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:WO-2025010390-A1 优先权日:2023-07-05 标题 :Synthesis of pyruvate kinase activators 发明人:FANDRICK DANIEL; LEUNG CHUN YUEN; CRANE SHELDON; LACHANCE NICOLAS; LE ROUX ANTOINE; PATEL JIGNESH; VALAMALE ASHALATHA 权利人:AGIOS PHARMACEUTICALS INC 摘要:Provided herein are methods for preparing activators of Pyruvate Kinase (PK) or a salt or a hydrate thereof.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-10226449-B2 优先权日:2013-12-20 标 题:Heterocyclic modulators of lipid synthesis and combinations thereof 发明人:HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
专利号:US-9428502-B2 优先权日:2012-07-03 标题:Heterocyclic modulators of lipid synthesis 发明人:OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; WAGMAN ALLAN S 权利人:3-V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
专利号:WO-9505391-A1 优先权日:1993-08-18 标 题 :Applications of fluorescent n-nucleosides and fluorescent structural analogs of n-nucleosides 发明人:CONRAD MICHAEL J 权利人:CHROMAGEN INC 摘要:Structural analogs of the six non-fluorescent N-nucleosides commonly found in RNA and DNA, which are inherently fluorescent under physiological conditions, are identified and methods for their preparation provided. Such analogs may be incorporated into DNA and/or RNA oligonucleotides via either enzymatic or chemical synthesis to produce fluorescent oligonucleotides having prescribed sequences. Such analogous sequences may be identical to, or the analogous complement of, template or target DNA or RNA sequences to which the fluorescent oligonucleotides can be hybridized. Methods of preparing either RNA or DNA oligonucleotide probes of the invention, intermediates used in such methods, and methods of using the probes of the invention in oligonucleotide amplification, detection, identification, and/or hybridization assays are also provided.