专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-9884067-B2 优先权日:2013-03-14 标 题:Androgen receptor down-regulating agents and uses thereof 发明人:NJAR VINCENT C O; GEDIYA LALJI K; PURUSHOTTAMACHAR PURANIK; GODBOLE ABHIJIT; KWEGYIR AFFUL ANDREW; VASAITIS TADAS 权利人:UNIV OF MARYLAND EASTERN SHORE; UNIV JEFFERSON; UNIV MARYLAND 摘要:The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.
专利号:US-2024239805-A1 优先权日:2022-12-16 标 题:Aza-yang cyclization-buchner aromatic ring expansion: collective synthesis of cycloheptatriene-containing azetidine lactones 发明人:SINGH MANVENDRA PAL; BOSKOVIC ZARKO; GASKINS BRYCE 权利人:UNIV KANSAS 摘要:The present disclosure is directed to a compound of Formula I, Formula II, Formula III, Formula IV, or Formula Vor a pharmaceutically acceptable salt and/or solvate thereof.
专利号:WO-2025056767-A1 优先权日:2023-09-15 标题 :Process for the preparation of enantiomerically enriched aliphatic amines 发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS 权利人:SYNGENTA CROP PROTECTION AG 摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
1: Griffith R, Yaeger M, Hostetter S, Tell LA, Wetzlich S, Vickroy T, Lillie B, MacFarlane W, Laudenslager T, Whitley E, Dzikamunhenga R, Larson W. Safety of fenbendazole in Chinese ring-necked pheasants (Phasianus colchicus). Avian Dis. 2014 Mar;58(1):8-15. 4: Cray C, Watson T, Zaias J, Altman NH. Effect of fenbendazole on an autoimmune mouse model. J Am Assoc Lab Anim Sci. 2013;52(3):286-9. 5: Mason ME, Voris ND, Ortis HA, Geeding AA, Kaplan RM. Comparison of a single dose of moxidectin and a five-day course of fenbendazole to reduce and suppress cyathostomin fecal egg counts in a herd of embryo transfer-recipient mares. J Am Vet Med Assoc. 2014 Oct 15;245(8):944-51. doi: 10.2460/javma.245.8.944. doi: 10.1371/journal.pntd.0002752. eCollection 2014 Apr.
合成参考文献
参考文献:10.1016/j.vetpar.2011.06.014 摘要:George N, Persad K, Sagam R, Offiah VN, Adesiyun AA, Harewood W, Lambie N, Basu AK. Efficacy of commonly used anthelmintics: first report of multiple drug resistance in gastrointestinal nematodes of sheep in Trinidad. Vet Parasitol. 2011 Dec 29;183(1-2):194–7. doi: 10.1016/j.vetpar.2011.06.014. 参考文献:10.1093/neuonc/nor077 摘要:Bai RY, Staedtke V, Aprhys CM, Gallia GL, Riggins GJ. Antiparasitic mebendazole shows survival benefit in 2 preclinical models of glioblastoma multiforme. Neuro Oncol. 2011 Sep;13(9):974–82.