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1. 发明申请

WO2006034417A2 TRIVALENT METAL MEDIATED HOMOGENEOUS LUMINESCENT PROXIMITY ASSAY 审中-公开
标题翻译：多金属介质均质光致亲和性测定
公开(公告)号：WO2006034417A2
公开(公告)日：2006-03-30
申请号：PCT/US2005/034026
申请日：2005-09-19
申请人： CHIRON CORPORATION , KUO, Richard, C. , DAWES, Timothy, D. , MACHAJEWSKI, Timothy, D.
发明人： KUO, Richard, C. , DAWES, Timothy, D. , MACHAJEWSKI, Timothy, D.
IPC分类号： C12Q1/48 , C12Q1/42 , C09K11/06 , C09K11/07 , G01N33/58 , G01N33/50
CPC分类号： G01N33/542 , C12Q1/42 , C12Q1/44 , C12Q1/485
摘要： An in vitro protein kinase assay technology that (1) exhibits a high assay signal to background ratio (S/B) and range (S-B); (2) is homogenous; (3) is non-radioactive; and (4) does not require a phospho-specific antibody involves complexing a trivalent metal ion (e.g. Ga 3+ , Fe 3+ , Al 3+ , In 3+ , Ru 3+ , Sc 3+ , Y 3+ ) to the surface of amplified luminescent proximity assay acceptor or donor beads, e.g., via a suitable linker such as nitrilotriacetic acid (NTA; also referred to as carboxymethyl-lysine), iminodiacetic acid (IDA), or an appropriately substituted N-containing heterocycle, for example a triazoheterocycle, for example a triazocyclononaneononane, such as 1-propylamino-4-acetato-1,4,7-triazacyclononane. A protein (or constituent part) or other kinase substrate is bound to the surface of the other of an amplified luminescent proximity assay acceptor or donor bead and, if phosphorylated, brought into proximity with the trivalent metal ion-complexed acceptor bead to generate a luminescent signal. Presence of a kinase inhibitor inhibits phosphorylation and therefore signal generation and, in this way, is detectable. As the invention described herein recognizes the presence or absence of phosphate groups on a protein, (or constituent part), or other biological macromolecule (e.g., mono, di, or trinucleotides, cyclic nucleotides or phosphate substituted inositols), it is broadly applicable to any phosphorlylation or dephosphorylation reaction enzymes and provides a highly robust and flexible assay format for protein kinases and other enzyme classes, including lipid kinases, phosphatases, phosphodiesterases and others.
摘要翻译：（1）表现出高测定信号与背景比（S / B）和范围（S-B）的体外蛋白激酶测定技术; （2）是均匀的; （3）是非放射性的; 和（4）不需要磷酸特异性抗体涉及使三价金属离子（例如，Ga 3+，Fe 3+，N 3+， SUP>，In 3+，R 3+，S 3+，Y 3+ +）与表面例如通过合适的接头，例如次氮基三乙酸（NTA;也称为羧甲基赖氨酸），亚氨基二乙酸（IDA）或适当取代的含N的杂环，例如三唑杂环，例如三氮杂环壬烷，例如1-丙基氨基-4-乙酰-1,4,7-三氮杂环壬烷。蛋白质（或组成部分）或其他激酶底物与扩增的发光亲和测定受体或供体小珠的另一个的表面结合，并且如果磷酸化，则与三价金属离子络合的受体珠接近以产生发光信号。激酶抑制剂的存在抑制磷酸化并因此产生信号，并且以这种方式可检测。如本文所述的发明认识到蛋白质（或组成部分）或其他生物大分子（例如单，二或三核苷酸，环状核苷酸或磷酸酯取代的肌醇）上磷酸基团的存在或不存在，广泛适用于任何磷酸化或去磷酸化反应酶，并为蛋白激酶和其他酶类提供了强大而灵活的测定形式，包括脂质激酶，磷酸酶，磷酸二酯酶等。

2. 发明申请

WO2004043389A2 METHODS OF TREATING CANCER AND RELATED METHODS 审中-公开
标题翻译：治疗癌症的方法和相关方法
公开(公告)号：WO2004043389A2
公开(公告)日：2004-05-27
申请号：PCT/US2003/035806
申请日：2003-11-12
申请人： CHIRON CORPORATION , MACHAJEWSKI, Timothy, D. , HANNAH, Alison , HARWOOD, Eric , HAROLDSEN, Peter , HEISE, Carla, C. , SAMARA, Emil , SHANG, Xiao , VORA, Jayesh , ZHU, Shuguang
发明人： MACHAJEWSKI, Timothy, D. , HANNAH, Alison , HARWOOD, Eric , HAROLDSEN, Peter , HEISE, Carla, C. , SAMARA, Emil , SHANG, Xiao , VORA, Jayesh , ZHU, Shuguang
IPC分类号： A61K
CPC分类号： C07D401/04 , A61K9/0019 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , A61K47/26 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of treating cancer using 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one are provided. In particular, the methods are effective for the treatment of solid tumors or leukemias, including prostate, colorectal, breast, multiple myeloma, pancreatic, small cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, or myelo-proliferative disease. Further provided are methods of measuring the amount of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one and determining a metabolic profile therefore.
摘要翻译：使用4-氨基-5-氟-3- [6-（4-甲基哌嗪-1-基）-1H-苯并咪唑-2-基]喹啉-2（1H） - 酮的治疗方法，提供一个。特别地，所述方法对于治疗实体瘤或白血病（包括前列腺癌，结肠直肠癌，乳腺癌，多发性骨髓瘤，胰腺癌，小细胞癌，急性骨髓性白血病，慢性骨髓性白血病或骨髓增生性疾病）是有效的。进一步提供了测量4-氨基-5-氟-3- [6-（4-甲基哌嗪-1-基）-1H-苯并咪唑-2-基]喹啉-2（1H） - 酮的量并测定因此代谢特征。

3. 发明申请

WO2006113498A2 2-AMINO-QUINAZOLIN-5-ONES 审中-公开
标题翻译： 2-氨基喹唑啉-5-酮
公开(公告)号：WO2006113498A2
公开(公告)日：2006-10-26
申请号：PCT/US2006/014194
申请日：2006-04-14
申请人： CHIRON CORPORATION , MACHAJEWSKI, Timothy, D. , GAO, Zhenhai , LEVINE, Barry, H. , ANTONIOS-MCCREA, William , BELLAMACINA, Cornelia, R. , COSTALES, Abran , DOUGHAN, Brandon, M. , FONG, Susan , HENDRICKSON, Thomas , LIN, Xiaodong , MCBRIDE, Christopher , MCKENNA, Maureen , RICO, Alice, C. , SHAFER, Cynthia, M. , WANG, X., Michael , ZHOU, Yasheen , XIA, Yi , MENDENHALL, Kris, G.
发明人： MACHAJEWSKI, Timothy, D. , GAO, Zhenhai , LEVINE, Barry, H. , ANTONIOS-MCCREA, William , BELLAMACINA, Cornelia, R. , COSTALES, Abran , DOUGHAN, Brandon, M. , FONG, Susan , HENDRICKSON, Thomas , LIN, Xiaodong , MCBRIDE, Christopher , MCKENNA, Maureen , RICO, Alice, C. , SHAFER, Cynthia, M. , WANG, X., Michael , ZHOU, Yasheen , XIA, Yi , MENDENHALL, Kris, G.
CPC分类号： C07D401/14 , C07D239/84 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D409/10 , C07D413/10 , C07D417/10 , C07D417/12 , C07D417/14
摘要： 2-Amino-quinazolin-5-one compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cell proliferative diseases.
摘要翻译： 2-氨基 - 喹唑啉-5-酮化合物，立体异构体，互变异构体，药用盐和前药; 包括药学上可接受的载体和一种或多种2-氨基 - 喹唑啉-5-酮化合物的组合物，单独或与至少一种另外的治疗剂组合。将2-氨基 - 喹唑啉-5-酮化合物单独使用或与至少一种另外的治疗剂组合使用的方法用于预防或治疗细胞增殖性疾病。

4. 发明申请

WO2004018419A2 BENZIMIDAZOLE QUINOLINONES AND USES THEREOF 审中-公开
标题翻译：苯并咪唑喹诺酮及其用途
公开(公告)号：WO2004018419A2
公开(公告)日：2004-03-04
申请号：PCT/US2003/025990
申请日：2003-08-19
申请人： CHIRON CORPORATION , BARSANTI, Paul, A. , BUSSIERE, Dirksen , HARRISON, Stephen, D. , HEISE, Carla, C. , JANSEN, Johanna, M. , JAZAN, Elisa , MACHAJEWSKI, Timothy, D. , McBRIDE, Christopher , McCREA, William, R. , NG, Simon , NI, Zhi-Jie , PECCHI, Sabina , PFISTER, Keith , RAMURTHY, Savithri , RENHOWE, Paul, A. , SHAFER, Cynthia, M. , SILVER, Joel, B. , WAGMAN, Allan , WEISMANN, Marion
发明人： BARSANTI, Paul, A. , BUSSIERE, Dirksen , HARRISON, Stephen, D. , HEISE, Carla, C. , JANSEN, Johanna, M. , JAZAN, Elisa , MACHAJEWSKI, Timothy, D. , McBRIDE, Christopher , McCREA, William, R. , NG, Simon , NI, Zhi-Jie , PECCHI, Sabina , PFISTER, Keith , RAMURTHY, Savithri , RENHOWE, Paul, A. , SHAFER, Cynthia, M. , SILVER, Joel, B. , WAGMAN, Allan , WEISMANN, Marion
IPC分类号： C07D
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或1B的化合物，其药学上可接受的盐，其互变异构体或其药学上可接受的盐互变异构体。具有结构I和IB的化合物具有以下结构并且具有本文所述的变量。此类化合物可用于制备用于抑制各种酶的药物和用于治疗由这些酶介导的病症的药物。

5. 发明申请

WO2005047244A2 INHIBITION OF FGFR3 AND TREATMENT OF MULTIPLE MYELOMA 审中-公开
标题翻译： FGFR3的抑制和多发性骨髓瘤的治疗
公开(公告)号：WO2005047244A2
公开(公告)日：2005-05-26
申请号：PCT/US2004/036956
申请日：2004-11-05
申请人： CHIRON CORPORATION , CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , HEISE, Carla, C. , MACHAJEWSKI, Timothy, D. , RYCKMAN, David , SHANG, Xiao , WIESMANN, Marion , ZHU, Shuguang
发明人： CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , HEISE, Carla, C. , MACHAJEWSKI, Timothy, D. , RYCKMAN, David , SHANG, Xiao , WIESMANN, Marion , ZHU, Shuguang
IPC分类号： C07D
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C51/412 , C07C59/08
摘要： Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.
摘要翻译：提供了抑制成纤维细胞生长因子受体3并治疗由成纤维细胞生长因子受体3介导的各种病症的方法，其包括向受试者施用结构I的化合物，其药学上可接受的盐，其互变异构体或其药学上可接受的盐互变异构体。具有结构I的化合物具有以下结构，并且具有本文所述的变量。这样的化合物可以用于制备用于抑制成纤维细胞生长因子受体3的药物，并且用于治疗由成纤维细胞生长因子受体3如多发性骨髓瘤介导的病症。

6. 发明申请

WO2005046590A3 METHODS FOR SYNTHESIZING QUINOLINONE COMPOUNDS 审中-公开
公开(公告)号：WO2005046590A3
公开(公告)日：2005-05-26
申请号：PCT/US2004/037051
申请日：2004-11-05
申请人： CHIRON CORPORATION , CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , RYCKMAN, David , SHANG, Xiao , ZHU, Shuguang , MACHAJEWSKI, Timothy, D.
发明人： CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , RYCKMAN, David , SHANG, Xiao , ZHU, Shuguang , MACHAJEWSKI, Timothy, D.
IPC分类号： C07D401/14
摘要： A method of synthesizing a substituted or unsubstituted 4-amino-3-benzimidazolyl quinolinone compound includes reacting a first compound having the formula I with a second compound having the formula II in a suitable solvent in the presence of a sodium or potassium salt of a base. The first compound and the second compound have the following structures where the variables have the values described herein.

7. 发明公开

EP1565187A2 METHODS OF TREATING CANCER AND RELATED METHODS 审中-公开
标题翻译：方法癌症UNDVERWANDTE手术的治疗
公开(公告)号：EP1565187A2
公开(公告)日：2005-08-24
申请号：EP03783281.3
申请日：2003-11-12
申请人： CHIRON CORPORATION
发明人： MACHAJEWSKI, Timothy, D. , HANNAH, Alison , HARWOOD, Eric , HAROLDSEN, Peter , HEISE, Carla, C. , SAMARA, Emil , SHANG, Xiao , VORA, Jayesh , ZHU, Shuguang
IPC分类号： A61K31/496 , C07D401/14
CPC分类号： C07D401/04 , A61K9/0019 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , A61K47/26 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of treating cancer using 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one are provided. In particular, the methods are effective for the treatment of solid tumors or leukemias, including prostate, colorectal, breast, multiple myeloma, pancreatic, small cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, or myelo-proliferative disease. Further provided are methods of measuring the amount of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one and determining a metabolic profile therefore.

8. 发明公开

EP1692085A2 INHIBITION OF FGFR3 AND TREATMENT OF MULTIPLE MYELOMA 审中-公开
标题翻译： FGFR3的抑制和多发性骨髓瘤的治疗
公开(公告)号：EP1692085A2
公开(公告)日：2006-08-23
申请号：EP04810419.4
申请日：2004-11-05
申请人： CHIRON CORPORATION
发明人： CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , HEISE, Carla, C. , MACHAJEWSKI, Timothy, D. , RYCKMAN, David , SHANG, Xiao , WIESMANN, Marion , ZHU, Shuguang
IPC分类号： C07C1/00
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C51/412 , C07C59/08
摘要： Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.

9. 发明公开

EP1682529A2 METHODS FOR SYNTHESIZING QUINOLINONE COMPOUNDS 审中-公开
标题翻译： METHOD FOR合成喹啉酮化合物的
公开(公告)号：EP1682529A2
公开(公告)日：2006-07-26
申请号：EP04810468.1
申请日：2004-11-05
申请人： CHIRON CORPORATION
发明人： CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , RYCKMAN, David , SHANG, Xiao , ZHU, Shuguang , MACHAJEWSKI, Timothy, D. , OKHAMAFE, Augustus, O.
IPC分类号： C07D401/14
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C51/412 , C07C59/08
摘要： A method of synthesizing a substituted or unsubstituted 4-amino-3-benzimidazolyl quinolinone compound includes reacting a first compound having the formula I with a second compound having the formula II in a suitable solvent in the presence of a sodium or potassium salt of a base. The first compound and the second compound have the following structures where the variables have the values described herein.

10. 发明公开

EP1539754A2 BENZIMIDAZOLE QUINOLINONES AND USES THEREOF 审中-公开
标题翻译：苯并咪唑喹诺酮及其用途
公开(公告)号：EP1539754A2
公开(公告)日：2005-06-15
申请号：EP03781286.4
申请日：2003-08-19
申请人： Chiron Corporation
发明人： BARSANTI, Paul, A. , BUSSIERE, Dirksen , HARRISON, Stephen, D. , HEISE, Carla, C. , JANSEN, Johanna, M. , JAZAN, Elisa , MACHAJEWSKI, Timothy, D. , McBRIDE, Christopher , McCREA, William, R. , NG, Simon , NI, Zhi-Jie , PECCHI, Sabina , PFISTER, Keith , RAMURTHY, Savithri , RENHOWE, Paul, A. , SHAFER, Cynthia, M. , SILVER, Joel, B. , WAGMAN, Allan , WIESMANN, Marion
IPC分类号： C07D471/04 , A61K31/435 , A61P35/00
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或1B的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。具有结构I和IB的化合物具有以下结构并且具有本文所述的变量。此类化合物可用于制备用于抑制各种酶的药物和用于治疗由这些酶介导的病症的药物。

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