CAS: 17230-88-5; Danazol

上下游产品

17α-ethenyl-17β-hydroxy-2-hydroxymethylene-4-androsten-3-one 3-ethoxy-17α-ethynylandrosta-3,5-dien-17β-ol-3-one Androstenedione 3-ethoxyandrosta-3,5-dien-17-one17β-hydroxy-2-(hydroxymethyl)-17α-pregna-1,4-dien-20-yn-3-one 17α-ethynyl-17β-hydroxy-2α-hydroxymethyl-4-androsten-3-one

雄烯二酮置于吡啶,硫酸,盐酸羟胺,Sodium Ethanolate,Sodium Acetate,对甲苯磺酸,溶剂黄146,Potassium Hydroxide体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应 93.0H,反应生成达那唑
参考文献:达那唑的制备方法
标题:达那唑的制备方法
摘要:本发明公开了一种达那唑及其中间体的制备方法,它是以雄甾烯二酮为起始原料,经3位烯醇醚化,17位羰基乙炔化,3位水解化,2位次甲羟化以及肟化制得达那唑.3位烯醇醚化是先由雄甾烯二酮与原甲酸三乙酯在无水乙醇以及对甲苯磺酸的存在下,在30~50oc的温度下反应4~10H;然后再在0~10oc的温度下加入三乙胺继续反应0.2~1H;17位羰基乙炔化是先将氢氧化钾粉在乙炔气流中,在5~10oc的温度下反应1~2H;然后再与3位烯醇醚化产物在四氢呋喃以及催化剂的存在下,在15~30oc的温度下在乙炔气流中反应2~4H.本发明的3位烯醇醚化反应条件温和,收率较高,而17位羰基乙炔化反应收率较高,时间也较短.

专利信息

专利号:US-2008146656-A1
优先权日:2005-06-01
标题:Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone
发明人：REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD
权利人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD
摘要:There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.

专利号:US-5438134-A
优先权日:1990-07-09
标 题:Process for the production of unsaturated 17 α-cyanomethyl-17 β-h
发明人：TEICHMUELLER GERHARD; MUELLER GERD
权利人:JENAPHARM GMBH
摘要:The unsaturated 17α-cyanomethyl-17β-hydroxy steroids of the formula I, ##STR1## in which R 1 =Me, Eth; R 2 =H, Me; R 3 =H, OH, an acetoxy or alkoxy group; R 4 =H, R 5 =OH, an acetoxy, alkoxy group of R 4 and R 5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R 1 to R 5 by reacting the unsaturated 17-ketosteroids with LiCH 2 CN and subsequently hydrolyzing. n The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions. n The compounds are suitable for the treatment of endometriosis and also in combination with preparations with ethinylestradiol for fertility control.

专利号:US-12054512-B2
优先权日:2017-11-10
标 题 :Sting modulator compounds, and methods of making and using
发明人：VYSKOCIL STEPAN; CIAVARRI JEFFREY; CULLIS COURTNEY; ENGLAND DYLAN BRADLEY; GOULD ALEXANDRA E; GREENSPAN PAUL; HU YONGBO; LANGSTON STEVEN; LI GANG; MIZUTANI HIROTAKE; OKANIWA MASANORI
权利人:TAKEDA PHARMACEUTICALS CO
摘要:The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases.The present disclosure relates to a compound represented by the Formula (I):wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.

专利号:US-8372881-B2
优先权日:2005-06-20
标题 :Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use
发明人：ZERANGUE NOA; JANDELEIT BERND; LI YUNXIAO; GALLOP MARK A
权利人:XENOPORT INC; ZERANGUE NOA; JANDELEIT BERND; LI YUNXIAO; GALLOP MARK A
摘要:Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

专利号:US-6333317-B1
优先权日:1997-03-28
标 题:Regulation of amyloid precursor protein (APP) expression by administration of an estrogenic compound
发明人：LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that lipophilic hormones that interact with cytosolic or nuclear receptors regulate APP expression and synthesis, through modification of APP mRNA stability and/or regulation of APP gene transcription and translation activities. These studies demonstrate that the treatment of brain cells with estrone or 17β-estradiol results in a reduction in the level of APP holoprotein expression, without a concomitant change in the total level of cell protein. The reduction in the level of APP holoprotein caused by estrone or 17β-estradiol is also expected to reduce the production of neurotoxic APP fragments. In as much as estrogen deficiency in postmenopausal women is associated with a higher incidence of Alzheimer's disease, this discovery opens the possibility that estrogen therapy may prevent some of the neurodegenerative and cognitive changes associated with Alzheimer's disease, aging and other disease conditions associated with such neurodegenerative and cognitive decline.

专利号:US-12180228-B2
优先权日:2019-06-05
标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
发明人：MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.