专利号:US-12304912-B2 优先权日:2020-07-28 标 题 :Fused bicyclic RAF inhibitors and methods for use thereof 发明人:BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA 权利人:JAZZ PHARMACEUTICALS IRELAND LTD 摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
专利号:US-9763953-B2 优先权日:2005-09-22 标题:Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment 发明人:MAELICKE ALFRED 权利人:GALANTOS PHARMA GMBH; NEURODYN LIFE SCIENCES INC 摘要:The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugsâ€?, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.
专利号:CA-2693182-A1 优先权日:2007-06-29 标 题:Pyrimidine compounds, methods of synthesis thereof, and use thereof in the treatment of raf kinase-mediated disorders
专利号:CA-2693182-C 优先权日:2007-06-29 标题:Pyrimidine compounds, methods of synthesis thereof, and use thereof in the treatment of raf kinase-mediated disorders