43 results about "Thyroid hormone receptor" patented technology

The invention discloses a novel compound as well as a pharmaceutical composition and application thereof, the novel compound is represented by formula I or pharmaceutically acceptable salt, tautomer, isotope substitute or solvate, the definition of substituent groups is detailed in the specification, and the novel compound can prevent and / or treat thyroid hormone receptor related diseases. # imgabs0 #

The invention relates to the field of bioengineering, in particular to a mutant of a thyroid stimulating hormone receptor as well as a preparation method and application of the mutant. The invention provides a mutant of a thyroid stimulating hormone receptor. One or more of amino acids from the 321 site to the 360 site of wild type amino acids of the thyroid stimulating hormone receptor are deleted. According to the mutant provided by the invention, the stability of protein is improved, the temperature sensitivity is improved, the functions of gradient, titer and the like are improved, and the capability of combining with an enzyme-labeled antibody and an autoantibody is not changed.

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

Provided herein are methods of generating Gata6-positive brown adipose progenitor cells, and brown adipose cells and tissue therefrom. Additionally, provided herein are methods of generating UCP1 positive organoids. Generally, the methods include a step of culturing brown adipose progenitor cells in a medium containing an FGF signaling pathway activator, a BMP signaling pathway activator, a TGFβ activator, a Wnt inhibitor, and a thyroid hormone receptor activator.

The present invention provides a pyridazinone compound, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, and further provides a related preparation method for the compound and a use thereof, a pharmaceutical composition containing the compound, and a method for treating related metabolic disorders. The compound of the present invention shows an excellent thyroid hormone receptor agonistic effect, and has a wide application prospect in the field of metabolic disorder treatment.

The invention discloses thyroid hormone receptor beta subtype agonist derivatives, and a preparation method and application thereof.

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.

Provided herein is a method for generating Gata6 positive brown adipose precursor cells and brown adipocytes and tissues therefrom.Furthermore, provided herein is a method for generating UCP1 positive organoids.Generally, this method comprises culturing brown adipose precursor cells in a medium that contains FGF signaling pathway activator, BMP signaling pathway activator, TGFβ activator, Wnt inhibitor and thyroid hormone receptor activator.

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 belongs to the field of medicine and detection, and relates to a thyroid stimulating hormone receptor complex, a kit, a preparation method and use. Specifically, it relates to a thyroid stimulating hormone receptor complex, comprising: a thyroid stimulating hormone receptor, a thyroid stimulating hormone receptor C-terminal monoclonal antibody and magnetic particles, wherein the thyroid stimulating hormone receptor is connected to the magnetic particles through the thyroid stimulating hormone receptor C-terminal monoclonal antibody.

The present invention relates to an antibody or an antigen-binding fragment thereof that specifically binds to TSHR, a pharmaceutical composition containing the antibody or the antigen-binding fragment thereof, a nucleic acid molecule encoding the antibody or the antigen-binding fragment thereof, a host cell comprising the same, and related uses. In addition, this invention relates to therapeutic and diagnostic uses of these antibodies or antigen-binding fragments thereof.

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.

The present invention provides a stimulatory thyroid stimulating hormone receptor antibody subtype detection kit and its preparation method and application, which belongs to in vitro diagnostic reagents. The kit provided by the present invention includes a solid phase reagent, a labeling reagent, a calibration solution, and a quality control product, wherein the sequence of the mutant thyroid stimulating hormone receptor in the labeling reagent is shown in SEQ ID No. 1. The kit provided by the present invention only needs to test the sample to directly obtain the concentration value of the sample; the relevant test has been fully automated, and the addition of reagents and samples is completed by instruments, which is more convenient to operate and reduces human errors.

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.

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.

Described herein are compounds of formula I:and pharmaceutically acceptable salts, solvates, and stereoisomers thereof, and their uses as thyroid hormone receptor (THR) β activators.

Described herein are compounds of Formula I and pharmaceutically acceptable salts, solvates and stereoisomers thereof, and their use as thyroid hormone receptor (THR) beta activators. # imgabs0 #

The invention concerns a compound of Formula (I) or a salt thereof, wherein R1 is H, (C1-C3)alkyl or CF3; R2 is H, (C1-C3)alkyl or CF3; A is CH2COOH, XCH2COOCH2CH3, XCH2COOH, XCH2CH2NH2, where X is nitrogen or oxygen atom; Ar is an aromatic fragment selected from the group consisting of (Ar1), (Ar2) and (Ar3); where R3 is H, —CH3, —CH2CH3 or CH3CO—, R4 is H or —CH3, R5 is H or —CH3, and R6 is H or —CH3. The compounds of Formula (I) can be used in the treatment of diseases modulated by thyroid hormone receptor-beta (TRb or TRβ).

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 belongs to the field of biological medicine, and particularly relates to an oxazolone compound and a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound as shown in a formula (I) or a stereoisomer, a geometric isomer, a tautomer, a deuterated compound, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the stereoisomer, the geometric isomer, the tautomer, the deuterated compound, the nitrogen oxide, the solvate, the metabolite and the pharmaceutically acceptable salt of the compound as shown in the formula (I), and also provides a preparation method of the compound. The invention also relates to application of the compound in preparation of drugs for thyroid hormone receptor mediated diseases. According to the compound, good THR-beta agonist activity is maintained, selectivity to THR-alpha and druggability of the compound are improved, and certain activity is shown in an in-vitro molecular level experiment.

The invention belongs to the field of biological medicine, and discloses application of a thyroid hormone receptor gene Thrb or Thra inhibitor in preparation of a medicine for treating nerve injury. Researches show that thyroid hormone is not beneficial to recovery of spinal cord after zebra fish is completely transected, and siRNA fragments of Thrb or Thra have a remarkable effect on promoting growth of cortical neurons and can also promote expression of p-S6. Therefore, Thrb and Thra are taken as molecular intervention targets, and an inhibitor is used for inhibiting expression of the molecular intervention targets, so that growth and regeneration of cortical neurons can be promoted, expression of p-S6 is promoted, activation of a PI3K-AKT pathway is promoted, and a new possibility is provided for preparing the medicine for treating nerve injury.

The present invention provides a compound, preferably a thyroid hormone receptor beta, THRbeta, agonist compound, compositions thereof, methods of making and methods of agonizing THRbeta, and methods for treating conditions mediated by THRbeta.

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.

The present invention provides quinoline compounds and their preparation methods, pharmaceutical compositions and uses. Specifically, the present invention provides a compound represented by formula (I) and its stereoisomers, deuterated compounds, solvates, metabolites, pharma- ceutically acceptable salts, cocrystals or prodrugs and its pharmaceutical compositions. The present invention also provides a preparation method for the above compounds and their use in the manufacture of drugs for diseases mediated by thyroid hormone receptors. Related diseases include, but are not limited to, non-alcoholic fatty liver disease, atherosclerosis, coronary heart disease, hypertension, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, dyslipidemia, obesity, diabetes, metabolic disorders, dyslipidemia, glycogen storage disease type IA, hypothyroidism or thyroid cancer.

The invention relates to a substituted aza-uracil compound as shown in a formula (I), and an isotope form, a stereoisomer, a tautomer, a cis-trans-isomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a hydrate, a prodrug and a polymorphic substance of the substituted aza-uracil compound. The compound has a good agonistic effect and high selectivity, so that the compound has a good application prospect in the aspect of preparing medicines for preventing and / or treating THR-beta activity mediated diseases.

The present disclosure relates to the technical field of antibody engineering, and specifically provides a polypeptide fragment thyroid hormone receptor betal (THRB)-CVD20, and a polyclonal antibody prepared using the same and use thereof. The present disclosure provides a polypeptide fragment THRB-CVD20, wherein the polypeptide fragment has an amino acid sequence shown in SEQ ID NO: 1. The present disclosure further provides a preparation method of the polypeptide fragment and a polyclonal antibody prepared using the polypeptide fragment. In the present disclosure, the polyclonal antibody can accurately identify target cells due to high sensitivity and specificity, and can be further used to identify, identify, and screen the THRB.

The present invention provides a recombinant thyroid stimulating hormone receptor protein, a preparation method therefor and an application thereof. The recombinant thyroid stimulating hormone receptor protein comprises a TSHR protein extracellular segment and a TSHR protein intracellular segment. The C-terminus of the TSHR protein extracellular segment is linked to the N-terminus of the TSHR protein intracellular segment. The protein achieves extracellular soluble expression, and is high in purity, high in activity and good in stability.

The invention belongs to the field of biological medicine, and particularly relates to a quinoline carboxylic acid compound and a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound as shown in a formula (I) or a stereoisomer, a geometric isomer, a tautomer, a deuterated compound, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the stereoisomer, the geometric isomer, the tautomer, the deuterated compound, the nitrogen oxide, the solvate, the metabolite and the pharmaceutically acceptable salt of the compound as shown in the formula (I), and also provides a preparation method of the compound. The invention also relates to application of the compound in preparation of drugs for thyroid hormone receptor mediated diseases. According to the compound, good THR-beta agonist activity is maintained, selectivity to THR-alpha and druggability of the compound are improved, and certain activity is shown in an in-vivo pharmacological experiment.