52 results about "Thyroid Gland Hormone" patented technology

The invention discloses a method for constructing a secondary subclinical hypothyroidism screening model based on conventional physical examination data, which comprises the following steps of: constructing a high-quality data set containing the conventional physical examination data, and defining a sample tag in the high-quality data set as a G2SCH positive group or negative group; performing feature selection on the data set by adopting different feature selection methods, and screening out key feature subsets; an oversampling method is adopted to synthesize minority class samples in the data set according to different class balance proportions; adopting a plurality of machine learning algorithms to carry out model prediction training with sample labels as supervision on the basis of data sets of different classes of balance proportions and different key feature subsets, and constructing a plurality of candidate G2SCH screening models; and evaluating and selecting an optimal G2SCH screening model. According to the method, G2SCH screening can be carried out based on conventional physical examination data, dependence on thyroid hormone specialized detection indexes in an existing medical scene is overcome, and the method is suitable for the medical scene with limited resources.

The present invention provides an application of thyroid hormones and its analogues in preparation of drugs for treating alpha-thalassemia, especially in preparation of drugs for regulating expression of zeta-globin gene. During differentiation of K562 cells, thyroid hormone analogue (Triac) can significantly up-regulate the expression of zeta-globin gene (HBZ) by 50 folds or above. The expression of zeta-globin gene (hbae5) can also be up-regulated by 30-70 folds in zebrafish treated with thyroid hormones and thyroid hormones analogues. Therefore, according to the present invention, the expression of zeta-globin gene can be significantly activated by thyroid hormones and its analogues, which may develop new potential therapies for patients with alpha-thalassemia. It provides an economical, safe and effective method for treating alpha-thalassemia and can be widely used.

The invention discloses a traditional Chinese medicine composition for treating hyperthyroidism and a preparation method thereof, and relates to the technical field of traditional Chinese medicines. The traditional Chinese medicine composition for treating hyperthyroidism is prepared from cyclodextrin grafted modified hollow mesoporous organic silicon nanoparticles, traditional Chinese medicine ferment powder and a traditional Chinese medicine extracting solution, the cyclodextrin-grafted modified hollow mesoporous organic silicon nano-particles are used as a carrier, traditional Chinese medicine ferment powder and a traditional Chinese medicine extracting solution are loaded, the medicine concentration of a focus part is increased, traditional Chinese medicine ingredients are rapidly released through rapid response fracture of tetrasulfide bond functional groups, and the traditional Chinese medicine composition is prepared in an active targeting and fixed-point blasting mode. The bioavailability and the onset time of the medicine are improved, the leakage risk of the medicine is jointly reduced through the gating effect of cyclodextrin and responsive release of tetrasulfide bonds, synthesis of thyroid hormone is more thoroughly inhibited under the precise effect of high-concentration medicine and multi-target immunoregulation of traditional Chinese medicine, and the recurrence rate of hyperthyroidism is reduced.

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

The present application provides a kind of compound with indazole group, THR beta receptor agonist and use, compound with indazole group or its pharmaceutically acceptable salt.The present application develops a kind of THR beta selective agonist with better specificity and drugability, the present agonist is better selective agonist THR beta and avoids the activation of THR alpha, separates the harmful influence of thyroid hormone excess from potential beneficial effects such as lowering cholesterol and blood lipids, provides a kind of new type of treatment drug with broad prospects for treating a series of major metabolic diseases in urgent need of solution.

Disclosed are a compound of formula I and a stereoisomer, pharmaceutically acceptable salt or deuterated compound thereof, wherein each substituent is as defined in the present disclosure.

The application discloses a method for regulating body color of ornamental fish and belongs to the technical field of aquaculture. The application finds that, by using thyroid hormone to soak ornamental fish in the fry period and the juvenile fish period, excessive thyroid hormone can significantly reduce the number of red pigment cells and the size of pigment granules of ornamental fish in different periods, and reduce the content of carotenoids; when the synthesis of thyroid hormone is inhibited, the expression of melanin cells and related synthesis pathway genes is promoted, and the carotenoid level is increased. The application first clearly defines the inhibitory effect of thyroid hormone on the development of red pigment cells and the accumulation of carotenoids of gourami, fills the knowledge gap in the field, and provides important guiding information for future regulation of body color and genetic improvement of ornamental fish and other aquatic animals.

The invention belongs to the field of biological medicine, particularly discloses pharmaceutical application of a Dio3 inhibitor screened based on a thyroid hormone disorder algorithm in sepsis cardiomyopathy, and discloses that the core pathological mechanism of SIC is thyroid hormone signal axis disorder caused by Dio3 abnormal up-regulation, further mitochondrial autophagy key protein is inhibited, and the application of the Dio3 inhibitor in sepsis cardiomyopathy is developed for the first time. And myocardial mitochondrial homeostasis imbalance and functional cardiac dysfunction are caused. Through single intraperitoneal injection (25mg / kg) of a compound PBENZ-DBRMD (specific Dio3 inhibitor) within 12 hours after sepsis occurs, heart function indexes (EF% / FS%) can be remarkably recovered, and mitochondrial autophagy disorder can be reversed. Meanwhile, serum transT3 (rT3) is provided as an SIC early diagnosis marker (rT3 is strongly negatively correlated with EF%). The scheme provides a new targeted intervention strategy for SIC, and has the characteristics of simplicity and convenience in operation and definite curative effect.

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.

The present invention provides the use of thyroid hormone and its analogs in the preparation of a drug for treating α-thalassemia. Specifically, the drug can be used to regulate ζ-globin gene expression. During K562 cell differentiation, the thyroid hormone analogs can specifically and significantly upregulate the expression of the ζ-globin gene (HBZ) by as much as 50 times. After treatment with thyroid hormone and its analogs in model animal zebrafish embryos, the expression of the ζ-globin gene (hbae5) can also be specifically upregulated by as much as 30-70 times. Therefore, the present invention uses thyroid hormone and its analogs to specifically activate the expression of the ζ-globin gene, that is, to reactivate the silenced ζ-globin gene in α-thalassemia patients to inhibit the destruction of red blood cells. This method provides a method for preparing a drug for treating α-thalassemia, provides an economical, safe and effective method for the treatment of α-thalassemia, and can be widely promoted and used.

This disclosure relates to methods of treating or preventing heart malformations or cardiovascular diseases comprising administering an effective amount of thyroid hormone in combination with i) an agent that decreases DUSP5 and / or DUSP6 expression and / or ii) a beta-adrenergic blocking agent to a subject in need thereof. In certain embodiments, this disclosure relates to in vivo and in vitro methods of inducing proliferation of cardiomyocytes using agents or combinations of agents disclosed herein.

The invention provides a compound with a heterocyclic structure, a THRbeta receptor agonist and application, and the compound with the heterocyclic structure or pharmaceutically acceptable salt thereof. The invention develops a THRbeta selective agonist with better specificity and druggability, the THRbeta selective agonist can better selectively agonize THRbeta so as to avoid activation of THRalpha, and the harmful effect of excessive thyroid hormone is separated from the potential beneficial effects of lowering cholesterol and blood fat and the like; the invention provides a novel therapeutic drug with a wide prospect for treating a series of serious metabolic diseases to be solved urgently.

The present application relates to the technical field of traditional Chinese medicine, and in particular, to a traditional Chinese medicine composition, a method for preparing same, and use thereof in preparing a medicament for preventing and treating a thyroid disease. The traditional Chinese medicine composition consists of Ranunculi Ternati radix, Taraxaci herba, Cyperi rhizoma, and Semiaquilegiae radix. The method comprises: mixing and crushing formulation amounts of Ranunculi Ternati radix, Taraxaci herba, Cyperi rhizoma, and Semiaquilegiae radix; or extracting formulation amounts of Ranunculi Ternati radix, Taraxaci herba, Cyperi rhizoma, and Semiaquilegiae radix. The compounding of the four traditional Chinese medicines, Ranunculi Ternati radix, Taraxaci herba, Cyperi rhizoma, and Semiaquilegiae radix, can significantly treat hypothyroidism, thyroid nodules, and the like caused by insufficient thyroid hormones. Compared with the prior art, the traditional Chinese medicine composition features clear ingredients, good safety, and better therapeutic effects, providing technical support for the treatment of thyroid diseases with traditional Chinese medicines.

Sulfophenyl and polyethylene glycol derivatives of the thyroid hormones L-thyroxine (T4) and triiodothyronine (T3), and methods of making same, are disclosed. Advantageously, the thyroid hormone derivatives are water soluble, have long-term stability, and don't stick to the surface of common container materials. The derivatives were prepared as calibrators, in non-serum-based solutions, for in vitro thyroid immunoassays to measure the concentration of test samples and were found to perform as well as thyroxine / serum-based solutions.

To provide a pharmaceutical composition for treating nervous system disorders by inducing remyelination, neuroprotection, and immunomodulation.SOLUTION: A pharmaceutical composition comprising a therapeutically effective amount of a RXR agonist for use in combination with a thyroid hormone in the treatment of demyelination or neuroinflammation associated with a central nervous system disorder, the RXR agonist is 3, 7-dimethyl-6 (S), 7 (S) - methano, 7 - [1,1,4,4 - tetramethyl - 1,2,3,4 - tetrahydronaphth-7-yl] 2 (E), 4 (E) heptadienoic acid, and the RXR agonist is used in combination with a thyroid hormone to provide greater improvement in a central nervous system disorder than either the RXR agonist or the thyroid hormone alone.SELECTED DRAWING: Figure 1

Disclosed herein are pharmaceutical compositions for the treatment of neurologic disorders comprising an effective amount of one or more mTOR inhibitors and / or one or more BDNF inducers and optionally an effective amount of one or more thyroid hormones. Further disclosed herein are methods of treating or preventing neurologic disorders comprising administering an effective amount of a pharmaceutical composition comprising one or more mTOR inhibitors and / or one or more BDNF inducers and optionally an effective amount of one or more thyroid hormones.

The technical scheme provided by the invention is application of quercetin in aquaculture, in particular to application of quercetin in preparation of drugs and / or feeds for preventing and treating thyroxine disorder and / or serotonin disorder of aquatic animals. The invention has the beneficial technical effects that the natural plant component quercetin which is originally applied to medicines and health care products for people is expanded to be applied to the field of aquatic animals, so that the nutrition required by the aquatic animals can be provided, the effect of regulating thyroid hormone and / or serotonin disorder of the aquatic animals can be achieved, the quercetin is used for replacing hormone medicines, and the health care effect is good. The method is friendly to an ecological chain, and green, cyclic and sustainable development is realized.

Described herein is a hepatocyte maturation composition (Hepatocyte Differentiation Cocktail 6"(HDC6)) comprising a TGF-beta inhibitor, a Notch inhibitor, a cAMP activator, a tryptophan pathway metabolite, a PPAR activator, and a thyroid hormone. Methods for generating mature iPSC-derived hepatocytes and 3D liver spheroids are presented. The 3D liver spheroids described herein are suitable for predicting drug-induced liver injury and identifying a preferred therapeutic agent for an individual.

The invention discloses a traditional Chinese medicine composition containing dandelion exosomes for treating goiter as well as a preparation method and application of the traditional Chinese medicine composition. The traditional Chinese medicine composition is prepared from the following components in parts by mass: 4 to 10 parts of dandelion exosome, 1 to 2 parts of blueberry exosome and 1 to 4 parts of compound extract, and the compound extract is prepared from fructus jujubae, tremella fuciformis, honeysuckle flower and fructus momordicae. The traditional Chinese medicine composition can achieve the effects of promoting blood circulation to remove blood stasis and eliminating phlegm and resolving masses, can remarkably reduce the thyroid coefficient, callback the thyroid hormone level in serum, inhibit cell proliferation, promote cell apoptosis in thyroid tissues and relieve inflammatory response of the thyroid tissues, and has the characteristics of good curative effect and simple components.

The present disclosure provides, among other things, methods of drying porcine thyroid gland material and manufacturing DTE comprising vacuum drying porcine thyroid gland material in a way such that the temperature of the porcine thyroid gland material is maintained above a threshold temperature. Since applying vacuum, or reducing pressure, has a cooling effect on the porcine thyroid gland material, maintaining the porcine thyroid gland material above a threshold temperature can be achieved by gradually reducing pressure while simultaneously increasing the heat applied to the porcine thyroid gland material during the period of gradual pressure change. Such methods are advantageous in reducing bioburden (killing and impeding the growth of microorganisms) while maintaining therapeutic levels of thyroid hormones, as compared to certain methods of drying porcine thyroid gland material and / or manufacturing DTE known in the art.

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.

Provided are a method and drug for enhancing the anti-tumor efficacy of an immune checkpoint inhibitor, and use thereof in the treatment of tumors. The method for enhancing the anti-tumor efficacy of the immune checkpoint inhibitor is to improve the level of thyroid-stimulating hormone (TSH) in the body of a patient, and comprises combined use of the immune checkpoint inhibitor and TSH or / and a substance having the function of improving the level of TSH in the body. Compared with using the immune checkpoint inhibitor alone, the provided method and drug, when combined with the immune checkpoint inhibitor in an anti-tumor experiment, can significantly improve the anti-tumor efficacy: reducing the tumor volume, improving the survival time, etc., which can solve the current technical problem that the therapeutic effect of treatment with the immune checkpoint inhibitor is generally unsatisfactory.

The present disclosure relates generally to the field of biological detection technology, and in particular to a quality control for thyroid hormone related assays. The quality control is a solution with serum matrix as the main solvent and contains an antigen coupled with T3 and / or T4, including both bound and free states, and a biomedical carrier material with a contact angle θ greater than 90°.

On the basis of a Galpha s-cAMP-PKA signal channel, which plays a normal physiological role in vivo, of thyroid stimulating hormone and the regulation and control effect of the thyroid stimulating hormone on thyroid hormone synthesis, a normal human thyroid follicular epithelial cell line Nthy-ori 3-1 is transformed into a TSHR overexpressed stable cell line for the first time, the expression quantity of TSHR in a cell membrane is obviously increased, and the TSHR expression level is improved; the response sensitivity of the Nthy-ori 3-1 cell to a thyroid stimulating hormone drug is obviously improved; by detecting the synthesis level of cAMP and thyroid hormone before and after the stimulation of the thyroid stimulating hormone, it is verified that the TSHR overexpression Nthy-ori 3-1 cell line established in the research has great superiority for determining the biological activity of the human thyroid stimulating hormone.

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 discloses a method for online separation and absolute determination of free thyroid hormone in serum, comprising the following steps: (1) setting up a two-dimensional liquid chromatography (2) online separation and removal of macromolecular interferences in serum; (3) retention of free thyroid hormone; (4) online separation of free thyroid hormone; (5) online determination by isotope dilution mass spectrometry; and (6) cleaning of the two-dimensional liquid chromatography system. The method of the present invention achieves online separation and absolute determination of free thyroid hormone in serum. Since the first-dimensional chromatographic mobile phase is a mild ammonium salt buffer solution that does not contain organic solvents, it can ensure that the thyroid hormone bound to proteins in the serum remains in a bound state, and the target substance entering the mass spectrometry analysis is the free thyroid hormone; and the determination result can be traced back to the International System of Units through national certified reference materials. Compared with traditional serum offline processing methods such as solid phase extraction and equilibrium dialysis, the method is efficient, reliable, and easy to operate.

Described herein are compositions, pharmaceutical compositions, kits, and methods of use relating to anti-Dio3os antisense RNA. In embodiments, antisense Dio3os compositions, kits, and methods are described to improve symptoms of osteoporosis, for example, osteoporosis induced by a disorder characterized by a thyroid hormone imbalance (i.e., hyperthyroidism or hypothyroidism). In embodiments, antisense Dio3os compositions, kits, and methods are described to improve sensitivity of cancer cells to anti-cancer therapeutics, for example, sensitivity of ER+ breast cancer or other breast cancer cells, thyroid cancer cells, prostate cancer cells, hepatocellular cancer cells, pancreatic cancer cells, and ovarian cancer cells that are sensitized or otherwise non-responsive to cancer therapeutics (for example, aromatase inhibitors or HDAC inhibitors). Combination therapies are also contemplated utilizing antisense RNA according to the present disclosure and other drugs, for example, thyroid and anti-cancer medications.

This invention discloses a stability-improved complete thyroid hormone antigen, its preparation, and its application. The free amino group of the thyroid hormone or its deiodinated derivative moiety of this complete antigen is protected by a tert-butoxycarbonyl (Boc) group, and its carboxyl group is coupled to a carrier protein via an amide bond. The preparation method includes: protecting the amino group of a thyroid hormone molecule (such as T4, T3, etc.) with Boc2O, followed by activating its carboxyl group using the EDC / NHS method and coupling it to a carrier protein. This invention effectively overcomes the chemical instability problems of traditional complete antigens, such as easy photo-oxidative deiodination, easy racemization, and easy deamination reactions. In vitro detection reagents coated with the complete antigen of this invention exhibit longer shelf life, lower batch-to-batch variability, and extremely stable detection performance.

The invention discloses an improved TR beta selective thyroid hormone GC-1 preparation method, and relates to the field of pharmaceuticals, p-hydroxybenzaldehyde and 3, 5-dimethyl-4-bromophenol are used as starting raw materials, and the TR beta selective thyroid hormone GC-1 is obtained through eight-step reactions of Friedel-Crafts alkylation, phenolic hydroxyl group protection, aldehyde addition reaction, alcoholic hydroxyl group protection, selective deprotection, phenol alkylation, acid catalytic hydrogenation and the like. The Sobetirome is synthesized by the method with the total yield of 54%. Compared with the prior art, the method has the advantages that a protecting group is easy to remove, the product stability is improved, and the yield is high.