2-氨基-6-氯吡嗪置于n-溴代丁二酰亚胺(Nbs)体系中,用 氯仿 用作溶剂,化学反应生成2-氨基-5-溴-6-氯吡嗪 参考文献:N-Heterocyclyl Sulphonamide Derivatives And Their Use As Endothelin 标题:N-Heterocyclyl Sulphonamide Derivatives And Their Use As Endothelin 摘要:这项发明涉及药用价值的n-杂环磺胺衍生物,它们的药用盐,其制备方法,它们在人类或其他温血动物中拮抗内皮素一种或多种作用的用途,以及它们在治疗疾病或医疗状况的方法中的应用,其中内皮素的升高或异常水平起重要致病作用.
专利信息
专利号:US-2024239799-A1 优先权日:2021-04-02 标 题:(s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo [1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer 发明人:DI FABIO ROMANO; MONTALBETTI CHRISTIAN; PETROCCHI ALESSIA; GRILLO ALESSANDRO; RANDAZZO PIETRO; ROSSETTI ILARIA; CIAMMAICHELLA ALINA 权利人:C N C C S S C A R L COLLEZIONE NAZ DEI COMPOSTI CHIMICI E CENTRO SCREENING; IRBM S P A 摘要:The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-41H,6′H-spiro[piperidine-4,5′-pyrrolo[1,2-b]pyrazol]-41-amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
专利号:US-2024409557-A1 优先权日:2023-05-09 标 题 :5,6-fused and 6,6-fused bicyclic alcohols and ethers and compositions for use as 15-prostaglandin dehydrogenase modulators 发明人:GREENMAN KEVIN LLOYD; PICKRELL ALEXANDER J; LI KEXUE; AMEGADZIE ALBERT K; WANG HUI-LING; WEIRES NICHOLAS ANTHONY; ALLEN JOHN G; BOURBEAU MATTHEW P 权利人:AMGEN INC 摘要:The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a general Formula (A).Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (A).
专利号:CN-117946013-B 优先权日:2024-01-25 标题:One-pot synthesis of 5,6-dihalogenated-3-aminopyrazine-2-carboxylic acid methyl ester
专利号:US-7772246-B2 优先权日:2007-08-01 标题:Pyrazole compounds as RAF inhibitors 发明人:CUI JINGRONG JEAN; DEAL JUDITH GAIL; GU DANLIN; GUO CHUANGXING; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; KEPHART SUSAN ELIZABETH; LINTON MARIA ANGELICA; MCALPINE INDRAWAN JAMES; PAIRISH MASON ALAN; PALMER CYNTHIA LOUISE 权利人:PFIZER 摘要:The present invention is directed to compounds of Formula (I), n nand to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
专利号:CN-112724089-B 优先权日:2021-01-05 标题 :A kind of synthesis technique of 2-amino-3-bromo-6-chloropyrazine
专利号:CN-112724089-A 优先权日:2021-01-05 标 题 :A kind of synthesis technique of 2-amino-3-bromo-6-chloropyrazine
参考文献:10.1021/jm2007326 摘要:Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, de Haven Brandon A, Box G, van Montfort RL, Williams DH, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011 Dec 22;54(24):8328–42.