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-9623125-B2 优先权日:2011-10-24 标 题:Controlled synthesis of polyglutamates with low polydispersity and versatile architectures 发明人:VICENT DOCON MARIA JESUS; BARZ MATTHIAS; CANAL FABIANA; CONEJOS SANCHEZ INMACULADA; DURO CASTANO AROA; ENGLAND RICHARD MARK 权利人:FUND DE LA COMUNIDAD VALENCIANA “CENTRO DE INVESTIG PRINCIPE FELIPEâ€? 摘要:Polyglutamates are well known to be highly biocompatible, biodegradable and multifunctional polymers, which have been already used as building blocks in polymer drug conjugates and polymeric micelles. Those systems have been applied to various medical applications ranging from therapy to molecular imaging. Furthermore a polyglutamic acid (PGA) paclitaxel conjugate has already entered clinical studies (Opaxioâ„¢ PGA-PTX conjugate currently in phase III of Clinical trials). n In this context, a synthetic pathway to a plethora functional polyglutamates (homopolymers, block-co-polymers, tribocks) with well-defined structure, adjustable molecular weight (Mw) and low dispersity (D=Mw/Mn<1.2) applying the ring opening polymerization (ROP) of N-carboxyanhydrides (NCA) has been developed. Additionally, the acid moieties of the polyglutamates can be activated with 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium (DMTMM) and various functionalities can be easily introduced by “post-polymerization modificationâ€? yielding a set orthogonal reactive attachment sides. The reactive moieties, such as azides, maleimides, thiols, akynes (linear or cyclic) offer the opportunity of specific conjugation of the drugs, targeting moieties or markers. Besides introducing reactive groups the functionalization strategy was also used for PEGylation of PGA reducing charge induced interactions and therefore pharmacological properties, such as blood circulation time may be adjusted. n In summary, a tool kit of various polyglutamates has been developed enabling the synthesis of a variety of polymer drug conjugates or polymer based imaging agents. The functional polymeric precursors developed will allow us to functionalize and therefore adjust the polymer properties to a desired aplication.
专利号:US-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
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: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.
1: PLOS Neglected Tropical Diseases Staff. Correction: Efficacy of Albendazole-Chitosan Microsphere-based Treatment for Alveolar Echinococcosis in Mice. PLoS Negl Trop Dis. 2015 Oct 29;9(10):e0004181. doi: 10.1371/journal.pntd.0004181. eCollection 2015 Oct. doi: 10.1186/s13071-015-1105-x. 3: Thomsen EK, Sanuku N, Baea M, Satofan S, Maki E, Lombore B, Schmidt MS, Siba PM, Weil GJ, Kazura JW, Fleckenstein LL, King CL. Efficacy, Safety, and Pharmacokinetics of Co-Administered Diethylcarbamazine, Albendazole, and Ivermectin for the Treatment of Bancroftian Filariasis. Clin Infect Dis. 2015 Oct 20. pii: civ882. [Epub ahead of print] The effect of albendazole treatment on seizure outcomes in patients with symptomatic neurocysticercosis. Trans R Soc Trop Med Hyg. 2015 Nov;109(11):738-46. doi: 10.1093/trstmh/trv078. Epub 2015 Oct 3. doi: 10.1016/j.actatropica.2015.09.016. [Epub ahead of print] doi: 10.1371/journal.pntd.0004057. eCollection 2015 Sep. 10: Abulaihaiti M, Wu XW, Qiao L, Lv HL, Zhang HW, Aduwayi N, Wang YJ, Wang XC, Peng XY. Efficacy of Albendazole-Chitosan Microsphere-based Treatment for Alveolar Echinococcosis in Mice. PLoS Negl Trop Dis. 2015 Sep 9;9(9):e0003950. doi: 10.1371/journal.pntd.0003950. eCollection 2015 Sep.
合成参考文献
参考文献:10.1007/s00436-010-1748-7 摘要:Xue J, Xiao SH, Xu LL, Qiang HQ. The effect of tribendimidine and its metabolites against Necator americanus in golden hamsters and Nippostrongylus braziliensis in rats. Parasitol Res. 2010 Mar;106(4):775–81. doi: 10.1007/s00436-010-1748-7. 参考文献:10.1055/s-0029-1243830 摘要:Sharma M, Somasundaram A, Pathak A, Simon EG, Cloa MM. Endoscopic ultrasound in hepatobiliary hydatid disease. Endoscopy. 2010;42 Suppl 2():E56–7. doi: 10.1055/s-0029-1243830. 参考文献:10.1155/2011/340869 摘要:Pitanga Lukashok H, Robles-Jara C, Robles-Medranda C. Multiple Intestinal Erosions as a Result of Hemorrhage due to Parasites: Case Reports and Review of the Literature. Diagnostic and Therapeutic Endoscopy. 2011 Jun 01;2011():1–3. doi: 10.1155/2011/340869. 参考文献:10.1007/s00436-011-2551-9 摘要:Yadav AK, Temjenmongla. Efficacy of Lasia spinosa leaf extract in treating mice infected with Trichinella spiralis. Parasitol Res. 2012 Jan;110(1):493–8. doi: 10.1007/s00436-011-2551-9. 参考文献:10.1186/1475-2875-10-188 摘要:Meyrowitsch DW, Pedersen EM, Alifrangis M, Scheike TH, Malecela MN, Magesa SM, Derua YA, Rwegoshora RT, Michael E, Simonsen PE. Is the current decline in malaria burden in sub-Saharan Africa due to a decrease in vector population Malaria Journal. 2011 Jul 13;10(1):188. doi: 10.1186/1475-2875-10-188.