专利号:US-2021107859-A1 优先权日:2018-04-06 标题 :A process for the synthesis of carbon labeled organic compounds 发明人:AUDISIO DAVIDE; CANTAT THIBAULT; DESTRO GIANLUCA 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A process for the synthesis of a carbon labeled organic compound containing a carbon labeled carboxyl group is described. A method of using carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; a process for manufacturing labeled pharmaceuticals and agrochemicals comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; and a process for producing tracers comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure are also described.
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-8367841-B2 优先权日:2006-09-08 标 题 :Processes for the preparation of 1,2,4-oxadiazole benzoic acids 发明人:ALMSTEAD NEIL G; HWANG PETER SEONGWOO; PINES SEEMON; MOON YOUNG-CHOON; TAKASUGI JAMES J 权利人:PTC THERAPEUTICS INC; ALMSTEAD NEIL G; HWANG PETER SEONGWOO; PINES SEEMON; MOON YOUNG-CHOON; TAKASUGI JAMES J 摘要:Provided herein are processes for the preparation of compounds useful for the treatment, prevention or management of diseases associated with a nonsense mutation. More specifically, provided herein are processes for the synthesis of 1,2,4-oxadiazoles. In particular, provided herein are processes useful for the preparation of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid.
专利号:US-6355490-B1 优先权日:1996-09-13 标题:Attached tags for use in combinatorial chemistry synthesis 发明人:HOCHLOWSKI JILL EDIE; SOWIN THOMAS J; NORBECK DANIEL W; GRILLOT ANNE-LAURE MARIE; SWENSON ROLF E 摘要:The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.
专利号:US-2009215080-A1 优先权日:2005-10-13 标题:Methods for identification of inhibitors of enzyme activity 发明人:SINHA SUKANTO; CHILCOTE TAMIE JO 权利人:ACTIVESITE PHARMACEUTICALS 摘要:The invention discloses compositions and methods of synthesis to create novel ligands and drugs and identifying such compounds as inhibitors of enzyme targets for use in the treatment of clinical disorders, including cancer, infectious diseases, parasitic infestations, neurological disorders, reproductive disorders, inflammatory disorders, circulatory disorders, and metabolic disorders.
专利号:WO-2005113580-A1 优先权日:2004-05-21 标题 :Anticoronviral compounds and compositions, their pharmaceutical uses and materials for their synthesis 发明人:HOFFMAN ROBERT LOUIS; KANIA ROBERT STEVEN; NIEMAN JAMES ANDREW; PLANKEN SIMON PAUL; SMITH GEORGE JOSEPH III 权利人:PFIZER; HOFFMAN ROBERT LOUIS; KANIA ROBERT STEVEN; NIEMAN JAMES ANDREW; PLANKEN SIMON PAUL; SMITH GEORGE JOSEPH III 摘要:The invention relates to methods of inhibiting SARS-related coronavirus viral replication activity comprising contacting a SARS-related coronavirus protease with a therapeutically effective amount of a SARS 3C like protease inhibitor of formula (I), and compositions comprising the same.