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-8420850-B2 优先权日:2010-05-14 标 题:Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers 发明人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE 权利人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE; IBERHOSPITEX SA 摘要:The invention comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. The invention also comprises the processes for preparing the compounds and the polymers, and to the use of these polymers for the manufacture of medical devices.
专利号:US-5043328-A 优先权日:1986-05-09 标 题 :Formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems 发明人:WEITHMANN KLAUS U 权利人:HOECHST AG 摘要:The present invention relates to formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems and to the use of such formulations for the preparation of medicaments which are suitable for curing prostaglandin deficiencies in humans or animal, for example healing or preventing diseases of the gastro-intestinal tract.
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-8304409-B2 优先权日:2002-07-03 标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA 摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
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.
1: Sanphui P, Bolla G, Nangia A, Chernyshev V. Acemetacin cocrystals and salts: structure solution from powder X-ray data and form selection of the piperazine salt. IUCrJ. 2014 Feb 28;1(Pt 2):136-50. doi: 10.1107/S2052252514004229. eCollection 2014 Mar 1. 2: Shehata TM, Abdallah MH, Ibrahim MM. Proniosomal oral tablets for controlled delivery and enhanced pharmacokinetic properties of acemetacin. AAPS PharmSciTech. 2015 Apr;16(2):375-83. doi: 10.1208/s12249-014-0233-5. Epub 2014 Oct 16. 3: Cebeci F, Yaşar Ş, Aytekin S, Güneş P. Acemetacin-induced fixed drug eruption. Indian J Pharmacol. 2016 Mar-Apr;48(2):219-20. doi: 10.4103/0253-7613.178824.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 摘要:Lead Optimization for Medicinal Chemists. Zaragoza Dorwald F. (2012). Wiley-VCH 摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355