专利号:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-8546533-B2 优先权日:2008-08-29 标 题:Pipecolic linker and its use for chemistry on solid support 发明人:MARTINEZ JEAN; ZAJDEL PAWEL; PAWLOWSKI MACIEJ; SUBRA GILLES 权利人:MARTINEZ JEAN; ZAJDEL PAWEL; PAWLOWSKI MACIEJ; SUBRA GILLES; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER 1; UNIV JAGELLONE; UNIV MONTPELLIER II 摘要:The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.
专利号:US-2005009924-A1 优先权日:2003-07-08 标 题 :Synthesis and pharmaceuticals of novel bis-substituted anthraquinone derivatives 发明人:HUANG HSU-SHAN 摘要:This invention relates to novel anthraquinone compounds useful in the treatment of allergic, inflammatory conditions, antioxidant, tumor condition, stem cell application, tissue engineering, applied in treating age-associate tissue degeneration, reverse organ failure in chronic high-turnover disease and therapeutic compositions containing such compounds. The compounds of the present invention are 1,4-, 1,5- and 1,8-difunctionalized anthraquinones or analogs thereof. According to the practice of the invention, there are provided bis-symmetrical substituted anthraquinone compounds according to formula I: n n nwherein R1, R2, R3 and R4 present a straight, aminoalkylamino side chains or branched chain alkyl group having 1 to 6 carbons which may be substituted with one or more groups of R5, or R1, R2, R3 and R4 present phenyl or benzyl which may be substituted with one or two groups of R6; wherein R5 is selected from the group consisting of halogen, —RNH 2 , —RNH 2 R, —ROH, —NO 2 , —OCH 3 , —OCH 2 CH 3 , and —OCH 2 CH 2 CH 3 ; and wherein R6 is selected from the group consisting of a straight or branched chain alkyl group having 1 to 4 carbons, halogen, —RNH 2 , —RNH 2 R, —ROH, —NO 2 , —OCH 3 , —OCH 2 CH 3 , —OCH 2 CH 2 CH 3 , —CH 2 Br, —CH 2 Cl, —CH 2 OH, —C(CH 3 ) 3 , —(CH 2 ) 2 0H, —(CH 2 ) 3 OH, —(CH 2 ) 4 OH, —CH 2 NH 2 , —(CH 2 ) 2 NH 2 , —(CH 2 ) 3 NH 2 , —(CH 2 ) 4 NH 2 , —(CH 2 ) 5 NH 2 , —CH 2 N(CH 3 ) 2 , —(CH 2 ) 2 N(CH 3 ) 2 , —(CH 2 ) 2 NH(CH 2 ) 2 OH, —(CH 2 ) 3 NH(CH 2 ) 2 OH, —(CH 2 ) 2 NHCH 2 OH, —(CH 2 ) 3 NHCH 2 OH, —CH 2 CH(CH 3 ) 2 , —CHCl 2 , —CH(CH 3 )Cl, —(CH 2 ) 2 Cl, —(CH 2 ) 3 Cl, —(CH 2 ) 3 Br, —(CH 2 ) 4 Br, and —(CH 2 ) 4 Cl. n n Chart 1. Activation of hTERT promoter-driven SEAP expression by c-Myc. About 1×10 7 hTERT-BJ1 cells were transfected with 13.5 μg each of plasmid pSEAP or pPhTERT-SEAP and of plasmid pMT2T or pMT2T-cMyc by electroporation. After 24 h, viable cells were harvested, and reinoculated at a density of 3×10 5 /mL, and the SEAP activity after 24 h at 37 â–¡. The transfection efficiency of each experiment was determined by cotransfection with 1.5 μg of plasmid pCMVβ. The values were determined from three experiments. P<0.05 is presented by an asterisk.
专利号:US-5936128-A 优先权日:1993-11-19 标题:5,6-dihydropyrone derivatives as protease inhibitors and antiviral agents 发明人:ELLSWORTH EDMUND LEE; LUNNEY ELIZABETH; TAIT BRADLEY DEAN 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
专利号:US-10233182-B2 优先权日:2014-04-04 标题 :Substituted spirocyclic inhibitors of autotaxin 发明人:BABISS LEE; CLARK MATTHEW; KEEFE ANTHONY D; MULVIHILL MARK J; NI HAIHONG; RENZETTI LOUIS; RUEBSAM FRANK; WANG CE; XIE ZHIFENG; ZHANG YING 权利人:X RX INC 摘要:The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
专利号:US-6369246-B2 优先权日:1999-04-14 标题 :Synthesis and pharmaceuticals of novel 9-substituted-1, 5-dichloroanthracene analogs 发明人:HUANG HSU-SHAN; LEE KUNG-YUAN; SHI CHANG-HSIN; HSU HSIEN-CHIN 权利人:KEITH CHAN GLOBOASIA LLC DR 摘要:The invention relates to novel anthracene compounds useful in the treatment of allergic, inflammatory conditions, tumor conditions and therapeutic compositions containing such compounds. The compounds of the present invention are 9-acyloxy-substituted 1,5-dichloroanthracene or analogs thereof. According to the practice of the invention, there are provided 9-acyloxy substituted 1,5-dichloroanthracene compounds according to formula III:wherein R represents a straight or branched chain alkyl group having 1 to 6 carbons which may be substituted with one or more groups of R1, or R represents phenyl or benzyl which may be substituted with one or two groups of R2; wherein R1 is selected from the group consisting of halogen, -NO2, -OCH3, OCH2CH3, and -OCH2CH2CH3; and wherein R2 is selected from the group consisting of a straight or branched chain alkyl group having 1 to 4 carbons, halogen, -NO2, -OCH3, -OCH2CH3, and -OCH2CH2CH3.
摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 103. 摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 704. 摘要:Li, D.-D.; Wang, G.-W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 375. 摘要:Gigiena i Sanitariya. For English translation, see HYSAAV., 55(7)(93), 1990 摘要:Kwiecień, H. U., Science of Synthesis: Knowledge Updates, (2024) 3, 137.