(5-Fluoro-2-Nitro-Phenyl)-Pyruvic Acid置于ammonium Hydroxide,Iron(II) Sulfate体系中,化学反应生成 5-氟吲哚-2-甲酸 参考文献:Bergmann; Pelchowicz,Journal Of The Chemical Society,1959,P. 1913 标题:Bergmann; Pelchowicz,Journal Of The Chemical Society,1959,P. 1913
专利号:US-11572354-B2 优先权日:2018-01-10 标题 :Inhibitor of indoleamine 2,3-dioxygenase-1 and methods of manufacture and use thereof 发明人:WEAVER DONALD; BRANT MICHAEL G; WOHNIG STEPHANIE; WU FAN; GOODWIN-TINDALL JAKE; MEEK AUTUMN; SCHIAVINI PAOLO 权利人:UNIV HEALTH NETWORK 摘要:Inhibition of indoleamine 2,3-dioxygenase (IDO1) is an attractive immunotherapeutic approach for the treatment of a variety of cancers. Dysregulation of this enzyme has also been implicated in other severe diseases such as Alzheimer's disease and arthritis. Small molecule inhibitors of Formula (Ia) and (Ib) of IDO, their synthesis, and uses thereof are provided.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
专利号:US-6989384-B2 优先权日:2000-06-14 标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:HUA YE; LUU HIEP THE; CHAN FORA P; JOHNSON JR THEODORE O; REICH SIEGFRIED HEINZ; SKALITZKY DONALD JAMES; YANG YI; HENDRICKSON THOMAS F; CHU SHAO SONG; EASTMAN BRIAN WALTER 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n nwhere the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-7122549-B2 优先权日:2000-11-03 标题:Saframycins, analogues and uses thereof 发明人:MYERS ANDREW G; PLOWRIGHT ALLEYN T 权利人:HARVARD COLLEGE 摘要:In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. n n n n n n n n n n In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.
专利号:US-2024327418-A1 优先权日:2021-08-04 标 题 :Multi-target inhibitor targeting hdac and nad synthesis and use of multi-target inhibitor
专利号:WO-2023011416-A1 优先权日:2021-08-04 标题:Multi-target inhibitor targeting hdac and nad synthesis and use of multi-target inhibitor
[参考文献]: Chung-Yi Wu, Et Al. Stable Benzotriazole Esters As Mechanism-Based Inactivators Of The Severe Acute Respiratory Syndrome 3Cl Protease. Chem Biol. 2006 Mar;13(3):261-8. [参考文献]: R Kamiński, Et Al. Effect Of 5-Fluoroindole-2-Carboxylic Acid (An Antagonist Of The Nmda Receptor-Associated Glycine Site) On The Anticonvulsive Activity Of Conventional Antiepileptic Drugs. J Neural Transm (Vienna). 1998;105(2-3):133-46. [参考文献]: R Kapoor, Et Al. Enhanced Sensitivity Of Medullary Depressor Neurons To N-Methyl-D-Aspartate-Glycine Site Antagonists In The Spontaneously Hypertensive Rat. Clin Exp Pharmacol Physiol. 1998 Mar-Apr;25(3-4):216-9. [参考文献]: Shigeo Hayashi, Et Al. Design, Synthesis And Structure-Activity Relationship Studies Of Novel And Diverse Cyclooxygenase-2 Inhibitors As Anti-Inflammatory Drugs. J Enzyme Inhib Med Chem. 2014 Dec;29(6):846-67. [参考文献]: T J Grudt, Et Al. Quisqualate Activates N-Methyl-D-Aspartate Receptor Channels In Hippocampal Neurons Maintained In Culture. Mol Pharmacol. 1990 Apr;37(4):477-81.
合成参考文献
参考文献:10.1038/ncb3255 摘要:Lin R, Elf S, Shan C, Kang HB, Ji Q, Zhou L, Hitosugi T, Zhang L, Zhang S, Seo JH, Xie J, Tucker M, Gu TL, Sudderth J, Jiang L, Mitsche M, DeBerardinis RJ, Wu S, Li Y, Mao H, Chen PR, Wang D, Chen GZ, Hurwitz SJ, Lonial S, Arellano ML, Khoury HJ, Khuri FR, Lee BH, Lei Q, Brat DJ, Ye K, Boggon TJ, He C, Kang S, Fan J, Chen J. 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. Nat Cell Biol. 2015 Nov;17(11):1484–96. 参考文献:10.1371/journal.pone.0218897 摘要:Miller TW, Amason JD, Garcin ED, Lamy L, Dranchak PK, Macarthur R, Braisted J, Rubin JS, Burgess TL, Farrell CL, Roberts DD, Inglese J. Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. PLoS ONE. 2019 Jul 05;14(7):e0218897. doi: 10.1371/journal.pone.0218897. 摘要:https://pubs.acs.org/doi/abs/10.1021/acs.analchem.7b01709