11 results about "Hormone Receptor Modulators" patented technology

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.

Relates to androgen receptor modulators and uses thereof. The present invention relates to compounds of formula (I)-(VI), in particular to compounds of formula (I)-(VI), pharmaceutical compositions comprising these compounds and the use of these compounds for the prophylaxis or treatment of diseases, in particular for modulating androgen receptor activity and treating diseases including prostate cancer.

This invention relates to an activator of FXR, which can be used to treat autoimmune diseases, liver diseases, intestinal diseases, kidney diseases, cancer, and other diseases in which FXR plays a role, and has the formula (I): wherein L1, A, X1, X2, R 1 R 2 and R 3 As described in this article.

The invention relates to a polymorphic form of a compound capable of serving as a thyroid hormone beta receptor modulator, a preparation method and application of the polymorphic form and a pharmaceutical composition containing the polymorphic form. The polymorphic form is applied to preparation of drugs for treating various thyroid-related diseases.

The present disclosure relates to methods of treating a disease or disorder comprising administering a combination of an MC4R agonist with a GCHR modulator.

The present disclosure provides compounds and methods for treating cancer, such as prostate cancer responsive to inhibition and / or degradation of androgen receptor ("AR") polypeptide, and / or breast cancer responsive to inhibition and / or degradation of estrogen receptor ("ER") polypeptide and / or AR polypeptide.

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.

The present disclosure relates to methods of treating a disease or disorder comprising administering a combination of GLP1R agonists and MC4R agonists.

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.

The present invention relates to a polymorph of a compound that can be used as a thyroid hormone β receptor modulator, a preparation method therefor and a use thereof, and a pharmaceutical composition containing the polymorph. The use is a use in the preparation of drugs for treating various thyroid-related diseases.

The present disclosure provides compounds 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 39, 38, 39 JPEG2026500166000038.jpg48165 or a pharmaceutically acceptable salt thereof. The unit dosage forms described herein are suitable for oral administration. There remains a need for anti-estrogen agents that can completely inhibit estrogen receptors, including those encoded by both wild-type and mutant forms (e.g., those containing activating mutations) of the genes encoding estrogen receptor alpha (ERα) and estrogen receptor 1 (ESR1). Selective estrogen receptor modulators (SERMs) or degraders (SERDs) are particularly useful or promising tools for such treatment.