专利号:US-7026339-B2 优先权日:2003-11-07 标题 :Inhibitors of HCV NS5B polymerase 发明人:YANG FAN; ZHANG BO; WICNIENSKI NANCY ANNE; PFEFFERKORN JEFFREY ALLEN; GREENE MEREDITH L; CHEN KE; NUGENT RICHARD A; REDING MATTHEW TODD; KELLY ROBERT CHARLES; MITCHELL MARK A; FUNK LEE A; HEIER III RICHARD FREDERICK; ANDERSON REBECCA MERRY 权利人:YANG FAN; ZHANG BO; WICNIENSKI NANCY ANNE; PFEFFERKORN JEFFREY ALLEN; GREENE MEREDITH L; CHEN KE; NUGENT RICHARD A; REDING MATTHEW TODD; KELLY ROBERT CHARLES; MITCHELL MARK A; FUNK LEE A; HEIER III RICHARD FREDERICK; ANDERSON REBECCA MERRY 摘要:The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.
专利号:US-2012053350-A1 优先权日:2009-04-30 标题 :Preparation of alkyl esters of n-protected oxo-azacycloalkylcarboxylic acids 发明人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 权利人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 摘要:A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein P G1 is an amine protective group; k is 0, 1, or 2; and R U , R 1 , R 2 , and R 3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (R U ) 3 S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-12286405-B2 优先权日:2019-05-17 标题 :Scalable synthesis of dual-target inhibitor of cannabinoid-1 receptor and inducible nitric oxide synthase 发明人:ALIMARDANOV ASAF RAGIM; HUANG JUNFENG 权利人:US HEALTH 摘要:A process for the preparation of racemic and optically active (1E,NE)-N-(1-aminoethylidene)-3-(4-chlorophenyl)-4-phenyl-N′-((4-(trifluoromethyl)phenyl)sulfonyl)-4,5-dihydro-1H-pyrazole-1-carboximidamide in high enantiomerical purity is provided.
专利号:US-9604985-B2 优先权日:2013-06-10 标 题 :Process for the preparation of chiral tert-butyl 4-((1R,2S,5R)-6(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carb derivatives and (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide 发明人:MILLER STEVEN P; LIMANTO JOHN; ZHONG YONG-LI; YASUDA NOBUYOSHI; LIU ZHIJIAN 权利人:MERCK SHARP & DOHME 摘要:A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R 4 —SO 2 W (II-Su) in the presence of tertiary amine base, wherein P G1 and P G2 are amine protective groups; k, p and q are 0, 1, or 2, and W, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
专利号:US-2023192718-A1 优先权日:2018-03-30 标 题 :Bicyclic enone carboxylates as modulators of transporters and uses thereof 发明人:SANDANAYAKA VINCENT 权利人:NIROGY THERAPEUTICS INC 摘要:The invention generally relates to the field of monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate enone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.
摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 296. 摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 284. 摘要:Huy, P.; Czekelius, C., Science of Synthesis Knowledge Updates, (2019) 2, 162. 摘要:Kashemirov, B. A.; Błażewska, K.; Justyna, K.; Lyu, J.; McKenna, C. E., Science of Synthesis Knowledge Updates, (2021) 1, 414. 摘要:Zhang, M.; Su, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 127.