16 results about "Estrogen receptor modulator" patented technology

The present invention relates to the technical field of medicine. Provided are an estrogen receptor modulator and a use thereof, particularly a compound as represented by general formula (i) or an isomer or pharmaceutically acceptable salt thereof and a use thereof, particularly a use thereof as an estrogen receptor degrading agent, a use thereof in the preparation of a medicament for treating and / or preventing an estrogen receptor-mediated or dependent disease or condition, and a use thereof in the preparation of a medicament for treating and / or preventing a disease or condition by degrading a target protein.

The present disclosure provides compounds that are estrogen receptor modulators (e.g., estrogen receptor agonists, estrogen receptor antagonists, and / or complete estrogen receptor antagonists), and uses thereof.

Tetrahydropyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulating activity or function are described, having the structure of Formula I (see Formula), and pharmaceutically acceptable stereoisomers, tautomers, or salts thereof, with the substituents and structural features described herein. Pharmaceutical compositions and medicinal products comprising the compounds of Formula I are also described, as well as methods of using such estrogen receptor modulators, alone or in combination with other therapeutic agents, to treat diseases or pathological conditions that are mediated by or dependent on estrogen receptors.

Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure:and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM.

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.

The invention belongs to the technical field of medicines, and relates to an estrogen receptor modulator and application thereof, in particular to a compound shown as a general formula (i), an isomer or pharmaceutically acceptable salt thereof and application thereof. The invention also relates to the use thereof as an estrogen receptor degradation agent, in particular as an estrogen receptor degradation agent, in the preparation of medicaments for treating and / or preventing estrogen receptor mediated or dependent diseases or disorders, and in the preparation of medicaments for treating and / or preventing diseases or disorders by degrading target proteins.

Disclosed is a method for treating of cancer, specifically pancreatic cancer by administering a selective estrogen receptor modulator (SERM), e.g., levormeloxifene, alone or in combination with one or more additional cancer therapies.

The present disclosure provides 2,3,4,9-tetrahydro-lH-pyrido[3,4-b]indole derivatives of formula I as estrogen receptor modulators for the treatment of cancer.

A pharmaceutical composition capable of forming free burst release effect in-situ forming implant useful for injection inside bone injuries without surgery is provided. This pharmaceutical composition includes; biodegradable polymer, selective estrogen receptor modulator, organic solvent and liquid lipid, solidifies upon contacting with the surrounding medium and form solid implant with compact framework by in-situ phase separation method to deliver the selective estrogen receptor modulator. This compact framework restores the porous structure of the implant by time which is essential in promoting bone healing.

The invention provides an amplified preparation method of a key intermediate of an estrogen receptor modulator, and belongs to the field of medical intermediates. The method comprises the following steps: by taking azetidine-3-one hydrochloride and 3-fluoro-1-halogenated propane as raw materials, reacting in the presence of alkali to obtain an intermediate 1; then carrying out reductive amination reaction on the intermediate 2 and 5-amino-2-methylpyridine to obtain an intermediate 2; reacting with nitrous acid ester in the presence of alkali to obtain an intermediate 3; and finally, reacting in the presence of acid to obtain the 5-((1-(3-fluoropropyl) azetidine-3-yl) amino) pyridinealdehydes. The method is simple and reliable in process and easy for industrial production; the generation amount of an isomer is reduced, and the reaction yield is improved.

This application provides a compound or a pharmaceutically acceptable salt thereof having estrogen receptor modulating activity or function, wherein the compound has the structure of Formula (I) and possesses the substituents and structural features described herein. This application also provides a pharmaceutical composition comprising the compound of Formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound of Formula (I) or a pharmaceutically acceptable salt thereof in the preparation of a medicament for preventing or treating estrogen receptor-related diseases. #imgabs0#

The invention relates to an indazole derivative, a preparation method thereof and application of the indazole derivative in medicine. In particular, the disclosure relates to an indazole derivative as shown in general formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, and an application of the indazole derivative as an estrogen receptor modulator for preventing and / or treating estrogen receptor mediated or dependent diseases or symptoms, particularly breast cancer. Wherein each substituent in the general formula (I) is as defined in the specification. # imgabs0 #

To provide an estrogen receptor inhibitor (ER).SOLUTION: The present invention provides a compound represented by formula (I) or a stereoisomer, tautomer or pharmaceutical salt thereof, and use thereof in preparation of a medicament for preventing and / or treating estrogen receptor-related diseases or disorders.SELECTED DRAWING: None

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.

Compounds of Formula I'as estrogen receptor modulators are described herein. Also described are pharmaceutical compositions and medicaments including compounds described herein, and methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treatment of estrogen receptor mediated or dependent diseases or conditions;