📜4-氨基-3-甲基苯甲醇置于18-冠醚-6,Potassium Acetate,戴斯-马丁氧化剂,Sodium Hydroxide,亚硝酸异戊酯体系中,用 甲醇,二氯甲烷,氯仿 用作溶剂,化学反应 30.0H,反应生成1H-吲唑-5-甲醛 参考文献:Discovery Of Potent And Selective Nonsteroidal Indazolyl Amide Glucocorticoid Receptor Agonists 标题:Discovery Of Potent And Selective Nonsteroidal Indazolyl Amide Glucocorticoid Receptor Agonists 摘要:Modification Of A Phenolic Lead Structure Based On Lessons Learned From Increasing The Potency Of Steroidal Glucocorticoid Agonists Lead To The Discovery Of Exceptionally Potent,Nonsteroidal,Indazole Gr Agonists. Sar Was Developed To Achieve Good Selectivity Against Other Nuclear Hormone Receptors With The Ultimate Goal Of Achieving A Dissociated Gr Agonist As Measured By Human In Vitro Assays. The Specific Interactions By Which This Class Of Compounds Inhibits Gr Was Elucidated By Solving An X-Ray Co-Crystal Structure. (C) 2013 Published By Elsevier Ltd. Doi:10.1016/j.Bmcl.2013.06.089
专利号:US-11970456-B1 优先权日:2023-09-21 标题:Synthesis of thiosemicarbazide analogue as inhibitor of tyrosinase, skin hyperpigmentation, and fruit and/or vegetable browning 发明人:BARI AHMED MUHAMMAD; GHANI USMAN 权利人:UNIV KING SAUD 摘要:A 2-((1H-indazol-5-yl)methylene)hydrazinecarbothioamide compound, its synthesis, and its use as a tyrosine kinase inhibitor. In particular, the synthesis of the 2-((1H-indazol-5-yl)methylene)hydrazinecarbothioamide compound as shown below. This compound has a high efficacy of inhibiting mushroom tyrosinase enzyme, and is a potent inhibitor of tyrosinase that can be used as an inhibitor of skin hyperpigmentation as well as an inhibitor of fruit and vegetable browning.
专利号:WO-2023072966-A1 优先权日:2021-10-26 标题:Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4 发明人:DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC 权利人:PERHA PHARMACEUTICALS 摘要:The present invention relates to a compound of formula (I) wherein R 1 represents a (C 4 -C 6) alkyl group, a (C 3 -C 8) cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R''-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R'' is an optionally substituted phenyl group; R 2 is selected from the group consisting of a hydrogen atom and a (C 1 -C 3 )alkyl group; R 5 represents a hydrogen atom, a (C 1 -C 4 )alkyl group or a (C 3 -C 6 )cycloalkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; osteoarthritis and tendinopathy; Duchenne muscular dystrophy; cancers and leukemias; neuroinflammation, anemia, infections caused by unicellular parasites, viral infections and for regulating body temperature.
参考文献:10.1055/s-0030-1261181 摘要:Augustine J, Bombrun A, Atta R. A Practical and Cost-Efficient, One-Pot Conversion of Aldehydes into Nitriles Mediated by ‘Activated DMSO’. Synlett. 2011 Aug 12;2011(15):2223–7. doi: 10.1055/s-0030-1261181.