CAS: 108-33-8; 2-Amino-5-Methyl-1,3,4-Thiadiazole

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14068-53-2 27115-74-8 4005-51-0

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(1E)-3-氨基-1-亚乙基硫脲置于iron(III) Chloride体系中,化学反应生成2-氨基-5-甲基-1,3,4-噻二唑
参考文献:新型短效催眠药hie-124的噻二唑[3,2-A ] [1,3]二氮杂analogue类似物的合成,生物学评价和分子建模研究
标题:新型短效催眠药hie-124的噻二唑[3,2-A ] [1,3]二氮杂analogue类似物的合成,生物学评价和分子建模研究
摘要:合成了一系列新的6,7-二氢-[1,3,4]噻二唑[3,2-A ] [1,3]二氮杂analogue类似物,并对其进行了生物学评估.与硫喷妥钠(6)相比,化合物gs-62(33)表现出强大的体内短效催眠活性,其起效时间,睡眠时间和治疗指数分别为6.4+/-0.2,94.8+/-5.3分钟,6.62 .维持剂量为6时,化合物33没有显示出任何急性耐受的迹象.同时33增强了6的体内催眠作用等摩尔量(0.06 Mmol)的组合分别显示起效和持续时间分别为7.5+/-1.3,62.5+/-5.9分钟.这种组合允许使用较低剂量的两种药物,以避免不良的副作用.对接研究揭示了非常好的相互作用和与gaba A受体的bdz结合位点的结合,尤其是与arg87,Arg149和thr151氨基酸残基的结合.
Doi:10.1016/j.Ejmech.2016.08.038

专利信息

专利号:US-2025129021-A1
优先权日:2023-09-19
标 题:Small molecule protein synthesis modulators
发明人：GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.

专利号:US-11512097-B2
优先权日:2019-11-25
标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use
发明人：ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO
权利人:AMGEN INC
摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:US-9828386-B2
优先权日:2013-11-15
标题:Sulfur-substituted podophyllotoxin derivative, synthesis method thereof, and use thereof
发明人：TANG YAJIE; LI JIANLONG; ZHAO WEI; LI HONGMEI
权利人:UNIV HUBEI TECHNOLOGY
摘要:The present invention discloses a sulfur-substituted podophyllotoxin derivative, synthesis method thereof, and use thereof. The present invention introduces a rigid aromatic heterocyclic compound, as well as a further sulfonamidated product of 3-amino-5-mercapto-1,2,4-triazole, 2-amino-5-mercapto-1,3,4-thiadiazole, 4-methylbenzenesulfonyl chloride, or 4-methoxybenzenesulfonyl chloride as a substituent group, into position 4 of the C-ring of podophyllotoxin or 4′-demethylepipodophyllotoxin to obtain the podophyllotoxin derivative shown in formula (V), said derivative having significantly increased antitumor activity and reduced toxic side effects. Experiments on in vitro tumor cell inhibition indicate that the antitumor activity of the compound of formula (V) of the present invention is significantly higher than the antitumor activity of podophyllotoxin or 4′-demethylepipodophyllotoxin.

专利号:US-2010286211-A1
优先权日:2004-10-08
标题:Oxazolidinone derivatives as antimicrobials
发明人：DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK
权利人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK
摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

专利号:US-6852752-B2
优先权日:1999-12-17
标 题:Urea compounds, compositions and methods of use and preparation
发明人：JACOBS JEFFREY W; PATEL DINESH; LEWIS JASON; NI ZHI-JIE
权利人:VICURON PHARM INC
摘要:Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.

专利号:CN-102276551-A
优先权日:2010-06-10
标题 :Synthesis of Cyanoacrylate Compounds Containing Heterocyclic Long-chain Amino-substituted Cyanoacrylates and Their Application in Pesticides