378 results about "Enzyme Inhibitor Agent" patented technology

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

Described herein, in part, are solid-state forms of the compound represented by Formula (I), pharmaceutical compositions comprising the solid-state forms, processes of making the solid-state forms and methods of using the solid-state forms

An improved solvent system for the formulation and application of N-alkyl thiophosphoric triamide urease inhibitors. These formulations provide safety and performance benefits relative to existing alternatives and enable storage, transport and subsequent coating or blending with urea based or organic based fertilizers. These formulations are comprised primarily of environmentally friendly aprotic and protic solvents (particularly dimethyl sulfoxide and alcohols / polyols) to stabilize the urease inhibitor.

The invention relates to a long-acting oral medicine containing a hypoxia-inducible factor-proline hydroxylase inhibitor (HIF-PHI) and application of the long-acting oral medicine. Specifically, the present application discloses a long-acting oral pharmaceutical preparation containing a hypoxia-inducible factor-proline hydroxylase inhibitor (HIF-PHI) or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers, adjuvants or excipients, the long-acting oral pharmaceutical preparation being suitable for administration at an administration interval of one week or more, therefore, the composition is suitable for long-term administration in treatment of chronic anemia.

The invention discloses a sulfanilamide thiazolyl resorcinol derivative and application of the sulfanilamide thiazolyl resorcinol derivative in preparation of a tyrosinase inhibitor and whitening cosmetics. The structural formula of the derivative is # imgabs0 #, in the formula, R represents a fat (aromatic) group substituent, and R'represents a hydrogen atom or methyl; the preparation method comprises the following steps: taking 2-chloro-1-(2, 4-dimethoxyphenyl) ethanone as an initial raw material, carrying out cyclization condensation on the 2-chloro-1-(2, 4-dimethoxyphenyl) ethanone and thiourea to obtain 4-(2-amino-1, 3-thiazole-4-yl) benzene-1, 3-dimethanol, carrying out reaction on 2-amino of thiazole and different fat (aromatic) sulfonyl chloride, and then removing methyl to prepare the 4-(2-amino-1, 3-thiazole-4-yl) benzene-1, 3-dimethanol. Pharmacological activity tests show that the compound has good inhibitory activity on tyrosinase, which indicates that the sulfanilamide thiazolyl resorcinol derivative can be researched and utilized as a novel tyrosinase inhibitor and whitening cosmetics.

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 an application of a CTH inhibitor and / or an xCT inhibitor in preparation of a medicine for inhibiting mammal embryo implantation, and relates to the technical field of medicines. The application effect of a cystathionine-gamma-lyase (CTH) inhibitor and / or a solute carrier family 7 member 11 (xCT) inhibitor in inhibition of mammalian embryo implantation is verified through research. The research result shows that the xCT inhibitor and / or the CTH inhibitor can obviously inhibit proliferation of corpus luteinized granular cells and secretion of progesterone of a model mouse; meanwhile, by injecting the xCT inhibitor and / or the CTH inhibitor into the mouse model in vivo, ovary ovulation and the maturation rate of the ovulated oocyte nucleus can be remarkably inhibited, functional corpus luteum formation and embryo implantation can be remarkably reduced, and then a new thought and method are provided for development of contraceptive drugs.

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.

Conjugates comprising a fibroblast activation protein α (FAP-α)-targeted ligand, a bifunctional or trifunctional linker, and a phosphatidylinositol-3-kinase (PI3k) inhibitor; uses of the conjugates in the manufacture of a medicament for inhibiting progression of fibrosis in a subject; and a method of use in inhibiting progression of fibrosis in a subject.

The invention relates to a TANK binding kinase 1 inhibitor and pharmaceutical application thereof, and belongs to the technical field of biological medicine. The TANK binding kinase 1 inhibitor is a compound ITA-9. The invention also provides an application of the compound ITA-9 in preparation of a pharmaceutical composition for preventing and / or treating TBK1 activity-related diseases, wherein the TBK1 activity-related diseases comprise infectious diseases, autoimmune diseases, metabolic diseases or cancers and the like. The invention discloses an application of a compound ITA-9 as a TANK binding kinase 1 (TBK1) inhibitor in preparation of a pharmaceutical composition for preventing and / or treating TBK1 activity related diseases for the first time. The compound has the potential of being developed into TBK1 inhibitor drugs and drugs for treating TBK1-related diseases such as infectious diseases, autoimmune diseases, metabolic diseases and cancers, provides a new treatment drug for clinic, and has good clinical application value and wide application prospects.

Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

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.

Methods and systems for determining and / or confirming a response to a checkpoint kinase 1 (Chk1) inhibitor, a Wee1 inhibitor, an ATR inhibitor, or a combination thereof, and methods of administering a Chk1 inhibitor, a Wee1 inhibitor, an ATR inhibitor, or a combination thereof to a subject determined to be responsive to such therapy are provided herein. The present disclosure, inter alia, solves this problem by identifying responder and non-responder populations to Chk1 inhibition therapy (e.g., prexasertib), Wee1 inhibition therapy, ATR inhibition therapy, or combinations thereof (e.g., prior to initiation of therapy) by defining a simple treatment benefit prediction biomarker signature (also referred to throughout as a response prediction signature) that effectively predicts treatment benefit.

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).

The invention belongs to the technical field of biology, and relates to an exosome preserving fluid and an exosome preserving method. The preservation solution comprises glycerol with the concentration of 4-6% (V / V), trehalose with the concentration of 0.5-1.5% (W / V), albumin with the concentration of 0.05-0.2% (W / V), a sterile protective agent with the concentration of 0.01-0.03% (W / V), vitamin E with the concentration of 0.05-0.1% (W / V), ethylenediamine tetraacetic acid with the concentration of 0.05-0.2 mM, a protease inhibitor with the concentration of 0.05-0.1 mM and a basic solvent of 0.1 M phosphate buffer solution. The invention relates to an exosome preserving fluid and an exosome preserving method which are extremely low in toxic effect on a human body and can effectively preserve exosomes and maintain biological activity of the exosomes.

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.

The present disclosure provides, inter alia, pharmaceutical compositions comprising IL-2 inducible T cell kinase (ITK) inhibitors, as well as methods for increasing Th1 cell activity, treating cancer, treating autoimmune diseases, treating allergies, and reversing T cell exhaustion by administering to a patient an effective amount of an IL-2 inducible T cell kinase (ITK) inhibitor.

The present invention relates to a plasmin inhibitor, a preparation method thereof and an application in the pharmaceutical field. Specifically, the present invention provides a compound represented by formula I, a preparation method thereof and an application in the pharmaceutical field, which relates to the field of medicinal chemistry. In formula I, R1 is H or halogen; R2 and R3 are each independently selected from H, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalicyclic group, substituted or unsubstituted heteroaryl; n = 0, 1 or 2. The compound provided by the present invention has high blood coagulation and hemostasis activities, high blood drug concentration and exposure in vivo, good safety, and has good clinical application prospects.

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.