专利号:US-10807962-B2 优先权日:2017-04-14 标 题 :Process for the synthesis of firocoxib 发明人:CELESTINI PAOLO; BARETTI SERGIO; PIZZATTI ENRICA 权利人:COSMA S P A 摘要:The present invention concerns a process for the preparation of firocoxib, i.e. 3-(cyclopropylmethoxy)-5,5-dimethyl-4-(4-methylsulfonylphenyl)-furan-2-one, comprising steps (a)-(g), wherein the process provides for step (d) of the reaction of a new intermediate, i.e. 2-methyl-1-[4-(methylsulfanyl)phenyl]-1-oxopropan-2-yl (acetyloxy)acetate (compound VII) in the same organic solvent of step (a) in the presence of a catalyst and a phase transfer catalyst solution in the same organic solvent with hydrogen peroxide.
专利号:US-2023047214-A1 优先权日:2020-02-03 标题:Methods for microwave synthesis of degradable polymers for drug delivery 发明人:MURATOGLU ORHUN K; ORAL EBRU; GRINDY SCOTT 权利人:MASSACHUSETTS GEN HOSPITAL 摘要:Provided herein are methods of making degradable, additive-blended polymeric materials using microwave radiation and catalysts. The methods can include incorporation of therapeutic materials into the polymeric materials. There also are provided polymeric materials made by the methods and medical devices comprising the polymeric materials made by the methods.
专利号:US-11918657-B2 优先权日:2017-11-10 标 题 :Dendrimer delivery system and methods of use thereof 发明人:RANGARAMANUJAM KANNAN; SHARMA RISHI; SHARMA ANJALI; KANNAN SUJATHA; ZHANG ZHI; KAMBHAMPATI SIVA PRAMODH 权利人:UNIV JOHNS HOPKINS 摘要:Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. Ëœ120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.
专利号:WO-2018188763-A1 优先权日:2017-04-14 标 题:New process for the synthesis of firocoxib
专利号:US-9580409-B2 优先权日:2011-11-07 标 题:Modulators of opioid receptors and methods of use thereof 发明人:MALCOLM SCOTT; BOWEN CARRIE; MELNICK LAURENCE; XIE LINGHONG 权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., μ-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:EP-3609877-B1 优先权日:2017-04-14 标 题 :Process for the synthesis of firocoxib
1: Donnell JR, Frisbie DD. Use of firocoxib for the treatment of equine osteoarthritis. Vet Med (Auckl). 2014 Nov 4;5:159-168. doi: 10.2147/VMRR.S70207. 2: Wagner SA, Fajt VR, Lo CP, Byrd CJ. Pharmacokinetics of oral firocoxib in un- weaned calves. J Vet Pharmacol Ther. 2021 Sep;44(5):793-798. doi: 10.1111/jvp.12971. Epub 2021 Apr 4. 63(8):386-392. doi: 10.1002/jlcr.3842. Epub 2020 May 5. 13(1):60. doi: 10.3390/ani13010060. 5: Fadel C, Giorgi M. Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses. Vet Anim Sci. 2023 Jan 11;19:100286. doi: 10.1016/j.vas.2023.100286.
合成参考文献
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