1991results about "Endocrine system disorder" patented technology

The invention provides a compound of a GLP-1R agonist or modulator with a structure as shown in a formula (I).

Embodiments of the present invention provide a pharmaceutical intervention in the neonatal pig that inhibits and delays development and activation of the HPG axis, growth of the boar testis and inhibits testicular production of testosterone and androstenone, which prevents the development of aggressive behavior in the maturing boars and the presence of boar taint in the meat. The invention comprises treatment with a combination of an androgen and an estrogen in the newborn male piglet using extended drug delivery methods, with a defined duration of no more than 12 weeks, for the purpose of inhibiting the production of testosterone and androstenone and the accumulation of the boar taint-inducing molecules androstenone and skatole in the fat.

Provided in the present invention are a TSHR antagonist compound, a pharmaceutical composition, and a preparation method therefor and the use thereof. The compound has good TSHR antagonism, and is used in the treatment of thyroid-associated conditions and / or diseases, such as hyperthyroidism, Graves' disease, Graves' ophthalmopathy, and thyroid eye disease, and in the preparation of a drug for treating such conditions or diseases.

The invention discloses an RGD-click chemical crosslinking siRNA nano-carrier, a preparation method thereof and application of the nano-carrier in preparation of a medicine for treating secondary thyroidism, and belongs to the technical field of medicines.The nano-carrier is RGD-PEG-PLys (N), and the preparation method of the nano-carrier comprises the steps of synthesis of PLys (ss-DBCO), synthesis of RGD-PEG-PLys (N) and the like. According to the application, the nano-carrier is used for preparing siRNA composite nanoparticles; vascular endothelial targeting (RGD), dynamic stability (click crosslinking) and microenvironment responsiveness (disulfide bond) are organically combined for the first time to achieve mutual synergistic interaction, and the effect ceiling of an existing material is broken through; according to the siRNA composite nanoparticle, the silence effect of the PTH gene as long as 70 days can be achieved through single intravenous injection, the PTH inhibition rate is larger than 85%, the siRNA accumulation amount in parathyroid gland tissue is remarkably increased through RGD targeting (8.6 times that of a non-targeting group), the liver and kidney distribution amount is reduced by 60%, and the system toxicity is controllable.

The present invention concerns the use of aprotic polar solvents and an ionization stabilizing agent to prepare stable therapeutic formulations of levothyroxine by dissolving levothyroxine in an aprotic polar solvent system that can then be used to treat, prevent, and / or diagnose certain diseases and disorders in humans and veterinary animals by administration of the formulation thereto. In certain embodiments, the invention is directed to formulations comprising levothyroxine, and optionally one or more additional therapeutic agents, dissolved in an aprotic polar solvent system, such as a DMSO / water admixture comprising at least one ionization stabilizing excipient in a concentration sufficient to impart physical and chemical stability to the therapeutic agent. The invention also provides methods of use of such formulations in treating, preventing, and / or diagnosing diseases and disorders, and methods of manufacturing such formulations.

The invention discloses a cationic lipid compound, a lipid carrier containing the same and application, and belongs to the technical field of gene therapy. The cationic lipid compound disclosed by the invention has a structure as shown in a formula I, or an isomer, a pharmaceutically acceptable salt and a prodrug thereof. The lipid nanoparticles have the advantages of stable nanostructure, uniform size distribution, good biological biocompatibility, high in-vivo and in-vitro mRNA delivery efficiency, selective organ targeting and the like. The cationic lipid reaction operation is simple, the raw materials are cheap and easy to obtain, and the cationic lipid has high safety, is beneficial to industrial production and quality control, and has a good application prospect.

The invention provides a pancreatic islet organ capable of efficiently maintaining pancreatic islet beta cell identity and a preparation method and application thereof. Specifically, the invention provides the preparation method for the in-vitro pancreatic islet organ, and the preparation method comprises the following steps: carrying out induced differentiation culture on the ZnT8-knocked-out pluripotent stem cells, so as to obtain the mature pancreatic islet organ. The invention also provides a corresponding transplantation composition and application thereof. The invention discloses that ZnT8 knockout is a key factor for effectively maintaining the identity stability of beta cells in pancreatic islet organs. In addition, the pancreas islet beta cell identity maintenance agent is combined with the ZnT8-knocked-out pancreas islet organ for use, so that the identity stability of the pancreas islet organ beta cell can be obviously maintained. The invention provides a new strategy for transplantation treatment of type 2 diabetes, and has excellent clinical transformation value.

The invention provides a composition for assisting in reducing blood sugar and improving insulin resistance and a preparation method of the composition, and relates to the technical field of functional fiber processing. The composition for assisting in reducing blood sugar and improving insulin resistance comprises the following raw materials in parts by weight: 10-15 parts of depolymerization type composite cereal fibers, 3-5 parts of konjac fibers, 3-5 parts of psyllium husk powder, 2-3 parts of sesame powder, 1-2 parts of xylitol and 0.1-0.5 part of vitamin C, the mass ratio of wheat fiber to corn fiber to sweet potato fiber to pea fiber in the depolymerization type composite grain fiber is (25-30): (35-40): (20-25): (10-15). The composition disclosed by the invention can assist in reducing blood sugar and has a good effect of improving insulin resistance.

The invention relates to the field of animal consumer goods, and particularly discloses application of glucan in preparation of animal products for relieving pet stress syndromes. Pet experiments find that beta-1, 3 / alpha-1, 3-glucan can improve the stress syndromes of the indoor cats, specifically, abnormal behaviors of the cats are corrected, and abnormity of multiple systems of organisms such as the immune system, the endocrine system and the urinary system is improved. And when the method is applied to pets, the life quality of the pets can be remarkably improved, more emotional support is provided for pet owners, and the method has practical popularization and application values.

The application discloses a solid dispersion of tolvaptan, and the raw material composition of the solid dispersion comprises tolvaptan, a hydrophilic carrier material, a hydrogen carbonate, and can further comprise a plasticizer and / or an organic acid. The solid dispersion is prepared by a hot melt extrusion process, the solubility of tolvaptan raw material can be obviously increased, and the oral preparation prepared from the solid dispersion can meet the sink condition of dissolution detection, and the accuracy of the detection result is ensured.

The invention discloses a composition containing D-chiro-inositol as well as a preparation method and application of the composition. The composition comprises D-chiro-inositol, Myo-inositol and microcapsule powder, wherein the wall material of the microcapsule powder consists of anhydride modified edible protein and a polysaccharide compound; the edible protein is selected from at least one of spirulina protein, quinoa protein, whey protein and soybean protein; the polysaccharide compound comprises at least one of fucoidin and larch arabinogalactan. Active components are also embedded in the microcapsule powder, and comprise at least one of Omega-3, coenzyme Q10, astaxanthin and vitamin. According to the composition, the stability and bioavailability of fat-soluble active ingredients are improved through microencapsulation, and the composition has a synergistic effect with components such as D-chiro-inositol and Myoinositol, so that insulin resistance is effectively improved, female hormone balance is adjusted, and polycystic ovarian syndrome is improved. The process is simple, is suitable for large-scale production, and can be widely applied to dietary supplements or functional foods.

The present invention relates to methods for treating or reducing the severity of thyroid eye disease. In particular, the present invention provides methods for treating or reducing the severity of thyroid eye disease in patients in need thereof comprising administering an IGF-1R antagonist antibody according to specific dosage regimens. Pharmaceutical compositions comprising the IGF-1R antagonist antibody for use in the methods are also described.

The present disclosure features, among other things, compounds and related compositions that modulate nucleic acid splicing, eg, pre-mRNA splicing, and methods of their use.

The invention discloses a saussurea involucrata culture as well as a preparation method and application thereof, and belongs to the technical field of bioengineering and medicines. The invention relates to a saussurea involucrata culture, in particular to a selenium-rich and chromium-rich saussurea involucrata cell culture with DPP-IV inhibitory activity. The content of selenium in the saussurea involucrata culture reaches 200 mg / Kg dry weight or above, and the content of chromium Cr < 3 + > reaches 20 mg / Kg dry weight or above; in addition, chromium Cr < 6 + > is not detected, and the 70% ethanol extract of the saussurea involucrata cell culture is applied to an in-vitro DPP-IV inhibition test, and the inhibition rate of the 70% ethanol extract of the saussurea involucrata cell culture reaches 99.08%. The selenium-rich and chromium-rich saussurea involucrata culture with the high DPP-IV inhibition rate can be widely applied to preparation of medicines, health foods or functional foods for preventing and / or treating type 2 diabetes, obesity and related metabolic diseases.

Disclosed herein are novel formulations containing relacorilant ((R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone) that are suitable for administration, including oral administration, to patients suffering from disorders amenable to treatment by glucocorticoid receptor modulators (GRMs). Single unit dosage forms comprise softgel capsules containing these formulations. Such softgel capsules may contain, e.g., relacorilant formulations containing 25 milligrams (mg), 50 mg, 100 mg, 200 mg, 300 mg, 400 mg, 500 mg, or other amounts of relacorilant. These novel formulations and single unit dosage forms may be used to treat diseases and disorders including Cushing's syndrome, Cushing's Disease, and other disorders.

Bromocriptine citrate administered to a vertebrate, animal or human, can be used for any purpose including, e.g., the long-term modification and regulation of metabolic disorders, including prediabetes, obesity, insulin resistance, hyperinsulinemia, hyperglycemia and type 2 diabetes mellitus (T2DM) and / or, e.g., the treatment of other medical disorder(s) including immune or endocrine disorders or diseases. Bromocriptine citrate is administered over a limited or extended period at a time of day dependent on re-establishing the normal circadian rhythm of central dopaminergic activity of healthy members of a similar species and sex. Insulin resistance, hyperinsulinemia and hyperglycemia, T2DM, prediabetes, MS or all, can be controlled in humans on a long term basis by such treatment inasmuch as the daily administration of bromocriptine citrate resets neuronal activity timing in the neural centers of the brain to produce long term effects.

The invention discloses an endogenous small molecule metabolite for treating obesity and related metabolic diseases thereof, and belongs to the field of biological medicine. Specifically, the invention relates to application of hippuric acid in preparation of anti-obesity drugs. The invention discloses a technical scheme for treating obesity and related metabolic disorders by hippuric acid, and overcomes the defects of single curative effect, larger side effect or unclear action mechanism and the like in the prior art through the advantages of targeted improvement of liver fatty degeneration, improvement of insulin sensitivity, higher potential safety, provision of a new treatment strategy and the like. The method has remarkable technical progress and clinical application value.

The application relates to the field of biological medicine, and discloses a long-chain modified GHRH agonist and application thereof. The application provides several GHRH agonists which are modified by long-chain fatty acylation at C terminals. Compared with natural GHRH and existing GHRH agonists, the GHRH agonists modified by long-chain fatty acylation at C terminals have greatly improved biological activity, are not prone to be enzymolyzed in vivo, have better stability, have a serum half-life of more than 24 hours, can realize long-acting GHRH receptor agonism, and can play multiple therapeutic effects.

The invention relates to pamoate drug sustained release microspheres and a preparation method thereof. According to the sustained-release microsphere preparation for injection prepared by the preparation method disclosed by the invention, the particle size distribution of the microspheres is relatively narrow, and the release time of active pharmaceutical ingredients can last for about three months to four months. Besides, the microsphere preparation prepared by the invention can maintain stable blood concentration in an animal body, has no large fluctuation of the blood concentration within 3-4 months, and better avoids the occurrence of toxic and side effects.

The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).

The invention belongs to the field of biotechnology and nutritional medicine, relates to a maternal obesity intervention preparation, and particularly relates to a preparation method of a plant embryo fermentation product and application of the plant embryo fermentation product in blocking of trans-generation delivery metabolic diseases. FWG is prepared through a probiotic fermentation technology, obesity, glucose and lipid metabolism disorder and oxidative stress induced by high-fat diet of a parent body can be remarkably improved, and cross-generation transmission of metabolic diseases is blocked by adjusting composition of intestinal flora of the parent body and offspring and a hypothalamic PI3K-Akt signal channel. The invention reveals that maternal FWG intervention passes through a mechanism that a PI3K-Akt pathway is dominated and multiple pathways are coordinated on the transcriptome level for the first time, the HFD-induced offspring hypothalamus metabolism programming abnormality is reversed, and a new central regulation target is provided for cross-generation metabolic disease prevention. The FWG is a wheat processing byproduct, is free of chemical additives, is suitable for long-term dietary supplement, is a natural and safe nutrition intervention scheme, and is suitable for the field of maternal and infant health.

Relacorilant is useful in the treatment of hypercortisolism and cancer. Many drugs useful in treating hypercortisolism or cancer are metabolized by CYP2C9 enzymes. The effects of concomitant administration of relacorilant and a CYP2C9 substrate are disclosed herein.Relacorilant potently inhibited CYP2C9 in an in vitro test, indicating that co-administration of relacorilant and a CYP2C9 substrate would be expected to increase the CYP2C9 substrate plasma exposure more than five-fold in vivo. Significant reductions in CYP2C9 substrate doses would be expected to be required when administered with relacorilant.Surprisingly, no such increase in plasma exposure was seen in human studies. Applicant discloses that relacorilant may be safely co-administered with unmodified doses of a CYP2C9 substrate such as, e.g., tolbutamide, glimepiride, and glipizide. Relacorilant and unmodified doses of CYP2C9 substrate such as tolbutamide, glimepiride, and glipizide may be co-administered to treat hypercortisolism, or may be co-administered to a cancer patient.

The invention relates to a nanoparticle system for small intestine delivery, which is used for delivering exogenous miR-122-5p to the intestinal tract and comprises a miRNA-protamine compound inner core, a liposome middle layer wrapping the inner core and a p123 functional shell wrapping the liposome. Due to the adoption of the technical scheme, a nano-targeting delivery technology is combined with paternal epigenetic programming intervention for the first time, and a brand-new nano-drug treatment thought is provided for intergenerational genetic diseases caused by exposure of environmental adverse factors. By delivering exogenous miR-122-5p to the intestinal tract, the miRNA spectrum unbalanced due to exposure of paternal BaP can be directly improved.

Compositions comprising a first polypeptide comprising a first fragment of an N-terminal extracellular domain of TSHR or an analog or derivative thereof and a dimerization domain and a second polypeptide comprising a second fragment of an N-terminal extracellular domain of TSHR or an analog or derivative thereof and a dimerization domain are provided. Polypeptides comprising fragments of an N-terminal extracellular domain of TSHR comprising at least one mutation that increases solubility, decreases aggregation or both are also provided. Pharmaceutical compositions comprising the composition, polypeptide, nucleic acid systems and molecules encoding the polypeptides of the composition and invention and methods of treatment and determining suitability for treatment using the compositions or polypeptides; as well as methods of producing the compositions or proteins are also provided.

The invention provides an application of synbiotics in preparation of a composition for improving glucagon-like peptide-1 (GLP-1). The composition comprises litchi polyphenol, probiotics and methionine. The probiotics comprise bifidobacterium animalis BCRC910645, bifidobacterium longum BCRC910812, or a combination of the bifidobacterium animalis BCRC910645 and the bifidobacterium longum BCRC910812, so that the content of the glucagon-like peptide-1 is increased.

Disclosed are compounds that are thyroid stimulating hormone receptor antagonists, and methods useful for preventing or treating a thyroid disease.

The invention discloses a lactobacillus rhamnosus HX-4F3 strain and application thereof, and belongs to the technical field of biology. The lactobacillus rhamnosus HX-4F3 disclosed by the invention is preserved in the China Center for Type Culture Collection, and the preservation number of the lactobacillus rhamnosus HX-4F3 is CCTCC (China Center for Type Culture Collection) NO: M 20251454. The invention discloses an application of a strain HX-4F3 in preparation of drugs or food for lowering lipid or / and blood sugar. The invention also discloses application of the compound in preparation of functional food or / and medicines for preventing or / and treating metabolic diseases. The invention also discloses a composition for lowering lipid or / and blood sugar, which comprises a live bacterium of the strain HX-4F3 or freeze-dried powder, a spore preparation, a metabolic supernatant or an inactivated bacterium of the strain HX-4F3, and a pharmaceutically or food acceptable carrier. According to the lactobacillus rhamnosus HX-4F3 provided by the invention, the glucose and lipid metabolism disorder can be remarkably improved through a multiple synergistic mechanism, and the glucose and lipid metabolism disorder can be remarkably improved through the lactobacillus rhamnosus HX-4F3.