专利号:US-6555686-B2 优先权日:2000-03-23 标题:Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 发明人:PARSONS RODNEY L; DOROW ROBERTA L; DAVULCU AKIN H; FORTUNAK JOSEPH M; HARRIS GREGORY D; KAUFFMAN GOSS S; NUGENT WILLIAM A; RADESCA LILIAN A 权利人:BRISTOL MYERS SQUIBB PHARMA 摘要:This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
专利号:US-8618311-B2 优先权日:2005-06-15 标题:Synthetic processes for the preparation of aminocyclohexyl ether compounds 发明人:JUNG GRACE; YEE JAMES GEE KEN; CHOU DOUG TA HUNG; PLOUVIER BERTRAND M C 权利人:JUNG GRACE; YEE JAMES GEE KEN; CHOU DOUG TA HUNG; PLOUVIER BERTRAND M C; CARDIOME PHARMA CORP 摘要:This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): n nor a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.
专利号:US-6960601-B2 优先权日:2001-09-24 标题 :Preparation and use of imidazole derivatives for treatment of obesity 发明人:SMITH ROGER A; O'CONNOR STEPHEN J; WIRTZ STEPHAN-NICHOLAS; WONG WAI C; CHOI SOONGYU; KLUENDER HAROLD C E; SU NING; WANG GAN; ACHEBE FURAHI; YING SHIHONG 权利人:BAYER PHARMACEUTICALS CORP 摘要:This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:US-10759899-B2 优先权日:2017-08-03 标题 :Recyclable polymers based on ring-fused gamma-butyrolactones 发明人:CHEN EUGENE Y; Zhu jian-bo 权利人:UNIV COLORADO STATE RES FOUND 摘要:The invention discloses a class of new polymers, trans-ring-fused poly(4-hydroxybutyrate)s (RF-P4HB) that exhibit a unique set of properties, including robust thermal stability and mechanical strength, quantitative recyclability to the building block monomers via thermolysis and/or chemical catalysis, and convenient production from the chemical ring-opening polymerization under ambient temperature and pressure. Another unique property is the formation of crystalline stereocomplexed polymers with high melting temperature upon mixing the two enantiomeric RF-P4HB chains via stereocomplexing co-crystallization. This invention also provides the corresponding ring-fused lactone monomer structures that enable the synthesis of the RF-P4HB polymers, through trans-fusing of rings to the parent γ-butyrolactone ring. Furthermore, a polymerization or copolymerization process for the synthesis of RF-P4HB polymers and copolymers is disclosed.
专利号:US-8129411-B2 优先权日:2005-12-30 标题:Organic compounds 发明人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI 权利人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI; NOVARTIS AG 摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. n The compounds have the formula I′ n nwherein R1, R2, T, R3 and R4 are as defined in the specification.
[参考文献]: Alexander L Perryman, Et Al. Fragment-Based Screen Against Hiv Protease. Chem Biol Drug Des. 2010 Mar;75(3):257-68.
合成参考文献
摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 816. 摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 164.