554 results about "Enzyme Inhibitor Agent" patented technology

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

The presently disclosed subject matter relates to compositions comprising Werner Syndrome Helicase (WRN) inhibitors and methods of using the same.

The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a Raf family kinase inhibitor and a KRAS G12C inhibitor of Formula (I), Formula (I-A) or Formula (I-B), pharmaceutical compositions comprising a therapeutically effective amounts of the inhibitors, kits comprising the compositions and methods of use therefor.

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

The invention belongs to the technical field of medicine synthesis, and particularly relates to an inhibitor compound, application and a medicine for treating cancer. The invention provides an inhibitor compound or a pharmaceutically acceptable salt, which can be used for preparing an EGFR kinase inhibitor and preparing a medicine for treating or preventing cancers. The present invention also provides medicaments for the treatment of cancer comprising the inhibitor compound or a pharmaceutically acceptable salt. The compound or the medicine provided by the invention is efficient and low in toxicity, not only has higher anti-tumor activity and can effectively inhibit the growth of cancer cells, but also keeps higher brain permeability, and has wide application prospects.

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 relates to a xanthine oxidase inhibitory peptide derived from green and sweet tuna and application of the xanthine oxidase inhibitory peptide, and belongs to the technical field of polypeptides, and the amino acid sequence of the xanthine oxidase inhibitory peptide is Trp-Thr-Ala (WTA), Trp-Val-Pro (WVP), Trp-Leu-Pro (WLP) or Trp-Gly-Phe (WGF). The invention also provides an application of the inhibitory peptide as or in preparation of a xanthine oxidase inhibitor and an application of the inhibitory peptide as or in preparation of a medicine with an effect of inhibiting uric acid level. The invention also provides a xanthine oxidase inhibitor containing at least one inhibitory peptide or a composition or functional food for inhibiting uric acid. The selected inhibitory peptide is a novel food-borne XO inhibitory peptide, is good in water solubility, non-toxic and good in small intestine absorption and blood brain barrier permeability, has the potential of serving as a xanthine oxidase inhibitor and reducing the uric acid level, and can be used for preparing a medicine for preventing and treating hyperuricemia or serving as a functional food additive.

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.

The invention relates to a salt of a JAK kinase inhibitor and a crystal form of the salt, in particular to a polymorphic form of 2-{3-[3-amino-4-(7H-pyrrolo [2, 3-d] pyrimidine-4-yl)-1H-pyrazol-1-yl]-1-(isopropylsulfonyl) azetidin-3-yl} acetonitrile salt and a preparation method of the polymorphic form. The present application also relates to pharmaceutical compositions containing at least one polymorph and therapeutic or prophylactic uses of the polymorph and compositions.

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.

The invention relates to a novel crystalline form of a helicase-primase inhibitor compound, as well as to pharmaceutical compositions comprising the same, methods for its production, the use of the crystalline form in a medicament and for the treatment of herpes virus infections.

The invention relates to a novel crystalline form of a helicase-primase inhibitor compound, as well as to pharmaceutical compositions comprising the same, methods for its production, the use of the crystalline form in a medicament and for the treatment of herpes virus infections.

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.

Provided are chemical inducers of pluripotency (CIP) which include glycogen synthase kinase inhibitors, TGFβ receptor inhibitors, cyclic AMP agonists and S-adenosylhomocysteine hydrolase (SAH) inhibitors or histone acetylators. A method of inducing pluripotency in a partially or completely differentiated cell by using such chemical inducers of pluripotency is also provided. The method includes: (i) contacting a cell with the CIPs for a sufficient period of time to result in reprograming the cell into a pluripotent stem cell having ESC-like characteristics (CiPSC). Isolated chemically induced pluripotent stem cells (CiPSCs) and their progeny, produced by inducing differentiation of the CiPSCs, can be used in a number of applications, including but not limited to cell therapy and tissue engineering.

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 application of combination of tageteoside and difacitinib or ponatinib to blocking of esophageal squamous cell carcinoma progression. The tageteoside is combined with an FAK inhibitor defacitinib or an Src family kinase inhibitor ponatinib, so that the metastasis of esophageal squamous carcinoma, especially lymphatic metastasis, can be inhibited, the growth of primary focus and metastatic focus esophageal squamous carcinoma cells can be inhibited, and a synergistic anti-cancer effect is achieved.

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 present disclosure relates generally to processes for preparing compounds that are inhibitors of the kinase IRAK4 and the synthetic intermediates prepared thereby.

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 invention provides compounds that are 3CL protease inhibitors and their use in the treatment / or prophylaxis of viral infections, such as coronavirus infections. Experiments prove that the compounds have a relatively strong inhibition effect on 3CL protease, and can block virus replication by inhibiting the activity of the virus main protease 3CL so as to achieve an antiviral treatment effect. The compound has a novel structure prospect for treating and / or preventing coronavirus infection.

The invention discloses a virtual screening method of a tyrosinase inhibitor and a composition with a whitening function. The method comprises the following steps: firstly, constructing and preprocessing a data set of a tyrosinase inhibitor, then respectively establishing a QSAR classification model and a QSAR regression model, and carrying out model training and parameter optimization by utilizing various machine learning algorithms. Virtual screening is performed on a large-scale compound library through the two models, candidate compounds with high inhibitory activity on tyrosinase are preliminarily screened out, and the activity of the candidate compounds is further verified through an in-vitro tyrosinase inhibition test. Experimental results show that the screened compound has a remarkable inhibition effect on tyrosinase and has potential application prospects in whitening cosmetics and freckle-removing medical products. The method is low in cost and short in time consumption, the novel tyrosinase inhibitor can be efficiently found, and a powerful tool is provided for research and development of raw materials with whitening effects.

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.