CAS: 16790-49-1; Butazolamide

相似化合物

78851-85-1 14949-00-9 1623789-42-3

上下游产品

5-氨基-1,3,4-噻二唑-2-磺酰胺 5-Amino-1, 3, 4-Thiadiazole-2-Sulfonamide 14949-00-9

📜丁酸酐,5-氨基-1,3,4-噻二唑-2-磺酰胺 以 乙腈 用作溶剂,以81.5%的收率获得布他唑胺
参考文献:肿瘤相关碳酸酐酶ix的纳摩尔抑制作用的结构基础:乙酰唑胺骨架的亲脂性抑制剂的x射线晶体学和抑制研究
标题:肿瘤相关碳酸酐酶ix的纳摩尔抑制作用的结构基础:乙酰唑胺骨架的亲脂性抑制剂的x射线晶体学和抑制研究
摘要:这项研究提供了一系列具有乙酰唑酰胺骨架的亲脂性碳酸酐酶(ca)抑制剂的结构-活性关系研究.测试了抑制剂对肿瘤表达的ca同工酶ix(ca Ix),胞质ca I,Ca Ii和膜结合ca Iv的作用.该研究确定了几种针对ca Ix的低纳摩尔强效抑制剂,亲脂性跨越两个对数单位.非常有效的泛抑制剂与抗ca Ix纳摩尔效力和亚纳摩尔效力针对ca Ii和iv Ca,并用抗大小的ca我一个顺序比母体乙酰唑胺更好效力1在这项研究中,还鉴定出了与对膜结合的ca Iv具有选择性的化合物.全面的x射线晶体学研究(12个晶体结构)涉及ca Ii和可溶ca Ix模拟物(ca Ix-Mimic),揭示了这种特殊抑制曲线的结构基础,并为进一步开发更有效和更广泛的应用奠定了基础.肿瘤表达的ca Ix的选择性抑制剂.
Doi:10.1021/acs.Jmedchem.0C01390

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

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:WO-0034259-A1
优先权日:1998-12-04
标题 :Biologically active 2-r-5-amino-1,3,4-thiadiazole derivatives
发明人：ASHKINAZI RIMMA ILIINICHNA; KRUTIKOV VIKTOR IOSIFOVICH
权利人:ASHKINAZI RIMMA ILIINICHNA; KRUTIKOV VIKTOR IOSIFOVICH
摘要:The present invention pertains to the field of medicine, more precisely to that of pharmacology, and essentially relates to biologically active synthetic diazoles that consist of 2-R-5-amino-1,3,4-thiadiazole derivatives. These substances are mainly intended for use in medical practice for treating chlamydiae-mediated viral diseases as well as diseases resulting in immunodeficiency, including malignant tumours. The purpose of the present invention is to create new chemical compounds which have a high antiviral and an anti-microbial (anti-chlamydia) activity, which stimulate the production of endogenous interferons in the organism and which also have anti-aggregating, analgesic and psycho-depressive actions. This invention involves synthesising a new group of substances that consist of 2-R-5-amino-1,3,4-thiadiazole derivatives of general formula (1) where R1 is selected from the group comprising alkyl, aryl and -CH2-CH2C(0)NH-N=CH-Z, provided that Z is aryl or piperonyl, while R2 is selected from the group comprising H and (a), provided that Y is aryl or heteroaryl. This invention further relates to general methods for producing these substances, to 4 examples of the synthesis of said substances, to the identification results of each of the 42 synthesised substances as well as to data concerning the experimental verification of the substance biological activity relative to known preparations used for the same purposes.

专利号:KR-101513003-B1
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy compositions and applications

专利号:US-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:AU-2007308022-A2
优先权日:2006-10-05
标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications