57-83-0 = 52-39-1 + 80-75-1 反应条件:1.1 Catalysts: β-Cyclodextrin Solvents: Ethanol; 48 H,Ph 5.5,30 °C 标题:Approaches To Improve The Solubility And Availability Of Progesterone Biotransformation By Mucor Racemosus 作者:Mohamed,Sayeda Saleh; Et Al 参考文献:Biocatalysis And Biotransformation 日期:2014 卷标:32(3) 页码:141-150
📜Rac-21-Acetoxy-11β-Hydroxy-3,20-Dioxo-Pregn-4-En-18-Al置于1,4-二氧六环,Chromium(Vi) Oxide,盐酸,甲醇,Lithium Aluminium Tetrahydride,乙醚,对甲苯磺酸,乙二醇,溶剂黄146体系中,化学反应生成 醛固酮 参考文献:11-氧基-D-Progesteron-18-Säure-Lacton-(1811)und Teilsynthese冯d-Aldosteron Aus D-Corticosteron-18-Säure-Lacton-(1811).93岁的斯托夫.斯特凡(beoff Bestandteile Der Nebennierenrinde Und Verwandte) 标题:11-氧基-D-Progesteron-18-Säure-Lacton-(1811)und Teilsynthese冯d-Aldosteron Aus D-Corticosteron-18-Säure-Lacton-(1811).93岁的斯托夫.斯特凡(beoff Bestandteile Der Nebennierenrinde Und Verwandte) 摘要:死überführung冯d-Aldosteron在d-Progesteron-18-Säure-Lacton-(18 11)(x)wird Beschrieben,Ebenso死rückverwandlung冯d-Corticosteron-18-Säure-Lacton-(18 11)在d-Aldosteron. DOI:10.1002/hlca.19550380615
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-8198465-B2 优先权日:2005-10-17 标 题 :3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors 发明人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT 权利人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT; NOVARTIS AG 摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, n nor a salt thereof, and a compound of formula VIn n nor a salt thereof, wherein R 3 and R 4 as well as Act are as defined in the specification, and processes of manufacturing these.n n Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.
专利号:US-2004033532-A1 优先权日:2002-08-08 标题 :Use of three-dimensional crystal structure coordinates to design and synthesize domain-selective inhibitors for angiotensin-converting enzyme (ACE) 发明人:EHLERS MARIO R W; HOLMQUIST BARTON 摘要:It has now been discovered that the use of the three-dimensional crystal structure coordinates of angiotensin-converting enzyme (ACE) will enable the design and synthesis, by means of computational chemistry and structure-guided drug design, of inhibitors of ACE that are highly selective and specific for either the N domain or the C domain of the enzyme, for the treatment of diverse diseases. The invention also relates to methods and processes for the structure-guided design and synthesis of dual N- and C-domain ACE inhibitors, and inhibitors that operate by competitive, non-competitive, uncompetitive, and irreversible mechanisms.
专利号:US-5455157-A 优先权日:1989-05-22 标 题:Method for the non-radioactive measurement of the nucleic acid synthesis in eukaryotic cells 发明人:HINZPETER MATTHIAS; ELTZ HERBERT VON DER 权利人:BOEHRINGER MANNHEIM GMBH 摘要:For the determination of the rate of nucleic acid synthesis in eukaryotic cells a nucleotide which is non-radioactively labelled or derivatized with a hapten is introduced into the cells with the addition of liposomes and the rate of synthesis of the nucleic acids is determined by means of the incorporation of the nucleotide via its label or derivatization.
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-2009325918-A1 优先权日:2008-06-16 标 题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:SOMBERG JOHN C; RANADE VASSANT V 权利人:SOMBERG JOHN C; RANADE VASSANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effect mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and it the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in men.
1: Lutshumba J, Mirsky E, Bullens KA, Smith EG, Ndashaala EL, Finch R. Renin- Angiotensin-Aldosterone System in Preeclampsia: Pathophysiological Insights and Links to Vascular Dementia. Arterioscler Thromb Vasc Biol. 2026 Feb 19. doi: 10.1161/ATVBAHA.125.321675. Epub ahead of print. 41(1):36. doi: 10.1007/s11011-025-01780-x. 23(2):e1004900. doi: 10.1371/journal.pmed.1004900. 5: Ohannesian VA, Rajchenberg D, Menezes IR, Han ML, Pereira KLA, Castro WCN, Fagundes AF, Suruagy Motta RFO, Neto MJF, Braga CAP, Silva MRC, Queiroz MRG, Nogueira SA. Pooled diagnostic accuracy of 68Ga-pentixafor PET/CT for aldosterone-producing lesions in primary aldosteronism. Clin Imaging. 2026 Mar;131:110743. doi: 10.1016/j.clinimag.2026.110743. Epub 2026 Feb 3. 130:289-312. doi: 10.1016/bs.vh.2025.10.009. Epub 2025 Dec 16.
合成参考文献
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