专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-10233182-B2 优先权日:2014-04-04 标题 :Substituted spirocyclic inhibitors of autotaxin 发明人:BABISS LEE; CLARK MATTHEW; KEEFE ANTHONY D; MULVIHILL MARK J; NI HAIHONG; RENZETTI LOUIS; RUEBSAM FRANK; WANG CE; XIE ZHIFENG; ZHANG YING 权利人:X RX INC 摘要:The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
专利号:EP-4428132-A1 优先权日:2023-03-08 标题:Slack-activating compounds and their medical use 发明人:SCHMIDTKO ACHIM; PROSCHAK EUGEN; BALZULAT ANNIKA; ZHU WENXIN; FLAUAUS CATHRIN; STEINHILBER DIETER; LU RUIRUI; HERNANDEZ OLMOS VICTOR; HEERING JAN 权利人:JOHANN WOLFGANG GOETHE UNIV FRANKFURT AM MAIN 摘要:The present invention pertains to novel compounds and their synthesis which are structurally derived from 2-chloro-11-(4-methylpiperazin-1-yl)dibenzo[ b , f ][1,4]oxazepine. The compounds of the invention were shown in a comparative study to bind and activate potassium channels, in particular Slack. Based on their activating activity, the compounds of the invention and pharmaceutical compositions containing them can be used in various therapeutic applications for the treatment or prevention of pathologies.
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合成参考文献
参考文献:10.1515/biolog-2016-0148 摘要:Moustafa M, Mostafa O, Al-Shahrani D, Alrumman S. An application of genetics-chemicals constituents to the relatedness of three Euphorbia species. Biologia. 2016 Nov;71(11):1240–9. doi: 10.1515/biolog-2016-0148.