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1. 发明申请

WO2005046590A2 METHODS FOR SYNTHESIZING QUINOLINONE COMPOUNDS 审中-公开
标题翻译：合成喹啉酮化合物的方法
公开(公告)号：WO2005046590A2
公开(公告)日：2005-05-26
申请号：PCT/US2004037051
申请日：2004-11-05
申请人： CHIRON CORP , 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： A61K31/4375 , A61K31/4709 , A61K31/496 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D487/08 , A61K
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.
摘要翻译：合成取代或未取代的4-氨基-3-苯并咪唑基喹啉酮化合物的方法包括使第一种具有式I的化合物与具有式II的第二化合物在合适的溶剂中在碱的钠盐或钾盐。第一化合物和第二化合物具有以下结构，其中变量具有本文所述的值。

2. 发明申请

WO2005046589A3 PHARMACEUTICALLY ACCEPTABLE SALTS OF QUINOLINONE COMPOUNDS HAVING IMPROVED PHARMACEUTICAL PROPERTIES 审中-公开
公开(公告)号：WO2005046589A3
公开(公告)日：2005-05-26
申请号：PCT/US2004/036941
申请日：2004-11-05
申请人： CHIRON CORPORATION , CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , MACHAJEWSKI, Timothy D. , RYCKMAN, David , SHANG, Xiao , ZHU, Shuguang , OKHAMAFE, Augustus, O. , TESCONI, Marc, S.
发明人： CAI, Shaopei , CHOU, Joyce , HARWOOD, Eric , MACHAJEWSKI, Timothy D. , RYCKMAN, David , SHANG, Xiao , ZHU, Shuguang , OKHAMAFE, Augustus, O. , TESCONI, Marc, S.
IPC分类号： C07D471/04
摘要： A lacate salt of a compound of Formula: (I) or a tautomer of the compound, wherein Formula (I) has the following structure and R 1 -R 9 and R 12 -R 14 are as defined herein.

3. 发明申请

WO2011143106A1 BI - FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS 审中-公开
标题翻译：双功能吡唑啉化合物
公开(公告)号：WO2011143106A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/035741
申请日：2011-05-09
申请人： GILEAD SCIENCES, INC. , BAKER, William, R. , CAI, Shaopei , KAPLAN, Joshua, Aaron , KIM, Musong , PHILLIPS, Gary , PURVIS, II., Lafe, J. , STASIAK, Marcin , STEVENS, Kirk, L. , VAN VELDHUIZEN, Josh
发明人： BAKER, William, R. , CAI, Shaopei , KAPLAN, Joshua, Aaron , KIM, Musong , PHILLIPS, Gary , PURVIS, II., Lafe, J. , STASIAK, Marcin , STEVENS, Kirk, L. , VAN VELDHUIZEN, Josh
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/08
CPC分类号： C07D471/04
摘要： invention provides compounds of the formula: wherein R 1 and R 2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.
摘要翻译：本发明提供下式的化合物：其中R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，并且所有其它变量如本文所定义，它们在肺部炎症或支气管收缩治疗中的用途以及包含和过程提供了相同的准备。

4. 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。

5. 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.

6. 发明申请

WO2011143105A1 BIFUNCTIONAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：双功能喹啉衍生物
公开(公告)号：WO2011143105A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/035738
申请日：2011-05-09
申请人： GILEAD SCIENCES, INC. , BAKER, William, R. , CAI, Shaopei , KAPLAN, Joshua, Aaron , KIM, Musong , LOYER-DREW, Jennifer, Alissa , PERREAULT, Stephane , PHILLIPS, Gary , PURVIS, Lafe, J., II , STASIAK, Marcin , STEVENS, Kirk, L. , VAN VELDHUIZEN, Josh
发明人： BAKER, William, R. , CAI, Shaopei , KAPLAN, Joshua, Aaron , KIM, Musong , LOYER-DREW, Jennifer, Alissa , PERREAULT, Stephane , PHILLIPS, Gary , PURVIS, Lafe, J., II , STASIAK, Marcin , STEVENS, Kirk, L. , VAN VELDHUIZEN, Josh
IPC分类号： C07D215/54 , C07D401/12 , C07D409/14 , C07D413/12 , A61K31/4706 , A61K31/4709 , A61P11/00
CPC分类号： C07D215/54 , C07D401/12 , C07D409/14 , C07D413/12
摘要： Provided are compounds of Formula (I): Wherein X is:(Formula (II)) or (Formula (III)) R 1 and R 2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.
摘要翻译：提供式（I）的化合物：其中X是：（式（II））或（式（III））R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，以及所有其它变量如本文所定义，以及它们在治疗肺部炎症或支气管收缩中的应用以及包含其制备方法的组合物。

7. 发明申请

WO2005047244A3 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：WO2005047244A3
公开(公告)日：2006-12-21
申请号：PCT/US2004036956
申请日：2004-11-05
申请人： CHIRON CORP , 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： A61K31/496 , A61K31/4375 , A61K31/4709 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D487/08
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。

8. 发明申请

WO2005046589A2 PHARMACEUTICALLY ACCEPTABLE SALTS OF QUINOLINONE COMPOUNDS HAVING IMPROVED PHARMACEUTICAL PROPERTIES 审中-公开
标题翻译：具有改进的药物性质的喹诺酮化合物的药学上可接受的盐
公开(公告)号：WO2005046589A2
公开(公告)日：2005-05-26
申请号：PCT/US2004036941
申请日：2004-11-05
申请人： CHIRON CORP , CAI SHAOPEI , CHOU JOYCE , HARWOOD ERIC , MACHAJEWSKI TIMOTHY D , RYCKMAN DAVID , SHANG XIAO , ZHU SHUGUANG
发明人： CAI SHAOPEI , CHOU JOYCE , HARWOOD ERIC , MACHAJEWSKI TIMOTHY D , RYCKMAN DAVID , SHANG XIAO , ZHU SHUGUANG
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/496 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D487/08 , A61K
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C51/412 , C07C59/08
摘要： A lacate salt of a compound of Formula: (I) or a tautomer of the compound, wherein Formula (I) has the following structure and R -R and R -R are as defined herein.
摘要翻译：式（I）化合物或该化合物的互变异构体的拉坦酸盐，其中式（I）具有以下结构，R 1 -R 9和R 12 -R 14为本文定义。

9. 发明授权

US6087358A Nitro-[2,1-b]imidazopyran compounds and antibacterial uses thereof 失效
标题翻译：硝基 - [2,1-b]咪唑并吡喃化合物及其抗菌用途
公开(公告)号：US6087358A
公开(公告)日：2000-07-11
申请号：US924559
申请日：1997-09-05
申请人： William R. Baker , Cai Shaopei , Eric L. Keeler
发明人： William R. Baker , Cai Shaopei , Eric L. Keeler
IPC分类号： C07D487/04 , C07D498/04 , A61K31/535 , C07D498/00
CPC分类号： C07D487/04
摘要： Methods, compounds and compositions are provided for inhibiting the growth of pathogenic microbes in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial, Clostridium, Cryptosporidium and Helicobacter infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NR.sub.2, where R.sub.2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR.sub.3 or SO.sub.2 R.sub.4 CONR.sub.4 R.sub.5, where R.sub.3, R.sub.4 and R.sub.5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alloxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected from oxygen, CH.sub.2, CO, CR.sub.4 R.sub.5 or NR.sub.4, where R.sub.4 and R.sub.5 are as defined above; provided that when n is 2 or 3, the compounds of formula II can be additionally substituted as follows: ##STR2## wherein R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyalkylaryl, alkoxyalkylheterocycle, alkylary2alkylaryl, alkylarylaryl, alkylcycloalkyl, alkoxyaryl, alkylheterocycle, and alkoxyheterocycle; and the pharmaceutically acceptable salts thereof.
摘要翻译：提供了使用式（II）的双环硝基咪唑化合物在体内抑制病原微生物体外生长和治疗病原菌感染如分枝杆菌，梭菌，隐孢子虫和幽门螺杆菌感染的方法，化合物和组合物：其中R1 卤素，低级烷基，卤代低级烷基，环烷基，杂环，取代的杂环和杂环烷基; X是氧，硫或NR 2，其中R2是氢，低级烷基，芳基，环烷基，杂环，取代的杂环，杂环烷基，COR3或SO2R4CONR4R5，其中R3，R4和R5独立地选自氢，低级烷基，芳基，烷基芳基，烷氧基烷基，烷氧基芳基，烷氧基烷氧基芳基，烷基杂环和烷氧基杂环; n为1,2或3; Y和Z独立地选自氧，CH 2，CO，CR 4 R 5或NR 4，其中R 4和R 5如上所定义; 条件是当n为2或3时，式II化合物可另外被如下取代：其中R 6，R 7，R 8和R 9独立地选自氢，低级烷基，芳基，烷基芳基，烷氧基烷基，烷氧基烷基芳基，烷氧基烷基杂环，烷基芳基烷基芳基，烷基环烷基，烷氧基芳基，烷基杂环和烷氧基杂环; 及其药学上可接受的盐。

10. 发明授权

US5668127A Nitroimidazole antibacterial compounds and methods of use thereof 失效
标题翻译：硝基咪唑抗菌化合物及其使用方法
公开(公告)号：US5668127A
公开(公告)日：1997-09-16
申请号：US496850
申请日：1995-06-26
申请人： William R. Baker , Cai Shaopei , Eric L. Keeler
发明人： William R. Baker , Cai Shaopei , Eric L. Keeler
IPC分类号： A61K31/535 , A61K31/55 , A61P31/00 , C07D487/04 , C07D498/04 , C07D265/12 , C07D267/12 , C07D267/22
CPC分类号： C07D487/04
摘要： Methods, compounds and compositions are provided for inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial and clostridium infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NK.sub.2, where R.sub.2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR.sub.3 or SO.sub.2 R.sub.4 CONR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected CH.sub.2, CO, CR.sub.4 R.sub.5 or NR.sub.4, where R.sub.4 and R.sub.5 are as defined above; provided that when n is 2 or 3, the compounds of formula II can be additionally substituted as follows: ##STR2## wherein R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis and Clostridium difficile.
摘要翻译：提供了使用式（II）的双环硝基咪唑化合物在体内抑制致病性分枝杆菌体外生长和治疗致病细菌感染如分枝杆菌和梭状芽胞杆菌感染的方法，化合物和组合物：其中R1是氢，卤素，低级烷基，卤代低级烷基，环烷基，杂环，取代杂环和杂环烷基; X是氧，硫或NK2，其中R2是氢，低级烷基，芳基，环烷基，杂环，取代的杂环，杂环烷基，COR3或SO2R4CONR4R5，其中R4和R5独立地选自氢，低级烷基，芳基，烷基芳基，烷氧基烷基，烷氧基芳基，烷氧基烷氧基芳基，烷基杂环和烷氧基杂环; n为1,2或3; Y和Z独立地选自CH 2，CO，CR 4 R 5或NR 4，其中R 4和R 5如上所定义; 条件是当n为2或3时，式II化合物可以另外被如下取代：其中R 6，R 7，R 8和R 9独立地选自氢，低级烷基，芳基（IIa）烷基芳基，烷氧基烷基，烷氧基芳基，烷氧基烷氧基芳基，烷基杂环和烷氧基杂环; 及其药学上可接受的盐。方法，化合物和组合物特别可用于抑制结核分枝杆菌和艰难梭菌的生长。

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