48 results about "Hydrolase inhibitor" patented technology

The invention discloses a baloxvir derivative and application thereof, and belongs to the field of pharmacy, the baloxvir derivative, a stereoisomer thereof, a crystalline hydrate thereof, a deuterated compound thereof, a solvate thereof, a prodrug thereof and a pharmaceutically acceptable salt thereof, and the structural formula of the baloxvir derivative is shown as a formula I, and the sEH inhibitor is a residue after the esterification of the soluble epoxy hydrolase inhibitor. The application refers to application of the baloxvir derivative or the pharmaceutical composition thereof in preparation of anti-inflammatory and antiviral drugs. A series of sEH inhibitors and BAX are connected to synthesize twin drugs to simultaneously inhibit an NF-kappa B pathway and target virus cap-dependent endonuclease to play anti-inflammatory and antiviral dual roles, and new compounds with anti-inflammatory and antiviral activity are identified in vitro and in vivo. # imgabs0 #

A first aspect of the invention relates to a method of treating or preventing tissue damage, or treating or preventing tissue destruction, in a subject, said method comprising administering to the subject a therapeutically or prophylactically effective amount of a soluble epoxide hydrolase (sEH) inhibitor. A further aspect of the invention relates to a method of treating or preventing leishmaniasis in a subject, said method comprising administering to the subject a therapeutically or prophylactically effective amount of a soluble epoxide hydrolase inhibitor.

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.

This invention is directed to compounds of formula (I):where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

The present application relates to an aromatic-substituted benzimidazole compound, a cis-trans isomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof. The present application also relates to a method for preparing an aromatic-substituted benzimidazole compound, and the use of the aromatic-substituted benzimidazole compound as a soluble epoxide hydrolase inhibitor. The aromatic-substituted benzimidazole compounds described herein exhibit extremely high inhibitory activity against soluble epoxide hydrolase, with IC 50 values in the nanomolar range or even lower.

The invention provides new heterocyclic compounds having the general formula (I) wherein X, Y, A, B, C, and R1 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as soluble epoxide hydrolase inhibitors.

The present invention relates to the technical field of compound synthesis, and more specifically, to a compound containing benzothiazole or benzoxazole, a preparation method thereof, and an application thereof. The structural formula of the compound containing benzothiazole or benzoxazole is as follows: wherein Y represents O or S, X represents hydrogen or halogen, and R represents any one of a substituted or unsubstituted C3-C8 cycloalkyl, a substituted or unsubstituted phenyl, a substituted or unsubstituted C1-C10 alkyl, and a substituted or unsubstituted C3-C10 alkenyl. The compound can be used as a soluble epoxide hydrolase inhibitor, thereby having a certain therapeutic effect on diseases caused by soluble epoxide hydrolase disorders.

Provided herein are methods of preventing, suppressing, or treating cancer cachexia in a subject as well as methods of prolonging survival of a subject in need of cancer cachexia treatment. Such methods include administering an inhibitor of soluble epoxide hydrolase (sEH).

The invention discloses a micro alien soil matrix and a preparation method and application thereof, and the preparation method comprises the following steps: adding organic matters, metal complex ions, fertilizers, urea hydrolase inhibitors and adhesives into soil, and uniformly mixing to obtain micro alien soil aggregates, namely the micro alien soil matrix; seeds of a salt-alkali-tolerant pioneer plant variety are put into the micro soil replacement matrix to obtain seeds wrapped by the micro soil replacement matrix, and then the seeds are sown in soil to be treated. According to the method, the urea hydrolase inhibitor is used for improving the micro alien soil, the improved micro alien soil matrix is used for saline-alkali soil vegetation restoration, the improved micro alien soil matrix creates an excellent microenvironment for seed germination, nutrients and a good structure required by plant growth are provided, germination and growth of pioneer plant seeds are promoted, and the survival rate of saline-alkali soil is increased. The ecological environment of the saline-alkali soil is improved.

Disclosed in the present invention are a soluble epoxide hydrolase inhibitor, synthesis therefor and the use thereof. The structure of the soluble epoxide hydrolase inhibitor is shown as general formula (I), the definition of each substituent being as described in the description and the claims. Compounds represented by general formula (I) of the present invention as the soluble epoxide hydrolase inhibitor can be used for preparing drugs for treating sEH-related or mediated diseases.

The invention relates to a heteroaryl or phenyl imidazole compound containing an aromatic substituent group, and a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug of the heteroaryl or phenyl imidazole compound. The invention also relates to a preparation method of the heteroaryl or phenyl imidazole compound containing the aromatic substituent group, and application of the heteroaryl or phenyl imidazole compound containing the aromatic substituent group as a soluble epoxide hydrolase inhibitor. The aromatic substituent group-containing heteroaryl or phenyl imidazole compound disclosed by the invention shows extremely high inhibitory activity on soluble epoxide hydrolase, and the IC50 value is at the nanomole level or even lower.

Described herein are novel piperidine urea derived compounds and pharmaceutical compositions thereof for the treatment of conditions and diseases mediated by soluble epoxide hydrolases.

The application belongs to the field of new use of drugs, and more particularly relates to application of 3-Deazaadenosine in preparation of a therapeutic drug for treating hypertrophic scars. 3-Deazaadenosine is an S-adenosylhomocysteine hydrolase inhibitor, and has antiviral, anti-inflammatory and other activities. Experiments show that the compound can significantly reduce the modification level of m6A in fibroblasts in hypertrophic scar tissue, inhibit the proliferation and migration of fibroblasts, promote the apoptosis of fibroblasts, and also can reduce the expression levels of Collagen I, Collagen III and alpha-SMA in fibroblasts. Therefore, the compound can be used for preparing a drug for relieving or treating hypertrophic scars, and has important clinical application value.

The invention relates to an application of a soluble epoxide hydrolase inhibitor in the field of transplantation, the soluble epoxide hydrolase inhibitor is TPPU, and the soluble epoxide hydrolase inhibitor is applied in the fields of organ transplantation and tissue transplantation. The TPPU is used for relieving allogeneic mouse heart and skin transplantation immunological rejection, reducing immune cell infiltration in transplantation operation, and inhibiting CD4 + T cell proliferation, CXCR3 chemokine receptor positive and Th1 cell subset proportion. The TPPU inhibits proliferation of primary CD4 + T cells of normal mice and differentiation of Th1 cell subgroups. In organ transplantation and tissue transplantation, the invention provides a single soluble epoxide hydrolase inhibitor TPPU, which can relieve allogeneic mouse heart and skin transplantation immunological rejection, inhibit normal mouse primary CD4 + T cell proliferation and differentiation, and reduce toxic and side effects caused by the use of an immunosuppressant.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a soluble epoxide hydrolase inhibitor, a pharmaceutical composition, a pharmaceutical preparation and application of the soluble epoxide hydrolase inhibitor in rheumatoid arthritis drugs. The invention provides a soluble epoxide hydrolase inhibitor which is a compound shown in a formula (I) or a tautomer, a stereoisomer, a hydrate, a solvate, a crystal form, a pharmaceutically acceptable salt or a prodrug thereof, and substituent groups R1-R23 are defined in the text. The soluble epoxide hydrolase inhibitor provided by the invention can remarkably inhibit proliferation, migration and invasion of fibroblast-like synovial cells, promote apoptosis of the fibroblast-like synovial cells and relieve the symptoms of rheumatoid arthritis, has relatively low side effects, and can prolong the half-life period of a drug in vivo.

Methods of reducing viability of a parasite in a subject involve administering an effective amount of an inhibitor of guanosine-5′-triphosphate cyclohydrolase I (GCH) to the subject. Methods of identifying an agent that reduces viability of an apicomplexan parasite involve culturing an apicomplexan parasite in a cell culture; adding an agent to the cell culture; and detecting a concentration of one or more of 7,8-dihydroncopterin triphosphate, 6-pynivoyl-tetrahydropterin, tetrahydrobiopterin, tetrahydrofolate, folate, dihydrofolate, or dihydrobiopterin in the cell culture after a period of time.

The present disclosure provides compounds, in part, compounds of Formula I or Formula II, and their use in treating medical diseases or disorders, such as neurodegenerative diseases, e.g., Parkinson's disease. Pharmaceutical compositions and methods of making the disclosed compounds are provided. It is contemplated that the compounds are modulators, e.g., inhibitors, of cyclic ADP-ribose hydrolase (CD38). The present disclosure is directed, at least in part, to compounds that modulate (e.g., inhibit) the expression and / or activity of CD38. Also disclosed herein are pharmaceutical compositions comprising at least one disclosed compound and a pharmaceutically acceptable excipient.

This invention is directed to compounds of formula (I):where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

The present invention relates to potent soluble epoxide hydrolase inhibitors. The present invention discloses a series of novel soluble epoxide hydrolase (sEH) inhibitors with improved physical properties that enhance the drug-like properties of the soluble epoxide hydrolase inhibitors for treating sEH-related diseases such as chronic diabetic neuropathic pain.

The invention belongs to the field of biological medicines, and relates to a DDX10 fusion protein and a preparation method thereof. The amino acid sequence of the DDX10 fusion protein is as shown in SEQ ID NO: 1. The method comprises the following steps: 1) amplifying a nucleic acid sequence for coding the DDX10 fusion protein; 2) cloning the nucleic acid sequence into a prokaryotic expression vector; (3) transforming the prokaryotic expression vector into an E. coli strain; 4) inducing expression of the DDX10 fusion protein; and 5) purifying the DDX10 fusion protein. The DDX10 fusion protein disclosed by the invention has ATP hydrolase activity and helicase activity, the method disclosed by the invention is easy for large-scale production and can be used for high-throughput screening of helicase or ATP hydrolase inhibitors, and an expression system of the DDX10 fusion protein is simple.

Disclosed are a long-acting oral pharmaceutical comprising a hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI) and use thereof. Specifically, disclosed is a long-acting oral pharmaceutical formulation comprising a hypoxia-inducible factor prolyl 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 formulation is suitable for administration at intervals of once every one week or longer, making it suitable for long-term administration in the treatment of chronic anemia.

A first aspect of the invention relates to a method of treating or preventing tissue damage, or treating or preventing tissue destruction, in a subject, said method comprising administering to the subject a therapeutically or prophylactically effective amount of a soluble epoxide hydrolase (sEH) inhibitor. A further aspect of the invention relates to a method of treating or preventing leishmaniasis in a subject, said method comprising administering to the subject a therapeutically or prophylactically effective amount of a soluble epoxide hydrolase inhibitor.

The present invention provides novel heterocyclic compounds having the general formula (I) wherein X, Y, A, B, C and R 1 as described herein; compositions comprising the compounds; methods of making the compounds; and methods of using the compounds as soluble epoxide hydrolase inhibitors.(I)

The present disclosure provides compounds and pharmaceutical compositions that inhibit F-ATP hydrolase and methods for treating a disease or condition associated with F-ATP hydrolase.

The present invention relates to soluble epoxide hydrolase (sEH) inhibitors of formula (I)to processes for their obtention and to their therapeutic indications.

Compositions and methods for treating Obstructive Sleep Apnea (OSA)-associated atherosclerosis comprising administering to a subject in need thereof an effective amount of a bile salt hydrolase (BSH) inhibitor such as caffeic acid phenethyl ester

To provide cell permeable PARG inhibitors.SOLUTION: Provided herein are a compound having the following formula, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, Ar, X1, X2, and ring B have the meanings as provided herein. The provided compounds are useful Poly ADP-ribose glycohydrolase (PARG) inhibitors.SELECTED DRAWING: None

The present disclosure provides compounds, in part, compounds of Formula I, Formula II, or Formula III, and their use in treating medical diseases or disorders, such as neurodegenerative diseases, e.g., Parkinson's disease. Pharmaceutical compositions and methods of making the disclosed compounds are provided. It is contemplated that the compounds are modulators, e.g., inhibitors, of cyclic ADP-ribose hydrolase (CD38). The present disclosure is directed, at least in part, to compounds that modulate (e.g., inhibit) the expression and / or activity of CD38. Also disclosed herein are pharmaceutical compositions comprising at least one disclosed compound and a pharmaceutically acceptable excipient.

The present application relates to the technical field of medicines, and in particular to a compound, and a preparation method therefor and a use thereof in the preparation of a soluble epoxide hydrolase (sEH) inhibitor and a peroxisome proliferators-activated receptors (PPARs) agonist. The present application provides a compound, having a structure represented by formula I, II, III, IV, V or VI. The compound provided by the present application has a typical urea structure as the primary pharmacophore of an sEH, and the thiazolidinedione part serves as the primary pharmacophore of PPARs. The sEH inhibitor and PPARs agonist compound provided by the present application has high inhibitory activity against human-derived HsEH and high agonistic activity against a PPAR, and can be used for the preparation of a drug for treating soluble epoxide enzyme and PPARs-mediated diseases.