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: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-2023346952-A1 优先权日:2015-09-22 标题:Cannabinoid glycoside prodrugs and methods of synthesis 发明人:ZIPP BRANDON J; HARDMAN JANEE’ M; BROOKE ROBERT T; DEUTSCHER TYREL R 权利人:GRAPHIUM BIOSCIENCES INC 摘要:The present invention provides tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs and pharmaceutical compositions comprising these compounds, and their use for the site-specific delivery of tetrahydrocannabinol or cannabidiol. Also provided are processes for the preparation of purified tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs.
专利号:US-7888394-B2 优先权日:2006-08-21 标 题:Synthesis, polymorphs, and pharmaceutical formulation of FAAH inhibitors 发明人:PUTMAN DAVID; DASSE OLIVIER 权利人:ORGANON NV 摘要:Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.
专利号:US-11407837-B2 优先权日:2017-09-11 标 题 :GPCR binding proteins and synthesis thereof 发明人:GLANVILLE JACOB 权利人:TWIST BIOSCIENCE CORP 摘要:Provided herein are methods and compositions relating to G protein-coupled receptor (GPCR) libraries having nucleic acids encoding for a scaffold comprising a GPCR binding domain. Libraries described herein include variegated libraries comprising nucleic acids each encoding for a predetermined variant of at least one predetermined reference nucleic acid sequence. Further described herein are protein libraries generated when the nucleic acid libraries are translated. Further described herein are cell libraries expressing variegated nucleic acid libraries described herein.
专利号:US-11207414-B2 优先权日:2015-09-22 标 题 :Cannabinoid glycoside prodrugs and methods of synthesis 发明人:ZIPP BRANDON J; HARDMAN JANEE M; BROOKE ROBERT T 权利人:GRAPHIUM BIOSCIENCES INC 摘要:The present invention relates to cannabinoid glycoside prodrugs suitable for site- and tissue-specific delivery of cannabinoid molecules. The present invention also relates to methods of forming the cannabinoid glycoside prodrugs through glycosyltransferase mediated glycosylation of cannabinoid molecules.
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.