专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-2012208232-A1 优先权日:2009-07-15 标 题:Cell-Free Synthesis of Active Reprogramming Transcription Factors 发明人:YANG WILLIAM; PATEL KEDAR; GHEBREMARIAM YOHANNES T; LEE JI EUN; WONG HANN-CHUNG; COOKE JOHN P; SWARTZ JAMES ROBERT 权利人:YANG WILLIAM; PATEL KEDAR; GHEBREMARIAM YOHANNES T; LEE JI EUN; WONG HANN-CHUNG; COOKE JOHN P; SWARTZ JAMES ROBERT 摘要:Compositions and methods are provided for the cell-free synthesis of active reprogramming factor polypeptides. The reprogramming factors may be synthesized as fusion proteins comprising a permeant domain, such as polyarginme. The cell free-synthesis may be conducted at about 25 C in a bacterial cell extract from genetically alterd cells having decreased endogenous protease activity Further, the proteins may comprise a fusion partner which enhances solubility and may be refolded on a column.
专利号:EP-0790982-B1 优先权日:1994-06-17 标 题 :Methods of synthesis of peptidyl argininals 发明人:WEBB THOMAS R; REINER JOHN E; TAMURA SUSAN Y; RIPKA WILLIAM C; DAGNINO RAYMOND JR; NUTT RUTH F 权利人:CORVAS INT INC 摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein, which have formula (I), wherein R1 is selected from the group consisting of hydrogen, benzyloxycarbonyl, isonicotinyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, t-butoxycarbonyl, t-amyloxycarbonyl, isobornyloxycarbonyl, adamantyloxycarbonyl, 2-(4-biphenyl)-2-propyloxycarbonyl, 9-fluorenylmethoxycarbonyl and methylsulfonylethoxycarbonyl; R2 is selected from the group consisting of alkyl of 1 to about 12 carbon atoms and aralkyl of about 7 to about 15 carbon atoms, either of which is optionally substituted with hydroxy or -CO-Y, wherein Y is hydroxy, alkoxy of 1 to about 12 carbon atoms, aralkoxy of about 7 to about 15 carbon atoms, O-polymeric support or NH-polymeric support; R3 is selected from the group consisting of hydrogen, Fmoc, nitro, benzyloxycarbonyl, t-butoxycarbonyl and adamantyloxycarbonyl; and R4 is selected from the group consisting of hydrogen, alkyl of 1 to about 12 carbon atoms, aryl of about 6 to about 14 carbon atoms and aralkyl of about 7 to about 15 carbon atoms; and salts thereof.
专利号:US-2013302247-A1 优先权日:2012-05-09 标 题:Synthesis of fluoroarachidonic acid and methods of use thereof 发明人:PICHIKA RAMAIAH; ECKELMAN WILLIAM C; RAPOPORT STANLEY I; TAHA AMEER; KOTTA KISHORE 权利人:US HEALTH; UNIV CALIFORNIA 摘要:There are provided, inter alia, methods for diagnosis of the extent of neuroinflammation in a subject. The methods include administering an 18 F-labeled arachidonic acid to a subject in need thereof, obtaining a positron emission tomography (PET) scan of the subject, and determine the extent of neuroinflammation from the PET scan. There are provided, inter alia, methods of synthesis of reagents useful for the production of an 18 F-labeled arachidonic acid.
专利号:US-5731413-A 优先权日:1994-06-17 标 题:Method of synthesis of peptidyl aldehydes 发明人:WEBB THOMAS ROY; REINER JOHN EUGENE; TAMURA SUSAN YOSHIKO; RIPKA WILLIAM CHARLES; DAGNINO JR RAYMOND; NUTT RUTH FOELSCHE 权利人:CORVAS INT INC 摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel! reagents useful therein.
专利号:WO-2017100796-A1 优先权日:2015-12-11 标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI 权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.
1: Star K, Edwards IR, Choonara I. Valproic acid and fatalities in children: a review of individual case safety reports in VigiBase. PLoS One. 2014 Oct 10;9(10):e108970. doi: 10.1371/journal.pone.0108970. eCollection 2014. Review. 2: Vázquez M, Fagiolino P, Maldonado C, Olmos I, Ibarra M, Alvariza S, Guevara N, Magallanes L, Olano I. Hyperammonemia associated with valproic acid concentrations. Biomed Res Int. 2014;2014:217269. doi: 10.1155/2014/217269. Epub 2014 Apr 29. 3: Martínez-Lazcano MT, Esplá-González S, Herraiz-Robles P, Hernández-Pérez P, Chillerón-Cuenca R, Pol-Yanguas E. [Use of valproic acid in long stay units of psychiatry]. Farm Hosp. 2015 Mar 1;39(2):92-101. doi: 10.7399/fh.2015.39.2.8460. Spanish. doi: 10.1002/pds.3761. Epub 2015 Feb 5.
合成参考文献
参考文献:10.1192/bjp.187.6.559 摘要:Chisholm D, van Ommeren M, Ayuso-Mateos JL, Saxena S. Cost-effectiveness of clinical interventions for reducing the global burden of bipolar disorder. Br J Psychiatry. 2005 Dec;187():559–67. doi: 10.1192/bjp.187.6.559. 参考文献:10.1007/s00228-010-0785-6 摘要:Djordjevic N, Carrillo JA, Gervasini G, Jankovic S, Aklillu E. In vivo evaluation of CYP2A6 and xanthine oxidase enzyme activities in the Serbian population. European Journal of Clinical Pharmacology. 2010 Feb 13;66(6):571–8. doi: 10.1007/s00228-010-0785-6. 参考文献:10.2165/11532900-000000000-00000 摘要:Balossier A, Dörner L, Emery E, Heese O, Mehdorn HM, Menei P, Singh J. Incorporating BCNU wafers into malignant glioma treatment: European case studies. Clin Drug Investig. 2010;30(3):195–204. doi: 10.2165/11532900-000000000-00000. 参考文献:10.2165/11530130-000000000-00000 摘要:Hasnain M, Vieweg WV, Fredrickson SK. Metformin for atypical antipsychotic-induced weight gain and glucose metabolism dysregulation: review of the literature and clinical suggestions. CNS Drugs. 2010 Mar;24(3):193–206. doi: 10.2165/11530130-000000000-00000. 参考文献:10.1007/s11481-010-9192-0 摘要:Suh H, Choi S, Khattar P, Choi N, Lee SC. Histone Deacetylase Inhibitors Suppress the Expression of Inflammatory and Innate Immune Response Genes in Human Microglia and Astrocytes. Journal of Neuroimmune Pharmacology. 2010 Feb 17;5(4):521–32. doi: 10.1007/s11481-010-9192-0.