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1. 发明申请

WO2006012395A3 PEPTIDASE INHIBITORS 审中-公开
公开(公告)号：WO2006012395A3
公开(公告)日：2006-02-02
申请号：PCT/US2005/025837
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： C07D207/09 , C07D207/10 , A61K31/4025
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 R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.

2. 发明申请

WO0119406A2 AMPHIPHILIC PRODRUGS 审中-公开
标题翻译：大众产品
公开(公告)号：WO0119406A2
公开(公告)日：2001-03-22
申请号：PCT/US0024520
申请日：2000-09-07
申请人： NOBEX CORP , EKWURIBE NNOCHIRI N , DYAKONOV TATYANA A , PRICE CHRISTOPHER H
发明人： EKWURIBE NNOCHIRI N , DYAKONOV TATYANA A , PRICE CHRISTOPHER H
IPC分类号： A23L1/30 , A61K9/08 , A61K9/107 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/7048 , A61K47/48 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： A61K47/60
摘要： The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.
摘要翻译：本发明提供了包含与PEG-低聚物/聚合物缀合的治疗化合物的两亲前药，以及使用所述前体药物以使药物能够穿过血脑屏障进入中枢神经系统的口服药物递送和/或递送的方法。

3. 发明申请

WO2007134169A2 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：WO2007134169A2
公开(公告)日：2007-11-22
申请号：PCT/US2007/068671
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 , 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-α) 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

WO2006050236A2 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：WO2006050236A2
公开(公告)日：2006-05-11
申请号：PCT/US2005/039204
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： C07D207/02
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-α) 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

WO2006050054A2 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：WO2006050054A2
公开(公告)日：2006-05-11
申请号：PCT/US2005/038854
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.
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-α) in a subject in need thereof.
摘要翻译：描述了苯并内酰胺硼酸化合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。

6. 发明申请

WO2004043396A2 MODIFIED CARBAMATE-CONTAINING PRODRUGS AND METHODS OF SYNTHESIZING SAME 审中-公开
标题翻译：改性含碳酸酯的制剂及其合成方法
公开(公告)号：WO2004043396A2
公开(公告)日：2004-05-27
申请号：PCT/US2003/035995
申请日：2003-11-07
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri, N. , RIGGS-SAUTHIER, Jennifer , DYAKONOV, Tatyana
发明人： EKWURIBE, Nnochiri, N. , RIGGS-SAUTHIER, Jennifer , DYAKONOV, Tatyana
IPC分类号： A61K
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：公开了具有可水解氨基甲酸酯部分的前药，包含前药的组合物，制备前体药物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，R是修饰生物活性剂的各种性质的部分。生物活性剂还包括官能团，例如酰胺，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。相对于常规氨基甲酸酯基团，另外的羰基或磺酰基的存在使得氨基甲酸酯基团更易于水解。前药在某些环境中比生物活性剂更稳定，并且可以允许药物口服给药，在那些其中生物活性剂必须通过注射或静脉内给药施用的那些实施方案中。

7. 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。

8. 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。

9. 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。

10. 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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