CAS: 51-98-9; Norethisterone Acetate

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CAS号68-22-4 炔诺酮 | CAS号64-19-7 冰醋酸 | CAS号108-24-7 乙酸酐 | CAS号2205-78-9 (17α)-19-去甲孕烯酸-... | CAS号472-54-8 19-去甲睾酮

19-去甲-17-Alpha-孕甾-3,5-二烯-20-炔-3,17-二醇二乙酸酯置于四氢呋喃,氢氧化钾体系中,化学反应生成 炔诺酮醋酸酯
参考文献:Steroids. Cvii.1 δ5(6)-19-Nor Steroids,A New Class Of Potent Anabolic Agents2
标题:Steroids. Cvii.1 δ5(6)-19-Nor Steroids,A New Class Of Potent Anabolic Agents2
摘要:
DOI:10.1021/ja01511A042

专利信息

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-10022366-B2
优先权日:2013-04-23
标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery
发明人：STINCHCOMB AUDRA L; GHOSH PRIYANKA
权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND
摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.

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.

专利号:US-7667056-B2
优先权日:2002-08-02
标 题 :Process and new intermediates for the preparation of steroids with a progestogen activity
发明人：GRISENTI PARIDE; PECORA FABIO; VERZA ELISA; LEONI MASSIMO; BOSSI LAURA
权利人:POLI IND CHIMICA SPA
摘要:The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III).

专利号:US-6225298-B1
优先权日:1994-11-22
标 题 :Compositions and methods for contraception and for treatment of benign gynecological disorders
发明人：SPICER DARCY V; PIKE MALCOLM CECIL; DANIELS JOHN R
权利人:BALANCE PHARMACEUTICALS INC
摘要:Compositions and methods for use in preventing conception or treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixtures thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premenstrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.

专利号:US-2008234340-A1
优先权日:2007-03-09
标 题:Synthesis and characterization of polymorph form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-YL)thiazol-4-YL)benzonitrile
发明人：MIRMEHRABI MAHMOUD; NIU YUPING; TADAYON ABDOLSAMAD; DESHMUKH SUBODH; KU MANNCHING SHERRY
权利人:WYETH CORP
摘要:A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. n Further provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.