专利号:US-2010022541-A1 优先权日:2006-09-25 标题:Chemical inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors 发明人:ESCAICH SONIA; DENIS ALEXIS; MOREAU FRANCOIS; GERUSZ VINCENT; DESROY NICOLAS 权利人:ESCAICH SONIA; DENIS ALEXIS; MOREAU FRANCOIS; GERUSZ VINCENT; DESROY NICOLAS 摘要:The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR 1 , C1-C10 alkyl-NR 1 R 1 , alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO 2 R 1 , NR 1 R 1 , NR 1 C(O)R 1 , C(O)NR 1 R 1 , NR 1 C(S)R 1 , C(S)NR 1 R 1 , SO 2 NR 1 R 1 , SO 2 R 1 , NR 1 SO 2 R 1 , NR 1 C(O)NR 1 R 1 , NR 1 C(O)OR 1 , NR 1 C(S)NR 1 R 1 , NR 1 C(S)OR 1 , R 1 Câ•?NOR 1 , C(O)R 1 , aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B 1 , B 2 , B 3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B 4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined aboe.
专利号:US-2006293307-A1 优先权日:2002-07-29 标题:Oxazolidinone derivatives as antimicrobials 发明人:MEHTA ANITA; RUDRA SONALI; RAJA RAO AJJARAPU VENKATA S; RATTAN ASHOK; YADAV AJAY S 权利人:MEHTA ANITA; RUDRA SONALI; RAJA RAO AJJARAPU VENKATA S; RATTAN ASHOK; YADAV AJAY S 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 such as multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
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:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial libraries
专利号:US-11584752-B2 优先权日:2020-09-08 标题 :Method for controlled release using mechanical force 发明人:ROBB MAXWELL J; HU XIAORAN; ZENG TIAN 权利人:CALIFORNIA INST OF TECHN 摘要:A general and modular mechanophore platform that efficiently releases a cargo molecule via a mechanically triggered cascade reaction is described, along with methods of synthesis and use thereof. The mechanophore platform comprises a stable Diels-Alder adduct mechanophore comprising a 2-furylcarbinol derivative as its diene component, wherein the 2-furylcarbinol derivative is, in turn, pre-loaded with a covalently attached cargo molecule, and wherein the Diels-Alder adduct mechanophore is embedded into a polymer chain or polymer network, such that the mechanophore platform undergoes the retro [4+2] cycloaddition reaction under mechanical force to reveal the unstable 2-furylcarbinol derivative, which, in turn, easily decomposes under mild conditions to release its molecule cargo.
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
参考标题:A Facile Microwave And Sncl2 Synthesis Of 2,3-Dihydroquinazolin-4(1H)-Ones 作者:Nicholas S. O'Brien,Adam Mccluskey 摘要:An Elegantly Simple, Facile, And Robust Approach To A Scaffold Of Biological Importance, 2,3-Dihydroquinazolin-4(1H)-Ones, Is Reported. A Catalytic 1 % Sncl2/microwave-Mediated Approach Afforded Access To Pure Material, Collected By Cooling And Filtration After 20-Min Microwave Irradiation At 120°C. A Total Of 41 Analogues Were Prepared In Isolated Yields Of 17-99 %. This Process Was Highly Tolerant
合成参考文献
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