16 results about "Thyroid hormone receptor" patented technology

The present disclosure relates generally to compounds and compositions thereof for inhibition of thyroid stimulating hormone receptor (TSHR).

The invention provides a pyridazinone compound, or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, and also provides a method related to preparation and application of the compound, a pharmaceutical composition containing the compound and a treatment method of related metabolic diseases. The compound disclosed by the invention shows an excellent thyroid hormone receptor excitation effect and has a wide application prospect in the field of metabolic disease treatment.

The invention relates to pyridazinone or pyridazine compounds as well as derivatives and pharmaceutical compositions thereof. Specifically, the invention provides a pyridazinone or pyridazine compound as shown in a formula (I) or (Ia) or a stereoisomer, a tautomer, an enantiomer, a diastereoisomer, a resonator, a pharmaceutically acceptable salt, a hydrate, a solvate or a crystal form of the pyridazinone or pyridazine compound. The compound shown in the formula (I) or (Ia) has excellent agonistic effect and pharmacodynamic performance on a thyroid hormone beta receptor.

The present invention provides pyridazinone compounds, their stereoisomers, tautomers, or pharmaceutically acceptable salts, as well as methods related to the preparation and use of these compounds, pharmaceutical compositions containing these compounds, and methods for treating related metabolic diseases. The compounds of the present invention exhibit excellent thyroid hormone receptor activating effects and show promising potential for application in the field of metabolic disease treatment.

Provided is a compound useful as a thyroid hormone receptor β-selective thyroid hormone analog. A compound represented by Formula (1), a salt thereof, or a solvate thereof is provided.

This invention provides a recombinant thyroid-stimulating hormone receptor (TSHR) protein, its preparation method, and its applications. The recombinant TSHR protein comprises an extracellular TSHR protein segment and an intracellular TSHR protein segment, with the C-terminus of the extracellular TSHR protein segment linked to the N-terminus of the intracellular TSHR protein segment. The protein achieves extracellular soluble expression, high purity, high activity, and good stability.

The invention provides application of thyroxine and a thyroxine receptor inhibitor in preparation of a medicine for regulating primordial follicle activation, and belongs to the technical field of biology. It is found that thyroxine can promote primordial follicle activation, the thyroxine receptor inhibitor inhibits primordial follicle activation, and the thyroxine receptor inhibitor can serve as a medicine for adjusting primordial follicle activation of a patient suffering from premature ovarian insufficiency and has a good application prospect.

The application discloses a novel pyridazine compound and a pharmaceutical composition and application thereof, and particularly relates to a compound, a solvate, a stereoisomer, a tautomer, an isotopic derivative or a pharmaceutically acceptable salt of formula (I0-1) or (I0-2), a pharmaceutical composition containing the compound and an application in preventing and / or treating a thyroid hormone receptor related disease.

The present application relates to the field of bioengineering, and particularly relates to a mutant of thyroid stimulating hormone receptor and a preparation method and application thereof. The present application provides a mutant of thyroid stimulating hormone receptor, wherein one or more of the 321st-360th amino acids of the wild-type amino acid of the thyroid stimulating hormone receptor are deleted. The mutant provided by the present application improves the stability of the protein, improves the temperature sensitivity, and improves the gradient and potency and other functions, and does not change the ability of binding with enzyme-labeled antibodies and autoantibodies.

Provided are a selective thyroid hormone receptor-β agonist, a pharmaceutical composition comprising same, and a use thereof. Specifically provided is a compound represented by formula (I). The compound has excellent efficacy and / or specificity, and can be used for treating metabolism-related diseases.

Provided are a polycyclic thyroid hormone β receptor agonist and the use thereof. Specifically, the present invention relates to a compound as represented by formula (1) or a pharmaceutically acceptable form thereof, a pharmaceutical composition containing same, and a preparation method therefor and the use thereof. The compound or pharmaceutical composition can be used for the preparation of a drug for preventing, treating or alleviating diseases regulated by the thyroid hormone β receptor.

The idea of the patent includes a new principle, which is the detection of immune complexes using ELISA technology, which is a new and modern principle that is added to the four principles of ELISA, the new principle (the fifth ELISA) depends on detection of immune complexes, which consist of two different parts of proteins (an antigen - an antigen). This complex can be detected through this new principle, and it was applied to the immune complex (thyroid-stimulating hormone receptors and antibodies formed against it) Hashimoto's patients. It was considered an example of applying this theory, the immune complex was actually detected, its concentration determined, and compared to other techniques. A standard solution specially designed for this purpose was used to prove this theory. In this patent, a new kit is specifically designed to detect these immune complexes. Immune complex, the group is considered successful. In terms of use.

The present invention discloses compounds of formula (I), as thyroid hormone receptor β subtype agonists or modulators for use in methods of treatment of obesity, hyperlipidemia, hypercholesterolemia, diabetes mellitus, nonalcoholic steatohepatitis (NASH), hepatic steatosis, arteriosclerosis, cardiovascular disease, hypothyroidism, overweight, fibrosis, thyroid cancer and alopecia, and in chronic weight management or weight management.

Disclosed in the present invention is a thyroid hormone receptor β (THR-β) agonist. The present invention provides a compound as represented by formula I, or a stereoisomer or pharmaceutically acceptable salt thereof. Compared with VK-2809, the compound provided in the present invention has significantly superior agonistic activity against THR-β than VK-2809, or in terms of in vivo organ / tissue distribution, has a liver / heart distribution ratio or plasma / heart distribution ratio superior to that of VK-2809.

The present invention relates to a thyroid hormone receptor β subtype agonist derivative, a method for producing the same, and uses thereof.

The present application relates to compounds of formulae (B') and (C) and compositions thereof for inhibition of thyroid stimulating hormone receptor (TSHR) and their use in the treatment of diseases such as Grave's disease.