专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20060199809A1 Factor Xa compounds 有权
标题翻译：因子Xa化合物
公开(公告)号：US20060199809A1
公开(公告)日：2006-09-07
申请号：US11257208
申请日：2005-10-24
申请人： Tianbao Lu , Tho Thieu , Yu-Kai Lee , Daniel Parks , Thomas Markotan , Wenxi Pan , Karen Milkiewicz , Mark Player
发明人： Tianbao Lu , Tho Thieu , Yu-Kai Lee , Daniel Parks , Thomas Markotan , Wenxi Pan , Karen Milkiewicz , Mark Player
IPC分类号： A61K31/54 , A61K31/5377 , A61K31/519 , C07D487/02
CPC分类号： C07D413/14 , C07D231/56 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D409/14 , C07D413/04 , C07D417/10
摘要： The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.
摘要翻译：本发明涉及式I的新型化合物及其形式和药物组合物，以及其作为因子Xa抑制剂的用途。

2. 发明申请

US20050159457A1 Aminopyridinyl-, aminoguanidinyl- and alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors 审中-公开
标题翻译：氨基吡啶基 - ，氨基胍基和烷氧基胍基取代的苯基乙酰胺作为蛋白酶抑制剂
公开(公告)号：US20050159457A1
公开(公告)日：2005-07-21
申请号：US11032297
申请日：2005-01-10
申请人： Wenxi Pan , Tianbao Lu , Thomas Markotan , Bruce Tomczuk
发明人： Wenxi Pan , Tianbao Lu , Thomas Markotan , Bruce Tomczuk
IPC分类号： A61K31/155 , A61K31/165 , A61K31/18 , A61K31/255 , A61K31/44 , A61K45/00 , A61L31/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P29/00 , A61P43/00 , C07C279/00 , C07C279/04 , C07C291/02 , C07C309/67 , C07C309/73 , C07C311/13 , C07C311/21 , C07D213/73 , C07D213/75 , C07C279/20 , C07C311/45
CPC分类号： C07D213/73 , A61K31/155 , A61K31/44 , C07C279/00 , C07C309/73 , C07C311/13 , C07C311/21 , C07D213/75 , A61K2300/00
摘要： Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
摘要翻译：描述了苯基乙酰胺化合物，包括式I化合物或其溶剂合物，水合物或其药学上可接受的盐; 其中R 3，R 6，R 11，B，Y和W在说明书中列出。本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样的丝氨酸蛋白酶，如凝血酶和因子Xa。描述了抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制栓塞形成的组合物。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。另外，化合物可以被可检测地标记并用于血栓的体内成像。

3. 发明申请

US20070066610A1 Acylhydrazones as kinase modulators 有权
标题翻译：酰腙作为激酶调节剂
公开(公告)号：US20070066610A1
公开(公告)日：2007-03-22
申请号：US11377077
申请日：2006-03-16
申请人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
发明人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/404 , C07D413/14 , C07D405/14
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
摘要： The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的酰腙化合物：其中R 1，R 2和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是 c-Met的抑制剂以及这些化合物在细胞或受试者中降低或抑制c-Met的激酶活性并调节细胞或受试者中的c-Met表达的用途，以及这些化合物用于预防或在受试者中治疗与c-Met相关的细胞增殖性疾病和/或障碍。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

4. 发明申请

US20070203136A1 TRIAZOLOPYRIDAZINES AS KINASE MODULATORS 有权
标题翻译：三唑吡啶作为激酶调节剂
公开(公告)号：US20070203136A1
公开(公告)日：2007-08-30
申请号：US11612020
申请日：2006-12-18
申请人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
发明人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
IPC分类号： A61K31/503 , A61K31/5377 , C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7， >，R 8和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及这些化合物用于降低或抑制激酶活性的用途 c-Met在细胞或受试者中的调节，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与c-Met有关的障碍的用途。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

5. 发明申请

US20060211719A1 Heteroaryl aminoguanidine and alkoxyguanidines and their use as protease inhibitors 有权
标题翻译：杂芳基氨基胍和烷氧基胍被用作蛋白酶抑制剂
公开(公告)号：US20060211719A1
公开(公告)日：2006-09-21
申请号：US11254086
申请日：2005-10-19
申请人： Tianbao Lu , Bruce Tomczuk , Thomas Markotan , Colleen Siedem
发明人： Tianbao Lu , Bruce Tomczuk , Thomas Markotan , Colleen Siedem
IPC分类号： A61K31/513 , C07D403/02
CPC分类号： C07D213/74 , C07D213/75 , C07D401/12 , C07D409/12 , C07K5/06139
摘要： Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
摘要翻译：描述了氨基胍和烷氧基胍化合物，包括式VII的化合物：其中X是O或NR 9和Het，R 1，R 7， R 8，R 12，R 15，R 12，R 12，R 12，说明书中描述的R，Z和n以及其抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。还描述了制备这些化合物的方法。本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。另外，化合物可以被可检测地标记并用于血栓的体内成像。

6. 发明申请

US20050209225A1 Substituted indoles and their use as integrin antagonists 审中-公开
标题翻译：取代的吲哚及其作为整联蛋白拮抗剂的用途
公开(公告)号：US20050209225A1
公开(公告)日：2005-09-22
申请号：US11005596
申请日：2004-12-06
申请人： Tianbao Lu , Louis LaFrance , Bruce Tomczuk , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
发明人： Tianbao Lu , Louis LaFrance , Bruce Tomczuk , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
IPC分类号： A61K31/404 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/5383 , A61P3/06 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D213/74 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D498/04 , A61K31/538 , A61K31/405 , A61K31/4745 , A61K31/506
CPC分类号： C07D213/74 , C07D209/08 , C07D401/12 , C07D401/14 , C07D471/02 , C07D471/04 , C07D471/14
摘要： The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
摘要翻译：本发明涉及作为αV（alphav）整联蛋白的拮抗剂的新的取代的吲哚化合物，例如α缬氨酸和/ β5整联蛋白，其药学上可接受的盐及其药物组合物。该化合物可用于治疗由α3β3和α5β5 5介导的病理状况。整合素，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。化合物具有以下通式：其中R 1，R 2，R 3，R 4，R 4， R 5，R 6，R 7，R 8，R 9，R 9， D 10，R 11，R 12，R 13，R 14，D， X，W，a，m，n，i，j，k和v在本文中定义。

7. 发明申请

US20070219233A1 Substituted Indoles and Their Use as Integrin Antagonists 审中-公开
标题翻译：取代的吲哚及其作为整合素拮抗剂的用途
公开(公告)号：US20070219233A1
公开(公告)日：2007-09-20
申请号：US11755831
申请日：2007-05-31
申请人： Tianbo Lu , Bruce Tomczuk , Louis LaFrance , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
发明人： Tianbo Lu , Bruce Tomczuk , Louis LaFrance , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
IPC分类号： A61K31/4353 , C07D471/04
CPC分类号： C07D213/74 , C07D209/08 , C07D401/12 , C07D401/14 , C07D471/02 , C07D471/04 , C07D471/14
摘要： The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
摘要翻译：本发明涉及作为αV（alphav）整联蛋白的拮抗剂的新的取代的吲哚化合物，例如α缬氨酸和/ β5整联蛋白，其药学上可接受的盐及其药物组合物。该化合物可用于治疗由α3β3和α5β5 5介导的病理状况。整合素，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。化合物具有以下通式：其中R 1，R 2，R 3，R 4，R 4， R 5，R 6，R 7，R 8，R 9，R 9， D 10，R 11，R 12，R 13，R 14，D， X，W，a，m，n，i，j，k和v在本文中定义。

8. 发明申请

US20050250771A1 Substituted indoles and their use as integrin antagonists 有权
标题翻译：取代的吲哚及其作为整联蛋白拮抗剂的用途
公开(公告)号：US20050250771A1
公开(公告)日：2005-11-10
申请号：US11005294
申请日：2004-12-06
申请人： Tianbo Lu , Bruce Tomczuk , Louis LaFrance , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
发明人： Tianbo Lu , Bruce Tomczuk , Louis LaFrance , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
IPC分类号： A61K31/404 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/5383 , A61P3/06 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D213/74 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D498/04 , A61K31/538 , A61K31/405 , A61K31/4745 , A61K31/506 , C07D413/02 , C07D43/02
CPC分类号： C07D213/74 , C07D209/08 , C07D401/12 , C07D401/14 , C07D471/02 , C07D471/04 , C07D471/14
摘要： The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, , R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
摘要翻译：本发明涉及作为αV（alphav）整联蛋白拮抗剂的新型取代的吲哚化合物，例如阿尔茨海默氏症和/ 整联蛋白，其药学上可接受的盐及其药物组合物。该化合物可用于治疗由α3β3和α5β5 5介导的病理状况。整合素，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。化合物具有以下通式：其中R 1，R 2，R 3，R 4，R 4， R 5，R 6，R 7，R 8，R 9，R 9， R 10，R 11，R 12，R 12，R 14，D 12，，X，W，a，m，n，i，j，k和v在本文中定义。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式