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    Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
    51.
    发明授权
    Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors 有权
    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：US07402586B2

    公开(公告)日：2008-07-22

    申请号：US11254086

    申请日：2005-10-19

    申请人： Tianbao Lu ,  Bruce Tomczuk ,  Thomas P. Markotan ,  Colleen Siedem

    发明人： Tianbao Lu ,  Bruce Tomczuk ,  Thomas P. Markotan ,  Colleen Siedem

    IPC分类号： C07D239/54 ,  A61K31/513

    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。

    Heteroaryl aminoguanidine and alkoxyguanidines and their use as protease inhibitors
    54.
    发明申请
    Heteroaryl aminoguanidine and alkoxyguanidines and their use as protease inhibitors 有权
    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。

    Substituted 1,4-benzodiazepines and uses thereof
    56.
    发明申请
    Substituted 1,4-benzodiazepines and uses thereof 审中-公开
    取代的1,4-苯并二氮杂及其用途

    公开(公告)号：US20060148792A1

    公开(公告)日：2006-07-06

    申请号：US11371964

    申请日：2006-03-09

    申请人： Tianbao Lu ,  Louis LaFrance ,  Daniel Parks ,  Karen Milkiewicz ,  Raul Calvo ,  Maxwell Cummings ,  Alexander Kim ,  Bruce Grasberger ,  Theodore Carver

    发明人： Tianbao Lu ,  Louis LaFrance ,  Daniel Parks ,  Karen Milkiewicz ,  Raul Calvo ,  Maxwell Cummings ,  Alexander Kim ,  Bruce Grasberger ,  Theodore Carver

    IPC分类号： A61K31/551 ,  C07D243/12 ,  C07D243/18

    CPC分类号： C07D401/04 ,  C07D243/14 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04

    摘要： The present invention is directed to novel 1,4-benzodiazepines, 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: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M arm defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl: aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0-8, m is 0-8, i is 1-8 and j is 0-8.

    摘要翻译： 本发明涉及新的1,4-苯二氮卓类药物，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：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d，R d和M臂; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6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 9是环烷基：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; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

    Substituted 1,4-benzodiazepines and uses thereof
    57.
    发明授权
    Substituted 1,4-benzodiazepines and uses thereof 失效
    取代的1,4-苯并二氮杂及其用途

    公开(公告)号：US07067512B2

    公开(公告)日：2006-06-27

    申请号：US10292876

    申请日：2002-11-13

    申请人： Tianbao Lu ,  Louis V Lafrance, III ,  Daniel J Parks ,  Karen L Milkiewicz ,  Raul R Calvo ,  Maxwell D Cummings ,  Alexander J Kim ,  Bruce L Grasberger ,  Theodore E Carver, Jr.

    发明人： Tianbao Lu ,  Louis V Lafrance, III ,  Daniel J Parks ,  Karen L Milkiewicz ,  Raul R Calvo ,  Maxwell D Cummings ,  Alexander J Kim ,  Bruce L Grasberger ,  Theodore E Carver, Jr.

    IPC分类号： C07D243/12 ,  C07D243/18 ,  C07D243/24 ,  A61K31/55

    CPC分类号： C07D401/04 ,  C07D243/14 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04

    摘要： The present invention is directed to novel 1,4-benzodiazepines, 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: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M are defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0–8, m is 0–8, i is 1–8 and j is 0–8.

    摘要翻译： 本发明涉及新的1,4-苯二氮卓类药物，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：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d和M在本文中定义; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6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 9是环烷基，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; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

    Cyclic oxyguanidine pyrazinones as protease inhibitors
    58.
    发明授权
    Cyclic oxyguanidine pyrazinones as protease inhibitors 有权
    环氧乙酰吡嗪酮作为蛋白酶抑制剂

    公开(公告)号：US07030110B2

    公开(公告)日：2006-04-18

    申请号：US10263663

    申请日：2002-10-04

    申请人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    发明人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    IPC分类号： A61K31/535 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/553 ,  A61K31/55

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. 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. 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： 描述了环状氧基胍吡嗪酮化合物，包括式I化合物：其中R 3，R 4，R 5，W和A是 如说明书中所述，以及其水合物，溶剂合物或其药学上可接受的盐。 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。 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。