专利号:US-8063062-B2 优先权日:2006-12-20 标 题 :Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL 权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL; SOLVAY PHARM BV 摘要:Embodiments of this invention relate to compounds having a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition is a compound of formula (1) n nwherein the symbols have the meanings given in the specification.
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.
专利号:ES-2794012-T3 优先权日:2008-10-27 标题 :Intermediaries for the synthesis of mTOR kinase inhibitors
专利号:KR-20040089082-A 优先权日:2001-11-23 标 题 :Improved Synthesis of Polyanhydrides
专利号:US-9550795-B2 优先权日:2011-08-31 标 题:Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS 权利人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS; 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.
专利号:WO-2012172449-A1 优先权日:2011-06-13 标题:Lactams as beta secretase inhibitors 发明人:BRODNEY MICHAEL AARON 权利人:PFIZER; BRODNEY MICHAEL AARON 摘要:Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compound of formula I is useful as beta secretase inhibitor for use in the treatment of Alzheimer's and other neurodegenerative and/or neurological disorders.
1: Gilhus NE, Andersen H, Andersen LK, Boldingh M, Laakso S, Leopoldsdottir MO, Madsen S, Piehl F, Popperud TH, Punga AR, Schirakow L, Vissing J. Generalized myasthenia gravis with acetylcholine receptor antibodies: A guidance for treatment. Eur J Neurol. 2024 Feb 6:e16229. doi: 10.1111/ene.16229. Epub ahead of print. 11(3):409-417. doi: 10.5599/admet.2023. 3: Zhang Q, Lv J, Xia J, Wang L, Qu G, Yang Y, Yang Y, Liu S. Rapid detection of carbamate nerve agent analogues using dually functionalized gold nanoclusters. Anal Bioanal Chem. 2023 Jul;415(16):3275-3284. doi: 10.1007/s00216-023-04707-6. Epub 2023 Jun 2. 17(4):e0267471. doi: 10.1371/journal.pone.0267471.
合成参考文献
摘要:Journal of Pharmacology and Experimental Therapeutics., 115(185), 1955 [] 摘要:Drugs in Japan, 6(132), 1982 摘要:Schafer, E.W. 1972. The acute oral toxicity of 369 pesticidal, pharmaceutical and other chemicals to wild birds. Toxicology and Applied Pharmacology. 21:315-330. 摘要:Schafer, E. W., Jr., W. A. Bowles Jr., and J. Hurlbut. 1983. The acute oral toxicity and repellency and hazard potential of 998 chemicals to one or more species of wild and domestic birds. Archives of Environmental Contamination and Toxicology 12:355-382. 摘要:Schafer, E.W. Jr. and D.J. Cummings. 1972. An evaluation of 148 compounds as avian immobilizing agents. U.S. Fish and Wildlife Service, Special Scientific Report-Wildlife No.150. 30pp. https://www.aphis.usda.gov/ws/nwrc/chem-effects-db/E_SchaferCunningham72.pdf