专利号:US-8193180-B2 优先权日:2007-01-24 标 题 :N-amino tetrahydrothiazine derivatives, method of manufacture and use 发明人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE 权利人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE; WOMEN & INFANTS HOSPITAL 摘要:This invention comprises the innovative synthesis of N-amino tetrahydrothiazine free bases and their salts. This invention further comprises the use of the derivatives and their therapeutic application as anticancer agents. Further this invention comprises their manufacture and use.
专利号:US-9382288-B2 优先权日:2010-10-06 标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action 发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO 权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG 摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
专利号:WO-2012149093-A1 优先权日:2011-04-26 标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof 发明人:LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
专利号:WO-2009026858-A1 优先权日:2007-08-28 标题 :Derivatives of acridinone as anti-parasitic, anti-fungal and anti-viral agents 发明人:PELLON CONDOM ROLANDO F; DOCAMPO PALACIOS MAITE L; PARDO ANDREU GILBERTO L; FERNANDEZ-CALIENES VALDES AYME; MENDIOLA MARTINEZ BARBARA JUDITH; ROJAS RIVERO LAZARA; D ACCORSO HAICCK NORMA BEATRIZ; FASCIO SILVA MIRTA LILIANA; DAMONTE LOTITO ELSA BEATRIZ; GARCIA CATTEBEKE CYBELE CARINA; SEPULVEDA SUCHECKI CLAUDIA SOLEDAD; MAZZUCCO GAVIEIRO MARIA BELEN; TALARICO SALINAS LAURA BEATRIZ; MAES LOUIS 权利人:CT DE QUIMICA FARMACEUTICA; PELLON CONDOM ROLANDO F; DOCAMPO PALACIOS MAITE L; PARDO ANDREU GILBERTO L; FERNANDEZ-CALIENES VALDES AYME; MENDIOLA MARTINEZ BARBARA JUDITH; ROJAS RIVERO LAZARA; D ACCORSO HAICCK NORMA BEATRIZ; FASCIO SILVA MIRTA LILIANA; DAMONTE LOTITO ELSA BEATRIZ; GARCIA CATTEBEKE CYBELE CARINA; SEPULVEDA SUCHECKI CLAUDIA SOLEDAD; MAZZUCCO GAVIEIRO MARIA BELEN; TALARICO SALINAS LAURA BEATRIZ; MAES LOUIS 摘要:The invention relates to the synthesis and evaluation of novel organic products as anti-parasitic, anti-fungal and anti-viral agents. More specifically, the invention relates to novel derivatives of 10-alyl- (I), 10-(3methyl-2-butenyl)- (II) and 10-(1,2propanodienyl)-9(10H)-acridinone (III) and a novel family of acridinones, 10-{[3-(6-hydroxy-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-il)-4,5-dihydro-5-isoxazolyl] methyl}-9(10H) acridinone (IV) having the following formulas: wherein positions 1, 2, 3, 4, 5, 6, 7 and 8 of the acridinone ring are hydrogen atoms or halogens, groups consisting of hydroxyl, amino, nitro, alkyl with between 1 and 5 carbon atoms, trichloromethyl, trifluoromethyl, alkoxyl with between 1 and 6 carbon atoms (aryloxy substituted), aryl and alkylamino with between 1 and 6 carbon atoms (mono- and di-substituted), aryl and alkylamide with between 1 and 4 atoms of carbon, cyano, carboxyl, formyl, alkyl and arylsulfonic, mercapto substituted with alkylic chains having up to 5 carbon atoms, and sulfoxide aryl. Said derivatives have an activity against Plasmodium falciparum, Trypanosoma brucei and Trypanosoma cruzi protozoans, as well as Microsporum canis and strains of the Junin virus and Dengue.
专利号:US-6452050-B1 优先权日:1997-04-16 标 题:Synthesis and use of α-ketoamide derivatives and arrays 发明人:BALDINO CARMEN M; COFFEN DAVID L; CHIPMAN STEWART D; CHENG HONG 权利人:ARQULE INC 摘要:The invention is based on new methods for making and using compounds and arrays of novel alpha-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 alpha-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.
专利号:WO-2012149097-A2 优先权日:2011-04-26 标 题 :Guanidylimidazole and guanidylimidazoline derivatives as antimalarial agents, synthesis of and methods of use thereof
1: Singh RK, Dorf L, DeMartino A, Illenye S, Koto K, Currier EA, Ashikaga T, Kim KK, Brard L, Sholler GL. Oral RKS262 reduces tumor burden in a neuroblastoma xenograft animal model and mediates cytotoxicity through SAPK/JNK and ROS activation in vitro. Cancer Biol Ther. 2011 Jun 15;11(12):1036-45. Epub 2011 Jun 15. doi: 10.3892/ijo.2011.971. Epub 2011 Mar 10. doi: 10.1097/MPH.0b013e3181f47061. doi: 10.1007/s10637-009-9335-4. Epub 2009 Oct 29. doi: 10.1097/MPH.0b013e3181984d91.
合成参考文献
参考文献:10.1515/znc-2005-9-1009 摘要:Rubio J, Calderón JS, Flores A, Castroa C, Céspedes CL. Trypanocidal activity of oleoresin and terpenoids isolated from Pinus oocarpa. Z Naturforsch C J Biosci. 2005 Sep;60(9-10):711–6. doi: 10.1515/znc-2005-9-1009. 参考文献:/s0034-98872011000200016 摘要:Apt W, Zulantay I. [Update on the treatment of Chagas' disease]. Rev Med Chil. 2011 Feb;139(2):247–57. doi: /s0034-98872011000200016.