专利号:US-2005239808-A1 优先权日:2002-05-10 标题 :Active substances for the treatment, diagnosis and prophylaxis of diseases in which abnormal protein structures occur 发明人:SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA 权利人:SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA 摘要:The invention on hand refers to diseases associated with abnormal protein structures, including Alzheimer's disease, Creutzfeldt-Jakob's disease, BSE and other prion-associated diseases. It is the task of the invention on hand to provide new active agents preventing the formation of amyloid plaques and to dissolve existing plaques, such agents being convenient for therapy, diagnosis and prophylaxis of diseases that are associated with abnormal protein structures. This task is performed in terms of the current invention by heterocyclic or aromatic agents with a rigid structure and a donor-acceptor-donor pattern (DAD), the latter being formed by donors and acceptors of hydrogen bridge linkages which comply with the β-sheet structure of the peptide or protein and thus fit as binding partners. The heterocyclic or aromatic agents are available at least as dimers. They recognise peptides and proteins with a β-sheet structure, form stable complexes with them and inhibit their aggregation to β-amyloid plaques. Furthermore, the new active agents are able to dissolve β-amyloid plaques that already exist. Another task of the current invention is to provide methods for the synthesis of said heterocyclic or aromatic compounds.
专利号:US-10035796-B2 优先权日:2014-08-14 标题:Crystalline forms of a BACE inhibitor, compositions, and their use 发明人:KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
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-2009093521-A1 优先权日:2005-06-14 标 题 :2, 5-Bis-Diamine [1,4] Benzoquinone-Derivatives 发明人:BOLOGNESI MARIA LAURA; BANZI RITA; MINARINI ANNA; MELCHIORRE CARLO 权利人:BOLOGNESI MARIA LAURA; BANZI RITA; MINARINI ANNA; MELCHIORRE CARLO 摘要:Synthesis of 2,5-bis-diamine-[1,4]benzoquinonic derivatives having the general formula (I), products and intermediates of said synthesis; the synthesis involves the use of p-benzoquinones having the general formula (IX) and diamines having the general formula (XI).
专利号:US-12201669-B2 优先权日:2021-03-11 标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology 发明人:TSAI LI-HUEI; BLANCHARD JOEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.
专利号:US-6214847-B1 优先权日:1997-08-14 标题 :Crystalline 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone and an improved process for preparing the same 发明人:PESTI JAAN A; FORTUNAK JOSEPH M; HUHN GEORGE F; MAURIN MICHAEL; YIN JIANGUO 权利人:DU PONT PHARM CO 摘要:The present invention relates to processes for the synthesis of a crystalline polymorph of 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone in high purity. The product is useful in the synthesis of pharmaceutical compounds for the reduction of cholinergic system dysfunction.
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合成参考文献
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