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1. 发明授权

US07829584B2 Pyridines and pyridine N-oxides as modulators of thrombin 有权
标题翻译：吡啶和吡啶N-氧化物作为凝血酶的调节剂
公开(公告)号：US07829584B2
公开(公告)日：2010-11-09
申请号：US11685544
申请日：2007-03-13
申请人： Mark R. Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
发明人： Mark R. Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
IPC分类号： C07D213/00 , A61K31/44
CPC分类号： C07D213/89 , C07D213/74 , C07D213/84 , C07D401/14 , C07D413/14
摘要： The present invention describes compounds of Formula I: wherein W, X, Y, Z, and Q are defined herein, or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal.
摘要翻译：本发明描述了式I的化合物：其中W，X，Y，Z和Q在本文中定义，或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。

2. 发明申请

US20070225282A1 PYRIDINES AND PYRIDINE N-OXIDES AS MODULATORS OF THROMBIN 有权
标题翻译：吡啶和吡啶N-氧化物作为THROMBIN的调节剂
公开(公告)号：US20070225282A1
公开(公告)日：2007-09-27
申请号：US11685544
申请日：2007-03-13
申请人： Mark Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
发明人： Mark Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
IPC分类号： A61K31/5377 , A61K31/4439 , C07D413/14
CPC分类号： C07D213/89 , C07D213/74 , C07D213/84 , C07D401/14 , C07D413/14
摘要： The present invention describes compounds of Formula I: wherein W, X, Y, Z, and Q are defined herein, or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal.
摘要翻译：本发明描述了式I的化合物：其中W，X，Y，Z和Q在本文中定义，或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。

3. 发明申请

US20060241148A1 Fluorinated pyridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls 有权
标题翻译：氟化吡啶N-氧化物凝血酶调节剂和含氮杂芳基的N-氧化方法
公开(公告)号：US20060241148A1
公开(公告)日：2006-10-26
申请号：US11385056
申请日：2006-03-21
申请人： Kevin Kreutter , Tianbao Lu , Yu Lee , Christopher Teleha , Mark Player , Xizhen Zhu
发明人： Kevin Kreutter , Tianbao Lu , Yu Lee , Christopher Teleha , Mark Player , Xizhen Zhu
IPC分类号： A61K31/444 , C07D213/84 , C07D401/02
CPC分类号： C07D213/89 , C07D215/60 , C07D239/24 , C07D241/10
摘要： The present invention describes compounds of Formula I or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal. The present invention also relates to a novel method of N-oxidation of nitrogen containing heteroaryls.
摘要翻译：本发明描述了式I化合物或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。本发明还涉及含氮杂芳基的N-氧化的新方法。

4. 发明授权

US07262210B2 Fluorinated pyridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls 有权
标题翻译：氟化吡啶N-氧化物凝血酶调节剂和含氮杂芳基的N-氧化方法
公开(公告)号：US07262210B2
公开(公告)日：2007-08-28
申请号：US11385056
申请日：2006-03-21
申请人： Kevin Kreutter , Tianbao Lu , Yu Kai Lee , Christopher Teleha , Mark Player , Xizhen Zhu
发明人： Kevin Kreutter , Tianbao Lu , Yu Kai Lee , Christopher Teleha , Mark Player , Xizhen Zhu
IPC分类号： A61K31/44 , C07D213/00
CPC分类号： C07D213/89 , C07D215/60 , C07D239/24 , C07D241/10
摘要： The present invention describes compounds of Formula I or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal. The present invention also relates to a novel method of N-oxidation of nitrogen containing heteroaryls.
摘要翻译：本发明描述了式I化合物或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。本发明还涉及含氮杂芳基的N-氧化的新方法。

5. 发明授权

US07446210B2 Factor Xa compounds 有权
标题翻译：因子Xa化合物
公开(公告)号：US07446210B2
公开(公告)日：2008-11-04
申请号：US11257208
申请日：2005-10-24
申请人： Tianbao Lu , Tho V. Thieu , Yu-Kai Lee , Daniel J. Parks , Thomas P. Markotan , Wenxi Pan , Karen L. Milkiewicz , Mark R. Player
发明人： Tianbao Lu , Tho V. Thieu , Yu-Kai Lee , Daniel J. Parks , Thomas P. Markotan , Wenxi Pan , Karen L. Milkiewicz , Mark R. Player
IPC分类号： C07D207/00 , C07D213/00 , C07D231/00 , C07D231/54 , C07D239/02 , C07D241/04 , C07D265/28 , C07D295/00 , C07D487/00
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。

6. 发明授权

US07968725B2 Pyridinyl modulators of γ-secretase 有权
标题翻译： γ-分泌酶的吡啶基调节剂
公开(公告)号：US07968725B2
公开(公告)日：2011-06-28
申请号：US12478820
申请日：2009-06-05
申请人： Tianbao Lu
发明人： Tianbao Lu
IPC分类号： C07D213/55 , A01N43/40
CPC分类号： C07D213/74 , C07D213/55 , C07D401/04 , C07D405/04 , C07D409/04
摘要： The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.
摘要翻译：本发明涉及如下所示的式I化合物，其中A，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9的定义在说明书中提供。式I化合物可用于治疗与γ-分泌酶活性相关的疾病，包括阿尔茨海默氏病。

7. 发明申请

US20060235007A1 Substituted 1,4-diazepines and uses thereof 审中-公开
标题翻译：取代的1,4-二氮杂及其用途
公开(公告)号：US20060235007A1
公开(公告)日：2006-10-19
申请号：US11452861
申请日：2006-06-14
申请人： Tianbao Lu , Karen Milkiewicz , Pierre Raboisson , Maxwell Cummings , Raul Calvo , Daniel Parks , Louis LaFrance , Juan Marugan Sanchez , Joan Gushue , Kristi Leonard
发明人： Tianbao Lu , Karen Milkiewicz , Pierre Raboisson , Maxwell Cummings , Raul Calvo , Daniel Parks , Louis LaFrance , Juan Marugan Sanchez , Joan Gushue , Kristi Leonard
IPC分类号： A61K31/5513 , C07D403/02 , C07D413/02 , C07D243/18
CPC分类号： C07D243/14
摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein; X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; and R3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino; or R3—X— is hydrogen or an electron pair; R4 is oxygen or —NR9R10; R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; and R6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
摘要翻译：本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R SUP， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4，或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。

8. 发明授权

US06638931B1 Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06638931B1
公开(公告)日：2003-10-28
申请号：US09722363
申请日：2000-11-28
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
IPC分类号： A61K31255
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present 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, or are intermediates useful for forming compounds having antithrombotic activity. 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.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及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是描述。还描述了制备式I化合物的方法。本发明的新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，例如胰凝乳蛋白酶，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，或者是用于形成具有抗血栓形成活性的化合物的中间体。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。

9. 发明授权

US06518310B2 Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06518310B2
公开(公告)日：2003-02-11
申请号：US09809293
申请日：2001-03-16
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L Fedde , Carl R Illig , Thomas P. Markotan , Thomas P Stagnaro
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L Fedde , Carl R Illig , Thomas P. Markotan , Thomas P Stagnaro
IPC分类号： A61K31255
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present 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, or are intermediates useful for forming compounds having antithrombotic activity. 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.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X为O或NR 9，R 1 -R 4，R 6 -R 9，R 11，R 12，R a，R b，R c，Y，Z，n和m在说明书中阐述，以及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。还描述了制备式I化合物的方法。本发明的新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，例如胰凝乳蛋白酶，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，或者是用于形成具有抗血栓形成活性的化合物的中间体。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。

10. 发明授权

US06350764B2 Heteroaryl aminoguanidines 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及其作为蛋白酶抑制剂的用途
公开(公告)号：US06350764B2
公开(公告)日：2002-02-26
申请号：US09827292
申请日：2001-04-06
申请人： Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
发明人： Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
IPC分类号： A61K314412
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，Het，R 1，R 7，R 8，R 12 -R 15，R a，R b，R c，Z和n在说明书中阐述，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。

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