专利号:US-5633260-A 优先权日:1994-04-19 标 题 :11,7 Substituted camptothecin derivatives and formulations of 11,7 substituted camptothecin derivatives and methods for uses thereof 发明人:HAUSHEER FREDERICK H; HARIDAS KOCHAT 权利人:BIONUMERIK PHARMACEUTICALS INC 摘要:The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients. The present invention also claims 11,7-HECPT and 11,7-HMCPT compositions, the synthesis of 11,7-HECPT or 11,7-HMCPT, the methods of formulation of 11,7-HECPT or 11,7 -HMCPT, and the methods of use of 11,7-HECPT or 11,7-HMCPT. Additionally, the claimed invention is directed to novel dosages, schedules, and routes of administration for both the 11,7-HECPT or 11,7-HMCPT formulations to humans with various forms of cancer. Other embodiments of this invention include isolation methods and methods of synthesis of certain camptothecin derivatives.
专利号:WO-2025099082-A1 优先权日:2023-11-09 标 题:Improved process for the synthesis of 2,5-dihydroxymethylfuran (bhmf) from 5-hydroxymethylfurfural (hmf) 发明人:MAZZONI RITA; MESSORI ALESSANDRO; PIAZZI ANDREA; SANTARELLI NICOLÃ’; MARTELLI GIULIA; CURCIO MASSIMILIANO; ALBONETTI STEFANIA; TABANELLI TOMMASO 权利人:UNIV BOLOGNA ALMA MATER STUDIORUM 摘要:A synthesis process comprising a step of reacting HMF to obtain BHMF under hydrogen pressure and wherein HMF is contacted with a catalyst mixture, said catalyst mixture comprising a metal catalyst of a transition metal of Group 8 or a salt of said catalyst and optionally an organic solvent.
专利号:US-11717498-B2 优先权日:2013-12-31 标题 :Methods of treatment using amphetamine controlled release, prodrug, and abuse deterrent dosage forms 发明人:POPP KARL; MECKLER HAROLD 权利人:Chemapotheca LLC; PHARMAPOTHECA A INC 摘要:The invention also relates to pharmaceutical compositions comprising highly pure amphetamine and amphetamine-class compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds, and to methods of manufacturing, delivering, and using the amphetamine compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds.
专利号:WO-2008103866-A1 优先权日:2007-02-22 标题 :Synthesis of indoles 发明人:TALLEY JOHN JEFFREY; RENZE JUERGEN T 权利人:MICROBIA INC; TALLEY JOHN JEFFREY; RENZE JUERGEN T 摘要:Method for preparing indoles, including methods that permit high yield production of particular compounds, are described.
专利号:US-8569265-B2 优先权日:2011-05-06 标题:Deuterated analogs of (4S)-4-ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3′, 4′:6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof 发明人:CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H 权利人:CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H; BIONUMERIK PHARMACEUTICALS INC 摘要:The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.
专利号:US-11565995-B2 优先权日:2020-04-17 标题:Methods of forming imines, imine-related and imine-derived compounds using green solvents 发明人:HELMS ERIC; BENNETT JACQUELINE 权利人:RESEARCH FOUNDATION FOR THE STATE UNIV OF NEW YORK; UNIV NEW YORK STATE RES FOUND 摘要:The present disclosure relates to using green solvents to synthesize an array of imines, imine-related and imine-derived compounds in an efficient and eco-friendly matter, satisfying green chemistry requirements. Reaction embodiments are performed using solvents, such as ethyl lactate and dimethyl isosorbide, which are both individually characterized as green. In embodiments, solvents include lactic whey and/or water as co-solvents. In these green solvents, the synthesis process discussed herein can produce up to quantitative yields of product at room temperature in a short duration. Embodiments include a method of forming an imine, imine-related or imine-derived compound product. In embodiments, the methods include mixing an aldehyde reactant with a nucleophilic/nitrogen-containing reactant in a green solvent at a temperature between negative twenty degrees Celsius (−20° C.) and positive fifty degrees Celsius (50° C.); stirring the mixture; and forming an imine, imine-related or imine-derived compound product.
1: Aricò F, Aldoshin AS, Tundo P. One-Pot Preparation of Dimethyl Isosorbide from d-Sorbitol via Dimethyl Carbonate Chemistry. ChemSusChem. 2017 Jan 10;10(1):53-57. doi: 10.1002/cssc.201601382. Epub 2016 Dec 22. 24(1):354-358. doi: 10.1021/acs.orglett.1c04018. Epub 2021 Dec 28. 8(4):502-4. doi: 10.1023/a:1015807413141. 46(3):265-71. doi: 10.1016/s0939-6411(98)00030-7.
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