CAS: 516-72-3; (8S,9S,10R,13S,14S,17S)-17-((R)-2-Hydroxy-6-Methylheptan-2-yl)-10,13-Dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-Tetradecahydro-1H-Cyclopenta[a]Phenanthren-3-Ol

上下游产品

Pregnenolone acetate isohexylmagnesium bromide cholesterol 3,6-Dioxo-20α-hydroxy-5α-cholestan Pregnenolone

📜3β-T-Butyldimethylsilyloxy-Cholest-5-En-22-Yn-20(R)-Ol置于10% Pd/c,氢气体系中,用 二氯甲烷,乙酸乙酯 作为反应溶剂,化学反应生成 20Alpha-羟基胆固醇
参考文献:新型氧固醇激活刺猬通路并诱导成骨
标题:新型氧固醇激活刺猬通路并诱导成骨
摘要:在涉及骨骼修复的整形外科手术过程中,例如局部手术治疗非骨性骨折和椎间盘退变,骨形成的局部诱导是必不可少的.本文中,我们公开了设计为合成代谢骨生长剂的新型氧固醇衍生物的合成和生物学评估.氧固醇的结构-活性关系研究4已经确定类似物如18,21和30.这些新的类似物的特征在于成骨细胞分化测定法中的效力更高和/或人肝微粒体中代谢稳定性的提高.氧固醇4,18和21 在大鼠脊髓融合模型中进行体内评估.
DOI:10.1016/j.Bmcl.2012.07.073

专利信息

专利号:US-7339065-B2
优先权日:2003-07-21
标题 :Design and synthesis of optimized ligands for PPAR
发明人：AVERY MITCHELL A; PERSHADSINGH HARRIHAR A
权利人:BETHESDA PHARMACEUTICALS INC; UNIV MISSISSIPPI
摘要:This invention provides new chemical entities useful for treating a variety of clinical disorders including those that are influenced by the activity of peroxisome proliferator activated receptors (PPAR). The structures of the compounds and methods to design, make and use the compounds are provided. Compounds and methods for administering therapeutic compositions comprising the compounds in cases of the disease psoriasis are provided. An exemplary compound having the formula compound is 5adamantan-2-yl-pentanoic acid {2-[4-(2,4-dioxo-thiazolidin-5-yl-methyl)-phenoxy]-ethyl}-methyl-amide is provided.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:EP-1886695-A1
优先权日:2006-06-27
标 题:Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist
发明人：SCHUMACHER CHRISTOPH
权利人:SPEEDEL EXPERIMENTA AG
摘要:The invention relates to a pharmaceutical combination comprising (a) an aldosterone synthase inhibitor or a pharmaceutically acceptable salt thereof, and (b) a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a cortisol re-synthesis inhibitor or a corticotrophin-releasing hormone receptor antagonist or combinations thereof or in each case a pharmaceutically acceptable salt thereof. Said composition is useful for the manufacture of a medicament, in particular for the manufacture of a medicament for the prevention of, delay of progression of treatment of a disease or condition characterized by the metabolic syndrome.

专利号:US-2024299311-A1
优先权日:2022-04-05
标题 :Ionizable cationic lipids and lipid nanoparticles
发明人：KARMALI PRIYA PRAKASH; TANIS STEVEN
权利人:KARMALI PRIYA PRAKASH; TANIS STEVEN; CAPSTAN THERAPEUTICS INC
摘要:Ionizable cationic lipids, methods for synthesizing them, as well as intermediates useful in synthesis of these lipids and methods of synthesizing the intermediates are disclosed. The ionizable cationic lipids are useful as a component of lipid nanoparticles (LNP), which in turn can be used for the delivery of nucleic acids into cells in vivo or ex vivo. LNP compositions are also disclosed, including LNP comprising a functionalized lipid to enable conjugation of a binding moiety, and targeted LNP (tLNP), that is a LNP in which a binding moiety has been conjugated to the functionalized lipid and can serve as a targeting moiety to direct the tLNP to a desired tissue or cell type.

专利号:US-2012258938-A1
优先权日:2008-02-28
标题:Enzymatic Production or Chemical Synthesis and Uses for 5,7-Dienes and UVB Conversion Products Thereof
发明人：SLOMINSKI ANDREJ; TUCKEY ROBERT C; TANG EDITH; TIEU ELAINE; NGUYEN MINH; JANJETOVIC ZORICA; CHEN JIANJUN; LI WEI; LU YAN; MILLER DUANE D; ZJAWIONY JORDAN K; POSTLETHWAITE ARNOLD E
权利人:SLOMINSKI ANDREJ; TUCKEY ROBERT C; TANG EDITH; TIEU ELAINE; NGUYEN MINH; JANJETOVIC ZORICA; CHEN JIANJUN; LI WEI; LU YAN; MILLER DUANE D; ZJAWIONY JORDAN K; POSTLETHWAITE ARNOLD E
摘要:Provided herein are steroidal compounds that are androsta-5,7-dienes or pregna-5,7-dienes and ultraviolet B (UVB) conversion products thereof and cholecalciferol derivatives hydroxylated at one or more of C1, C17, C20, C23, C24, C25, and C26 which includes pharmaceutical, cosmeceutical or nutraceutical compositions of the steroidal compounds as shown in Tables 1A, 2A and 3. Also provided is a method for producing hydroxylated metabolites of cholecalciferol via CYP11A1, CYP24, CYP27A1, or CYP27B1 enzyme systems where the hydroxylase has an activity to hydroxylate position C1 or C20 or other position of the sidechain of a secosteroid or its 5,7-dieneal precursor and the hydroxylated metabolites so produced. Methods are provided for inhibiting proliferation of either a normally or abnormally proliferating cell, for modifying immune activity, or for treating a condition associated with the proliferating or quiescent cell or immune cells by contacting the cell with or administering any of the compounds described herein.

专利号:WO-2025217452-A1
优先权日:2024-04-11
标 题 :Constrained ionizable cationic lipids and lipid nanoparticles
发明人：KARMALI PRIYA; TANIS STEVEN
权利人:CAPSTAN THERAPEUTICS INC
摘要:Ionizable cationic lipids, methods for synthesizing the same, intermediates useful in synthesis of the ionizable cationic lipids, and methods of synthesizing the intermediates are disclosed. The ionizable cationic lipids are useful as a component of lipid nanoparticles (LNP), which in turn can be used for delivering nucleic acids into cells in vivo or ex vivo. LNP compositions are also disclosed, including LNPs comprising a functionalized lipid to enable conjugation of a binding moiety, and targeted LNPs (tLNPs), that is, LNPs in which a binding moiety has been conjugated to the functionalized lipid and can serve as a targeting moiety to direct the tLNPs to a desired tissue or cell type.