2-甲基-5-乙烯基吡啶置于sodium Periodate,四氧化锇体系中,用 乙二醇二甲醚,水 作为反应溶剂,化学反应生成 5-甲酰基-2-甲基吡啶 参考文献:Pyridine-Pyrimidinone Derivatives,A Process For Their Production And 标题:Pyridine-Pyrimidinone Derivatives,A Process For Their Production And 摘要:该发明涉及与以下一般式相对应的新吡啶-嘧啶酮衍生物 ##str1## 其中r.Sup.1代表线性c.Sub.1-6烷基或环烷基,R.Sup.2代表线性c.Sub.1-6烷基或r.Sup.1和r.Sup.2与氮原子一起形成吡咯烷或哌嗪环;alk代表线性烷基链c.Sub.1-6;q代表苯环,呋喃环,噻吩环或噻唑环;x代表氧,Y是单键,当q代表苯时,M为2,3或4;x代表亚甲基,Y代表硫,当q为呋喃,噻吩或噻唑时,M为2或3;r.Sup.3代表氢原子或低烷基基团.这些化合物显示出改善的h.Sub.2-拮抗活性.
专利号:US-12319691-B2 优先权日:2020-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI 权利人:AMGEN INC; VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9938258-B2 优先权日:2012-11-29 标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof 发明人:BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
专利号:WO-2015088564-A1 优先权日:2013-12-13 标 题:P2x4 receptor modulating compounds 发明人:NEWCOM JASON S; SPEAR KERRY L 权利人:SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are P2X4 receptor modulating compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including but not limited to, chronic pain, neuropathy, inflammatory diseases and central nervous system disorders.
专利号:US-9192612-B2 优先权日:2013-02-13 标题:Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; BECK ELIZABETH MARY; DAVOREN JENNIFER ELIZABETH; LACHAPELLE ERIK ALPHIE; O'NEILL BRIAN THOMAS 权利人:PFIZER 摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nand the variables R 1 and R 2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.