CAS: 1961-77-9; Chlormadinone

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CAS号302-22-7 氯地孕酮醋酸盐

醋酸氯地孕酮置于sodium Hydroxide,水体系中,用 甲醇 用作溶剂,化学反应 2.0H,以56.9%的收率获得氯地孕酮
参考文献:新型 C-6 取代和未取代孕烷衍生物作为 5α-还原酶抑制剂及其对仓鼠胁腹器官直径大小的影响
标题:新型 C-6 取代和未取代孕烷衍生物作为 5α-还原酶抑制剂及其对仓鼠胁腹器官直径大小的影响
摘要:本研究旨在确定在 C-6 (12A-12D) 处具有氯取代基,在 C-6 和 14A-14D 处具有溴取代基的 15,C-6 处没有任何卤素原子的几种孕酮衍生物的抑制作用所有在人前列腺中存在的 5α-还原酶活性的 C-17(苯甲酸酯在苯环的 C-4 位置带有一个 Cl,F 和一个 Br 原子)具有酯侧链.此外,研究对仓鼠胁腹器官直径大小的药理作用也很有趣.为了研究类固醇 12A-12D,14A-14D 和 15 的构效关系,我们确定了这些类固醇抑制人前列腺 5α-还原酶 (Ic(50)) 50% 活性的浓度,以及由于这些化合物对仓鼠胁腹器官直径大小的体内作用.我们还使用标记的米勃龙 (Mib) 监测与雄激素受体的结合,确定了这些类固醇与大鼠前列腺细胞质中存在的雄激素受体结合的能力.该研究的结果表明,化合物 12A-12D(在 C-6 处具有氯取代基),14A-14D(在 C-6 处缺少卤素原子),13
Doi:10.1016/j.Steroids.2009.04.009

专利信息

专利号:WO-2013056547-A1
优先权日:2011-10-22
标题 :Synthesis of a group of hydantoin derivatives and use thereof
发明人：CHEN DEGUI
权利人:CHEN DEGUI
摘要:Provided in the present invention are the pharmaceutical composition, synthesis procedure and medicinal use of a group of HYDANTOIN derivatives. Since these compounds have an inhibiting effect on an androgen receptor, the compounds can be used to treat prostate cancer and other diseases and physiological disorders related to androgen receptor activity.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

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-6150403-A
优先权日:1997-10-14
标 题 :Topical compositions for regulating the oily/shiny appearance of skin
发明人：BIEDERMANN KIMBERLY A; SCHUBERT HARRY L; PARRAN JR JOHN J
权利人:PROCTER & GAMBLE
摘要:The present invention relates to methods for inhibiting sebaceous gland activity in mammalian skin comprising administration of a topical composition comprising dehydroacetic acid or pharmaceutically acceptable salts thereof, and a dermatologically-acceptable carrier. The present invention also relates to methods and topical compositions further comprising agents which regulate the oily and/or shiny appearance of skin, and agents which treat acne and related skin disorders in mammalian skin and scalp. Methods of reducing sebum synthesis with the use of dehydroacetic acid, methods of regulating the oily and/or shiny appearance of skin, and methods of treating acne and other skin disorders are also encompassed by the present invention.

专利号:US-2004024230-A1
优先权日:2002-04-29
标 题:Synthesis of cyproterone acetate

专利号:US-2006211873-A1
优先权日:2002-04-29
标 题 :Synthesis of cyproterone acetate
发明人：MANOSROI ARANYA; MANOSROI JIRADEJ; BUDDHASUKH DUANG; SRIPALAKIT PATTANA; MAIER ROLAND; WERNER ROLF G
权利人:BOEHRINGER INGELHEIM INT
摘要:The present invention relates to improved methods for synthesising cyproterone acetate (17α-Acetoxy-6-chloro-1α, 2(α-methylene-4,6-pregnadiene-3,20-dione) from solasodine.