CAS: 535-65-9; 4-Amino-N-(5-Tert-Butyl-1,3,4-Thiadiazol-2-yl)Benzenesulfonamide

上下游产品

N-(4-(N-(5-Tert-Butyl-1,3,4-Thiadiazol-2-yl)Sulfamoyl)Phenyl)Acetamide 432539-49-6

📜2-氨基-5-叔-丁基-1,3,4-噻二唑置于吡啶,盐酸体系中,用 水 作为反应溶剂,化学反应 1.5H,反应生成 4-氨基-N-(5-叔丁基-1,3,4-噻二唑-2-基)苯磺酰胺
参考文献:Development Of Sulfonamide Akt Ph Domain Inhibitors
标题:Development Of Sulfonamide Akt Ph Domain Inhibitors
摘要:Disruption Of The Phosphatidylinositol 3-Kinase/akt Signaling Pathway Can Lead To Apoptosis In Cancer Cells. Previously We Identified A Lead Sulfonamide That Selectively Bound To The Pleckstrin Homology (Ph) Domain Of Akt And Induced Apoptosis When Present At Low Micromolar Concentrations. To Examine The Effects Of Structural Modification,A Set Of Sulfonamides Related To The Lead Compound Was Designed,Synthesized,And Tested For Binding To The Expressed Ph Domain Of Akt Using A Surface Plasmon Resonance-Based Competitive Binding Assay. Cellular Activity Was Determined By Means Of An Assay For Pakt Production And A Cell Killing Assay Using Bxpc-3 Cells. The Most Active Compounds In The Set Are Lipophilic And Possess An Aliphatic Chain Of The Proper Length. Results Were Interpreted With The Aid Of Computational Modeling. This Paper Represents The First Structure-Activity Relationship (Sar) Study Of A Large Family Of Akt Ph Domain Inhibitors. Information Obtained Will Be Used In The Design Of The Next Generation Of Inhibitors Of Akt Ph Domain Function. (C) 2011 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2011.01.049

专利信息

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:EP-1551403-B1
优先权日:2002-10-10
标 题 :5-substituted 2h-pyrazone-3-carboxylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia
发明人：SEMPLE GRAEME; AVERBUJ CLAUDIA; SKINNER PHILIP; GHARBAOUI TAWFIK; SHIN YOUNG-JUN
权利人:ARENA PHARM INC
摘要:The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R₂ is H, halogen, C_1-12 alkyl or C_1-12 haloalkyl; and R₃ is C_3-6 cycloalkyl, C_1-12 alkyl, C_1-12 haloalkyl, C_3-6 cycloalkyl-C_1-4-alkylene, aryl-C_1-4-alkylene or heteroaryl-C_1-4-alkylene, wherein said aryl-C_1-4-alkylene and heteroaryl-C_1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.

专利号:US-2006122240-A1
优先权日:2002-11-05
标题 :Benzotriazoles and methods of prophylaxis or treatment of metabolic-related disorders thereof
发明人：SEMPLE GRAEME; SKINNER PHILIP J; CHERRIER MARTIN C; WEBB PETER; TAMURA SUSAN Y
权利人:ARENA PHARM INC
摘要:The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR referred to as hRUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.

专利号:US-2007032537-A1
优先权日:2003-06-13
标题:5-Substituted 2h-pyrazole-3-carboxylic acid derivatives as agonists for the acid receptor rup25 for the treatment of dyslipidemia and related diseases
发明人：SEMPLE GRAEME; GHARBAOUI TAWFIK; SHIN YOUNG-JUN; DECAIRE MARC; AVERBUJ CLAUDIA L; SKINNER PHILIP J
权利人:ARENA PHARM INC
摘要:The present invention relates to certain pyrazole carboxylic acid and ester derivatives, and pharmaceutically acceptable salts thereof, which exhibit useful pharmaceutical properties, for example as agonists for the RUP25 receptor. (I) Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like the substituents are defined in claim 1.

专利号:TW-201518323-A
优先权日:2013-07-25
标题 :Synthesis of biological conjugates of APELIN polypeptides