专利号:EP-0948511-B1 优先权日:1996-12-24 标 题:Chemical synthesis of nucleosides analogs and their incorporation into polynucleotides 发明人:KARPEISKY ALEXANDER; BEIGELMAN LEONID; MATULIC-ADAMIC JASENKA 权利人:SIRNA THERAPEUTICS INC 摘要:Novel nucleosides, process for chemical synthesis of nucleosides and incorporation of the nucleosides into polynucleotides are disclosed. Also described are polynucleotides, such as antisense, TFO and nucleic acid catalysts with one or more modifications, such as 2'-O-amino, L-nucleotides and the others.
专利号:US-6635767-B2 优先权日:2000-05-23 标 题 :Synthesis of heteroarylamine intermediate compounds 发明人:SONG JINHUA J; YEE NATHAN K; KAPADIA SURESH R 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
专利号:US-6822093-B2 优先权日:2000-05-23 标题 :Synthesis of heteroarylamine intermediate compounds 发明人:SONG JINHUA J; YEE NATHAN K 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
专利号:US-2006025421-A1 优先权日:2004-06-25 标 题:Pyridyl piperazines for the treatment of CNS disorders 发明人:BRODNEY MICHAEL A 权利人:PFIZER 摘要:This invention is directed to compounds of Formula I and to pharmaceutical compositions comprising the compound of Formula I. n n where the dashed line represents an optional double bond; and where n is 1 or 2, and Ar 1 , Ar 2 , . . . and Z are as defined in the specification. The invention is also directed to a method of treating a disorder or condition that can be treated by altering serotonin-mediated neurotransmission, such as migraine, headache, cluster headache, anxiety, depression, etc. This invention is also directed to intermediates useful in the synthesis of compounds of Formula I.
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-9695147-B2 优先权日:2013-07-25 标题 :Process for the preparation of perampanel 发明人:BUCHLOVIC MARIAN 权利人:TEVA PHARMACEUTICALS INT GMBH 摘要:The present invention provides intermediates useful for the synthesis of Perampanel and processes employing said intermediates for preparing Perampanel. The invention also provides processes for making the intermediates, crystalline forms of the intermediates and the use of the crystalline forms for preparing Perampanel.
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 198. 摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 219. 摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 202. 摘要:Scholz, U.; Dong, W.; Feng, J.; Shi, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 89. 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 1985. Acute oral toxicity and repellency of 933 chemicals to house and deer mice. Archives of Environmental Contamination and Toxicology 14:111-129. https://www.aphis.usda.gov/ws/nwrc/chem-effects-db/S_schafer851.pdf