- A new compound and its preparation method and elimination method (by machine translation)
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The invention relates to medical and chemical field, provides a new compound, the compounds have the formula I structure, is preparing novel anti-breast cancer drug of fulvestrant in the process more difficult to avoid one of the impurity. The present invention provides a compound of formula I of the synthetic route, and to reduce or avoid the preparation of fluorine Uygursi Qun produced in the process of method, and in its generated after the method of removing it, not only reduces the growing into this impurity the waste of raw materials, also there to have ruled out the impurities to the rear edge of fulvestrant to purification of the product and the impact of the yield. (by machine translation)
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Paragraph 0034; 0035
(2018/01/06)
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- TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
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Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
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Page/Page column 59
(2016/12/22)
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- Fulvestrant process for the preparation of intermediates
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The invention provides a preparation method of a fulvestrant intermediate. The preparation method of the fulvestrant intermediate is characterized in that a water extraction starting material 1,9-nonanediol is adopted for controlling the content of 1,8-octylene glycol, an antioxidant is added for reducing byproducts which are generated by Michael addition and difficult to purify and pH value is regulated for reducing production of aromatized impurities difficult to remove, so that a route for preparing fulvestrant by virtue of the fulvestrant intermediate has the advantages that a final product is difficult to purify, the cost is low and industrialization can be easily realized. The prepared fulvestrant intermediate lays a key foundation for obtaining a route for synthesizing fulvestrant which is easy to purify and easy for industrialization.
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Paragraph 0106-0108
(2017/03/08)
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- PROCESS AND INTERMEDIADES FOR THE PREPARATION OF 7-ALKYLATED STEROIDS
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A process for preparing compounds of formula (I), or a salt, solvate or stereoisomer thereof, including Fulvestrant, which process comprises free radical to a compound of formula (III), or a salt, solvate or stereoisomer thereof. The invention also refers to intermediates of said process.
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Page/Page column 58
(2015/12/17)
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- PROCESS FOR PREPARING 7-ALPHA-[9-(4,4,5,5,5-PENTAFLUOROTHIOPENTYL) NONYL]ESTRA-1,3,5(10)-TRIENE-3,17-BETA-DIOL
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A process is described for the industrial scale preparation of 7a-[9-(4,4,5,5,5- 5 pentafluorothiopentyI)nonyl]estra-1,3,5(10)-triene-3,17?-diol, a precursor of steroids with hormonal activity which include Fulvestrant.
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Paragraph 0080; 0081; 0082
(2014/09/02)
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- GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, MANUFACTURING METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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Disclosed are compounds useful as gonadotropin-releasing hormone ("GnRH") receptor antagonist.
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Page/Page column 86
(2011/12/12)
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- ITZ-1, a Client-Selective Hsp90 Inhibitor, Efficiently Induces Heat Shock Factor 1 Activation
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ITZ-1 is a chondroprotective agent that inhibits interleukin-1β-induced matrix metalloproteinase-13 (MMP-13) production and suppresses nitric oxide-induced chondrocyte death. Here we describe its mechanisms of action. Heat shock protein 90 (Hsp90) was identified as a specific ITZ-1-binding protein. Almost all known Hsp90 inhibitors have been reported to bind to the Hsp90 N-terminal ATP-binding site and to simultaneously induce degradation and activation of its multiple client proteins. However, within the Hsp90 client proteins, ITZ-1 strongly induces heat shock factor-1 (HSF1) activation and causes mild Raf-1 degradation, but scarcely induces degradation of a broad range of Hsp90 client proteins by binding to the Hsp90 C terminus. These results may explain ITZ-1's inhibition of MMP-13 production, its cytoprotective effect, and its lower cytotoxicity. These results suggest that ITZ-1 is a client-selective Hsp90 inhibitor.
- Kimura, Haruhide,Yukitake, Hiroshi,Tajima, Yasukazu,Suzuki, Hirobumi,Chikatsu, Tomoko,Morimoto, Shinji,Funabashi, Yasunori,Omae, Hiroaki,Ito, Takashi,Yoneda, Yukio,Takizawa, Masayuki
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supporting information; experimental part
p. 18 - 27
(2010/08/06)
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- Fulvestrant: From the laboratory to commercial-scale manufacture
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The development of a commercial manufacturing process for fulvestrant (the active ingredient in 'Faslodex') is described. Key steps in the synthesis are stereoselective 1,6-addition of an organocuprate to a steroidal dienone followed by copper-mediated aromatisation of the A-ring. The strategy for dealing with noncrystalline intermediates is outlined. The production of drug substance of acceptable quality is critically dependent on limiting the formation of key impurities. The origin of these impurities is discussed, and measures to prevent or control their formation are described.
- Brazier, Eve J.,Hogan, Philip J.,Leung, Chiu W.,O'Kearney-McMullan, Anne,Norton, Alison K.,Powell, Lyn,Robinson, Graham E.,Williams, Emyr G.
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experimental part
p. 544 - 552
(2011/07/30)
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- Discovery of thiochroman and chroman derivatives as pure antiestrogens and their structure-activity relationship
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In order to develop pure antiestrogens, a series of 7-hydroxy-3-(4-hydroxyphenyl)-3-methylchroman and 7-hydroxy-3-(4-hydroxyphenyl)-3-methylthiochroman derivatives with sulfoxide containing side chains at the 4-position were designed, synthesized, and eva
- Kanbe, Yoshitake,Kim, Myung-Hwa,Nishimoto, Masahiro,Ohtake, Yoshihito,Kato, Nobuaki,Tsunenari, Toshiaki,Taniguchi, Kenji,Ohizumi, Iwao,Kaiho, Shin-ichi,Morikawa, Kazumi,Jo, Jae-Chon,Lim, Hyun-Suk,Kim, Hak-Yeop
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p. 4803 - 4819
(2007/10/03)
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- Process for the preparation of 7alpha-alkylated 19-norsteroids
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Processes useful in the preparation of pharmaceutical compounds such as fulvestrant and processes for the preparation of fulvestrant.
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Page/Page column 25
(2008/06/13)
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- PENTAFLUOROALKANESULFINYL NAPHTHALENES AND RELATED ESTROGEN RECEPTOR MODULATORS
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The present invention provides a compound of the formula (I) wherein R is -H, or -C1-C4 alkyl; R1 is -H, -OH, -O(C1-C4 alkyl), -SO2(C1-C4 alkyl), or halo; X is -O-, -C
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Page/Page column 13-14
(2008/06/13)
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- Benzopyran or thiobenzopyran derivatives
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The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.
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Page/Page column 107; 142-143
(2010/01/31)
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- Metal salts of 3-methyl-chromane or thiochromane derivatives
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The present invention relates to metal salts of 3-methyl-chromane or thiochromane derivatives, stereoisomers or hydrates thereof, and an anti-estrogenic pharmaceutical composition which comprises the above compound as an active component and exhibits a hi
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- 3-ethyl-, 3-propyl- or 3-butyl-chroman and thiochroman derivatives
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A compound having the following general formula (1): in whichR1 represents an ethyl group, etc.;R2 represents a hydrogen atom, etc.;R3 represents a C1-C5 perhalogenoalkyl group, etc.;each of R4 and R5 independently represents a hydrogen atom, etc.;X represents an oxygen atom or a sulfur atom;m represents an integer of 2 to 14; andn represents an integer of 2 to 7;or an enantiomer of the compound, or a hydrate or a pharmaceutically acceptable salt of the compound or its enantiomer is advantageous in pharmaceutical use because of its anti-estrogenic activity.
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