54 results about "Thyroid Hormone Receptor Agonists" patented technology

Provided herein are compounds, preferably thyroid hormone receptor beta (THR beta) agonist compounds, compositions thereof, and methods of their preparation, and methods of agonizing THR beta and methods for treating disorders mediated by THR beta.

The present invention discloses a compound represented by the following Formula (I) and a pharmaceutically acceptable salt thereof. The compound improves the THRα selectivity while maintaining good THRβ agonistic activity, thereby improving properties of the finished drug.

A compound of formula (I) or (Ia), or a tautomer or a pharmaceutically acceptable salt thereof is provided. Compounds of formula (II) to (V), or a tautomer or a pharmaceutically acceptable salt thereof are also provided. These compounds and the pharmaceutical compositions containing them are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto. (I), (Ia)

Provided herein are combinations comprising a glucagon-like peptide-1 receptor (GLP-1R) agonist and a thyroid hormone receptor beta (THRβ) agonist and methods comprising administering to a subject in need thereof such combinations.

Provided herein are combinations comprising a glucagon-like peptide-1 receptor (GLP-1R) agonist and a thyroid hormone receptor beta (THRβ) agonist and methods comprising administering to a subject in need thereof such combinations.

The present disclosure relates to methods of administering thyroid hormone receptor agonists. The present disclosure provides methods wherein the methods maintain the activity of a given thyroid receptor agonist in ameliorating or curing obesity, hyperlipidemia, hypercholesterolemia, diabetes, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, atherosclerosis, cardiovascular disease, hypothyroidism, and related conditions, meanwhile, thyroid-related and thyroid axis-related side effects are reduced or eliminated.

The invention belongs to the field of biological medicines, and particularly relates to 4-quinazolinone compounds serving as thyroid hormone beta receptor agonists and application of the 4-quinazolinone compounds. The invention discloses a thyroid hormone beta receptor agonist as shown in a formula (I), relates to a 4-quinazolinone compound and a preparation method thereof, and further relates to a pharmaceutical composition containing the compound and application. The compound or the pharmaceutical composition provided by the invention can be used for preventing, treating or relieving diseases regulated by thyroid hormone beta receptors, especially for treating non-alcoholic fatty liver diseases.

The invention relates to the field of biological medicine, in particular to an aryloxy indole formic acid compound as well as a preparation method and application thereof. The general formula (I) of the aryloxy indole carboxylic acid compound is shown in the specification, wherein R1 is a Cl atom or a Br atom; r2 and R3 are two methylene groups connected to the same oxygen atom, or R2 is any one of a methyl group, a methoxy group, an isopropyl group, a methylthio group and a hydrogen atom, and R3 is any one of a halogen atom, a methyl group, a methoxy group, an isopropyl group, a propoxy group, an isopropoxy group, a butoxy group, an isobutoxy group, a cyclopropyl methoxy group, a benzyl group, a benzyloxy group and a hydrogen atom. As a thyroid hormone receptor agonist, the aryloxy indole formic acid compound has good THRbeta selectivity and THRbeta agonist activity, has the advantages of low toxicity and good biological safety, and has high practical value.

The present invention relates to a compound that acts as a thyroid hormone beta receptor agonist and its use, and further relates to a compound represented by formula (1) or a pharmaceutically acceptable form thereof, a pharmaceutical composition comprising the same, and a method for preparing the same. The compound or pharmaceutical composition described herein can be used to prepare a medicament for preventing, treating, or alleviating diseases regulated by thyroid hormone beta receptors. #imgabs0#

The present invention provides a thyroid hormone receptor β (TRβ) agonist compound, a preparation method and an application thereof. The compound and the pharmaceutically acceptable salts, esters, amides or carbamates, as well as isomers, racemates, prodrugs, co-crystallized complexes or solvates of the compound can be used as thyroid hormone receptor β agonists, and the prepared thyroid hormone receptor β agonist has a good activation effect on wild-type and mutant thyroid hormone receptor β, has a weak effect or basically no effect on thyroid hormone receptor α (TRα) and prolyl hydroxylase (PHD2) targets, and has good selectivity. Therefore, the compound can be used in the prevention or treatment of thyroid hormone receptor β-mediated related diseases.

Provided herein are methods for treating depression using a fatty acid amide hydrolase (FAAH) cleavable prodrug of a thyroid hormone receptor (TR [beta]) agonist.

Provided herein are compounds, preferably thyroid hormone receptor beta (THR beta) agonist compounds, compositions thereof, and methods of their preparation, and methods of agonizing THR beta and methods for treating disorders mediated by THR beta.

Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with thyroid hormone receptor activity. The methods and compositions disclosed herein include the use of at least one thyroid hormone receptor agonist.

The present application provides a novel thyroid hormone β receptor agonist of formula (I) having better activity, selectivity or safety and the use thereof for preventing or treating diseases related to the action of β receptor agonists, including, for example, obesity, hyperlipidemia, hypercholesterolemia, diabetes, liver diseases (fatty liver, NASH, NAFLD, etc.), cardiovascular diseases (atherosclerosis, etc.), thyroid diseases (hypothyroidism, thyroid cancer, etc.), and the like.

The application relates to a compound of Formula (I′) or (I):or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of thyroid hormone receptors, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease or disorder regulated by thyroid hormone.

Disclosed in the present invention are a polymorph of a compound of formula I (R)-2-(3,5-dichloro-4-((7-(methyl-d3)-1-oxo-2,5,6,7-tetrahydro-1H-cyclopenta [d]pyridazin-4-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile, a preparation method, pharmaceutical composition and pharmaceutical use therefor.

To provide thyroid hormone receptor beta (THR beta) agonist compounds, compositions thereof, and methods of their preparation, and methods of agonizing THR beta and methods for treating disorders mediated by THR beta.SOLUTION: For example, the following compound (example 2) is illustrated.SELECTED DRAWING: None

Provided herein are compounds, in particular, Compound 1, and compositions useful for treating or preventing diseases or disorders that are modulated by thyroid hormone receptor agonists, such as non-alcoholic steatohepatitis (NASH) or non-alcoholic fatty liver disease (NAFLD).

Provided herein are method of thyroid hormone receptor beta (THRβ) agonist and combinations comprising a glucagon-like peptide-1 receptor (GLP-1R) agonist and a thyroid hormone receptor beta (THRβ) agonist and methods comprising administering to a subject in need thereof such combinations.

Provided herein are novel thyroid hormone receptor (TR) agonists, e.g., having Formula I, II, or III. Also provided are methods of preparing the novel TR agonists and method of using the novel TR agonists for treating diseases or disorder modulated by TR agonists, such as NAFLD, NASH, diabetes, hyperlipidemia and / or hypercholesterolemia.

The present application provides a novel medium composition for use in inducing differentiation of somatic cells into brown adipocytes. As the present application, for example, there can be mentioned a medium composition for use in inducing differentiation of somatic cells into brown adipocytes, which is characterized by comprising seven components of a thyroid hormone receptor agonist, a glucocorticoid receptor agonist, a phosphodiesterase inhibitor, insulin, an ascorbic acid derivative, albumin, and an antibiotic. According to the present application, differentiation induction of somatic cells into brown adipocytes can be effectively performed. In addition, according to the present application, brown adipocytes can be effectively maintained.

The present invention discloses a crystalline polymorph of the compound of formula I, (R)-2-(3,5-dichloro-4-((7-(methyl-d3)-1-oxo-2,5,6,7-tetrahydro-1H-cyclopenta[d]pyridazin-4-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile, and its preparation method, pharmaceutical composition and application in medicine. [Formula 1] TIFF2025505211000048.tif46160

The present application is directed to a combination therapy comprising a thyroid hormone receptor beta-1 (TKβ) agonist, and a primary cancer therapeutic. Methods of treating cancer and inducing differentiation in a population of cancer cells are also disclosed.

The invention relates to pharmaceutical compositions, and more specifically to pharmaceutical compositions comprising at least one fatty acid-bile acid conjugate and at least one thyroid hormone receptor agonist or thyroid hormone mimetic or pharmaceutically acceptable salts thereof, and use of such compositions in methods of treating, stabilizing or lessening the severity or progression of a liver disease including fibrosis, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and comorbidity ties associated with a liver disease.

Provided herein are method of thyroid hormone receptor beta (THRβ) agonist and combinations comprising a glucagon-like peptide-1 receptor (GLP-1R) agonist and a thyroid hormone receptor beta (THRβ) agonist and methods comprising administering to a subject in need thereof such combinations.

To provide thyroid hormone receptor beta agonist compounds, and compositions thereof.SOLUTION: The present invention provides a compound represented by the formula below, a tautomer thereof, or a pharmaceutically acceptable salt thereof. [In the formula, A is as defined below, and ring B is a 5-membered heterocyclyl or a 5- to 6-membered heteroaryl].SELECTED DRAWING: None

The invention discloses application of a thyroid hormone receptor beta agonist in reduction of erythrocyte apoptosis in an in-vitro erythrocyte differentiation process, and finds that the thyroid hormone receptor beta agonist can reduce the quantity of erythrocyte apoptosis or death in the erythrocyte differentiation process for the first time. The problem of cell apoptosis or death in the final stage in the erythrocyte differentiation process in the field at present is solved. The research greatly promotes large-scale production and preparation of in-vitro red blood cells, and solves the problems of clinical blood shortage and safety.