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1. 发明申请

WO0206248A2 CYCLIC OXYGUANIDINE PYRAZINONES AS PROTEASE INHIBITORS 审中-公开
标题翻译：作为蛋白酶抑制剂的环状氧杂胍吡唑啉酮
公开(公告)号：WO0206248A2
公开(公告)日：2002-01-24
申请号：PCT/US0122302
申请日：2001-07-17
申请人： DIMENSIONAL PHARM INC
发明人： WANG AIHUA , TOMCZUK BRUCE E , LU TIANBAO , SOLL RICHARD M , SPURLINO JOHN C , BONE ROGER FRANCIS
IPC分类号： A61K31/5355 , A61K31/5395 , A61K51/00 , A61L33/00 , A61P7/02 , A61P43/00 , C07D413/12 , C07D413/14 , C07D241/00
CPC分类号： C07D413/12 , C07D413/14
摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula (I): wherein R , R , R , W, and A are as set forth in the specidification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of protease, especially trypsin-like serine proteases, such as chymotripsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of trombin. Compositions for inhibiting loss of blood platelas, 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 labeled and employed fot in vivo imaging of thrombi.
摘要翻译：描述了环状氧胍吡嗪酮化合物，包括式（I）的化合物：其中R 3，R 4，R 5，W和A如分类中所述，以及水合物，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而表现出抗血栓形成活性。描述了用于抑制血小板丧失，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抗凝血剂嵌入或物理连接到用于血液采集，血液循环和血液储存的装置的制造中的材料，例如导管，血液透析机，血液采集注射器和管，血线和支架。另外，化合物可以被可检测地标记并且被用于标记并且用于血栓的体内成像。

2. 发明申请

WO03095625A2 METHOD FOR CYTOPROTECTION THROUGH MDM2 AND HDM2 INHIBITION 审中-公开
标题翻译：通过MDM2和HDM2抑制进行CYTOPROTECTION的方法
公开(公告)号：WO03095625A2
公开(公告)日：2003-11-20
申请号：PCT/US0314923
申请日：2003-05-13
申请人： DIMENSIONAL PHARM INC , KOBLISH HOLLY K , MANTHEY CARL L , MOLLOY CHRISTOPHER J , LU TIANBAO , PARKS DANIEL J , LAFRANCE III LOUIS V , MILKIEWICZ KAREN L , CARVER TED , GRASBERGER BRUCE L
发明人： KOBLISH HOLLY K , MANTHEY CARL L , MOLLOY CHRISTOPHER J , LU TIANBAO , PARKS DANIEL J , LAFRANCE III LOUIS V , MILKIEWICZ KAREN L , CARVER TED , GRASBERGER BRUCE L
IPC分类号： A61K31/5513 , C12N
CPC分类号： A61K31/5513
摘要： The present invention is directed to a method of protecting one or more cells from programmed cytotoxic cell death by contacting the cells with a cytoprotective amount of an MDM2 and/or HDM2 inhibitor. The cytoprotective amount of inhibitor is typically used as a pulsed administration. Useful inhibitors include a class of 1,4-benzodiazepines, which act as inhibitors of MDM2-p53 interactions. The method of the invention can be employed as an adjunct to chemotherapy or radiation therapy. In addition, the methods of the invention can be employed to treat a disease or condition that involves excessive cell death.
摘要翻译：本发明涉及通过使细胞与细胞保护剂量的MDM2和/或HDM2抑制剂接触来保护一种或多种细胞免受程序性细胞毒性细胞死亡的方法。抑制剂的细胞保护量通常用作脉冲给药。有用的抑制剂包括一类1,4-苯二氮卓类，其作为MDM2-p53相互作用的抑制剂。本发明的方法可以用作化疗或放射治疗的辅助物质。此外，本发明的方法可用于治疗涉及过度细胞死亡的疾病或病症。

3. 发明申请

WO2004091613A3 SUBSTITUTED PHENYL ACETAMIDES AND THEIR USE AS PROTEASE INHIBITORS 审中-公开
标题翻译：取代苯乙酸酯及其作为蛋白酶抑制剂的用途
公开(公告)号：WO2004091613A3
公开(公告)日：2005-01-27
申请号：PCT/US2004010034
申请日：2004-04-01
申请人： DIMENSIONAL PHARM INC , KREUTTER KEVIN D , LEE LILY , LU TIANBAO , MOHAN VENKATRAMAN , PATEL SHARMILA , HUANG HUI , XU GUOZHANG , FITZGERALD MARK
发明人： KREUTTER KEVIN D , LEE LILY , LU TIANBAO , MOHAN VENKATRAMAN , PATEL SHARMILA , HUANG HUI , XU GUOZHANG , FITZGERALD MARK
IPC分类号： A61K31/165 , A61K31/445 , A61K31/495 , A61K31/537 , A61K31/54 , A61K31/55 , A61P7/00 , C07C279/00 , C07C291/04 , C07D213/26 , C07D213/73 , C07D213/89 , C07D215/12 , C07D277/04 , C07D279/12 , C07D413/12 , C07D487/04 , A61K31/44 , C07D213/38 , C07D401/12
CPC分类号： C07D213/73 , C07C279/00 , C07C291/04 , C07D213/26 , C07D213/89 , C07D215/12 , C07D413/12 , C07D487/04
摘要： Phenyl acetamide compounds are described, including compounds of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R -R , R , 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）的化合物或其溶剂化物，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连接于制造用于血液收集，血液循环和血液储存的装置的材料的抗凝剂，例如导管，血液透析机，采血注射器和管，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。

4. 发明申请

WO0228825A3 AMINOPYRIDINYL-, AMINOGUANIDINYL- AND ALKOXYGUANIDINYL- SUBSTITUTED PHENYL ACETAMIDES AS PROTEASE INHIBITORS 审中-公开
标题翻译：氨基吡啶基 - ，氨基嘌呤 - 和烷氧基胍 - 取代的苯丙酰胺类作为蛋白酶抑制剂
公开(公告)号：WO0228825A3
公开(公告)日：2002-06-13
申请号：PCT/US0131249
申请日：2001-10-05
申请人： DIMENSIONAL PHARM INC
发明人： PAN WENXI , LU TIANBAO , MARKOTAN THOMAS P , TOMCZUK BRUCE E
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 , C07C317/14 , C07D213/40
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 R -R , R , 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 for thrombi.
摘要翻译：描述了苯基乙酰胺化合物，包括式（I）的化合物：或其溶剂化物，水合物或药学上可接受的盐; 其中R 3 -R 6，R 11，B，Y和W在说明书中给出。本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如凝血酶和因子Xa。描述了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栓塞形成的组合物。本发明化合物的其它用途是作为抗凝血剂嵌入或物理连接到用于血液采集，血液循环和血液储存的装置的制造中的材料，例如导管，血液透析机，血液采集注射器和管，血线和支架。此外，化合物可被可检测地标记并用于体内血栓成像。

5. 发明申请

WO9823565A3 Aminoguandines and alkoxyguandines as protease inhibitors 审中-公开
标题翻译：氨基嘌呤和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：WO9823565A3
公开(公告)日：1998-07-30
申请号：PCT/US9721649
申请日：1997-11-26
申请人： DIMENSIONAL PHARM INC
发明人： TOMCZUK BRUCE E , SOLL RICHARD M , LU TIANBAO , FEDDE CYNTHIA L , ILLIG CARL R , MARKOTAN THOMAS P , STAGNARO THOMAS P
IPC分类号： C07D295/22 , A01N1/02 , A61K20060101 , A61K31/155 , A61K31/165 , A61K31/18 , A61K31/225 , A61K31/255 , A61K31/305 , A61K31/335 , A61K31/341 , A61K31/36 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/535 , A61K33/42 , A61L33/00 , A61P7/00 , A61P7/02 , A61P9/10 , A61P29/00 , C07C20060101 , C07C69/76 , C07C279/00 , C07C279/10 , C07C281/16 , C07C291/04 , C07C303/30 , C07C303/40 , C07C305/00 , C07C309/00 , C07C309/63 , C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C317/26 , C07C323/17 , C07D20060101 , C07D207/14 , C07D207/16 , C07D207/48 , C07D209/04 , C07D211/22 , C07D211/58 , C07D211/64 , C07D211/96 , C07D213/24 , C07D213/42 , C07D213/74 , C07D215/12 , C07D215/36 , C07D217/12 , C07D217/22 , C07D229/00 , C07D231/04 , C07D237/02 , C07D239/42 , C07D239/72 , C07D243/04 , C07D245/02 , C07D261/02 , C07D263/54 , C07D265/02 , C07D267/04 , C07D269/00 , C07D285/14 , C07D295/12 , C07D307/02 , C07D307/52 , C07D307/66 , C07D311/66 , C07D311/74 , C07D317/08 , C07D317/14 , C07D317/34 , C07D317/40 , C07D317/64 , C07D333/06 , C07D333/34 , C07D333/54 , C07D333/62 , C07D403/04 , C07D413/04 , C07F9/22
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 formula (I) wherein X is O or NR?9 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.

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