CAS: 2098-66-0; Cyproterone

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cyproterone acetate

📜环丙氯地孕酮置于氢氧化钾体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,反应生成环丙孕酮
参考文献:Cyproterone Acetate Loading To Lipid Nanoparticles For Topical Acne Treatment: Particle Characterisation And Skin Uptake
标题:Cyproterone Acetate Loading To Lipid Nanoparticles For Topical Acne Treatment: Particle Characterisation And Skin Uptake
摘要:外用醋酸环丙孕酮(cpa)治疗皮肤病应减少副作用,目前男性不能使用这种药物,而女性则需要采取避孕措施.为了改善这种吸收率低的药物的皮肤渗透性,我们打算确定其活性分子,并将其装载到微粒载体系统中.我们测定了 Cpa 在人类成纤维细胞,角质细胞和皮脂细胞系中的代谢情况,以及原生 Cpa 和水解产物环丙孕酮的雄激素受体亲和力.利用人体体外皮肤对 Cpa 0.05%固体脂质纳米颗粒(sln),纳米结构脂质载体(nlc),纳米乳液和微球进行了药物-颗粒相互作用和 Cpa 吸收的表征.事实证明,原生 Cpa 是一种活性药物.应用附着在 Sln 上的 Cpa,其皮肤渗透率比从乳膏和纳米乳液中吸收的 Cpa 增加了至少四倍.与 Nlc 和微球的脂质基质结合后,Cpa 的吸收率增加了 2-3 倍.所有制剂在真皮层内的药量都很低.对完整皮肤和剥离皮肤的渗透率没有差异.使用微粒系统进行局部 Cpa 治疗可能是痤疮和其他皮脂腺疾病的另一种治疗选择.
Doi:10.1007/s11095-006-9225-9

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2024209029-A1
优先权日:2021-04-21
标题:Adiponectin glycopeptides and compositions and methods of use thereof
发明人：WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN
权利人:UNIV HONG KONG
摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.

专利号:US-2021220331-A1
优先权日:2016-05-03
标题:Inhibitors of ires-mediated protein synthesis
发明人：GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA
权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.

专利号:US-10975069-B2
优先权日:2014-04-01
标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
发明人：HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
权利人:UNIV WASHINGTON
摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

专利号:US-8481519-B2
优先权日:2005-02-05
标题 :Isolation of atraric acid, synthesis of atraric acid derivatives, and use of atraric acid and the derivatives thereof for the treatment of benign prostatic hyperplasia, prostate carcinoma and spinobulbar muscular atrophy
发明人：HOFFMANN HANS-RAINER; MATUSCH RUDOLF; BANIAHMAD ARIA
权利人:HOFFMANN HANS-RAINER; MATUSCH RUDOLF; BANIAHMAD ARIA; LOHMANN THERAPIE SYST LTS
摘要:A method for isolating atraric acid from biological material, atraric acid derivatives, the chemical synthesis thereof, and the use of atraric acid and the derivatives thereof for treating or producing a medicament for treating benign prostate hyperplasia, prostate carcinoma or spinobulbar muscular atrophy is provided. In addition, a basic substance for the development of other agents used for treating benign prostate hyperplasia, prostate carcinoma, or spinobulbar muscular atrophy is provided.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.