专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-6080860-A 优先权日:1992-08-31 标 题:Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor 发明人:KARIMIAN KHASHAYAR; MURTHY KESHAVA; HALL DARREN 权利人:BRANTFORD CHEMICALSS INC 摘要:Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
专利号:US-9884067-B2 优先权日:2013-03-14 标 题:Androgen receptor down-regulating agents and uses thereof 发明人:NJAR VINCENT C O; GEDIYA LALJI K; PURUSHOTTAMACHAR PURANIK; GODBOLE ABHIJIT; KWEGYIR AFFUL ANDREW; VASAITIS TADAS 权利人:UNIV OF MARYLAND EASTERN SHORE; UNIV JEFFERSON; UNIV MARYLAND 摘要:The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.
专利号:US-4469701-A 优先权日:1983-06-23 标题 :Pyrrolid-3-en-2-ones and pharmaceutical methods of use thereof 发明人:DEBAUN JACK R; PALLOS FERENC M; MATSUMOTO KENT E; ROSS JOHN H 权利人:STAUFFER CHEMICAL CO 摘要:Novel compounds having the structural formula ##STR1## wherein R 1 and R 2 are independently selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, thioalkyl, thiohaloalkyl, alkoxy, cyano and nitro are provided. The compounds have various pharmacological effects, including cardiotropic, hypoglycemic, hypocholesterolemic and/or antiulcerative effects in mammals. Methods of achieving these various pharmacological effects in mammals by administering the compounds thereto are provided. Pharmaceutical compositions and formulations including the compounds are provided along with methods of synthesis of the novel compounds.
专利号:WO-9931506-A9 优先权日:1997-12-18 标题:Parallel solution phase synthesis of lactams 发明人:CWI CYNTHIA LYNN; SCOTT WILLIAM LEONARD 权利人:LILLY CO ELI; CWI CYNTHIA LYNN; SCOTT WILLIAM LEONARD 摘要:The present invention provides a parallel solution phase process for making combinatorial arrays of lactam derivatives which are useful for screening for therapeutically useful compounds.
专利号:US-4536334-A 优先权日:1979-06-28 标题 :Preparation of β-lactam derivatives 发明人:SUNAGAWA MAKOTO; MATSUMURA HARUKI; INOUE TAKAAKI; HIROHASHI TOSHIYUKI 权利人:SUMITOMO CHEMICAL CO 摘要:A process for preparing a β-lactam derivative having a hydrogen atom on the nitrogen atom of the β-lactam ring, which comprises reacting a β-lactam derivative having a mono- or diarylmethyl group on the nitrogen atom of the β-lactam ring with an acid or ceric ammonium nitrate to cleave the bond between the nitrogen atom and the mono- or diarylmethyl group; and novel β-lactam derivatives useful as intermediates for the synthesis of pharmaceutical agents.
[参考文献]: Chad D Iverson, Et Al. Diazonium Modification Of Porous Graphitic Carbon With Catechol And Amide Groups For Hydrophilic Interaction And Attenuated Reversed Phase Liquid Chromatography. J Chromatogr A. 2015 Nov 27:1422:186-193.
合成参考文献
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