专利号:US-2008051323-A1 优先权日:2004-08-21 标 题 :Chloroquine drug compositions and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2007060499-A1 优先权日:2005-09-15 标 题 :Chloroquine combination drugs and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-6800578-B2 优先权日:1999-01-29 标题:Process for producing anionic clay using boehmite which has been peptized with an acid 发明人:STAMIRES DENNIS; O'CONNOR PAUL; JONES WILLIAM; BRADY MICHAEL 权利人:AKZO NOBEL NV 摘要:This patent describes economical and environment-friendly processes for the synthesis of anionic clays. It involves reacting a slurry comprising boehmite, which has been peptized with acid with a divalent metal source followed by addition of source of base. The slurry is then hydrothermally aged. There is no necessity to wash or filter the product and it can be spray dried directly to form microspheres, or can be extruded to form shaped bodies. The product can be combined with other ingredients in the manufacture of catalysts, absorbents, pharmaceuticals, cosmetics, detergents, polymeric nanocomposites and other commodity products that contain anionic clays.
专利号:EP-0072318-A2 优先权日:1981-08-04 标 题 :Synthesis of human virus antigens by yeast
专利号:CA-1341642-C 优先权日:1981-08-04 标 题:Synthesis of hepatitis b virus surface antigen by yeast
专利号:US-7199128-B2 优先权日:2005-02-02 标题 :8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents 发明人:BRADBURY BARTON J; WILES JASON ALLAN; DESHPANDE MILIND; WANG QIUPING; HASHIMOTO AKIHIRO; LUCIEN EDLAINE 权利人:ACHILLION PHARMACEUTICALS INC 摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.
1: Harris C, Philpot CM. A comparative trial of chlorphenesin and pecilocin in a prison community. Br J Clin Pract. 1969 Nov;23(11):449-51. German. doi: 10.1016/j.bmc.2013.12.038. Epub 2013 Dec 25. Dutch. Japanese. Danish.
合成参考文献
摘要:Antibiotics: Origin, Nature, and Properties, Korzyoski, T., et al., eds., Washington, DC, American Soc. for Microbiology, 1978, 3(2004), 1978 参考文献:10.1007/s101560200022 摘要:Kumazawa J, Yagisawa M. The history of antibiotics: the Japanese story. J Infect Chemother. 2002 Jun;8(2):125–33. doi: 10.1007/s101560200022.