31 results about "Relaxin" patented technology

The present disclosure provides relaxin-2 fusion protein analogs having an enhanced in vivo half-life and methods of making the same. Also disclosed herein are methods of treating relaxin-2 related conditions or diseases using the relaxin-2 fusion protein analogs described herein.

Synthetic H2 RLN mRNA constructs that induce expression of relaxin, methods of preparing such synthetic H2 RLN mRNA constructs, and methods of administering such constructs to mammals to facilitate delivery of offspring or methods of administering such constructs to non-pregnant mammals to facilitate procedures involving the reproductive tract.

The present disclosure provides relaxin-2 fusion protein analogs with enhanced in vivo half-life and methods for making the same. Also disclosed herein are methods of treating relaxin-2-associated disorders or diseases using the relaxin-2 fusion protein analogs described herein.

The present invention relates to uses of heterodimeric Relaxin fusion polypeptides, in particular for the treatment of heart failure with pulmonary hypertension.

To provide small molecule relaxin family peptide receptor-1 (RXFP1) agonists and uses thereof.SOLUTION: The present invention provides a compound of the following formula, and a method of using the compound and a pharmaceutically acceptable salt thereof for treating a patient for cardiovascular, pulmonary, and / or renal conditions, diseases, and / or disorders.SELECTED DRAWING: None

The invention provides a monoclonal antibody aiming at recombinant porcine relaxin, an ELISA (enzyme-linked immunosorbent assay) detection method and application of the monoclonal antibody in a kit for improving the quality and conception rate of frozen semen of pigs. The recombinant porcine relaxin protein is obtained after analysis and optimization by bioinformatics software, and the monoclonal antibody and the polyclonal antibody obtained by using the recombinant porcine relaxin protein as the antigen have the advantages of strong specificity, high binding force with the antigen and the like; and the established ELISA kit is higher in sensitivity during detection. According to the method disclosed by the invention, the relaxin in the seminal plasma is originally and quantitatively detected, the quality of the frozen seminal fluid can be more effectively improved, and various indexes are obviously improved.

This invention discloses an interchain disulfide bond Cys A24 -Cys B23 H2Relaxin derivatives with thioether bonds as alternatives and their synthetic methods, wherein the structural formula of the H2Relaxin derivatives is shown below: This invention first utilizes diaminodioic acid molecules to synthesize interchain disulfide bonds (Cys) in a single solid-phase process using an N-fluorenemethyloxycarbonyl (Fmoc) solid-phase polypeptide synthesis method. A24 -Cys B23 The folded refolding precursor of H2Relaxin derivatives with thioether bonds as substitutes was then efficiently obtained via one-step oxidative folding and refolding to yield interchain disulfide bonds (Cys). A24 -Cys B23 The H2Relaxin derivative is replaced by a thioether bond.

The invention relates to a traditional Chinese medicine composition for treating ischemic heart failure and a preparation method thereof, and belongs to the field of traditional Chinese medicine pharmacy, and the traditional Chinese medicine composition is prepared from the following raw material medicines in parts by weight: 5-15 parts of cassia twig, 5-15 parts of bighead atractylodes rhizome, 5-15 parts of poria cocos, 6-12 parts of rhizoma zingiberis, 5-15 parts of acanthopanax, 10-30 parts of fructus polygoni orientalis, 3-9 parts of verbena, 6-12 parts of dogwood and 3-9 parts of honey-fried licorice root. The composition can remarkably reduce the level of N-terminal proB-type natriuretic peptide, remarkably improve pathological changes of heart tissues of model rats, regulate and control the heart functions of the model rats, improve the systolic function of the heart, relieve expression of inflammatory factors such as interleukin-1beta, interleukin-6 and tumor necrosis factor-alpha of the rats and improve the anti-inflammatory effect of the rats. The action mechanism of the compound relates to a plurality of pathways such as extracellular matrix receptor interaction, a chemotactic factor signal pathway, a relaxin signal pathway, a cyclic adenosine monophosphate signal pathway, a nuclear factor-kB signal pathway, fatty acid metabolism and a Toll-like receptor signal pathway, and the compound is an effective medicament for treating ischemic heart failure.

The present disclosure relates to a fusion protein of relaxin or an analogue and the medical use thereof. Specifically, the present disclosure relates to a fusion protein comprising relaxin or an analogue thereof and a serum albumin binding domain, and the medical use thereof for treating diseases (for example, heart failure). Moreover, the present disclosure relates to a serum albumin binding molecule, which comprises an immunoglobulin single variable domain (for example, VHH) capable of binding to serum albumin, has good plasma stability, and can be used for prolonging the plasma half-life of a drug.

Disclosed is a compound of formula (I), in which R1, R2, R3, R4, R5, X1, X2, X3, X4, and X5 are described herein. The small molecule compounds of formula (I) activate the functional activity of relaxin family peptide receptor 2 (RXFP2), thereby providing therapeutic treatments for a variety of disorders, such as a bone disorder, hypogonadism, cryptorchidism, polycystic ovary syndrome, cancer, infertility, or an ocular wound.

The present invention provides a monoclonal antibody targeting recombinant porcine relaxin, an ELISA detection method, and its use in a kit for improving the quality and conception rate of frozen porcine semen. The recombinant porcine relaxin protein, obtained through analysis and optimization using bioinformatics software, and the monoclonal and polyclonal antibodies generated using this as an antigen exhibit strong specificity and high antigen binding affinity. The resulting ELISA kit offers enhanced sensitivity. This invention uniquely quantitatively detects relaxin in seminal plasma, effectively improving post-freeze semen quality and significantly enhancing various indicators.

A tetrahydroisoquinoline compound, a preparation method therefor, a pharmaceutical composition containing said compound, and a use thereof are provided. Specifically, the nitrogen-containing heterocyclic compound of formula (I), a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, or a racemate thereof are provided. The compound may be used for preparing a pharmaceutical composition for treating a disease or condition related to the activity or expression levels of relaxin family receptor 4.

Disclosed herein are relaxin immunoglobulin fusion proteins useful for the treatment or prevention of a disease or condition in a subject.

The invention relates to an application technology in the field of drug research, in particular to an anti-tumor cell relaxin alkaloid compound as well as preparation and application thereof. The alkaloid compounds are compounds 1-4 as shown in a formula I, the molecular formula of the compound 1 is C29H35NO4, and the structural formula of the compound 1 is 1 in the formula I; the molecular formula of the compound 2 is C29H35NO4, and the structural formula is 2 in the formula I; the molecular formula of the compound 3 is C29H35NO5, and the structural formula is 3 in the formula I; the molecular formula of the compound 4 is C29H39NO5, and the structural formula is 4 in the formula I. Compared with a traditional chemical synthesis route, the method adopts a microbial fermentation technology to realize preparation of the target compound, not only avoids complex organic synthesis steps and use of expensive and toxic reagents, but also has the characteristics of simple and convenient process flow, mild culture conditions, shorter production period, lower raw material cost and the like, is suitable for large-scale production, and has a wide application prospect. The invention provides an economic and sustainable preparation way for subsequent drug development, and shows a good application prospect in the field of antitumor drug research and development.

Provided are a novel tetrahydroisoquinoline compound, a preparation method therefor, a pharmaceutical composition containing said compound, and a use thereof. Specifically, provided are a nitrogen-containing heterocyclic compound as represented by general formula (I), a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, or a racemate thereof. The compound may be used for preparing a pharmaceutical composition for treating a disease or condition related to the activity or expression levels of relaxin family receptor 4.

Provided are a novel tetrahydroisoquinoline compound, a preparation method therefor, a pharmaceutical composition containing said compound, and a use thereof. Specifically, provided are a nitrogen-containing heterocyclic compound as represented by general formula (I), a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, or a racemate thereof. The compound may be used for preparing a pharmaceutical composition for treating a disease or condition related to the activity or expression levels of relaxin family receptor 4.

The present disclosure provides relaxin-2 fusion protein analogs with enhanced in vivo half-lives and methods for making same. Also disclosed herein are methods of treating relaxin-2-associated disorders or diseases using the relaxin-2 fusion protein analogs described herein.

The present disclosure relates to pharmaceutical formulations comprising heterodimeric relaxin fusion polypeptides, particularly heterodimeric relaxin 2 fusion polypeptides, and uses thereof. Thus, the present disclosure provides pharmaceutical formulations comprising relaxin fusion polypeptides and kits comprising the pharmaceutical formulations as well as uses thereof, including methods of treatment. The pharmaceutical formulations of the present disclosure are particularly useful in the treatment of cardiovascular diseases, such as in the treatment of heart failure.

The invention relates to the technical field of dog and cat breeding health detection, in particular to a pregnancy detection kit and method for rapidly and quantitatively detecting dog and cat relaxin, and a sample processing unit is used for completing collection and pretreatment of dog and cat samples; a sample detection area, a quality control area, a water absorption area and a sample adding area are sequentially arranged on the detection card body; a standard curve reference module is arranged in the quantitative reference unit, and the standard curve reference module is a chip or a paper reference card used for storing standard curve data; the signal processing and output unit comprises a signal reading module, a result storage module and a transmission module, and the result storage and transmission module is used for recording detection data; the environment control unit comprises a temperature control module, the specific reaction efficiency and the signal stability are ensured, and the technical problems that in an existing dog and cat pregnancy detection technology, detection is slow, quantification is difficult, samples are limited, the environment is sensitive, and data are difficult to manage are solved.

The present disclosure relates to dosing regimens, methods, and pharmaceutical compositions for treating heart failure with pulmonary arterial hypertension comprising administering a heterodimer relaxin fusion protein.

Relaxin (RLN) analogs are disclosed including modifications that increase half-life when compared to native, human RLN, that maintain selectivity to the RXFP1 receptor and that provide in vitro and in vivo stability for improved druggability properties and less immunogenicity. Pharmaceutical compositions also are disclosed that include one or more of the RLN analogs described herein in a pharmaceutically acceptable carrier. Methods of making and using the RLN analogs also are disclosed, especially for treating cardiovascular, pulmonary and / or renal conditions, diseases or disorders.

Relaxin-2 is used as a broad spectrum substitute for glucocorticoids, mineralocorticoids, corticosteroids and analogs thereof for the treatment of tissue and endothelial injury without causing glycogen allogenesis, Cushing syndrome and Cushing-like adverse reactions. Particularly, under the condition of autoimmune diseases and organ transplantation, the medicine and treatment of tissue and endothelial injury repair are supported by promoting immunosuppressive regulatory T cells (Treg).

The present disclosure relates to a fusion protein of relaxin or an analog thereof and its pharmaceutical use. Specifically, the present disclosure relates to a fusion protein comprising relaxin or an analog thereof and a serum albumin binding domain, and its pharmaceutical use for treating diseases (such as heart failure). Further, the present disclosure relates to a serum albumin binding molecule comprising an immunoglobulin single variable domain (such as VHH) capable of binding to serum albumin, having good plasma stability, and being usable for extending the plasma half-life of a drug.

The present invention relates to heterodimeric relaxin fusion polypeptides, in particular to heterodimeric relaxin 2 fusion polypeptides and uses thereof. Accordingly, the present invention provides relaxin fusion polypeptides, nucleic acid molecules, vectors, host cells, pharmaceutical compositions and kits comprising the same as well as uses thereof including therapeutic methods. The polypeptides and compositions of the present invention are particularly useful for the treatment of cardiovascular diseases, for example for the treatment of heart failure.

Relaxin (RLN) analogs are disclosed including modifications that increase half-life when compared to native, human RLN, that maintain selectivity to the RXFP1 receptor and that provide in vitro and in vivo stability for improved druggability properties and less immunogenicity. Pharmaceutical compositions also are disclosed that include one or more of the RLN analogs described herein in a pharmaceutically acceptable carrier. Methods of making and using the RLN analogs also are disclosed, especially for treating cardiovascular, pulmonary and / or renal conditions, diseases or disorders.

The invention belongs to the technical field of tumor prevention and treatment, and particularly relates to a nano-drug capable of simultaneously inhibiting fibroblast activation and angiogenesis. The nano-drug for simultaneously inhibiting fibroblast activation and angiogenesis is a bionic nano-carrier SNPs (Single Nucleotide Polymorphism) loaded with modified relaxin analogue polypeptide B7-33. The bifunctional bionic nano-drug B7-33-SNPs adopted by the invention can be delivered to tumor tissues in a targeted manner, and meanwhile, the fibroblast activation-mediated extracellular matrix and angiogenesis are inhibited, and the fibroblast activation-mediated angiogenesis is also inhibited. The results can lay a good technical foundation for targeted prevention and treatment of bile duct cancer, and provide a new technical thought for prevention and treatment of other diseases.

The present disclosure provides relaxin-2 fusion protein analogs with enhanced in vivo half-lives and methods for making same. Also disclosed herein are methods of treating relaxin-2-associated disorders or diseases using the relaxin-2 fusion protein analogs described herein.

The present application relates to a kind of traditional Chinese medicine composition for treating ischemic heart failure and preparation method thereof, belong to the field of traditional Chinese medicine pharmacy, the traditional Chinese medicine composition includes: cassia 5-15 parts, white atractylodes 5-15 parts, poria 5-15 parts, dried ginger 6-12 parts, acanthopanax 5-15 parts, water red flower seed 10-30 parts, verbena 3-9 parts, dogwood 6-12 parts, fried licorice 3-9 parts.The composition can significantly reduce N-terminal B-type natriuretic peptide level, significantly improve model rat heart tissue pathological changes, regulate the heart function of model rat, improve the systolic function of heart, and can reduce the expression of rat interleukin-1 beta, interleukin-6, tumor necrosis factor-alpha and other inflammatory factors, involve extracellular matrix receptor interaction, chemotactic factor signal pathway, relaxin signal pathway, cyclic adenosine monophosphate signal pathway, nuclear factor-kappa B signal pathway and multiple pathways, and is effective drug for treating ischemic heart failure.

The invention belongs to the technical field of biology, and particularly relates to a composition for enhancing sensitivity of glioma chemotherapeutic drugs and application of the composition. The composition comprises a macropinocytosis inhibitor and an autophagy inhibitor, and the macropinocytosis inhibitor comprises any one or more of EIPA and cytochalasin D; the autophagy inhibitor is prepared from any one or more of 3-methyladenine, bajulomycin A1 and hydroxychloroquine. The glioma is glioblastoma, and the chemotherapeutic drug is temozolomide. The invention also provides a pharmaceutical composition for treating glioma. The pharmaceutical composition consists of the macropinocytosis inhibitor, the autophagy inhibitor and temozolomide. Researches prove that the combination of the macropinocytosis inhibitor and the autophagy inhibitor can effectively enhance the chemotherapy effect of glioma temozolomide and prolong the lifetime of glioblastoma patients. The composition provided by the invention has important significance and potential clinical application value for improving GBM chemotherapy resistance.

Relaxin-2 fusion protein analogs with enhanced in vivo half-life and methods for making the same are described. Also described are methods of treating relaxin-2-associated disorders or diseases using the relaxin-2 fusion protein analogs.