📜Methyl 3-Azido-2,3-Dideoxy-α-D-Arabino-Hexopyranoside置于palladium On Activated Charcoal 氢气,Sodium Nitrite体系中,用 甲酸,乙醇,N,N-二甲基甲酰胺 作为反应溶剂,25.0 °C,101.33 Kpa 条件下,反应 5.5H,反应生成 依考莫司汀 参考文献:Rationale For The Synthesis And Preliminary Biological Evaluation Of Highly Active New Antitumor Nitrosoureido Sugars 标题:Rationale For The Synthesis And Preliminary Biological Evaluation Of Highly Active New Antitumor Nitrosoureido Sugars 摘要:Various New Nitrosoureido Derivatives Of Di-Or Trideoxy Sugars Were Synthesized. The Influence Of The Hydroxyl Substitution Pattern,The Configuration At The Anomeric Center,And The Absolute Configuration Of The Sugar Moiety On The Antitumor Activity Of A Series Of Nitrosoureido Derivatives Of Di-And Trideoxy Sugars Was Studied. All Compounds Showed A Very Significant Activity In Vivo Against L1210 Leukemia,B16 Melanocarcinoma,And Lewis Lung Carcinoma. Methyl 3-[3-(2-Chloroethyl)-3-Nitrosoureido]-2,3-Dideoxy-Alpha-D-Arabino-Hexopyranoside,24 (Nsc 609224),Was Found To Be The Most Active Compound. When Treated With 24 (Nsc 609224) At 20 Mg/kg On Day 1,At Least 90% Of The L1210 Leukemia And B16 Melanocarcinoma Bearing Mice Showed A Survival Of Over 60 Days For A Ld50 Value For This Compound Of 42 Mg/kg. DOI:10.1021/jm00121A005
专利号:US-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-9220714-B2 优先权日:2006-03-16 标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis 发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG 权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND 摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.
专利号:US-2024382626-A1 优先权日:2023-05-16 标题 :Irradiation amenable liposomal dye aggregates and methods of synthesis and use thereof 发明人:PORTER TYRONE; STERN NOAH; TUNNELL JAMES; SHRESTHA BINITA 权利人:UNIV TEXAS 摘要:The present invention provides lipid nanoparticles that are amenable to an irradiation at a wavelength at or above 850 nm, have an absorption peak from about 850 to 1100 nm wavelength, and comprise a high transition temperature lipid and a dye (e.g., a J-aggregate of a dye). In some embodiments, the dye (e.g., J-aggregate of the dye) is encapsulated in the lipid nanoparticle. In various embodiments, the present invention also relates to compositions comprising said lipid nanoparticles and methods of generating said lipid nanoparticles and compositions thereof. The present invention further relates to methods relating to the said lipid nanoparticles for imaging, detection, and treatment of diseases or disorders (e.g., phototherapy) in a subject.
专利号:US-2008281105-A1 优先权日:2005-01-18 标题:Novel Quinolinium Salts and Derivatives 发明人:MACDONALD JAMES E; HYSELL MICHELLE K; YU DEHUA; LI HENRY; WONG-STAAL FLOSSIE 权利人:IMMUSOL INC 摘要:The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.
1: el Abed I, Roger P, Gosse C, Atassi G, Gouyette A. Chemical stability of ecomustine, a new antitumor agent in aqueous and biological media as assessed by high-performance liquid chromatography. Cancer Chemother Pharmacol. 1991;27(4):295-300.