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1. 发明申请

WO2006050053A3 COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：化合物及其使用方法
公开(公告)号：WO2006050053A3
公开(公告)日：2006-07-06
申请号：PCT/US2005038853
申请日：2005-10-27
申请人： NUADA LLC , BURNS JAMES F , CABANA LEONARD A , COLLUPY GLENN C , DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , MATHEW JESSYMOL , SCHOENEN FRANK J , VANVLIET DAVID N , MIDDLEMISS DAVID N
发明人： BURNS JAMES F , CABANA LEONARD A , COLLUPY GLENN C , DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , MATHEW JESSYMOL , SCHOENEN FRANK J , VANVLIET DAVID N , MIDDLEMISS DAVID N
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , C07D235/18 , C07D417/04
摘要： Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-a) in a subject in need thereof.
摘要翻译：描述了咪唑和苯并咪唑硼酸化合物，其类似物和药物制剂，以及其用于在有需要的受试者中抑制炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法。

2. 发明申请

WO2007134169A3 INDOLE, BENZIMIDAZOLE, AND BENZOLACTAM BORONIC ACID COMPOUNDS, ANALOGS THEREOF AND METHODS OF USE THEREOF 审中-公开
标题翻译：吲哚，苯并咪唑和苯并咪唑硼酸化合物，其模拟物及其使用方法
公开(公告)号：WO2007134169A3
公开(公告)日：2009-02-12
申请号：PCT/US2007068671
申请日：2007-05-10
申请人： NUADA LLC , DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , SCICINSKI JAN J , CABANA LEONARD A , MATHEW JESSYMOL , MIDDLEMISS DAVID N , COLLUPY GLENN C , SCHOENEN FRANK J , BURNS JAMES F , VANVLIET DAVID N
发明人： DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , SCICINSKI JAN J , CABANA LEONARD A , MATHEW JESSYMOL , MIDDLEMISS DAVID N , COLLUPY GLENN C , SCHOENEN FRANK J , BURNS JAMES F , VANVLIET DAVID N
IPC分类号： C07D235/06 , A61K31/4184 , A61K31/69 , A61P35/00 , C07D235/18 , C07D241/46 , C07D279/16 , C07D417/02 , C07F5/02
CPC分类号： C07D417/02 , C07D235/06 , C07D235/18 , C07D241/46 , C07D279/16 , C07F5/025
摘要： Benzimidazole, indole and benzolactam boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-a) in a subject in need thereof.
摘要翻译：还描述了苯并咪唑，吲哚和苯并内酰胺硼酸化合物，其类似物和药物制剂，以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法。

3. 发明申请

WO2007134169A9 INDOLE, BENZIMIDAZOLE, AND BENZOLACTAM BORONIC ACID COMPOUNDS, ANALOGS THEREOF AND METHODS OF USE THEREOF 审中-公开
标题翻译：吲哚，苯并咪唑和苯并咪唑硼酸化合物，其模拟物及其使用方法
公开(公告)号：WO2007134169A9
公开(公告)日：2008-07-24
申请号：PCT/US2007068671
申请日：2007-05-10
申请人： NUADA LLC , DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , SCICINSKI JAN J , CABANA LEONARD A , MATHEW JESSYMOL , MIDDLEMISS DAVID N , COLLUPY GLENN C , SCHOENEN FRANK J , BURNS JAMES F , VANVLIET DAVID N
发明人： DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , SCICINSKI JAN J , CABANA LEONARD A , MATHEW JESSYMOL , MIDDLEMISS DAVID N , COLLUPY GLENN C , SCHOENEN FRANK J , BURNS JAMES F , VANVLIET DAVID N
IPC分类号： C07D235/06 , A61K31/4184 , A61K31/69 , A61P35/00 , C07D235/18 , C07D417/02 , C07F5/02
CPC分类号： C07D417/02 , C07D235/06 , C07D235/18 , C07D241/46 , C07D279/16 , C07F5/025
摘要： Benzimidazole, indole and benzolactam boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-a) in a subject in need thereof.
摘要翻译：还描述了苯并咪唑，吲哚和苯并内酰胺硼酸化合物，其类似物和药物制剂，以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法。

4. 发明申请

WO2006050236A3 COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：化合物及其使用方法
公开(公告)号：WO2006050236A3
公开(公告)日：2009-04-16
申请号：PCT/US2005039204
申请日：2005-10-27
申请人： NUADA LLC , DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , MATHEW JESSYMOL , SCHOENEN FRANK J , SCICINSKI JAN J , MIDDLEMISS DAVID N
发明人： DIDSBURY JOHN R , DYAKONOV TATYANA , HAYDAR SIMON N , JONES MICHAEL L , LI FRANCINE F , MARKWORTH CHRISTOPHER J , MATHEW JESSYMOL , SCHOENEN FRANK J , SCICINSKI JAN J , MIDDLEMISS DAVID N
IPC分类号： C07F5/02
CPC分类号： C07D491/04 , C07D209/08 , C07F5/025
摘要： Indole boronic acid compounds, and analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-a) in a subject in need thereof.
摘要翻译：还描述了吲哚硼酸化合物及其类似物和药物制剂，以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法。

5. 发明申请

WO2006050054A3 COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：化合物及其使用方法
公开(公告)号：WO2006050054A3
公开(公告)日：2006-12-28
申请号：PCT/US2005038854
申请日：2005-10-27
申请人： NUADA LLC , DYAKONOV TATYANA , JONES MICHAEL L , MARKWORTH CHRISTOPHER J , MATHEW JESSYMOL , SCHOENEN FRANK J , VANVLIET DAVID N , MIDDLEMISS DAVID N
发明人： DYAKONOV TATYANA , JONES MICHAEL L , MARKWORTH CHRISTOPHER J , MATHEW JESSYMOL , SCHOENEN FRANK J , VANVLIET DAVID N , MIDDLEMISS DAVID N
IPC分类号： C07D241/36 , A61K31/498 , A61K31/538 , A61K31/5415 , C07D265/36 , C07D279/16
CPC分类号： C07F5/025
摘要： Benzolactam boronic acid compounds and pharmaceutical formulations are described along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-a) in a subject in need thereof.
摘要翻译：苯扎林内酯硼酸化合物和药物制剂以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法进行了描述。

6. 发明申请

WO2004043396A3 MODIFIED CARBAMATE-CONTAINING PRODRUGS AND METHODS OF SYNTHESIZING SAME 审中-公开
标题翻译：含有改性的氨基甲酸酯的前躯体及其合成方法
公开(公告)号：WO2004043396A3
公开(公告)日：2004-08-12
申请号：PCT/US0335995
申请日：2003-11-07
申请人： NOBEX CORP , EKWURIBE NNOCHIRI N , RIGGS-SAUTHIER JENNIFER , DYAKONOV TATYANA
发明人： EKWURIBE NNOCHIRI N , RIGGS-SAUTHIER JENNIFER , DYAKONOV TATYANA
IPC分类号： A61K31/16 , A61K31/325 , A61K31/66 , A61K47/48 , C07K7/04 , A61K37/24 , C07K37/43
CPC分类号： A61K31/325 , A61K47/54 , A61K47/58 , A61K47/60 , A61K47/61
摘要： Prodrugs having a hydrolyzable carbamate moiety, compositions including the prodrugs, methods of preparing the prodrugs and methods of treatment using the prodrugs are disclosed. The prodrug has the formula DC(X)XR, where D is a biologically active agent, X is O, S or NR , and R is a moiety that modifies various properties of the biologically active agent. The biologically active agent either includes a functional group such as an amide, thioamide, imide, thioimide, urea, thiourea, carbamate, thiocarbamate, sulfonamide, or sulfonimide group, or includes a hydroxy, amine, carboxylic acid or thiol group that is modified to include such a group. An NH group from the biologically active agent can be coupled to an activated form the C(X)XR moiety to form the prodrugs described herein. Relative to a conventional carbamate group, the presence of the additional carbonyl or sulfonyl group makes the carbamate group more susceptible to hydrolysis. The prodrugs are more stable in certain environments than the biologically active agent, and can permit the drugs to be administered orally, in those embodiments where the biologically active agent must otherwise be administered by injection or intraveneous administration.
摘要翻译：公开了具有可水解的氨基甲酸酯部分的前药，包括前药的组合物，制备前药的方法和使用前药的治疗方法。前药具有式DC（X）XR，其中D是生物活性剂，X是O，S或NR，并且R是改变生物活性剂的各种性质的部分。生物活性剂包括官能团如酰胺，硫代酰胺，酰亚胺，硫代酰亚胺，脲，硫脲，氨基甲酸酯，硫代氨基甲酸酯，磺酰胺或磺酰亚胺基团，或包括羟基，胺，羧酸或硫醇基，包括这样一个组。来自生物活性剂的NH基团可以与C（X）XR部分的活化形式偶联以形成本文所述的前药。相对于常规的氨基甲酸酯基团而言，额外的羰基或磺酰基团的存在使得氨基甲酸酯基团更易于水解。前药在某些环境下比生物活性剂更稳定，并且可以允许药物以口服方式施用，其中生物活性剂必须以其他方式通过注射或静脉内施用施用。

7. 发明申请

WO2006012395A2 PEPTIDASE INHIBITORS 审中-公开
标题翻译：肽抑制剂
公开(公告)号：WO2006012395A2
公开(公告)日：2006-02-02
申请号：PCT/US2005025837
申请日：2005-07-21
申请人： ROYALTY SUSAN MARIE , BURNS JAMES FORD , SCICINSKI JAN JOZEF , JAGDMANN JR GUNNAR ERIK , FOGLESONG ROBERT JAMES , GRIFFIN KELLEE RENEE , DYAKONOV TATYANA , MIDDLEMISS DAVID
发明人： ROYALTY SUSAN MARIE , BURNS JAMES FORD , SCICINSKI JAN JOZEF , JAGDMANN JR GUNNAR ERIK , FOGLESONG ROBERT JAMES , GRIFFIN KELLEE RENEE , DYAKONOV TATYANA , MIDDLEMISS DAVID
IPC分类号： A61K31/497 , C07D403/02
CPC分类号： C07D207/10 , C07D207/16 , C07D277/04 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR 3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R1 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.
摘要翻译：本发明涉及一系列具有式（I）的新化合物，其中：X为NR 3或O; n为1或2; A是双环碳环，R1和R1如本文所述。该化合物可用作DPP-IV抑制剂，例如治疗糖尿病。

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