62108-37-6Relevant articles and documents
ESTROGEN RECEPTOR ANTAGONIST
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Paragraph 0211, (2021/10/07)
Provided is an indole compound. In particular, disclosed are a compound represented by formula (II) or an isomer or pharmaceutically acceptable salt thereof and a use of the same as an estrogen receptor antagonist in preparing a drug for treating estrogen receptor-positive breast cancer.
CRYSTAL FORM OF ESTROGEN RECEPTOR INHIBITOR AND PREPARATION METHOD THEREFOR
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Paragraph 0097-0098, (2020/08/20)
Disclosed are a crystal form of an estrogen receptor inhibitor and a preparation method therefor, in particular disclosed are a crystal form A of a compound of formula (I) and a preparation method therefor, and the use of the crystal form in the preparation of a drug for treating breast cancer.
γ-Carboline synthesis enabled by Rh(iii)-catalysed regioselective C-H annulation
Jiang, Bo,Jia, Jingwen,Sun, Yufei,Wang, Yichun,Zeng, Jing,Bu, Xiubin,Shi, Liangliang,Sun, Xiaoying,Yang, Xiaobo
supporting information, p. 13389 - 13392 (2020/11/10)
A redox-neutral Rh(iii)-catalyzed C-H annulation of indolyl oximes was developed. Relying on the use of various alkynyl silanes as the terminal alkyne surrogates, the reaction exhibited a reverse regioselectivity, thus giving an exclusive and easy way for the synthesis of a wide range of substituent free γ-carbolines at C3 position with high efficiency. Deuterium-labelling experiments and kinetic analysis have preliminarily shed light on the working mode of this catalytic system. This journal is
INDOLO-SUBSTITUTED-PIPERIDINE COMPOUNDS AS ESTROGEN RECEPTOR DEGRADING AGENT
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Paragraph 0103; 0104, (2019/02/09)
Disclosed is a new indole compound, in particular, the compound as shown in formula (I), and a preparation method, pharmaceutical composition and use thereof as an estrogen receptor down-regulator in preparing drugs for treating estrogen receptor-positive breast cancer.
Regioselective Allylation of Carbon Electrophiles with Alkenyl-silanes under Dual Catalysis by Cationic Platinum(II) Species
Kinoshita, Hidenori,Kizu, Ryosuke,Horikoshi, Masahiro,Inoue, Gen,Fujimoto, Masayuki,Saito, Masanori,Ichikawa, Junji,Hosomi, Akira,Miura, Katsukiyo
supporting information, p. 520 - 534 (2016/02/16)
In the presence of catalytic amounts of platinum(II) chloride and silver(I) hexafluoroantimonate, (Z)-alkenylsilanes reacted with various carbon electrophiles (acetals, aminals, carboxylic anhydrides, alkyl chlorides, etc.) at the γ-position to give allylation products. A plausible mechanism for the platinum-catalyzed allylation involves alkene migration of alkenylsilanes to allylsilanes and subsequent allylation of carbon electrophiles, both of which are catalyzed by a cationic platinum(II) species.
TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
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Page/Page column 69, (2016/12/22)
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.
TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
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Paragraph 0203; 0204, (2016/12/22)
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.
Platinum-catalyzed allylation of carbon electrophiles with alkenylsilanes
Kinoshita, Hidenori,Kizu, Ryosuke,Inoue, Gen,Fujimoto, Masayuki,Saito, Masanori,Ichikawa, Junji,Hosomi, Akira,Miura, Katsukiyo
supporting information, p. 713 - 716 (2015/01/30)
In the presence of catalytic amounts of PtCl2 and AgSbF6, (Z)-alkenylsilanes react with various carbon electrophiles at the γ-position to give allylation products. A plausible mechanism for the Pt-catalyzed allylation involves alkene migration of alkenylsilanes to allylsilanes and subsequent allylation of carbon electrophiles.
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts
Lai, Andiliy,Kahraman, Mehmet,Govek, Steven,Nagasawa, Johnny,Bonnefous, Celine,Julien, Jackie,Douglas, Karensa,Sensintaffar, John,Lu, Nhin,Lee, Kyoung-Jin,Aparicio, Anna,Kaufman, Josh,Qian, Jing,Shao, Gang,Prudente, Rene,Moon, Michael J.,Joseph, James D.,Darimont, Beatrice,Brigham, Daniel,Grillot, Kate,Heyman, Richard,Rix, Peter J.,Hager, Jeffrey H.,Smith, Nicholas D.
supporting information, p. 4888 - 4904 (2015/07/02)
Approximately 80% of breast cancers are estrogen receptor alpha (ER-α) positive, and although women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, resistance often emerges. Although a variety of resistance mechanism may be at play in this state, there is evidence that in many cases the ER still plays a central role, including mutations in the ER leading to constitutively active receptor. Fulvestrant is a steroid-based, selective estrogen receptor degrader (SERD) that both antagonizes and degrades ER-α and is active in patients who have progressed on antihormonal agents. However, fulvestrant suffers from poor pharmaceutical properties and must be administered by intramuscular injections that limit the total amount of drug that can be administered and hence lead to the potential for incomplete receptor blockade. We describe the identification and characterization of a series of small-molecule, orally bioavailable SERDs which are potent antagonists and degraders of ER-α and in which the ER-α degrading properties were prospectively optimized. The lead compound 11l (GDC-0810 or ARN-810) demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer, and is currently in clinical trials in women with locally advanced or metastatic estrogen receptor-positive breast cancer.
POLYCYCLIC ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
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Paragraph 00372, (2014/10/04)
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.