86 results about "Metalloproteinase inhibitor" patented technology

Peptides of general formula (I): R1AA1-AA2-AA3-AA4-R2 stereoisomers thereof, mixtures thereof or the cosmetically or pharmaceutically acceptable salts thereof, a method for obtaining them, cosmetic or pharmaceutical compositions containing them, and their use for the treatment and / or care of those conditions, disorders and / or pathologies of the skin, mucosae and / or scalp resulting from matrix metalloproteinases (MMP) overexpression or an increase in the MMP activity.

The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.

The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.

A compound of formula (I)wherein X is a -CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.

The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in subjects suffering from or suspected of having a renal injury. In particular, the invention relates to using a plurality of assays, one or more of which is configured to detect a kidney injury marker selected from the group consisting of Hyaluronic acid, Immunoglobulin A, Immunoglobulin G1, Immunoglobulin G2, Insulin-like growth factor-binding protein 7, Alpha-1 antitrypsin, Serum amyloid P component, Metalloproteinase inhibitor 2, Hepatocyte growth factor, Intercellular adhesion molecule 1, Beta-2-glycoprotein 1, Interleukin-1 beta, Neutrophil Elastase, Tumor necrosis factor receptor superfamily member 11B, Interleukin-11, Cathepsin D, C—C motif chemokine 24, C—X—C motif chemokine 6, C—C motif chemokine 13, C—X—C motif chemokines -1, -2, and -3, Matrilysin, Interleukin-2 receptor alpha chain, Insulin-like growth factor-binding protein 3, and Macrophage colony-stimulating factor 1 as diagnostic and prognostic biomarkers in renal injuries.

The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in subjects suffering from or suspected of having a renal injury. In particular, the invention relates to using a plurality of assays, one or more of which is configured to detect a kidney injury marker selected from the group consisting of metalloproteinase inhibitor 2, soluble oxidized low-density lipoprotein receptor 1, interleukin-2, von Willebrand factor, granulocyte-macrophage colony-stimulating factor, tumor necrosis factor receptor superfamily member 11B, neutrophil elastase, interleukin-1 beta, heart-type fatty acid-binding protein, beta-2-glycoprotein 1, soluble CD40 ligand, coagulation factor VII, C—C motif chemokine 2, IgM, CA 19-9, IL-10, TNF-α, and myoglobin as diagnostic and prognostic biomarkers in renal injuries.

The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.

Compounds of formula (I) wherein n, V, R1, R2, R3 and R4 are as defined in the specification are matrix metalloproteinase inhibitors.

The invention provides an epidermal basement membrane structure formation accelerating preparation and a skin external preparation comprising a serine protease inhibitor, and optionally an accelerator of production of extracellular matrix protein components of the epidermal basement membrane. It also provides, as a means for producing artificial skin having an adequately formed basement membrane, an artificial skin-forming medium which comprises a serine protease inhibitor, and optionally an accelerator of production of extracellular matrix protein components of the epidermal basement membrane and a matrix metalloprotease inhibitor, as well as a method for producing the same.

The present invention relates to compounds that are capable of modulating CD154 mobilization and that are useful for stabilizing the thrombotic process and reducing the activation of cells involved in an inflammatory response. The present invention also relates to methods useful for identifying such compounds. The present invention also relates to the treatment of platelets for transfusion with metalloproteinase inhibitors to treat or prevent inflammation. The present invention also includes compositions and methods to treat injury and disease related to such biological processes.

The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in sepsis patients. In particular, the invention relates to using assays that detect one or more biomarkers selected from the group consisting of Insulin-like growth factor-binding protein 7, Beta-2-glycoprotein 1, Metalloproteinase inhibitor 2, Alpha-1 Antitrypsin, Leukocyte elastase, Serum Amyloid P Component, C-X-C motif chemokine 6, Immunoglobulin A, Immunoglobulin G subclass I, C-C motif chemokine 24, Neutrophil collagenase, Cathepsin D, C-X-C motif chemokine 13, Involucrin, Interleukin-6 receptor subunit beta, Hepatocyte Growth Factor, CXCL-1, -2, -3, Immunoglobulin G subclass II, Metalloproteinase inhibitor 4, C-C motif chemokine 18, Matrilysin, C-X-C motif chemokine 11, and Antileukoproteinase as diagnostic and prognostic biomarker assays of renal injury in the sepsis patient.

The present invention relates to a composition for intravaginal and / or for internal mucosal application, comprising an effective amount of a sulfated polysaccharide, one or more of a natural quaternary polymer, a quaternary molecular compound, a metalloproteinase inhibitor, one or more anti-inflammatory agent, an acid pH control buffering system or any combination thereof, and a pharmaceutically acceptable carrier. The invention is further related to a method of treating or alleviating vaginal infection, vaginal dryness, vaginal or vulvo vaginal atrophy, vaginal itching, dyspareunia, vaginal or vulvar pain, vaginal or perivaginal inflammation or for promoting vaginal or wound healing, vaginal atrophy / dryness caused by radiotherapy, chemotherapy and / or hormonal treatment and decreased vaginal boundary lubrication or a disease or condition associated therewith or of improving vaginal boundary lubrication

The present invention describes an improved blood product suitable for use in transfusions comprising, in combination, blood platelets and an inhibitor of platelet glycoprotein Ibα cleavage from platelets, such as a metalloproteinase inhibitor or a TACE inhibitor. Containers for storing the improved blood product for periods of up to about 10 days, and methods for testing and using the recovered improved blood product in patient transfusions, are also provided.

Peptides of general formula (I): R1AA1-AA2-AA3-AA4-R2 stereoisomers thereof, mixtures thereof or the cosmetically or pharmaceutically acceptable salts thereof, a method for obtaining them, cosmetic or pharmaceutical compositions containing them, and their use for the treatment and / or care of those conditions, disorders and / or pathologies of the skin, mucosae and / or scalp resulting from matrix metalloproteinases (MMP) overexpression or an increase in the MMP activity.

The invention relates to a 2-amino-1-(4-nitrobenzophenone)-1-ethanol metalloproteinase inhibitor as well as a preparation and application thereof. The 2-amino-1-(4-nitrobenzophenone)-1-ethanol metalloproteinase inhibitor is a compound with the following general formula (1). Dipeptide-like or kyrine-type compounds of different series can enhance the appetency and metabolization stability of a compound and an enzyme or a receptor and conforms to the basic requirement on inhibitor structures. The invention designs and synthesizes a group of aminopeptidase N inhibitors with totally new structures. A vitro test shows that the inhibitors have no cytotoxin activity, and four compounds which exhibit remarkable vitro inhibitory activity are close to positive control medicine bestatin and can be used as candidate anticancer medicines. The invention also relates to a pharmaceutical composition of a peptide-like compound with a structure indicated by formula (I), and also relates to the pharmacy usage of the pharmaceutical composition.

Compound of formula (I): in which: m represents an integer from 1 to 4 inclusive, and n and p an integer from 0 to 4 inclusive, X represents O, S or a single bond, R1 represent hydrogen or halogen, or alkyl, alkoxy, hydroxy, trihaloalkyl or trihaloalkoxy, R2, R3 and R4, which may be same or different, each represents hydrogen or alkyl, R5 represents hydrogen or halogen, or alkoxy, aryloxy or heteroaryloxy, R6, R7 and R8, which may be same or different, each represents hydrogen or alkyl, or together form, with the atoms carrying them respectively, an optionally substituted heterocycle, R9 represents SO3H, -CO2R10, -CO-NR11R12, or -NR13R14, wherein R10, R11, R12, R13 and R14 each represents hydrogen or alkyl or together (R11 / R12; R13 / R14) form, with nitrogen carrying them, heterocycle, isomers thereof, and addition salts thereof with a pharmaceutically-acceptable acid or base.

The invention discloses a liquid-state calibration product for determining the ProGRP content. The liquid-state calibration product for determining the ProGRP content is prepared from the following components: 10 to 200mmol / L of buffer solution, 0.1 to 0.5 percent (w / v) of preservative, 1 to 5 percent (w / v) of protein stabilizer, 5 to 10 percent (w / v) of sugar stabilizer, 1 to 5 percent (w / v) of EDTA (Ethylene Diamine Tetraacetic Acid), 0.1 to 0.5 percent (w / v) of surfactant, 0 to 5000pg / mL of ProGRP antigen, and 1 to 10mg / L of aprotinin. The liquid-state calibration product for determining the ProGRP content provided by the invention has the advantages that no freeze drying is needed, no redissolving is needed when in use, uncontrollable factors probably occurred in a redissolving processare reduced, and a clinical detection result is more accurate. The sugar stabilizer, a metalloproteinase inhibitor (EDTA), the aprotinin and other components are added, so that the stability of the ProGRP protein is effectively improved, and the prepared ProGRP liquid-state calibration product is better in stability and can be stably stored for 12 months by being refrigerated at 2 to 8 DEG C.

A novel metalloproteinase inhibitor, analogs thereof, polynucleotides encoding the same, and methods of production, are disclosed. Pharmaceutical compositions and methods of treating disorders caused by excessive amounts of metalloproteinase are also disclosed.

The invention provides inhibitors of matrix metalloproteinases that are useful for treating wounds. The inhibitors are peptides having sequences related to cleavage regions of the proenzyme forms of matrix metalloproteinases. The peptide inhibitors of the invention can be formulated into therapeutic compositions and wound dressings that facilitate healing.

Provided herein are methods and compositions for preventing small molecule permeability of the small intestine curing total ischemia by administering glucose to the lumen of the intestine, as well as administration of serine protease or metalloproteinase inhibitors. Also provided are compositions for performing the same.

The present invention relates to compounds that are capable of modulating CD154 mobilization and that are useful for stabilizing the thrombotic process and reducing the activation of cells involved in an inflammatory response. The present invention also relates to methods useful for identifying such compounds. The present invention also relates to the treatment of platelets for transfusion with metalloproteinase inhibitors to treat or prevent inflammation. The present invention also includes compositions and methods to treat injury and disease related to such biological processes.

Animal skins, pelts, and hides are protected from putrefaction, degradation or deterioration caused by metalloproteinases such as collagenase by applying at least one metalloproteinase inhibitor to a fluid in which the animal skin or hide is dipped or soaked, or applying at least one metalloproteinase inhibitor to a solid surface that directly or indirectly comes into contact with the animal skin or hide

A composition containing at least one NSAID formulated for topical administration to a mucous membrane and / or skin for prophylactic or symptomatic therapy. The composition may also contain an anti-irritant such as a non-nutritive sweetener, which improves compliance when applied to an oral or nasal mucous membrane. The composition may also contain a metalloproteinase inhibitor such as a tetracycline class compound at a neutral pH. The composition may be used for patients having or at risk for developing symptoms of viral infection such as cold sores, canker sores, or shingles, or for treatment of rashes due to allergies.

Selective MMP-13 inhibitors are pyrimidine derivatives of the formula or a pharmaceutically acceptable salt thereof,wherein:R2 is hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR4R5, CN, or CF3;E is independently O or S;A and B independently are OR4 or NR4R5;R4 and R5 independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted;n is an integer of from 0 to 6.

The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.

The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.

A composition containing at least one NSAID formulated for topical administration to a mucous membrane and / or skin for prophylactic or symptomatic therapy. The composition may also contain an anti-irritant such as a non-nutritive sweetener, which improves compliance when applied to an oral or nasal mucous membrane. The composition may also contain a metalloproteinase inhibitor such as a tetracycline class compound at a neutral pH. The composition may be used for patients having or at risk for developing symptoms of viral infection such as cold sores, canker sores, or shingles, or for treatment of rashes due to allergies.

The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in subjects suffering from or suspected of having a renal injury. In particular, the invention relates to using assays that detect one or more biomarkers selected from the group consisting of Immumoglobulin A, Metalloproteinase inhibitor 4, and Thrombomodulin as diagnostic and prognostic biomarker assays in renal injuries.

The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.