专利号:US-5139940-A 优先权日:1989-10-26 标题 :Activation compounds and methods of synthesis of activation compounds 发明人:ISAACS STEPHEN T; CIMINO GEORGE D; METCHETTE KENNETH C; TESSMAN JOHN W 权利人:ISAACS STEPHEN T; CIMINO GOERGE D; METCHETTE KENNETH C; TESSMAN JOHN W 摘要:The invention is directed to isopsoralen compound compositions that contain a variety of substitutions which yet permit their binding to nucleic acid polymers. Reaction conditions that activate these bound isopsoralens results in covalent crosslinking to the nucleic acid polymers. The resultant complex is inhibited from being a template for the template-directed enzymatic synthesis of a complementary nucleic acid polymer. Beside the isopsoralens compositions, the invention includes their synthesis, the nucleic acid complex production and detection, and the above inhibitory method of use of the isopsoralens.
专利号:US-8158817-B2 优先权日:2003-12-24 标 题 :Synthesis of acylureas and composition comprising acylureas 发明人:BERNARD JEAN-MARIE; REVELANT DENIS; AMOUYAL CEDRIC 权利人:BERNARD JEAN-MARIE; REVELANT DENIS; AMOUYAL CEDRIC; PERSTORP FRANCE 摘要:The invention relates to a process for the synthesis of a polyisocyanate composition comprising acylureas. According to the invention, a starting composition comprising a compound having at least two isocyanate functional groups is subjected to a reaction with at least two acid functional groups, with at least one of the acid functional groups having a pKa value of less than or equal to 3, and at least one of the acid functional groups having a pKa value of more than 3 and less than or equal to 6, at a temperature at least equal to 50 ° C., wherein the acid functional group having a pKa value of less than or equal to 3 and the acid functional group having a pKa value of more than 3 and less than or equal to 6 are present on two different acids or on the same acid.
专利号:US-7935837-B2 优先权日:2008-04-30 标 题:Process for synthesis of androstane 17-β carbothioic acid and relative compounds thereof 发明人:HSU NAI-HSUAN; PANG CHU-YI; WU CHIEN-JEN; HUANG CHI-JEN; HSU CHIA-JUNG; LEE PEIMIN 权利人:CORUM INC 摘要:A process for synthesis of androstane 17-β carbothioic acid is provided. The process includes mixing an androstane 17-β carboxylic acid and a coupling reagent, and adding an alkanethioic acid to form an androstane 17-β carbothioic acid, wherein the androstane 17-β carbothioic acid has the formula (I): n n n n n n n n n n n n wherein R 1 represents hydrogen or haloalkyl groups, R 2 represents C 1-8 linear alkyl groups, C 1-8 branched alkyl groups, C 1-6 unsaturated acyclic groups or aromatic groups, R 3 represents hydrogen or hydroxyl, R 4 represents hydrogen, bromine, chlorine or fluorine and R 5 represents hydrogen, bromine, chlorine or fluorine. The process is a one-pot reaction.
专利号:US-5597931-A 优先权日:1992-03-30 标 题:Total synthesis of taxol and analogues thereof 发明人:DANISHEFSKY SAMUEL J; MASTERS JOHN; YOUNG WENDY; LINK J THOMAS; ISAACS RICHARD; SNYDER LAWRENCE B 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.
专利号:US-5488116-A 优先权日:1992-03-30 标 题:Total synthesis of taxol and analogues thereof 发明人:DANISHEFSKY SAMUEL J; BORNMANN WILLIAM G; QUENEAU YVES; MAGEE THOMAS V; KROL WALTER J; MASTERS JOHN J; JUNG DAVID K 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.
专利号:US-5527924-A 优先权日:1992-03-30 标题 :Total synthesis of taxol 发明人:DANISHEFSKY SAMUEL J; BORNMANN WILLIAM G; QUENEAU YVES; MAGEE THOMAS V; KROL WALTER J 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides two basic routes for the total synthesis of taxol having the structure: The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogs to taxol. Both the intermediates and analogs to taxol may prove to be valuable anticancer agents.
[参考文献]: A Del Roso, Et Al. Exploring The Mechanisms Of In Vivo Regulation Of Liver Protein Breakdown In The Rat By The Use Of The New Antilipolytic-Agent Model. Acta Biol Hung. 1991;42(1-3):87-99. [参考文献]: C Redekopp, Et Al. An In Vivo Model For Testing Somatostatin Suppression Of Growth Hormone Release In Sheep. J Endocrinol Invest. 1980 Jul-Sep;3(3):237-41. [参考文献]: C Redekopp, Et Al. Suppression And Stimulation Of Growth Hormone Release In Sheep By Somatostatin Analogs. J Endocrinol Invest. 1984 Aug;7(4):277-81. [参考文献]: J M Orza, Et Al. Vibrational Spectra Of 3,5-Dimethylpyrazole And Deuterated Derivatives. Spectrochim Acta A Mol Biomol Spectrosc. 2000 Jul;56A(8):1469-98. [参考文献]: Sara Straniero, Et Al. Stimulation Of Autophagy By Antilipolytic Drugs May Rescue Rodents From Age-Associated Hypercholesterolemia. Rejuvenation Res. 2009 Apr;12(2):77-84.
合成参考文献
参考文献:10.1107/s1600536811010567 摘要:Crawford D, Hofer AK, Edler KL, Ferrence GM. Bis(3,5-dimethyl-1H-pyrazole-κN2)silver(I) hexafluoridoantimonate. Acta Crystallogr E Struct Rep Online. 2011 Mar 26;67(4):m496. doi: 10.1107/s1600536811010567. 参考文献:10.1107/s1600536811015169 摘要:Wang Y, Chang G, Liu B. Aquabis(3,5-dimethyl-1H-pyrazole-κN2)(oxydiacetato-κ3O,O′,O′′)copper(II) dihydrate. Acta Crystallogr E Struct Rep Online. 2011 May 07;67(6):m682. doi: 10.1107/s1600536811015169. 参考文献:10.1107/s1600536811016461 摘要:Davydenko YM, Fritsky IO, Pavlenko VO, Meyer F, Dechert S. Chloridotris(3,5-dimethyl-1H-pyrazole-κN2)(formato-κO)copper(II)–dichloridobis(3,5-dimethyl-1H-pyrazole-κN2)copper(II) (2/1). Acta Crystallogr E Struct Rep Online. 2011 May 07;67(6):m732–3. doi: 10.1107/s1600536811016461.