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1. 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。

2. 发明申请

US20080039489A1 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：US20080039489A1
公开(公告)日：2008-02-14
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： C07D471/04 , A61K31/4355 , A61P19/00 , A61P35/00 , A61P9/00
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。

3. 发明申请

US20070093482A1 THIENO-IMINO ACID DERIVATIVES FOR USE AS MATRIX METALLOPROTEINASE INHIBITORS 有权
标题翻译：用作基质金属蛋白酶抑制剂的噻二唑酸衍生物
公开(公告)号：US20070093482A1
公开(公告)日：2007-04-26
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： A61K31/5377 , A61K31/496 , A61K31/4743 , C07D498/02
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

US20120015933A1 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：US20120015933A1
公开(公告)日：2012-01-19
申请号：US13248366
申请日：2011-09-29
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： A61K31/438 , C07D209/54 , A61K31/403 , C07D471/10 , C07D319/14 , A61K31/357 , C07D491/113 , C07D498/10 , A61K31/5386 , C07C255/31 , A61K31/277 , C07D263/52 , A61K31/423 , A61K31/444 , A61P35/00 , A61P29/00 , A61P19/02 , A61P19/10 , A61P11/06 , A61P37/06 , A61P25/14 , A61P11/00 , A61P3/10 , A61P1/00 , A61P25/28 , C07D221/20
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。

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