专利号:US-2006069260-A1 优先权日:2004-09-28 标 题:Preparation of N-aryl pyridones 发明人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 权利人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 摘要:A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. n nThese compounds are useful as intermediates for the synthesis of clinical candidates.
专利号:US-7884125-B2 优先权日:2008-04-30 标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues 发明人:STEVENS CHRISTIAN; HEUGEBAERT THOMAS 权利人:UNIV GENT 摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
专利号:US-8853228-B2 优先权日:2007-06-04 标 题:Heterocyclic analogs of propargyl-linked inhibitors of dihydrofolate reductase 发明人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE 权利人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE; UNIV CONNECTICUT 摘要:The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
专利号:US-8426432-B2 优先权日:2007-06-04 标 题 :Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties 发明人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO 权利人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO; UNIV CONNECTICUT 摘要:The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
专利号:US-2009275616-A1 优先权日:2008-04-30 标 题 :Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues
专利号:US-7166619-B2 优先权日:2002-08-14 标题 :Prenylation inhibitors and methods of their synthesis and use 发明人:LI FRANCINE FEIRONG; REHDER KENNETH S; CAMPBELL MICHAEL GORDON; VISCARDI CELESTE PATRICE; STRACHAN JON-PAUL; GUO ZHENGMING 权利人:PPD DISCOVERY INC 摘要:The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.
参考文献:10.1007/bf01518078 参考文献:10.1007/bf01525493 参考文献:10.1007/bf02505594 摘要:Führer U, Deißler A, Schreitmüller J, Ballschmiter K. Analysis of halogenated methoxybenzenes and hexachlorobenzene (HCB) in the picogram m−3 range in marine air. Chromatographia. 1997 Jan;45(1):414–27. doi: 10.1007/bf02505594. 参考文献:10.1007/s00897000353a|10.1007/s00897990353a 摘要:Andersh B. Molecular Modeling and Nuclear Overhauser Enhancement Spectroscopy (NOESY): Tools for Studying the Regioselective Bromination of 3-Bromoanisole. The Chemical Educator. 2000 Feb;5(1):20–3. doi: 10.1007/s00897990353a.