297 results about "Enzyme Inhibitor Agent" patented technology

Described herein, inter alia, are GTPase inhibitors and uses thereof.

Disclosed are a kinase inhibitor and a pharmaceutical composition comprising the kinase inhibitor. The kinase inhibitor comprises a compound as represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug thereof. The compound and composition above can inhibit wild-type KIT and / or mutant KIT tyrosine kinase activity and treat, prevent, or alleviate diseases, disorders, or conditions associated with wild-type KIT and / or mutant KIT kinase activity.

A composition, comprising a D-amino acid oxidase (DAAO) inhibitor and a N-methyl-D-aspartate (NMDA) modulator. Also provided herein are the method of the uses of by administering to a subject in need thereof an effective amount of the composition.

The invention provides compositions and methods for treating diseases associated with expression of BCMA. The invention also relates to a method of administering a BCMA-targeting agent which is an anti-BCMA antibody molecule or a recombinant non-antibody protein that binds to BCMA, and a gamma secretase inhibitor.

The invention relates to the isolation and characterisation of one or more aptamers against staphylococcal C-S lyase. The invention also provides aptamers, aptamer-conjugates, and minimal functional fragments thereof which may be used to inhibit the activity of said lyases and thereby inhibit Staphylococcus associated malodour.

The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5D”). The compounds have a general Formula I.wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

Methods of treating or ameliorating multiple sclerosis by the dihydroorotate dehydrogenase (DHODH) inhibitor vidofludimus or a pharmaceutically acceptable salt and / or a solvate, in particular a hydrate, thereof or a solvate, in particular a hydrate, of a pharmaceutically acceptable salt thereof, by administering to a human patient a therapeutically effective amount of the DHODH inhibitor, more specifically a daily dose of about 10 mg to about 45 mg.

This invention discloses a compound of formula I, or a pharmaceutically acceptable salt, stereoisomer, ester, prodrug, or solvate thereof. Experimental results show that the compound provided by this invention exhibits high inhibitory activity against PAK4 kinase and PAK I / II selectivity, good liver microsomal stability, and rat PK pharmacokinetic properties, especially with low hERG cardiotoxicity risk, representing a significant improvement over prior art compounds.

This invention provides the application of CTH inhibitors and / or xCT inhibitors in the preparation of drugs for inhibiting mammalian embryo implantation, relating to the field of pharmaceutical technology. This invention verifies the efficacy of cystathionine-γ-lyase (CTH) inhibitors and / or solute carrier family 7 member 11 (xCT) inhibitors in inhibiting mammalian embryo implantation. The results show that xCT inhibitors and / or CTH inhibitors can significantly inhibit the proliferation of luteinized granulosa cells and progesterone secretion in mouse models. Furthermore, in vivo injection of xCT inhibitors and / or CTH inhibitors into mouse models not only significantly inhibits ovulation and the maturation rate of released oocytes, but also significantly reduces the formation of functional corpus luteum and embryo implantation. Therefore, this application provides new ideas and methods for the development of contraceptive drugs.

The application discloses application of a BLM helicase inhibitor in treating myocardial hypertrophy. The application firstly finds that the BLM helicase inhibitor ML216 can significantly inhibit cardiac hypertrophy and myocardial cell fibrosis, thereby providing a new drug for treating myocardial cell hypertrophy diseases in the field, and providing practical experimental evidence and scientific basis for treating myocardial cell hypertrophy diseases, and having a good application prospect in treating myocardial hypertrophy and / or cardiac hypertrophy.

Described herein are compositions comprising a lanthanide (III) modified fatty acid and methods of treating cancer with the composition. In particular, the application includes a lanthanide (III) modified fatty acid is a 9-R′, 10-R″ tri octadecanoate compound. This lanthanide (III) modified fatty acid can be combined with additional therapeutic agents, such as chemotherapeutic agents, radiopharmaceuticals, hormone therapies, CDK inhibitors, epigenetic modulators, selective estrogen receptor modulators, selective estrogen receptor degraders, aromatase inhibitors, phosphatidyl inositol-3-posphate kinase inhibitors, ATP-adenosine axis-targeting agents, signal transduction inhibitors, RAS signaling inhibitors, PI3K inhibitors, arginase inhibitors, HIF inhibitors, AXL inhibitors, PAK4 inhibitors, immunotherapeutic agents, immune checkpoint inhibitors, and agonists of stimulatory or co-stimulatory immune checkpoints.

The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for modulating the activity of Cytochrome BD oxidase, or a mutant thereof. The disclosure also provides pharmaceutically acceptable compositions comprising compounds of the present disclosure and methods of using said compositions in the treatment of various diseases and disorders related to Cytochrome BD oxidase. Formula (I) and (II).

This invention discloses the application of integrin αv inhibitors combined with γ-secretase inhibitors in the preparation of drugs for treating tumors. The study found that the combined use of integrin αv inhibitors and γ-secretase inhibitors in tumor treatment exhibits a synergistic effect, not only inhibiting in situ tumor growth but also significantly suppressing tumor invasion, distant metastasis, and other malignant progression, thus helping to slow tumor progression, improve treatment efficacy, and enhance patient prognosis. Furthermore, the study found that the combined use of integrin αv inhibitors and γ-secretase inhibitors can reduce the production of the intracellular free domain of integrin αv and inhibit the activation of the classical downstream pathway of integrin αv. The combined use of integrin αv inhibitors and γ-secretase inhibitors shows broad application prospects in tumor treatment.

Disclosed herein are methods for increasing sensitivity of a cancer cell to alternating electric fields by administering an AKT inhibitor, a mammalian target of rapamycin (mTOR) inhibitor, a Phosphatidylinositol 3-Kinase (PI3K) inhibitor, and / or a Glycogen synthase kinase 3β (GSK3β) inhibitor. Disclosed are methods of increasing treatment efficacy comprising applying alternating electric fields to a target site of the subject for a period of time, the alternating electric fields having a frequency and field strength, wherein the target site comprises one or more cancer cells, and administering a therapeutically effective amount of one or more of an mTOR inhibitor, AKT inhibitor, PI3K inhibitor, or GSK3β inhibitor to the subject. Disclosed are methods of reducing viability of cancer cells using alternating electric fields for a period of time, the alternating electric fields having a frequency and field strength in combination with either an mTOR inhibitor, AKT inhibitor, PI3K inhibitor, or GSK3β inhibitor and / or a composition or compound that increases cyclin D1. Disclosed are methods of increasing apoptosis of a cancer cell comprising exposing the cancer cell to alternating electric fields for a period of time, the alternating electric fields having a frequency and field strength; and exposing the cancer cell to a PI3K inhibitor.

A hypoxia inducible factor prolyl hydroxy lase inhibitor (PHD inhibitor) for use in the treatment of blood cancer.

Described herein, inter alia, are GTPase inhibitors and uses thereof.

The present invention provides a preparation which can use silver skin as a functional material for cosmetic effect-related applications. The preparation contains an extract derived from silver skin as an active ingredient, and is intended at least to inhibit skin darkness or prevent wrinkle formation. Wherein the preparation contains an elastin inhibitor component derived from a silver skin extract, and is used for preventing the formation of wrinkles. In addition, the preparation contains at least one of a glycosylation inhibitor component derived from a silver skin extract, a carbonylation inhibitor component of a protein, a nitration inhibitor component of a protein, and a nitrotyrosine decomposer component, and is used for inhibiting darkness.

This invention relates to compounds of formula (I) and methods of treatment using the compounds. The compounds of the invention can be used in combination with antibacterial agents to treat bacterial infections. More specifically, the compounds of formula (I) can be used in combination with a class of antibacterial agents known as carbapenems. The novel compounds of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.

The invention relates to process development of a preparation prescription of a coronavirus 3CL protease inhibitor compound Iscartrevir and a preparation method of the coronavirus 3CL protease inhibitor compound Iscartrevir. By strictly screening and optimizing the formula, the preparation with a specific prescription ratio is obtained. According to the preparation, the medicine stability is improved, through the overall synergistic effect of the dry granulation step, in the preparation process of the medicine components, the flowing property of totally mixed materials is good, and the sticking problem is further solved. Meanwhile, the preparation is simple in production process, short in production period, energy-saving, efficient, low in cost and suitable for industrial mass production.

The invention provides a special culture medium for prostate cancer organoid and a culture method thereof, and belongs to the technical field of biological medicines. The special culture medium for the prostatic cancer organoid is composed of a basic culture medium and a culture additive, and the basic culture medium does not contain exogenously added Noggin recombinant protein and R-spondin recombinant protein. The culture additive is prepared from a basic fibroblast growth factor, a keratinocyte growth factor, a fibroblast growth factor 10, insulin, a p38MAPK signal channel inhibitor, an insulin-like growth factor 1, B27, nicotinamide, N-acetylcysteine, hydrocortisone, a ROCK kinase inhibitor, retinoic acid, interleukin 6, prostaglandin E2, a eriocin and androgen. According to the special culture medium for the prostatic cancer organoid, the culture success rate is increased while the cost is reduced.

This disclosure relates to a single pharmaceutical composition comprising a therapeutically effective or prophylactically effective amount of both minoxidil, or a similar antihypertensive vasodilator, and a 5-alpha reductase inhibitor (in some embodiments, the 5-alpha reductase inhibitor is finasteride) for treating or preventing hair loss in a subject. This disclosure also relates to a pharmaceutical package comprising a pharmaceutical composition for oral administration of a therapeutically effective or prophylactically effective amount of minoxidil, or a similar antihypertensive vasodilator, and a pharmaceutical composition for oral administration comprising a therapeutically effective or prophylactically effective amount of a 5-alpha reductase inhibitor (in some embodiments, the 5-alpha reductase inhibitor is finasteride) for treating or preventing hair loss in a subject. The disclosure further provides methods of treating or preventing hair loss in a subject using the disclosed compositions and packages.

This invention discloses a compound of formula (I), or its stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, hydrates, or solvates, wherein X is a sulfur atom or an oxygen atom; and R is optionally an aliphatic substituted amino group, aniline group, or phenolic group. This invention also discloses pharmaceutical compositions containing the compound of formula (I). The compound of formula (I) exhibits excellent DCLK1 kinase activity inhibition ability and can be used to prepare DCLK1 kinase inhibitors, drugs for the prevention and / or treatment of inflammation or cancer.

The application discloses a composition containing a peripheral vasodilator and a 5alpha-reductase inhibitor, effectively solves the transdermal inhibition of the peripheral vasodilator on the 5alpha-reductase inhibitor by adding a specific penetration enhancer, improves the transdermal rate of the active ingredients in the pharmaceutical composition by proportion adjustment, greatly improves the synergistic effect of local combined medication, avoids the side effects brought by oral 5alpha-reductase inhibitor, and improves the safety of the medicine.

The invention belongs to the field of medicinal chemistry, and relates to carbonyl fused heterocyclic derivatives used as ubiquitin-specific protease inhibitors, in particular to a compound shown in the formula (I), an isomer thereof or pharmaceutically acceptable salt thereof.

The present application provides methods for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as a phosphoinositide 3-kinase-delta (PI3Ks) inhibitor, as well as salt forms and intermediates related thereto.

This invention relates to the synthesis of compounds that can be used to treat bacterial infections in combination with other antibacterial agents, and more specifically in combination with a class of antibacterial agents known as carbapenems. The compounds resulting from the novel methods of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.

The present disclosure provides combination therapies for treating a cancer having a BRAF mutation, the combination therapies comprising administering to a subject an effective amount of (a) an epidermal growth factor receptor (EGFR) inhibitor; (b) a mitogen-activated protein kinase (MEK) 1 / 2 inhibitor; (c) a cyclin-dependent kinase (CDK) 4 / 6 inhibitor. Also provided are compositions and kits related to the combination therapies.

Telomerase inhibitor compounds are provided. Some compounds contain a lactone or lactam group covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In other examples, a sulfonamide-containing moiety is covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In some embodiments, the telomerase inhibitor compounds have an amide moiety and a vinyl sulfonamide group bonded to an aromatic group. In other examples, the inhibitor compounds have an isothiazolidine 1,1-dioxide core bonded to a phenyl group. Aspects of the present invention also include pharmaceutical compositions containing the telomerase inhibitor compounds of the present invention, as well as methods for treating telomerase-related diseases or conditions.

The invention discloses a temperature-sensitive gel preparation containing a glutaminase inhibitor as well as a preparation method and application of the temperature-sensitive gel preparation, and belongs to the technical field of biological medicines. The temperature-sensitive gel preparation comprises outer-layer gel and inner-layer gel, the inner-layer gel is coated with the outer-layer gel, the outer-layer gel accounts for 40-75% of the total mass of the temperature-sensitive gel preparation, and the inner-layer gel accounts for 25-60% of the total mass of the temperature-sensitive gel preparation; the outer-layer gel is prepared from the following raw materials: an outer-layer gel matrix, a glutaminase inhibitor, a photosensitizer and a stabilizer; the raw materials of the inner-layer gel comprise an inner-layer gel matrix and an immune checkpoint inhibitor. According to the temperature-sensitive gel preparation, through photo-thermal control, the glutaminase inhibitor is firstly released to relieve the immunosuppression state, then the immune checkpoint inhibitor is released to kill tumors, and the glutaminase inhibitor and the immune checkpoint inhibitor act synergistically, so that efficient anti-tumor immunotherapy is achieved.

A 5α-reductase inhibitor contains saw palmetto extract and seaberry extract as an active ingredient in a synergistic compounding ratio, wherein the compounding ratio by weight of the saw palmetto extract and the seaberry extract is 3:1˜2. The 5α-reductase inhibitor containing the saw palmetto extract and seaberry extract or just the seaberry extract as a 5α-reductase inhibitor can be administered to the human body in order to inhibit 5α-reductase. The 5α-reductase inhibitor is useful as a prostate enlargement inhibitor, an androgenic alopecia inhibitor, and an acne prevention and amelioration agent. The 5α-reductase inhibitor can be part of a food or drink composition or a cosmetic composition.