D498/10 , A61P35/00
CPC分类号： C07D319/14 , C07C233/63 , C07C255/46 , C07C2601/02 , C07D211/66 , C07D213/26 , C07D221/20 , C07D231/54 , C07D263/52 , C07D295/215 , C07D295/26 , C07D317/72 , C07D471/10 , C07D491/10
摘要： The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.
摘要翻译：本发明涉及抑制巯基蛋白酶的式Ia的取代的碳杂环和杂环螺环化合物，其制备方法及其作为药物的用途。

8. 发明申请

US20070203118A1 SUBSTITUTED TETRAHYDROISOQUINOLINES USED IN THE FORM OF MMP INHIBITORS, METHOD FOR THE PRODUCTION AND USE THEREOF IN THE FORM OF DRUGS 审中-公开
标题翻译：用于MMP抑制剂形式的取代的四氢喹啉酮，其制备方法及其在药物形式中的用途
公开(公告)号：US20070203118A1
公开(公告)日：2007-08-30
申请号：US11612938
申请日：2006-12-19
申请人： Armin Hofmeister , Manfred Schudok , Hans Matter , Kristin Breitschopf , Antonio Ugolini
发明人： Armin Hofmeister , Manfred Schudok , Hans Matter , Kristin Breitschopf , Antonio Ugolini
IPC分类号： A61K31/55 , A61K31/4704 , A61K31/4035 , C07D217/22 , C07D223/16 , C07D209/44
CPC分类号： C07D217/26 , C07D217/14
摘要： The present invention is directed to a compound of formula (I) wherein R1, R2, R3, R4, A, L and n are as defined herein, or a pharmacologically acceptable salt thereof, its pharmaceutical composition and it use as a MMP inhibitor.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4， / SUB，A，L和n如本文所定义，或其药理学上可接受的盐，其药物组合物，并且其用作MMP抑制剂。

9. 发明授权

US06645992B2 Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use 有权
标题翻译：丙二酰胺和丙二酸酯衍生物具有抗血栓活性，其制备及其用途
公开(公告)号：US06645992B2
公开(公告)日：2003-11-11
申请号：US09965790
申请日：2001-10-01
申请人： Manfred Schudok , Otmar Klingler , Hans-Peter Nestler , Hans Matter , Herman Schreuder
发明人： Manfred Schudok , Otmar Klingler , Hans-Peter Nestler , Hans Matter , Herman Schreuder
IPC分类号： C07D25718
CPC分类号： A61K31/27 , A61K31/167 , A61K31/225 , C07C257/18 , C07C257/20
摘要： Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：具有权利要求中所述定义的R 1，R 2，A和B的式I化合物是有价值的药理活性化合物，其表现出很强的抗血栓形成作用，并且适用于例如治疗血栓栓塞性疾病和再狭窄。它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件下使用。还公开了制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

10. 发明授权

US06451824B1 Sulfonylaminocarboxylic acids 失效
标题翻译：磺酰氨基羧酸
公开(公告)号：US06451824B1
公开(公告)日：2002-09-17
申请号：US09074693
申请日：1998-05-08
申请人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase
发明人： Werner Thorwart , Wilfried Schwab , Manfred Schudok , Burkhard Haase
IPC分类号： C07C31119
CPC分类号： C07D213/42 , C07C311/19 , C07C311/29 , C07C311/44 , C07C317/48 , C07C323/59 , C07C381/10 , C07D203/24 , C07D207/16 , C07D209/08 , C07D209/20 , C07D211/96 , C07D213/75 , C07D233/64 , C07D235/16 , C07D249/06 , C07D317/60 , C07D333/24 , C07D409/04 , C07D413/04 , C07F9/301
摘要： Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
摘要翻译：式（I）化合物适用于生产用于预防和治疗病症的药物，其中涉及基质降解金属蛋白酶活性增加。

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