专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:US-2010286211-A1 优先权日:2004-10-08 标题:Oxazolidinone derivatives as antimicrobials 发明人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 权利人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
专利号:US-2012172350-A1 优先权日:2009-09-11 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:EP-3103803-B1 优先权日:2008-10-27 标 题 :Intermediates for the synthesis of mtor kinase inhibitors
专利号:US-6008367-A 优先权日:1996-06-25 标题:Intermediate for synthesis of anticoagulant agents
专利号:AU-2018387110-A1 优先权日:2017-12-19 标题 :Synthesis of the 1 :1 :1 co-crystal of 1 -cyano-2-(4-cyclopropyl-benzyl)-4-(beta-D-glucopyranos-1 -yl)-benzene, L-proline and water
[参考文献]: Keith W Woods, Et Al. Synthesis And Sar Of Indazole-Pyridine Based Protein Kinase B/akt Inhibitors. Bioorg Med Chem. 2006 Oct 15;14(20):6832-46.
合成参考文献
摘要:Primer, D. N.; Molander, G. A., Science of Synthesis, (2019) , 296. 摘要:Primer, D. N.; Molander, G. A., Science of Synthesis, (2019) , 324. 摘要:Kelly, C. B.; Matsui, J. K.; Phelan, J. P.; Gutiérrez Bonet, Á.; Lang, S. B.; Molander, G. A., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 353. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).