专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:US-6281003-B1 优先权日:1996-05-20 标 题 :Enzymatic synthesis of optically active hydroxamic acids and their conversion to optically active primary amines by a lossen rearrangement 发明人:HIRRLINGER BEATE; STOLZ ANDREAS; KNACKMUSS HANS-JOACHIM 权利人:FRAUNHOFER GES FORSCHUNG 摘要:A method is described for the preparation of optically active hydroxamic acids of the general formula n wherein R 1 , R 2 and R 3 are different and are a cyclic or linear, aliphatic or aromatic, substituted or unsubstituted hydrocarbon radical which can optionally contain heteroatoms, said method being characterized in that a racemate of chiral amides, carboxylic acid esters or carboxylic acids of the general formula n wherein R 1 , R 2 and R 3 are as defined above and X is —NH 2 , —OR or —OH, R being any organic radical, n is reacted with hydroxylamine, NH 2 OH, in the presence of an acyltransferase, and the optically active hydroxamic acid (I) formed is then separated from the unconverted enantiomer of general formula (II). The resulting optically active hydroxamic acid can be converted to the corresponding optically active primary amines by a Lossen rearrangement.
专利号:US-9687428-B2 优先权日:2001-05-01 标题 :Hydrogel compositions for tooth whitening 发明人:SINGH PARMINDER; CLEARY GARY W; MUDUMBA SRI; FELDSTEIN MIKHAIL M; BAYRAMOV DANIR F 权利人:A V TOPCHIEV INST OF PETROCHEMICAL SYNTHESIS RUSSIAN ACAD OF SCIENCES; CORIUM INT INC; A V TOPCHIEV INST OF PETROCHEMICAL SYNTHESIS RUSSIAN ACAD OF SCIENCES 摘要:A composition is provided, wherein the composition comprises a water-swellable, water insoluble polymer, a blend of a hydrophilic polymer and a complementary oligomer capable of hydrogen bonding to the hydrophilic polymer, and a whitening agent, preferably a peroxide. The composition finds utility as a tooth whitening composition and is applied to the teeth in need of whitening, and then removed when the degree of whitening has been achieved. In certain embodiments, the composition is translucent. Methods for preparing and using the compositions are also disclosed.
专利号:AU-2022276509-A1 优先权日:2021-05-20 标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
1: Pan Y, Nixon R. Allergic contact dermatitis to topical preparations of bufexamac. Australas J Dermatol. 2012 Aug;53(3):207-10. doi: 10.1111/j.1440-0960.2012.00876.x. doi: 10.1016/j.jpba.2011.02.025. doi: 10.1097/DER.0b013e318260d774. doi: 10.1007/s00105-008-1656-2. German. doi: 10.1111/j.1346-8138.2011.01261.x. German. doi: 10.1111/j.1600-0536.2011.01883.x. doi: 10.1038/srep25298. 10: Trommer H, Plätzer M, Raith K, Wohlrab W, Podhaisky HP, Neubert RH. Examinations of the antioxidative properties of the topically administered drug bufexamac reveal new insights into its mechanism of action. J Pharm Pharmacol. 2003 Oct;55(10):1379-88. doi: 10.1111/j.1600-0536.2007.01271.x. German.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1111/j.1346-8138.2004.tb00524.x 摘要:Arikawa J, Okabe S, Kaneko T. Allergic Contact Dermatitis with Spreading over Extensive Regions Due to Topical Use of 5% Bufexamac Ointment. The Journal of Dermatology. 2004 Feb;31(2):136–8. doi: 10.1111/j.1346-8138.2004.tb00524.x. 参考文献:10.1111/j.1600-0536.2007.01271.x 摘要:Belhadjali H, Ghannouchi N, Njim L, Mohamed M, Moussa A, Bayou F, Chakroun M, Zakhama A, Zili J. Acute generalized exanthematous pustulosis induced by bufexamac in an atopic girl. Contact Dermatitis. 2008 Apr;58(4):247–8. doi: 10.1111/j.1600-0536.2007.01271.x. 参考文献:10.1007/s00105-009-1812-3 摘要:Schauber J. [Topical therapy of perianal eczema]. Hautarzt. 2010 Jan;61(1):33–8. doi: 10.1007/s00105-009-1812-3.