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31. 发明授权

US07550474B2 Substituted phenyl acetamides and their use as protease inhibitors 有权
标题翻译：取代苯乙酰胺及其作为蛋白酶抑制剂的用途
公开(公告)号：US07550474B2
公开(公告)日：2009-06-23
申请号：US10816544
申请日：2004-04-01
申请人： Kevin D. Kreutter , Lily Lee , Tianbao Lu , Venkatraman Mohan , Sharmila Patel , Hui Huang , Guozhang Xu , Mark Fitzgerald
发明人： Kevin D. Kreutter , Lily Lee , Tianbao Lu , Venkatraman Mohan , Sharmila Patel , Hui Huang , Guozhang Xu , Mark Fitzgerald
IPC分类号： A61K31/435 , C07D221/02 , C07D335/00 , C07D309/00 , C07C321/00
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 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R3-R6，R11，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。

32. 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。

33. 发明授权

US06521663B2 Aminoguanidinyl- and Alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors 有权
标题翻译：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：US06521663B2
公开(公告)日：2003-02-18
申请号：US09971000
申请日：2001-10-05
申请人： Wenxi Pan , Tianbao Lu , Thomas P. Markotan , Bruce E. Tomczuk
发明人： Wenxi Pan , Tianbao Lu , Thomas P. Markotan , Bruce E. Tomczuk
IPC分类号： C07C30930
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R3-R6，R11，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。

34. 发明授权

US06204263B1 Pyrazinone protease inhibitors 有权
标题翻译：吡嗪酮蛋白酶抑制剂
公开(公告)号：US06204263B1
公开(公告)日：2001-03-20
申请号：US09330128
申请日：1999-06-11
申请人： Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan
发明人： Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan
IPC分类号： C07D23947
CPC分类号： C07K5/06139 , A61K38/00
摘要： Pyrazinone compounds are described, including compounds of the Formula I: wherein X is O, NR11 or CH═N, R3-R11, Ra, Rb, Rc, W, m, and n are 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：描述了吡唑啉酮化合物，包括式I的化合物：其中X是O，NR 11或CH = N，R 3 -R 11，R a，R b，R c，W，m和n在说明书中列出，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。

35. 发明授权

US08030305B2 Triazolopyridazines as kinase modulators 有权
标题翻译：三唑并嘧啶作为激酶调节剂
公开(公告)号：US08030305B2
公开(公告)日：2011-10-04
申请号：US11612020
申请日：2006-12-18
申请人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
发明人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
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，以及使用的这样的化合物以减少或抑制细胞或受试者中c-Met的激酶活性，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用于预防或治疗细胞增殖性病症和 /或与c-Met有关的障碍。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。

36. 发明授权

US07786116B2 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) 有权
标题翻译：可用作β-分泌酶抑制剂（BACE）的2-氨基 - 喹啉衍生物
公开(公告)号：US07786116B2
公开(公告)日：2010-08-31
申请号：US12362020
申请日：2009-01-29
申请人： Ellen Baxter , Christopher J. Creighton , Chih Yung Ho , Yifang Huang , Tianbao Lu , Chi Luo , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Ellen Sieber-McMaster
发明人： Ellen Baxter , Christopher J. Creighton , Chih Yung Ho , Yifang Huang , Tianbao Lu , Chi Luo , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Ellen Sieber-McMaster
IPC分类号： A61K31/5377 , A61K31/4709 , C07D413/14 , C07D215/38
CPC分类号： C07D405/14 , C07D405/06 , C07D409/14
摘要： The present invention is directed to novel 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and/or dementia. The compounds of the present invention are inhibitors of β-secretase, also known as β-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.
摘要翻译：本发明涉及新的2-氨基 - 喹啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD），轻度认知障碍，衰老和/或痴呆中的用途。本发明的化合物是分泌酶抑制剂，也称为淀粉样蛋白酶切割酶BACE，BACE1，Asp2或memapsin2。

37. 发明申请

US20100022583A1 PYRIDINYL MODULATORS OF gamma-SECRETASE 有权
标题翻译： γ-分泌酶的吡啶类调节剂
公开(公告)号：US20100022583A1
公开(公告)日：2010-01-28
申请号：US12478820
申请日：2009-06-05
申请人： Tianbao Lu
发明人： Tianbao Lu
IPC分类号： A61K31/4725 , C07D213/55 , A61K31/4418 , C07D401/04 , A61P25/28
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。

38. 发明申请

US20090227627A1 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 有权
标题翻译：作为β-分泌酶（BACE）抑制剂的6-取代的噻二氨基喹啉衍生物
公开(公告)号：US20090227627A1
公开(公告)日：2009-09-10
申请号：US12360611
申请日：2009-01-27
申请人： Ellen Baxter , Christopher J. Creighton , Tianbao Lu , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Ellen Sieber-McMaster
发明人： Ellen Baxter , Christopher J. Creighton , Tianbao Lu , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Ellen Sieber-McMaster
IPC分类号： A61K31/4709 , C07D405/06 , A61P25/28 , A61P25/00 , A61P25/16
CPC分类号： C07D209/14 , C07D307/81 , C07D333/58 , C07D409/12
摘要： The present invention is directed to 6-substituted-thio-2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and/or dementia. The compounds of the present invention are inhibitors of β-secretase, also known as β-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.
摘要翻译：本发明涉及6-取代硫代-2-氨基 - 喹啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD），轻度认知障碍，衰老和/或痴呆中的用途。本发明的化合物是β-分泌酶的抑制剂，也称为β位点淀粉样蛋白切割酶BACE，BACE1，Asp2或memapsin2。

39. 发明申请

US20080194624A1 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 有权
标题翻译：用作β-分泌酶（BACE）抑制剂的2-氨基喹啉衍生物
公开(公告)号：US20080194624A1
公开(公告)日：2008-08-14
申请号：US11671681
申请日：2007-02-06
申请人： Ellen Baxter , Allen B. Reitz , Umar Saibu Mohomed Maharoof , Yifang Huang , Christopher John Creighton , Charles H. Reynolds , Chi Luo , Brett A. Tounge , Tina Morgan Ross , Tianbao Lu
发明人： Ellen Baxter , Allen B. Reitz , Umar Saibu Mohomed Maharoof , Yifang Huang , Christopher John Creighton , Charles H. Reynolds , Chi Luo , Brett A. Tounge , Tina Morgan Ross , Tianbao Lu
IPC分类号： A61K31/47 , C07D215/38 , A61P25/00 , A61P25/28 , A61P25/16
CPC分类号： C07D215/38 , C07D401/12 , C07D405/06 , C07D405/14 , C07D413/14
摘要： The present invention is directed to 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
摘要翻译：本发明涉及2-氨基 - 喹啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关病症中的用途。本发明的化合物是β-分泌酶的抑制剂，也称为β-位点切割酶和BACE，BACE1，Asp2和memapsin2。

40. 发明授权

US07172742B2 Method of preparing wet process phosphoric acid 失效
标题翻译：湿法磷酸的制备方法
公开(公告)号：US07172742B2
公开(公告)日：2007-02-06
申请号：US10362845
申请日：2001-05-15
申请人： Yisheng Feng , Jiutian Feng , Xigang Liu , Yurui Wang , Tianbao Lu
发明人： Yisheng Feng , Jiutian Feng , Xigang Liu , Yurui Wang , Tianbao Lu
IPC分类号： C01B25/222 , C01B25/231
CPC分类号： C01F11/46 , C01B25/231
摘要： The present invention relates to a method of preparing wet process phosphoric acid, which comprises: dividing raw materials which contain phosphate rock slurry and sulfuric acid into two parts, and then feeding these two parts into two reactors separately. In the first reactor, feeding 70–90 wt. % of the total amount of the slurry and sulfuric acid, in which the ratio of phosphate rock slurry to sulfuric acid to recycled phosphoric acid is set to be 1:0.6˜0.8:1.0˜2.5. 10˜30% of the reaction solution directly flows into conversion cell, participating in the conversion reaction of dihydrate gypsum. Thus resulted phosphoric acid concentration is 33˜39 wt. %. The recovery efficiency of P2O5 is 99% or more. When putting coke powders in the conversion solution as filter aid, the filtration efficiency can be improved by 10˜30%, and in so produced hemihydrate gypsum, P2O5 is 0.05˜0.2%, water of hydration is 4˜8%. The product can be used for producing sulfuric acid and cement without baking dry.
摘要翻译：本发明涉及一种制备湿法磷酸的方法，包括：将含有磷酸盐岩浆和硫酸的原料分成两部分，然后分别将这两部分进料到两个反应器中。在第一反应器中，加入70-90wt。磷酸盐岩与硫酸与再生磷酸的比例为1：0.6〜0.8：1.0〜2.5的浆料和硫酸的总量的％。 10〜30％的反应溶液直接流入转化池，参与二水石膏的转化反应。因此磷酸浓度为33〜39wt。％。 P 5 <5的回收效率为99％以上。当将焦炭粉末作为助滤剂放入转化溶液中时，过滤效率可以提高10〜30％，在这样制造的半水石膏中，P 2 O 5 O 5 0.05〜0.2％，水合水质为4〜8％。该产品可用于生产硫酸和水泥，无需烘干。

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