专利号:US-9522192-B2 优先权日:2012-12-13 标 题:Polyethylene glycol derivatives of palmitoylethanolamide and analogous acylethanolamides 发明人:CALIGNANO ANTONIO; D'AGOSTINO GIUSEPPE; LANERI SONIA; MELI ROSARIA; OSTACOLO CARMINE; RUSSO ROBERTO; SACCHI ANTONIA; TRONINO DIANA; DELLA VALLE FRANCESCO; DELLA VALLE MARIA FEDERICA; MARCOLONGO GABRIELE 权利人:EPITECH GROUP SRL 摘要:The synthesis of a series of Polyethylene glycol conjugates (esters and carbonates) of PEA and its analogous acylethanolamides, have higher water solubility and good hydrophilic/lipophilic balance, resulting in (i) improved accumulation in tissues (particularly skin and mucosae), (ii) prolonged release, and (iii) increased bioavailability. Improvement of PEA and analogous acylethanolamides levels in the tissues—particularly in the skin and mucosae—and their prolonged release is due to the improved bioavailability of related conjugates. Conjugates are able to extend the time frame in which PEA and analogous acylethanolamides exert their pharmacological effects.
专利号:WO-2006109321-A1 优先权日:2005-04-15 标题:An improved process for the synthesis of palmidrol 发明人:SURI SANJAY; KASHYAP TAPAN; SINGH JAGAT 权利人:MOREPEN LAB LTD; SURI SANJAY; KASHYAP TAPAN; SINGH JAGAT 摘要:The process of this invention comprises preparing anhydride of palmitic acid and alkyl or cycloalkyl haloformate by any conventional method, reacting anhydride so formed with ethnolamine in-situ, and isolating the product by any known methods such as solvent recovery or filtration followed by purifying the title product by recrystallization using organic solvents if so desired.
专利号:US-12194020-B2 优先权日:2017-12-22 标 题:Reversing baldness through cannabinoid receptor activation 发明人:POSTREL RICHARD 权利人:POSTREL RICHARD 摘要:This invention reverses male pattern baldness by shocking dormant hair follicles out of their androgen induced hibernation phase back to the active hair-growing anagenic phase. The invention integrates two functions: 1) It blocks synthesis of compounds holding the follicles in the telogenic/hibernating phase and 2) It stimulates synthesis of compounds animating the hair-growing/anagenic phase in the follicular activity cycle. One preferred embodiment comprises an enzyme inhibitor blocking the conversion of testosterone to dihydrotestosterone (DHT), a flavonoid simultaneously increasing synthesis of prostaglandins alternative to prostaglandin D2, and a selected cannabinoid compound stimulating restore the hair follicle to its normal growth cycle. This novel trimodal therapy restores the hair follicles to their normal cycling processes and maintains these restorative properties so long as this rebalance in maintained.
专利号:US-4761404-A 优先权日:1985-07-01 标题:Phospholipid analogs useful as PAF synthesis inhibitors 发明人:BUGIANESI ROBERT L; PONPIPOM MITREE M; RUPPRECHT KATHLEEN M 权利人:MERCK & CO INC 摘要:There are disclosed phospholipid analogs which are useful as PAF synthesis inhibitors. These compounds inhibit PAF (platelet-activating factor) biosynthesis and are thereby useful in the treatment of various diseases or disorders mediated by the PAF such as, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, and adult respiratory distress syndrome.
专利号:US-12084407-B2 优先权日:2019-11-26 标 题 :Cannabigerol derivatives and use thereof as cannabinoid receptor modulators 发明人:AHMAR SIAWASH; GNANASEKARAN KRISHNA KUMAR; OMEARA JEFFREY ALAN 权利人:CANOPY GROWTH CORP 摘要:The synthesis of a range of pentylbezene-1,3-diol compounds of formula I is disclosed. These compounds bind to cannabinoid 1 and 2 receptors (CB1 and CB2), and are thus presumed to be useful in modulating the activity of such receptors. Accordingly, the use of such synthetic cannabinoids in the treatment of various disorders mediated by CB1 and CB2 is contemplated.
专利号:US-2005234244-A1 优先权日:2004-04-20 标题:Synthesis of COX-2 and FAAH inhibitors 发明人:BARTOLINI WILMIN; CALI BRIAN M; CHEN BARBARA; CHIEN YUEH-TYNG; CURRIE MARK G; MILNE G T; PEARSON JAMES P; TALLEY JOHN J; ZIMMERMAN CRAIG 权利人:BARTOLINI WILMIN; CALI BRIAN M; CHEN BARBARA; CHIEN YUEH-TYNG; CURRIE MARK G; MILNE G T; PEARSON JAMES P; TALLEY JOHN J; ZIMMERMAN CRAIG 摘要:Methods for preparing indoles that are useful COX-2 inhibitors and intermediates useful in such methods are described.
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合成参考文献
参考文献:10.1186/1743-7075-8-51 摘要:Piscitelli F, Carta G, Bisogno T, Murru E, Cordeddu L, Berge K, Tandy S, Cohn JS, Griinari M, Banni S, Di Marzo V. Effect of dietary krill oil supplementation on the endocannabinoidome of metabolically relevant tissues from high-fat-fed mice. Nutr Metab (Lond). 2011 Jul 13;8(1):51. 参考文献:10.1371/journal.pone.0020766 摘要:Murillo-Rodríguez E, Palomero-Rivero M, Millán-Aldaco D, Arias-Carrión O, Drucker-Colín R. Administration of URB597, Oleoylethanolamide or Palmitoylethanolamide Increases Waking and Dopamine in Rats. PLoS ONE. 2011 Jul 14;6(7):e20766. doi: 10.1371/journal.pone.0020766.