CAS: 198481-33-3; Bazedoxifene Acetate

1-[[4-[2-(氮杂环庚烷-1-基)乙氧基]苯基]甲基]-2-(4-羟基苯基)-3-甲基-吲哚-5-醇置于溶剂黄146体系中,化学反应生成醋酸巴多昔芬
参考文献:Processes For The Synthesis Of Bazedoxifene Acetate And Intermediates Thereof
标题:Processes For The Synthesis Of Bazedoxifene Acetate And Intermediates Thereof
摘要:高效合成药用化合物的过程,如(1-[4-(2-Azepan-1-Yl-Ethoxy)-Benzyl]-2-(4-Hydroxy-Phenyl)-3-Methyl-1H-Indol-5-Ol 醋酸,通常称为bazedoxifene 醋酸盐(化学式 Ix),使用公式 Iii 中的氰甲氧基苄卤代物,其中 X=卤素,如 Cl,F,Br,I;G=任何电子给体或电子受体取代基.

专利信息

专利号:US-2012253038-A1
优先权日:2009-04-13
标 题:Processes for the synthesis of bazedoxifene acetate and intermediates thereof
发明人：JOSHI SHREERANG; BHUTA SACHIN; TALUKDAR SANJAY; SAWANT SUDHIR; VENKATRAMAN DEEPAK
权利人:JOSHI SHREERANG; BHUTA SACHIN; TALUKDAR SANJAY; SAWANT SUDHIR; VENKATRAMAN DEEPAK; SANDOZ AG
摘要:Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent.

专利号:WO-2013001511-A1
优先权日:2011-06-30
标题 :Novel salt intermediates for the synthesis of bazedoxifene acetate and process thereof
发明人：LUTHRA PARVEN KUMAR; BHUTA SACHIN; NAIR RAJI; SALUNKE SANJUKUMAR; VENKATARAMAN DEEPAK
权利人:SANDOZ AG; LUTHRA PARVEN KUMAR; BHUTA SACHIN; NAIR RAJI; SALUNKE SANJUKUMAR; VENKATARAMAN DEEPAK
摘要:The present invention relates to novel salts of 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-5-benzyloxy-2-(4-benzyloxy-phenyl)-3-methyl-1-H-indole which are useful intermediates in the production of (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1-H- indol-5-ol acetic acid commonly known as bazedoxifene acetate and related compounds.

专利号:US-10844047-B2
优先权日:2018-06-21
标题:Process for the preparation of bazedoxifene
发明人：FERRARI MASSIMO; ZANI DANIELE DE; VEZZOSI STEFANO; BELOTTI PAOLO
权利人:ERREGIERRE SPA
摘要:The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate.

专利号:US-9365532-B1
优先权日:2011-02-14
标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
发明人：ISAACMAN STEVEN
权利人:ISAACMAN STEVEN; NANOMETICS LLC
摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.

专利号:US-2024336679-A1
优先权日:2021-08-06
标题 :Methods for the treatment of cancer
发明人：LINARES LÆTITIA; FIRMIN NELLY; MANTEAUX GABRIELLE
权利人:INST REGIONAL CANCER MONTPELLIER; INST NAT SANTE RECH MED; UNIV MONTPELLIER
摘要:The present disclosure relates to an Interleukin-6 (IL-6) signaling inhibitor selected from an IL-6 inhibitor, an IL-6 receptor inhibitor, an IL-6/IL-6 receptor complex inhibitor, a gp130 inhibitor and a STAT3 inhibitor or a pharmaceutical composition comprising such an IL-6 signaling inhibitor. for use in a method for treating and/or preventing cancer in a subject in need thereof. wherein the subject has been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin. The inventors have observed that cancers exhibiting recruitment of MDM2 to chromatin have been shown to secrete IL-6 that in turn acts on myoblast cells to activate serine synthesis. Following these surprising and unexpected observations. the inventors set up methods of treatment that are able to induce cancer cells death in subjects that have been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin.