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1. 发明申请

US20140349943A1 TOPICAL FORMULATIONS OF CHEMERIN C15 PEPTIDES FOR THE TREATMENT OF DERMATOLOGICAL CONDITIONS 审中-公开
标题翻译：用于治疗皮肤病症的化疗C15胶原蛋白的主题配方
公开(公告)号：US20140349943A1
公开(公告)日：2014-11-27
申请号：US14352296
申请日：2012-10-12
申请人： Thomas Gadek
发明人： Thomas Gadek
IPC分类号： A61K38/10 , A61K45/06
CPC分类号： A61K38/10 , A61K9/06 , A61K9/08 , A61K31/573 , A61K45/06
摘要： Described herein, are topical formulations for treating a dermatological disease, disorder, or condition. Topical formulation disclosed herein include a therapeutically-effective amount of a human chemerin C15 peptide formulated for dermal administration.
摘要翻译：本文描述的是用于治疗皮肤病，病症或病症的局部制剂。本文公开的局部制剂包括治疗有效量的配制用于皮肤给药的人酪蛋白C15肽。

2. 发明授权

US08367701B2 Crystalline pharmaceutical and methods of preparation and use thereof 有权
公开(公告)号：US08367701B2
公开(公告)日：2013-02-05
申请号：US13289172
申请日：2011-11-04
申请人： John Burnier , Thomas Gadek , Frederic Naud
发明人： John Burnier , Thomas Gadek , Frederic Naud
IPC分类号： A61K31/47 , C07D217/00
CPC分类号： C07D405/06 , A61K9/06 , A61K9/08 , A61K31/4709 , A61K31/4725 , A61K45/06 , A61K47/02 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/22 , A61K47/38 , C07C317/48 , C07D217/02 , C07D217/04 , C07D217/26 , C07D405/10
摘要： Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.

3. 发明申请

US20090258069A1 Delivery of LFA-1 antagonists to the gastrointestinal system 审中-公开
标题翻译：将LFA-1拮抗剂递送至胃肠系统
公开(公告)号：US20090258069A1
公开(公告)日：2009-10-15
申请号：US12386347
申请日：2009-04-15
申请人： John Burnier , Thomas Gadek
发明人： John Burnier , Thomas Gadek
IPC分类号： A61K9/14 , A61K39/395 , A61K33/30 , A61K33/06 , A61K33/00 , A61K31/56 , A61K31/437 , A61K31/47 , A61K31/165 , A61K31/4725
CPC分类号： A61K31/165 , A61K9/0014 , A61K9/0048 , A61K9/06 , A61K9/08 , A61K31/381 , A61K31/437 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/56 , A61K45/06 , A61K2300/00
摘要： The present invention provides compositions and methods for treating disorders and diseases by delivery of LFA-1 antagonists to the gastrointestinal system. Methods include delivery of LFA-1 antagonists to effect localized treatment.
摘要翻译：本发明提供了通过将LFA-1拮抗剂递送至胃肠系统来治疗疾病和疾病的组合物和方法。方法包括递送LFA-1拮抗剂以实现局部治疗。

4. 发明申请

US20070141630A1 IDENTIFICATION OF NON-COVALENT COMPLEXES BY MASS SPECTROMETRY 审中-公开
标题翻译：通过大量光谱鉴定非共价复合物
公开(公告)号：US20070141630A1
公开(公告)日：2007-06-21
申请号：US11627288
申请日：2007-01-25
申请人： Thomas Gadek , Denise Ockey
发明人： Thomas Gadek , Denise Ockey
IPC分类号： G01N33/53
CPC分类号： G01N33/54313 , G01N2500/02 , G01N2500/04
摘要： Methods for identifying novel drug leads or binding compounds that have an affinity for a target molecule involving screening known drug fragment molecules and derivatives thereof, preferably using mass spectrometry are disclosed.
摘要翻译：公开了用于鉴定涉及筛选已知药物片段分子及其衍生物的靶分子亲和性的新药物引线或结合化合物的方法，优选使用质谱法。

5. 发明授权

US5756452A Platelet aggregation inhibitors having high specificity for GP II.sub.b III.sub.a 失效
标题翻译：对GP IIbIIIa具有高特异性的血小板聚集抑制剂
公开(公告)号：US5756452A
公开(公告)日：1998-05-26
申请号：US567977
申请日：1995-12-06
申请人： John P. Burnier , Thomas Gadek , Robert S. McDowell
发明人： John P. Burnier , Thomas Gadek , Robert S. McDowell
IPC分类号： A61K38/00 , A61P7/02 , C07K7/02 , C07K7/06 , C07K7/56 , C07K14/75 , C07K14/78 , C07K5/12
CPC分类号： C07K14/78 , C07K14/75 , C07K7/02 , A61K38/00 , Y10S930/27
摘要： A peptide containing the tripeptide recognition sequences RGD or KGD in a cycle and an exocyclic group bearing a positive charge is provided. The compound is provided in therapeutic form for administration to a mammal and exhibits high specificity and potency as a platelet aggregation inhibitor without undesireable side effects.
摘要翻译：提供了包含三环识别序列RGD或KGD在一个循环中的肽和带有正电荷的环外基团的肽。该化合物以治疗形式提供给哺乳动物，并表现出作为血小板聚集抑制剂的高特异性和效力，而没有不合需要的副作用。

6. 发明授权

US5250679A Nonpeptidyl platelet aggregation inhibitors having specificity for the GPII.sub.b III.sub. receptor 失效
标题翻译：对GPIIbIII受体具有特异性的非肽基血小板聚集抑制剂
公开(公告)号：US5250679A
公开(公告)日：1993-10-05
申请号：US866931
申请日：1992-04-10
申请人： Brent Blackburn , Robert McDowell , Thomas Gadek , Peter Barker , Lawrence McGee , Rob Webb
发明人： Brent Blackburn , Robert McDowell , Thomas Gadek , Peter Barker , Lawrence McGee , Rob Webb
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/5517 , A61K31/553 , A61P7/02 , A61P43/00 , C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14 , C07D401/06 , C07D401/12 , C07D261/14
CPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14
摘要： A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
摘要翻译：提供作为非肽基血小板聚集抑制剂的苯并二氮二酮衍生物。该抑制剂有效地抑制纤维蛋白原与GPIIbIIIa受体的结合，并且提供在用于治疗阻断血小板聚集的疾病的治疗组合物中。这些非肽基抑制剂与溶血栓剂和抗凝剂组合提供。

7. 发明授权

US08168655B2 Compositions and methods for treatment of eye disorders 有权
标题翻译：用于治疗眼部疾病的组合物和方法
公开(公告)号：US08168655B2
公开(公告)日：2012-05-01
申请号：US11436906
申请日：2006-05-17
申请人： Thomas Gadek , John Burnier
发明人： Thomas Gadek , John Burnier
IPC分类号： A61K31/47
CPC分类号： A61K31/4725 , A61B3/101 , A61B3/145 , A61K9/0014 , A61K9/0019 , A61K9/0043 , A61K9/0048 , A61K9/0051 , A61K9/0053 , A61K31/197 , A61K31/198 , A61K31/275 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4162 , A61K31/4184 , A61K31/4192 , A61K31/44 , A61K31/4709 , A61K31/472 , A61K31/4745 , A61K31/495 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K33/00 , A61K33/06 , A61K38/07 , A61K38/08 , A61K38/12 , A61K38/1703 , A61K45/06 , C07C279/28 , C07C317/50 , C07D207/06 , C07D217/00 , C07D217/02 , C07D217/06 , C07D217/20 , C07D217/26 , C07D307/52 , C07D333/38 , C07D401/06 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , G01N33/5011 , G01N33/5032 , G01N33/5047 , G01N33/566 , G01N33/6872 , G01N2333/705 , G01N2333/70525 , G01N2333/70546 , G01N2500/02 , G01N2500/04 , G01N2500/10 , G01N2500/20 , G01N2800/16 , Y10S514/912 , Y10S514/914
摘要： The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
摘要翻译：本发明提供了用于治疗LFA-1介导的疾病的化合物和方法。特别地，本文描述了LFA-1拮抗剂，并且这些拮抗剂用于治疗LFA-1介导的疾病。在患者被诊断患有LFA-1介导的疾病之后，本发明的一个方面提供LFA-1介导的疾病的诊断和LFA-1拮抗剂的施用。在一些实施方案中，治疗的LFA-1介导的疾病是干眼症。本文还提供了用于鉴定LFA-1拮抗剂的化合物的方法。

8. 发明申请

US20110165228A1 Compositions and Methods for Treatment 有权
标题翻译：组合物和治疗方法
公开(公告)号：US20110165228A1
公开(公告)日：2011-07-07
申请号：US13011760
申请日：2011-01-21
申请人： John BURNIER , Thomas GADEK , Min ZHONG , Wang SHEN , Johan D. OSLOB , Kenneth BARR
发明人： John BURNIER , Thomas GADEK , Min ZHONG , Wang SHEN , Johan D. OSLOB , Kenneth BARR
IPC分类号： A61K31/472 , C07D217/26 , A61K9/127 , A61P11/06 , A61P29/00 , A61P17/06 , A61P1/00 , A61P27/02
CPC分类号： A61K31/4725 , A61B3/101 , A61B3/145 , A61K9/0014 , A61K9/0019 , A61K9/0043 , A61K9/0048 , A61K9/0051 , A61K9/0053 , A61K31/197 , A61K31/198 , A61K31/275 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4162 , A61K31/4184 , A61K31/4192 , A61K31/44 , A61K31/4709 , A61K31/472 , A61K31/4745 , A61K31/495 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K33/00 , A61K33/06 , A61K38/07 , A61K38/08 , A61K38/12 , A61K38/1703 , A61K45/06 , C07C279/28 , C07C317/50 , C07D207/06 , C07D217/00 , C07D217/02 , C07D217/06 , C07D217/20 , C07D217/26 , C07D307/52 , C07D333/38 , C07D401/06 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , G01N33/5011 , G01N33/5032 , G01N33/5047 , G01N33/566 , G01N33/6872 , G01N2333/705 , G01N2333/70525 , G01N2333/70546 , G01N2500/02 , G01N2500/04 , G01N2500/10 , G01N2500/20 , G01N2800/16 , Y10S514/912 , Y10S514/914
摘要： The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
摘要翻译：本发明提供了用于治疗LFA-1介导的疾病的化合物和方法。特别地，本文描述了LFA-1拮抗剂，并且这些拮抗剂用于治疗LFA-1介导的疾病。在患者被诊断患有LFA-1介导的疾病之后，本发明的一个方面提供LFA-1介导的疾病的诊断和LFA-1拮抗剂的施用。在一些实施方案中，治疗的LFA-1介导的疾病是干眼症。本文还提供了用于鉴定LFA-1拮抗剂的化合物的方法。

9. 发明申请

US20080021055A1 Novel cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists 审中-公开
标题翻译：新型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：US20080021055A1
公开(公告)日：2008-01-24
申请号：US11892235
申请日：2007-08-21
申请人： Volkmar Wehner , Jochen Knolle , Hans Stilz , Jean-Francois Gourvest , Denis Carniato , Thomas Gadek , Robert McDowell , Robert Pitti , Sarah Bodary
发明人： Volkmar Wehner , Jochen Knolle , Hans Stilz , Jean-Francois Gourvest , Denis Carniato , Thomas Gadek , Robert McDowell , Robert Pitti , Sarah Bodary
IPC分类号： A61K31/505 , A61K31/27 , A61P9/10 , C07D233/00 , C07D239/02 , C07C269/00 , A61K31/4164
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用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

10. 发明授权

US06762190B2 Thienylalanine derivatives as inhibitors of cell adhesion 有权
标题翻译：噻吩丙氨酸衍生物作为细胞粘附的抑制剂
公开(公告)号：US06762190B2
公开(公告)日：2004-07-13
申请号：US10169612
申请日：2002-09-23
申请人： Thomas Gadek , Jean-Francois Gourvest , Anuschirwan Peyman , Jean-Marie Ruxer , Karl-Heinz Scheunemann
发明人： Thomas Gadek , Jean-Francois Gourvest , Anuschirwan Peyman , Jean-Marie Ruxer , Karl-Heinz Scheunemann
IPC分类号： C07D40912
CPC分类号： C07D409/12
摘要： The present invention relates to compounds of formula (I), in which A, B, X, Y, R1, R2, R3 and n have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. 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 compositions comprising them.
摘要翻译：本发明涉及式（I）化合物，其中A，B，X，Y，R 1，R 2，R 3和n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。它们是玻连蛋白受体拮抗剂和细胞粘附抑制剂，并且适用于治疗和预防基于玻连蛋白受体及其配体在细胞 - 细胞或细胞 - 基质相互作用过程中的相互作用的疾病，或可被预防，缓解或通过影响这种相互作用来治愈。例如，它们可以用于抑制破骨细胞的骨吸收，从而用于治疗和预防骨质疏松症，或用于抑制血管平滑肌肉细胞的不期望的血管生成或增殖。本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。

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