96 results about "Endothelin I" patented technology

A compound of the formula (I):or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, a method of antagonizing endothelin, methods for the inhibition of bone metastases, methods for the prevention of growth of new metastases, methods for the inhibition of bone turnover, and methods for the prevention of bone loss in patients, including cancer patients, using an endothelin ET-A receptor antagonist.

Provided are devices and methods for treating or preventing smooth muscle cell proliferation caused by endothelin-mediated conditions. In particular, a medical device comprising a structure which is implantable within a body lumen and means on or within the structure for releasing an endothelin (A) receptor antagonist at a rate effective to inhibit smooth muscle cell proliferation. The device can be, for example, an expansible stent or a graft, and the means can include a matrix coating, wherein the endothelin (A) receptor antagonist can be dispersed within the coating or disposed directly on the structure and under the matrix. The methods and devices of this invention can be used to decrease the incidence of restenosis as well as other thromboembolic complications resulting from implantation of medical devices.

Methods, compositions and articles of manufacture for contributing to the treatment of a solid cancerous tumor are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ETB) to enhance the delivery of a chemotherapeutic agent to a solid tumor in mammals, including humans.

The invention discloses a method for separately culturing a human adipose mesenchymal stem cell and a dedicated culture medium thereof. The culture medium used for separately culturing the human adipose mesenchymal stem cell comprises an animal cell basic culture medium, fetal calf serum, an epidermal growth factor and a platelet-derived growth factor. The final concentration of the fetal calf serum is 1-200 mL / L, the final concentration of the epidermal growth factor is 1-100 ng / ml, and the final concentration of the platelet-derived growth factor is 1-100 ng / ml. The adipose mesenchymal stem cell of the invention has CD31-, CD34-, CD45- and HLA-DR-, as well as the phenotype of CD29+, CD44+, CD105+ and Flk-1+. The specificity cell surface marker and the relevant antihelion molecule of a skeletal muscle cell and a vascular endothelia cell can be expressed after inducement is performed in vitro. Muscle fiber, vascular endothelin and functional muscle satellite cells can be differentiated in a muscle injury model mouse body caused by medicine and the expression of dystrophin protein on the ducheme muscular dystrophy (DMD) model mouse (mdx) myolemma can be partially recovered, so as to release the pathological symptom of the model mouse.

Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

The invention relates to a composition of plant extracts and application thereof in skin whitening and moisture preservation. The composition comprises the following active ingredients in percentage by weight: 5 to 90 percent of green tea extract, 5 to 50 percent of ginkgo leaf extract and 5 to 45 percent of centella extract, wherein the composition accounts for 0.5 to 20 percent when applied to preparing external products of skin, and the composition is uniformly mixed with medically-acceptable excipients or carriers in proportion to prepare products in forms of gel, cream, serosity, aqueous solution agents, emulsions or solids. The composition has the effects on skin whitening and moisture preservation without adding moisture preserving components; compared with products with similar application, the composition has stronger effects on skin whitening and moisture preservation and smaller dosage; the composition is safe, has no toxic or side effect, has low allergy rates and inflammation probability, penetrates into skin dermis, does not change the normal apoptosis process of cells, restrains tyrosinase, dopachrome tautomerase, DHICA oxidase and endothelin appropriately and balances the metabolism of melanin, so that the color and luster of the skin is more natural; and in addition, the generated skin whitening effect is definite, and the composition is convenient to use in cosmetics.

Methods of administering and pharmaceutical compositions of a biphenyl sulfonamide compound which is a dual angiotensin and endothelin receptor antagonist are disclosed for treating diseases.

A novel targeting peptide from the C-terminal of endothelin and / or a novel fusogenic peptide from hemagglutinin are optionally conjugated to the carboxy group of 1,2-dioleoyl-sn-glycero-3-succinate and incorporated into liposomes for therapeutic treatment. The novel targeting peptide directs liposomes to lung cells, and, therefore, is useful for delivering liposomes encapsulating cholinesterase genes, particularly, the human serum butyryl cholinesterase (Hu BChE) gene, as a treatment against nerve agents. It is emphasized that this abstract is provided to comply with the rules requiring an abstract which will allow a searcher or other reader quickly to ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the appended issued claims. 37 CFR §1.72(b).

Aliquots of extracts from ethnopharmacological plants that have activity against the effects of sarafotoxins present in snake venom are isolated and identified as antagonists of endothelin using a fluorescence-based assay. A process is provided for the identification of an antagonist of an endothelin selected from the group consisting of endothelin-1, endothelin-2, endothelin-3 and mixtures thereof. The process comprises extraction of ethnopharmacological plants with a solvent followed by evaporation of the solvent to form an aliquot containing at least one component of the extract, optionally purifying and isolating one or more component by chromatography, and subjecting the aliquot or purified component to a competitive fluorescent binding assay using biotinylated endothelin-1, wherein the plants having activity against the effects of one or more sarafotoxins present in snake venom.

Methods, compositions and articles of manufacture for contributing to the treatment of cancers, including solid tumors, are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ETB) to enhance the delivery and resulting efficacy of a chemotherapeutic agent.

This invention relates to depilatories and external preparations, each of which contains endothelin or its agonist, and also to a depilating method characterized by administering endothelin or its agonist.As the depilatories and external preparations according to the present invention inhibit growth of hair in mammalian skin, their application to the human body as drugs or cosmetics permits safe and effective removal of hair from the body. These depilatories and external preparations are also usable as wool harvesting preparations.

The invention relates to an artificial transcription factor comprising a polydactyl zinc finger protein targeting specifically a receptor gene promoter fused to an inhibitory or activatory protein domain, a nuclear localization sequence, and a protein transduction domain. In particular examples these receptor gene promoters regulate the expression of the endothelin receptor A, the endothelin receptor B, the Toll-like receptor 4 or the high-affinity IgE receptor. Artificial transcription factors directed to the endothelin A or B receptors are useful in the treatment of diseases modulated by endothelin, such as cardiovascular diseases, and, in particular, eye diseases, e.g. retinal vein occlusion, retinal artery occlusion, macular edema, optic neuropathy, central serous chorioretinopathy, retinitis pigmentosa, Leber's hereditary optic neuropathy, and the like. Artificial transcription factors directed to the Toll-like receptor 4 or the IgE receptor are useful for the treatment of autoimmune disorders, and the like, and allergic disorders, respectively.

A combination therapy for cardiovascular diseases, in particular essential hypertension, pulmonary hypertension and / or congestive heart failure, involving administering a synergistic combination of at least one inhibitor of neutral endopeptidase, at least one inhibitor of the endogenous endothelin producing system, and at least one AT1 receptor antagonist.

The invention discloses a novel human epidermal culture method. The method includes the following steps of (1), skin sample treatment and cell separation; (2), culture of epidermal cells; (3), passage of the epidermal cells and stripping of tissue engineered skin; (4), quality inspection of the tissue engineered skin. A preparation method of a KMSFM culture medium includes: taking DSFM of Gibco as a basis; using low calcium ion concentration; adding bovine pituitary extract (BPE), bovine insulin, bovine transferrin, bFGF, cortisol, heparin and endothelin at the same time. By the novel human epidermal culture method, bovine serum is removed, mixing of non-human-derived ingredients can be reduced greatly, and cost and unsafe factors are reduced; a culture system coated by I-type collagen is used, cell growth slowness caused by removing of nourishing layer cells is avoided, and the novel human epidermal culture method can be used for treating skin pigment diseases such as leukoderma and giant pigmented nevus.

The invention relates to an in vitro method for detecting the formation of endothelins during serious illnesses, especially cardiovascular diseases, inflammations, sepsis and cancer, in whole blood, plasma or serum of a human patient for medical diagnosis. Using this method, relatively long-lasting peptide fragments, especially a C-terminal peptide fragment, of the processed primary prepro- or proendothelins that contain neither the actual biologically active endothelin nor its direct precursor, big endothelin, can be detected.

Methods for treating conditions or disorders which can be alleviated by reducing food intake are disclosed which comprise administration of an effective amount of an endothelin or an endothelin agonist, alone or in conjunction with other compounds or compositions that affect satiety. The methods are useful for treating conditions or disorders, including obesity, Type II diabetes, eating disorders, and insulin-resistance syndrome. Pharmaceutical compositions for use in the methods of the invention are also disclosed.

Methods and compositions for contributing to the treatment of cancers, especially ovarian tumors, are disclosed. The methods and compositions utilize an endothelin B agonist (ETB) to enhance the delivery and resulting efficacy of chemotherapeutic agent(s) (e.g., cisplatin and / or cyclophosphamide).

Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

The present invention relates to therapeutic protocols and pharmaceutical compositions designed to treat and prevent cancer. More specifically, the present invention relates to a novel method of treating cancer using antagonists to the endothelin B receptor (ETB) or inactive mimic forms of endothelin-1. The pharmaceutical compositions of the invention are capable of selectively inhibiting the early events associated with the development of cancer. The present invention further relates to screening assays to identify compounds which inhibit ETB activation.

Methods, compositions and articles of manufacture for contributing to the treatment of cancers, including solid tumors, are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ETB) to enhance the delivery and resulting efficacy of a chemotherapeutic agent.

The invention discloses an application of a traditional Chinese medicine composition in preparation of a medicine for improving the endothelium function of blood vessels. The traditional Chinese medicine composition of the invention can effectively decrease plasma endothelin (ET) of patients with heart failure, improve the level of nitric oxide (NO) and calcitonin gene-related peptide (CGRP); the traditional Chinese medicine composition of the invention can effectively improve the endothlelium function of blood vessels of patients with chronic heart failure, and the symptoms of heart failure and degree thereof are also reduced with the improvement of the endothelium function of blood vessels.

The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.

This invention relates to novel endothelin receptor antagonists that selectively inhibit the interaction between Endothelin-1 (ET-1) and endothelin type-A receptors, their derivatives, acceptable acid addition salts. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by endothelin receptor antagonists, particularly those diseases and conditions that are beneficially treated by selective inhibitors of endothelin type-A receptors.

The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease caused by abnormal increase of production of angiotensin II or endothelin I based on chymase activity, wherein the agent has a selective inhibitory action on chymase.