481results about "Phosphorous compound active ingredients" patented technology

The invention relates to the field of biological medicine, in particular to a compound and a preparation method and application thereof. Particularly, the invention relates to a compound shown in a formula (I) or pharmaceutically acceptable salt, stereoisomer, solvate, isotope labeled compound or polymorphic substance thereof, a preparation method thereof, a pharmaceutical composition containing the compound and application thereof, the compound can be used as a sodion channel inhibitor, has an analgesic effect, and can be used for preparing a sodion channel inhibitor. The compounds of the present application also have a variety of excellent properties. # imgabs0 #

Provided are novel prodrug salts of selective aquaporin inhibitors, their use as pharmaceuticals, and pharmaceutical compositions comprising them, and novel processes for their synthesis and novel intermediates for use in their synthesis. Also provided is use of a compound for the prophylaxis, treatment, and control of aquaporin-mediated conditions. Aquaporin inhibitors, e.g., inhibitors of AQP4 and / or AQP2, may be of utility in the treatment or control of diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord), hyponatremia, and excess fluid retention, as well as diseases such as epilepsy, retinal ischemia and other diseases of the eye, myocardial ischemia, myocardial ischemia / reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines.

Methods for enhancing weight loss, or preventing or treating obesity or other conditions related thereto, such as diabetes, involve administering a GLP-1 agonist together with, or prior to, administering a mitochondrial uncoupler. Use of the uncoupler increases weight loss and enhances treatment of obesity and obesity-related medical conditions, such as by preventing weight regain after cessation of administration of the GLP-1 agonist.

The present invention relates to mitochondrial-targeted agents and their utility in increasing telomere length and / or suppressing telomere shortening.

The invention relates to the technical field of medical chemistry, in particular to a bridge oxygen site regulatively modified rhodamine anti-cancer fluorescent compound as well as a preparation method and application thereof. The invention develops the rhodamine anti-cancer fluorescent compound of which the meso site is functionalized by tetraarylethene and the bridge oxygen site can be regulated and modified, the fluorescent compound has adjustable red light-near infrared fluorescence emission and excellent fluorescence quantum yield, and the quantum yield can be as high as 99%; the fluorescent compound specifically targets mitochondria, and mainly inhibits growth of tumor cells by inducing para-apoptosis; under irradiation of 655 nm near-infrared laser, ferroptosis is further triggered, efficient treatment of tumor cells is achieved through chemical-photodynamic synergistic effect, and a new treatment thought is provided for overcoming tumor drug resistance.

Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and / or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and / or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

Provided are compounds of formula (I) which can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Also provided are pharmaceutical compositions comprising the compounds, methods of preparing the compounds and the use in the manufacture of medicaments for preventing or treating a disease or condition related to p53 mutants.

The present invention relates to methods for treating endometriosis or preventing recurrence of endometriosis. In particular, the present invention relates to methods for treating endometriosis and recurrence thereof comprising administering to a female having endometriosis a pharmaceutical composition comprising an S-alkylisothiouronium derivative, specifically S-ethylisothiouronium diethylphosphate. The methods and pharmaceutical composition of the present invention preserve fertility and enable conception.

The present disclosure provides methods of treating an inflammatory skin disease (e.g., psoriasis) in a subject by administering an inhibitor of Hypoxia Inducible Factor 1α (HIF1α) or an inhibitor of glucose transporter 1 (Glut1). The present disclosure also provides topical formulations comprising an inhibitor of HIF1α or an inhibitor of Glut1.

Provided in the present invention are a phosphorus-containing compound, a pharmaceutical composition and the use thereof. Specifically, provided are a compound as represented by formula I, a pharmaceutically acceptable salt, an ester, a stereoisomer, a tautomer, a polymorph, a solvate, a metabolite, an isotopic derivative or a prodrug thereof. The phosphorus-containing compound of the present invention can effectively treat diseases and conditions mediated by TEAD, such as cancer.

Methods and compositions for treating and preventing cell ballooning and other diseases or medical conditions are provided. The diseases or medical conditions are characterized by cell degeneration or cell death as a part of the disease pathogenesis. Cell ballooning is a condition associated with storage of excess fat in the liver. nutritional or biochemical imbalance, damage to mitochondria, ATP depletion, or virus infection. A mitochondrially targeted antioxidant compound is administered to a subject in need thereof, whereby excess fat is metabolized.

The present invention relates to a drug, a combination agent, a pharmaceutical composition, a preparation, a treatment or prevention method, a drug for inhibiting drug resistance, a method for screening patients, and the like for ALK fusion gene-positive cancer, which has positive expression of FGFR1 and positive expression of FGF2, and which is obtained by combining a compound having ALK inhibitory activity with an FGFR inhibitor. The present invention also relates to a drug, a combination agent, a pharmaceutical composition, a preparation, a treatment or prevention method, or a drug for inhibiting drug resistance, a method for screening patients, and the like.

This disclosure relates to quaternary phosphonium compounds having lipophilic groups. In certain embodiments, this disclosure relates to quaternary phosphonium compounds having chemical formula as reported herein. In certain embodiments, this disclosure relates to compositions and devices comprising or coated with quaternary phosphonium compounds disclosed herein. In certain embodiments, this disclosure relates to preventing or treating a microbial infection or cancer using quaternary phosphonium compounds disclosed herein.

This present disclosure provides reliable methods and apparatus for delivering microdroplets containing an active pharmaceutical ingredient (API) to underlying substrates. A control system is provided to ensure that the API dosage is both accurate and repeatable.

Disclosed are newly designed polymeric compounds (lipid-polymer conjugates) useful for forming lipid bilayers and liposomes comprising them, lipid bilayers and liposomes formed thereby, and uses thereof. Also disclosed is a method of preparing a new design of a polymeric compound (lipid-polymer conjugate).

Provided are novel formulations of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate as described below and uses thereof.

Disclosed herein are compounds, pharmaceutical compositions, and methods for treating RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer, that inhibit RIPK1.

Cationic pillar[n]arenes, e.g., positively charged poly-ammonium, poly-phosphonium and poly-imidazolium pillar[5-6]arene derivatives are capable of inhibiting or preventing biofilm formation, and facilitating existing biofilm decomposition. A composition for inhibiting or disrupting biofilm, e.g., bacterial or fungal biofilm, formation, or reducing biofilm, can include a pharmaceutically acceptable carrier, and a cationic pillar[n]ene.

The present disclosure relates to compounds of formula (I), which are formylpeptide 2 (FPR2) receptor agonists and / or formylpeptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods using the compounds to treat, for example, atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. TIFF2023533037000263.tif35138

Triphenylphosphonium hydroxytyrosol TPP-HT, its synthesis method and application in the preparation of drugs for improving aortic endothelial cell function. TPP-HT can significantly increase the reduction of human aortic endothelial cell activity caused by saturated fatty acids, inhibit the inflammatory response and oxidative stress caused by saturated fatty acids, and at the same time increase the synthesis of ATP in vascular endothelial cells and the expression of mitochondrial complex II. By anti-inflammatory and protecting mitochondrial function, it can prevent the occurrence and development of atherosclerosis. Therefore, TPP-HT has good application prospects in preventing cardiovascular diseases such as atherosclerosis caused by high-fat-induced endothelial damage, opening up a new medical approach for preventing a series of problems of cardiovascular diseases such as atherosclerosis caused by endothelial damage due to unbalanced dietary structure, and providing a new basis for the development of new drugs.

The present disclosure relates to a technique for synthesizing with high yield a novel compound targeting mitochondria through a simple process, and the novel compound synthesized thereby. The novel compound targeting mitochondria of the present disclosure can be synthesized with high yield through a simple process and the compound thus prepared and nanoparticles containing same exhibit the therapeutic effects of targeting mitochondria, inhibiting gastric cancer, and treating inflammatory bowel disease, and systemic sclerosis and thus can be utilized for mitochondrial targeting applications, as anticancer compositions, or as therapeutic compositions for immune diseases.

The present invention relates to compounds containing a phosphonium salt group, as well as related salts, double salts, solvates, and pharmaceutical compositions. The present invention also relates to the use of such compounds and compositions in the treatment and prevention of medical disorders and diseases, particularly in the treatment and prevention of cancer.

Provided herein are gene replacement approaches to restore HOXA11AS in the colon for patients with IBD, e.g., UC. Further, since HOXA11os levels inversely correlate with disease severity this lncRNA can also be used as a sensitive colon specific disease relevant biomarker.

The present invention relates to an anti-tumor use of a phosphorus compound. Specifically, the present invention provides a use of a compound of formula (I), an optical isomer thereof, a racemate thereof, a solvate thereof, a pharmaceutically acceptable salt thereof or a deuterated compound thereof in preparation of a composition or a preparation, wherein the composition or the preparation is used for preventing and / or treating tumors. The compound of the present invention exhibits excellent precise therapeutic efficacy against tumors characterized by high expression of kinase B.

The invention discloses a serine hydrolase inhibitor as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The technical scheme of the invention provides a serine hydrolase inhibitor. The serine hydrolase inhibitor has one or more of the structural formulas provided by the invention. In addition, the invention also provides a preparation method of the serine hydrolase inhibitor. The preparation method comprises the following steps: mixing the warhead (1) # imgabs0 #, the benzaldehyde sulfonyl compound (2) and sodium sulfate to prepare an imine intermediate; and adding the imine intermediate into palladium on carbon under the action of a reducing agent to obtain the serine hydrolase inhibitor. In addition, the invention also provides an application of the serine hydrolase inhibitor in preparation of drugs for inhibiting PNPLA6 protein expression. The inhibitor provided by the invention can specifically inhibit the PNPLA6 protein.