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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

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。

3. 发明授权

US07399770B2 Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors 有权
标题翻译：噻吩并亚氨基酸衍生物用作基质金属蛋白酶抑制剂
公开(公告)号：US07399770B2
公开(公告)日：2008-07-15
申请号：US11461189
申请日：2006-07-31
申请人： Manfred Schudok , Hans Matter , Armin Hofmeister , Maxime Lampilas
发明人： Manfred Schudok , Hans Matter , Armin Hofmeister , Maxime Lampilas
IPC分类号： A61K31/4365 , C07D409/02 , C07D495/06
CPC分类号： C07D495/04
摘要： The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier.The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof.Furthermore the invention is directed to a method for preparing a compound of formula I.
摘要翻译：本发明涉及式I化合物，其中变量如本文所定义，或其立体异构形式，立体异构体形式的任何比例的混合物或其盐。本发明的另一方面涉及一种药物组合物，其包含药学有效量的一种或多种根据权利要求1的式I化合物与药学上可接受的载体的混合物。本发明还涉及一种用于预防和治疗退行性关节疾病如骨关节炎，椎关节强硬，关节创伤后的软骨损失或半月板或髌骨损伤或韧带断裂后相对较长的关节固定的方法，连接性疾病诸如胶原蛋白，牙周病，伤口愈合障碍和诸如炎症，免疫学或代谢相关的急性和慢性关节炎的关节病，关节病，肌痛和骨骼代谢紊乱的运动器官的组织，用于治疗溃疡，动脉粥样硬化和狭窄，并且用于在有需要的患者中治疗炎症，癌症疾病，肿瘤转移形成，恶病质，厌食症，心脏功能不全和败血性休克或用于预防心肌和脑梗死，包括向患者施用药学有效量的compou 根据权利要求1的式I的或其药学上可接受的盐，溶剂合物或前药。此外，本发明涉及制备式I化合物的方法。

4. 发明申请

US20050080127A1 Bicyclic imino acid derivatives as inhibitors of matrix metalloproteinases 有权
标题翻译：双环亚氨基酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US20050080127A1
公开(公告)日：2005-04-14
申请号：US10950802
申请日：2004-09-27
申请人： Manfred Schudok , Hans Matter , Armin Hofmeister
发明人： Manfred Schudok , Hans Matter , Armin Hofmeister
IPC分类号： C07D217/26 , C07D405/12 , A61K31/4035 , C07D209/48
CPC分类号： C07D217/26 , C07D405/12
摘要： The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.
摘要翻译：本发明涉及式（I）化合物或其任何比例的立体异构体或其立体异构体的混合物或其生理上可耐受的盐，其可用作基质金属蛋白酶的抑制剂。本发明还涉及包含药学有效量的至少一种式（I）化合物的药物制剂; 其准备过程; 使用具有活性的式（I）化合物作为基质金属蛋白酶抑制剂; 以及用于预防和治疗涉及基质金属蛋白酶活性增加的疾病状态。

5. 发明申请

US20080090821A1 SUBSTITUTED TETRAHYDROISOCHINOLINES AS MMP INHIBITORS, RELATED PRODUCTION METHOD AND USE AS MEDICINE 有权
标题翻译：作为基质金属蛋白酶抑制剂的相关生产方法和作为药物使用的取代的四氢吲哚
公开(公告)号：US20080090821A1
公开(公告)日：2008-04-17
申请号：US11862818
申请日：2007-09-27
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： A61K31/472 , A61K31/496 , A61K31/5377 , A61P19/00 , A61P29/00 , A61P35/00 , A61P9/00 , C07D401/02 , C07D413/02
CPC分类号： C07D217/26 , C07D403/12
摘要： The present invention is directed to a compound of formula (1), wherein R1, R2, R3, R4, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a MMP inhibitor.
摘要翻译：本发明涉及式（1）的化合物，其中R 1，R 2，R 3，R 4 A，L和n如本文所定义，其药物组合物，制剂和用作MMP抑制剂。

6. 发明授权

US07205315B2 Bicyclic imino acid derivatives as inhibitors of matrix metalloproteinases 有权
标题翻译：双环亚氨基酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US07205315B2
公开(公告)日：2007-04-17
申请号：US10950802
申请日：2004-09-27
申请人： Manfred Schudok , Hans Matter , Armin Hofmeister
发明人： Manfred Schudok , Hans Matter , Armin Hofmeister
IPC分类号： A61K31/4725 , C07D217/22 , C07D217/24
CPC分类号： C07D217/26 , C07D405/12
摘要： The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.
摘要翻译：本发明涉及式（I）化合物或其任何比例的立体异构体或其立体异构体的混合物或其生理上可耐受的盐，其可用作基质金属蛋白酶的抑制剂。本发明还涉及包含药学有效量的至少一种式（I）化合物的药物制剂; 其准备过程; 使用具有活性的式（I）化合物作为基质金属蛋白酶抑制剂; 以及用于预防和治疗涉及基质金属蛋白酶活性增加的疾病状态。

7. 发明授权

US07858619B2 Substituted tetrahydroisochinolines as MMP inhibitors, related production method and use as medicine 有权
标题翻译：取代的四氢异噻唑啉作为MMP抑制剂，相关制备方法和用作药物
公开(公告)号：US07858619B2
公开(公告)日：2010-12-28
申请号：US11862818
申请日：2007-09-27
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： C07D401/02 , A61K31/47
CPC分类号： C07D217/26 , C07D403/12
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, its pharmaceutical composition, preparation and uses as a MMP inhibitor.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，A，L和n如本文所定义，其药物组合物，制剂和用作MMP抑制剂。

8. 发明申请

US20070155778A1 4-Trifluoromethoxyphenoxybenzol-4-Sulfonic Acids, Method For The Production And Use Thereof In Medicaments 审中-公开
标题翻译： 4-三氟甲氧基苯氧基苯酚-4-磺酸，药物的生产和使用方法
公开(公告)号：US20070155778A1
公开(公告)日：2007-07-05
申请号：US11611199
申请日：2006-12-15
申请人： Manfred Schudok , Armin Hofmeister
发明人： Manfred Schudok , Armin Hofmeister
IPC分类号： A61K31/4741 , A61K31/4704 , C07D217/22 , C07D491/02
CPC分类号： C07D217/26 , C07D223/16 , C07D493/04
摘要： The present invention is directed to a compound of fomula 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R1，R2，R3X，A，m和n如本文所定义，其制备方法及其作为药物的用途。

9. 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。

10. 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。

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