CAS: 851983-85-2; (3S,8R,9S,10R,13S,14S)-17-(Benzimidazol-1-yl)-10,13-Dimethyl-2,3,4,7,8,9,11,12,14,15-Decahydro-1H-Cyclopenta[a]Phenanthren-3-Ol

上下游产品

CAS号851895-79-9 (3beta)-17-(1H-... | CAS号851895-78-8 (3BETA)-3-(乙酰氧基... | CAS号51-17-2 苯并咪唑 | CAS号1865-56-1 (10R,13S)-17-Ch...

(3Beta)-3-(乙酰氧基)-17-(1H-苯并咪唑-1-基)雄甾-5,16-二烯-16-甲醛置于氢氧化钾,Palladium On Activated Charcoal,苯甲腈体系中,用 甲醇 作为反应溶剂,化学反应 6.5H,反应生成 (3Beta)-17-(1H-苯并咪唑-1-基)雄甾-5,16-二烯-3-醇
参考文献:新型c-17-杂芳基甾体cyp17抑制剂/抗雄激素药物:在lapc4人前列腺癌异种移植模型中的合成,体外生物活性,药代动力学和抗肿瘤活性.
标题:新型c-17-杂芳基甾体cyp17抑制剂/抗雄激素药物:在lapc4人前列腺癌异种移植模型中的合成,体外生物活性,药代动力学和抗肿瘤活性.
摘要:合理设计和合成了新的化学实体,甾类c-17苯并唑(5,6,9和10)和吡嗪(14和15).合成苯并恶唑的关键反应涉及亲核性乙烯基"加成消除"取代反应,该反应包括3β-乙酰氧基-17-氯-16-甲醛基-5,16-二烯(2)和苯并恶唑亲核反应,而吡嗪的合成反应涉及钯催化的17-碘-雄甾烯5,16-Dien-3Beta-Ol(13)与三丁基锡烷基二嗪的交叉偶联反应.已显示某些化合物是人cyp17酶的有效抑制剂,以及野生型和突变雄激素受体(ar)的有效拮抗剂.最有效的cyp17抑制剂是3Beta-Hydroxy-17-(1H-Benzimidazole-1-Yl)androsta-5,16-Diene(5,代号vn / 124-1),3Beta-Hydroxy-17-(5(1)-嘧啶基)androsta-5,16-二烯(15)和17-(1H-苯并咪唑-1-基)androsta-4,16-Dien
DOI:10.1021/jm040202W

专利信息

专利号:US-12391725-B2
优先权日:2016-06-22
标题:Method for production of novel galeterone analogs and uses thereof
发明人：NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS
权利人:NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT
摘要:Galeterone and its C-3 analogs are of substantial interest because of their multi-target anticancer activities, including AR and Mnk degrading activities. Provided are novel procedures for gram-scale, high-yield synthesis of C-3 analogs of galeterone, including 3β-(1H-imidazole-1-yl)-17-(1H-benzimidazole-1-yl)-androsta-5,16-diene (galeterone 3β-imidazole) and 3β-(pyridine-4-ylmethoxy)-17-(1H-benzimidazol-1-yl)androsta-5,16-diene (galeterone 3β-pyridine methoxylate).

专利号:US-11708381-B2
优先权日:2016-11-25
标题:Inhibitors of androgen receptor signaling
发明人：WANG GUANGDI; LIU JIAWANG; ZHENG SHILONG; GUO SHANCHUN
权利人:XAVIER UNIV OF LOUISIANA
摘要:The present disclosure relates to androgen receptor signaling inhibitors and the synthesis of the same. Further, the present disclosure teaches the utilization of the androgen receptor signaling inhibitors in a treatment for proliferative diseases, including cancer, particularly prostate cancer, and especially castration-resistant prostate cancer.

专利号:US-9884067-B2
优先权日:2013-03-14
标 题:Androgen receptor down-regulating agents and uses thereof
发明人：NJAR VINCENT C O; GEDIYA LALJI K; PURUSHOTTAMACHAR PURANIK; GODBOLE ABHIJIT; KWEGYIR AFFUL ANDREW; VASAITIS TADAS
权利人:UNIV OF MARYLAND EASTERN SHORE; UNIV JEFFERSON; UNIV MARYLAND
摘要:The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.

专利号:WO-2017208132-A1
优先权日:2016-06-01
标 题 :Process for the preparation of galeterone
发明人：BARBIERI FRANCESCO; LENNA ROBERTO
权利人:IND CHIMICA SRL
摘要:A process for the synthesis of 3β-hydroxy-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (I) given below.

专利号:US-11390645-B2
优先权日:2016-08-08
标题:Process for the preparation of 3β-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene
发明人：BARBIERI FRANCESCO; LENNA ROBERTO
权利人:IND CHIMICA SRL
摘要:A process for the synthesis of β-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (6).

专利号:US-2012295932-A1
优先权日:2011-05-17
标 题 :Method for the treatment of cancer
发明人：FERLINI CRISTIANO; MARIANI MARISA; SHAHABI SHOHREH
权利人:FERLINI CRISTIANO; MARIANI MARISA; SHAHABI SHOHREH; WESTERN CONNECTICUT HEALTH NETWORK INC
摘要:Provided is a method for determining the prognosis of cancer in a female patient with a solid tumor. Also provided is a method of sensitizing a cancer cell from a solid tumor from a male patient other than a prostate cancer cell to treatment with a chemotherapeutic agent comprising administering an effective amount ofn (a)n (i) at least one antiandrogen; (ii) at least one inhibitor of androgen synthesis; or (iii) a combination of at least one antiandrogen and at least one inhibitor of androgen synthesis; and n (b) at least one chemotherapeutic agent other than an antiandrogen or an inhibitor of androgen synthesis for the treatment of cancer characterized by a solid tumor, other than prostate cancer, in a male patient. The antiandrogen, the inhibitor of androgen synthesis, or the combination of both may be administered before, after, or at the same time as the chemotherapeutic agent.