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31. 发明申请

US20040152694A1 Methods and compositions for treating inflammatory disorders of the airways 审中-公开
标题翻译：用于治疗气道炎症性疾病的方法和组合物
公开(公告)号：US20040152694A1
公开(公告)日：2004-08-05
申请号：US10358061
申请日：2003-02-04
发明人： Istvan Kurucz , Sandor Solyom , Viola Csillik nee Perczel
IPC分类号： A61K031/5513 , A61K031/517
CPC分类号： A61K31/517 , A61K31/5513 , A61K31/5517
摘要： The present invention provides compositions and methods for treating inflammatory disorders of the airways by the administration of a therapeutically effective amount of a modulator according to the invention. More specifically, the invention relates to the treatment of airway inflammations including asthma or an asthma-related pathologies.
摘要翻译：本发明提供了通过施用治疗有效量的根据本发明的调节剂来治疗气道炎症性疾病的组合物和方法。更具体地，本发明涉及气道炎症的治疗，包括哮喘或哮喘相关病理。

32. 发明申请

US20040121996A1 Benzoxazin-3-ones and derivatives thereof as therapeutic agents 失效
标题翻译：苯并恶嗪-3-酮及其衍生物作为治疗剂
公开(公告)号：US20040121996A1
公开(公告)日：2004-06-24
申请号：US10730680
申请日：2003-12-08
发明人： Nicole Barvian , Christine Nylund Kolz , Kimberly Suzanne Para , William Chester Patt , Melean Visnick
IPC分类号： A61K031/554 , A61K031/553 , A61K031/5513
CPC分类号： C07D413/06 , C07D405/06 , C07D413/14 , C07D417/06 , C07D417/14
摘要： The present invention provides compounds of Formula I 1 wherein W, Q, E, D, R6, R7, R8, Y, K, R9, R10, R12, G, and the double bond denoted null*null have any of the values defined therefore in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
摘要翻译：本发明提供式I化合物，其中W，Q，E，D，R 6，R 7，R 8，Y，K，R 9，R 10，R 12， G表示，并且表示为“*”的双键具有在本说明书中定义的任何值及其药学上可接受的盐，其可用作治疗疾病和病症（包括炎症性疾病，心血管疾病和癌症）的药剂。还提供了包含一种或多种式I化合物的药物组合物。

33. 发明申请

US20040029860A1 Anti-proliferative drugs 审中-公开
标题翻译：抗增生药
公开(公告)号：US20040029860A1
公开(公告)日：2004-02-12
申请号：US10432875
申请日：2003-09-16
发明人： Irit Gil-Ad , Abraham Weizman
IPC分类号： A61K031/553 , A61K031/554 , A61K031/5513 , A61K031/137
CPC分类号： A61K31/554 , A61K31/135 , A61K31/138 , A61K31/335 , A61K31/451 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/704 , A61K2300/00
摘要： The present invention relates to methods for the treatment of diseases associated with hyper-proliferation of cells by administering to a subject in need a therapeutically effective amount of at least one psychotropic agent. Specific proliferative diseases against which psychotropic agents were found to be effective are cancer, including multi-drug resistant cancer and diseases associated with hyper-proliferation of the skin cells, such as psoriasis and hyperkeratosis.
摘要翻译：本发明涉及通过向有需要的受试者施用治疗有效量的至少一种精神药物来治疗与细胞增殖相关的疾病的方法。发现精神药物有效的特异性增殖性疾病是癌症，包括多药耐药性癌症和与皮肤细胞的超增殖有关的疾病，例如牛皮癣和角化过度。

34. 发明申请

US20030212054A1 Substituted amino methyl factor Xa inhibitors 有权
标题翻译：取代氨基甲基因子Xa抑制剂
公开(公告)号：US20030212054A1
公开(公告)日：2003-11-13
申请号：US10304810
申请日：2002-11-26
发明人： Mimi L. Quan , Ruth R. Wexler
IPC分类号： A61K031/553 , A61K031/5513 , A61K031/554 , A61K031/542 , A61K031/538 , A61K031/498 , A61K031/519 , A61K031/47
CPC分类号： C07D401/12 , C07D403/12 , C07D413/14 , C07D471/04
摘要： The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
摘要翻译：本申请描述了可用作因子Xa抑制剂的取代氨基甲基取代的化合物及其衍生物或其药学上可接受的盐形式。

35. 发明申请

US20030191114A1 Assay for and uses of peptide hormone receptor agonists 审中-公开
标题翻译：测定和使用肽激素受体激动剂
公开(公告)号：US20030191114A1
公开(公告)日：2003-10-09
申请号：US10441757
申请日：2003-05-20
发明人： Alan S. Kopin , Martin Beinborn
IPC分类号： A61K031/5513
CPC分类号： C12Q1/02 , A61K38/00 , C07K14/72 , C07K2319/00 , G01N33/74 , G01N2333/72
摘要： The invention features a method for determining whether a candidate compound is a non-peptide agonist of a peptide hormone receptor. In this method, a candidate compound is exposed to a form of the peptide hormone receptor, or to a protein that interacts with a peptide hormone receptor, which has an enhanced ability to amplify the intrinsic activity of a non-peptide agonist. The second messenger signaling activity of the enhanced receptor is measured in the presence of the candidate compound, and compared to the second messenger signaling activity of the wildtype receptor measured in the absence of the candidate compound. A change in second messenger signaling activity indicates that the candidate compound is an agonist. An increase in second messenger signaling activity indicates that the compound is either a full or partial positive agonist; a decrease in second messenger signaling activity indicates that the compound is an inverse (also termed a nullnegativenull) agonist. The invention further embraces a method of using a peptide hormone receptor agonist for the treatment or prevention of a physiological disease, as well as particular enhanced receptors and the nucleic acid sequences which code for them.
摘要翻译：本发明的特征在于确定候选化合物是肽激素受体的非肽激动剂的方法。在该方法中，候选化合物暴露于肽激素受体的形式，或与肽激素受体相互作用的蛋白质，其具有增强的非肽激动剂的内在活性的能力。在候选化合物的存在下测量增强受体的第二信使信号活性，并与不存在候选化合物时测量的野生型受体的第二信使信号传导活性进行比较。第二信使信号活动的变化表明候选化合物是激动剂。第二信使信号活性的增加表明该化合物是全部或部分阳性激动剂; 第二信使信号传导活性的降低表明该化合物是反义（也称为“阴性”）激动剂。本发明还包括使用肽激素受体激动剂来治疗或预防生理疾病的方法，以及特定的增强受体和编码它们的核酸序列。

36. 发明申请

US20030181438A1 Bicyclic lactam derivatives as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE) 有权
标题翻译：作为基质金属蛋白酶和/或TNF-α转化酶（TACE）抑制剂的双环内酰胺衍生物
公开(公告)号：US20030181438A1
公开(公告)日：2003-09-25
申请号：US10271441
申请日：2002-10-16
发明人： Carl P. Decicco , Ying Song , Jingwu Duan , Matthew E. Voss
IPC分类号： A61K031/55 , A61K031/5513 , A61K031/503 , A61K031/4745 , A61K031/407 , A61K031/415
CPC分类号： C07D487/04 , C07D455/02 , C07D471/04
摘要： The present application describes novel bicyclic lactam derivatives of formula I: 1 or pharmaceutically acceptable salt forms thereof, wherein A, B, C, D, R1, and R2 are defined in the present specification, which are useful as metalloprotease, TNF-null, and/or aggrecanase inhibitors.
摘要翻译：本申请描述了式I的新型双环内酰胺衍生物或其药学上可接受的盐形式，其中A，B，C，D，R 1和R 2在本说明书中定义，其可用作金属蛋白酶，TNF-α和/或软骨聚集蛋白聚糖酶抑制剂。

37. 发明申请

US20030171364A1 Novel substituted pyrazolo[4,3-e]diazepines, pharmaceutical compositions containing them, use as medicinal products and processes for preparing them 失效
标题翻译：新型取代的吡唑并[4,3-e]二氮杂，含有它们的药物组合物，用作药物及其制备方法
公开(公告)号：US20030171364A1
公开(公告)日：2003-09-11
申请号：US10169375
申请日：2002-10-21
发明人： Catherine Burnouf , Amaya Berecibar , Michael Navet
IPC分类号： A61K031/5513 , C07D487/02
CPC分类号： C07D487/04
摘要： The invention relates to novel substituted pyrazolonull4,3-enull-diazepines of general formula (I), to pharmaceutical compositions containing them, to their use as medicinal products and to processes for preparing them.
摘要翻译：本发明涉及通式（I）的新的取代的吡唑并[4,3-e] - 二氮杂，其含有它们的药物组合物，用作药物用途及其制备方法。

38. 发明申请

US20030166598A1 Medicines for treating tumoral pathologies containing the ro5-4864 compound and an apoptosis-inducing agent 审中-公开
标题翻译：用于治疗含有ro5-4864化合物和凋亡诱导剂的肿瘤病理的药物
公开(公告)号：US20030166598A1
公开(公告)日：2003-09-04
申请号：US10258731
申请日：2003-04-08
发明人： Didier Decaudin , Guido Kroemer , Marie-France Poupon , Fariba Nemati , Arnaud Beurdeley-Thomas
IPC分类号： A61K048/00 , A61K031/5513
CPC分类号： A61K31/5513 , A61K45/06 , A61K2300/00
摘要： The invention concerns the use of Ro5-4864, and compounds derived therefrom, for preparing medicines for treating tumoral pathologies. The invention also concerns said compounds combined with an apoptosis-inducing agent, as combination products for simultaneous, separate or prolonged use, in cancer therapy.
摘要翻译：本发明涉及使用Ro5-4864及其衍生的化合物来制备治疗肿瘤病理学的药物。本发明还涉及与凋亡诱导剂组合的所述化合物，作为癌症治疗中用于同时，分别或长期使用的组合产物。

39. 发明申请

US20030133951A1 Pharmaceutical composition for treatment of acute, chronic pain and/or neuropathic pain and migraines 审中-公开
标题翻译：用于治疗急性，慢性疼痛和/或神经性疼痛和偏头痛的药物组合物
公开(公告)号：US20030133951A1
公开(公告)日：2003-07-17
申请号：US10348381
申请日：2003-01-21
申请人： Pfizer Inc.
发明人： Jotham W. Coe , Steven B. Sands , Edmund P. Harrigan , Brian T. O'Neill , Eric J. Watsky
IPC分类号： A61K035/78 , A61K031/57 , A61K031/5513 , A61K031/4709 , A61K031/485 , A61K031/454 , A61K039/08
CPC分类号： A61K31/4704 , A61K31/4748 , A61K31/5377 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： Pharmaceutical compositions are disclosed for the treatment of acute, chronic and/or neuropathic pain. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an analgesic agent and a pharmaceutically acceptable carrier. The analgesic agent is selected from opioid analgesics, NMDA antagonists, substance P antagonists, COX 1 and COX 2 inhibitors, tricyclic antidepressants (TCA), selective serotonin reuptake inhibitors (SSRI), capsaicin receptor agonists, anesthetic agents, benzodiazepines, skeletal muscle relaxants, migraine therapeutic agents, anti-convulsants, anti-hypertensives, anti-arrythmics, antihistamines, steroids, caffeine, and botulinum toxin. The method of using these compounds and a method of treating acute, chronic and/or neuropathic pain and migraine in a mammal including a human is also disclosed.
摘要翻译：公开了用于治疗急性，慢性和/或神经性疼痛的药物组合物。药物组合物由尼古丁受体部分激动剂和止痛剂和药学上可接受的载体的治疗有效组合组成。止痛剂选自阿片类止痛剂，NMDA拮抗剂，P物质拮抗剂，COX1和COX2抑制剂，三环抗抑郁药（TCA），选择性5-羟色胺再摄取抑制剂（SSRI），辣椒素受体激动剂，麻醉剂，苯二氮卓类，骨骼肌松弛剂，偏头痛治疗剂，抗惊厥药，抗高血压药，抗arrythmics，抗组胺药，类固醇，咖啡因和肉毒杆菌毒素。还公开了使用这些化合物的方法和治疗哺乳动物包括人的急性，慢性和/或神经性疼痛和偏头痛的方法。

40. 发明申请

US20030130257A1 Bicyclic hydroxamates as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE) 有权
标题翻译：双环异羟肟酸盐作为基质金属蛋白酶和/或TNF-α转化酶（TACE）的抑制剂
公开(公告)号：US20030130257A1
公开(公告)日：2003-07-10
申请号：US10219426
申请日：2002-08-15
发明人： James E. Sheppeck , Jingwu Duan
IPC分类号： A61K031/553 , A61K031/5513 , A61K031/55 , A61K031/542 , A61K031/538 , A61K031/519
CPC分类号： C07D401/12 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The present application describes to novel bicyclic hydroxamates derivatives of formula I: 1 or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, B1, B2, R1, and C are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-null converting enzyme (TACE), aggrecanase, or a combination thereof.
摘要翻译：本申请描述了式I的新型双环羟肟酸衍生物或其药学上可接受的盐或前体药物形式，其中A，B，B1，B2，R1和C在本说明书中定义，其可用作基质金属蛋白酶抑制剂（MMP），TNF-α转化酶（TACE），组蛋白聚糖蛋白聚糖酶或其组合。

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