35 results about "Calpain inhibitors" patented technology

The present invention relates to compounds derived from biphenyl with activity as calpain inhibitors. One compound of the present invention is a 2,2′-disubstituted biphenyl, where the substituents in the 2 and 2′ positions of the biphenyl skeleton are chains containing structures related to amino acids, including fragments of aminocarbonylic compounds where at least one of the substituents in said 2- or 2′-positions is bonded to the biphenyl skeleton via a thiocarbonyl group, forming compounds with thioamide functionality. The present invention also encompasses any of the conformational isomers (atropisomers) of said compound of formula I. The compounds of formula I have application in the preventive or therapeutic treatment of a degenerative disease.

The invention relates to derivative compounds of partially-reduced isoquinoline with substitution of a sec-butyl group at position 3 with calpain inhibitor activity. The inventive compound comprises an ester or amide derived from (3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-yliden)-acetic acid and (3-sec-butyl-1-thioxo-2, 3-dihydro-1H-isoquinolin-4-yliden)-acetic acid. Compounds having formula I or II can be used in the preventive or therapeutic treatment of a degenerative disease.

A process is provided of delivering at least one active agent cargo molecule into an neuronal cell whereby a cargo molecule is placed within a synthetic vesicle such as a liposome and a biotinylated protein such as an antibody is bound to the synthetic vesicle to form a protein bound synthetic vesicle whereby the protein recognizes a receptor expressed on the surface of a neuronal cell, and exposing the protein bound synthetic vesicle to the cell until the cargo molecule is delivered into the neuronal cell. Numerous cargo molecules are delivered by the inventive synthetic vesicle including a calpain inhibitor and a caspase inhibitor. The protein illustratively targets a cellular receptor for a ligand such as glutamate, glycine, dopamine, nicotine, muscarine, acetylcholine, or serotonin, and the like.

The invention discloses application of a calpain inhibitor to preparation of medicine for relieving lung inflammation caused by cigarette smoke. After the calpain inhibitor calpeptin is used for performing intraperitoneal injection on a passive smoking mouse and treating BEAS-2B cells treated by cigarette smoke extracts, the increase of lung and in vitro bronchus epithelial cell inflammation caused by cigarette smoke can be obviously relieved. Therefore the calpain inhibitor can be used for preparing medicine for relieving lung inflammation increase caused by cigarette smoke; potential and good application prospects are realized in the field of inflammatory lung disease treatment.

The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.

Methods for treatment and / or prevention of nerve degeneration in mammals using aza-peptide epoxide caspase inhibitors are provided. Aspects of the present disclosure include aza-peptide epoxide compositions to treat or prevent diseases, for example stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis, neuropathies, Huntington's disease, dentatorubropallidoluysian atrophy, spinocerebellar atrophies, spinal bulbar muscular atrophy, diabetes, amyotrophic lateral sclerosis and other motor neuron diseases. The disclosed methods can be used in combination with calpain inhibitors to treat disease or pathological conditions related to the activity of caspases and calpain associated with a specific disease or condition. Such treatable conditions include stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis, neuropathies, Huntington's disease, dentatorubropallidoluysian atrophy, spinocerebellar atrophies, spinal bulbar muscular atrophy, nerve degeneration associated with diabetes, amyotrophic lateral sclerosis and other motor neuron diseases, nerve degeneration secondary to primary demyelinating disorders, among others.

Molecules that selectively inhibit or stimulate the activity of isoforms of calpains are presented. Methods for screening and characterizing such molecules are also presented. Specific functions of calpain-1 calpain-2 in long term potentiation (LTP), learning and memory, neurodegeneration and diseases of synaptic dysfunction are characterized using novel calpain inhibitors, substrates and related methods. The compounds, compositions, and methods described herein are expected to be useful, for treating neurodegenerative diseases and other diseases of synaptic function, and for modulating cognition in patients in need thereof.

The invention discloses the substance used for treating or preventing the ischemic brain injuries or neurodegenerative diseases by sustaining the TRPC6 level of nerve cells. The substance may be calpain inhibitors, reinforcing agents of TRPC6 expression, or NMDA receptor antagonists. The invention also discloses the uses of said substance for manufacturing medicaments for preventing or treating ischemic brain injuries or neurodegenerative diseases.

The present invention relates to compounds derived from biphenyl with activity as calpain inhibitors. One compound of the present invention is a 2,2′-disubstituted biphenyl, where the substituents in the 2 and 2′ positions of the biphenyl skeleton are chains containing structures related to amino acids, including fragments of aminocarbonylic compounds where at least one of the substituents in said 2- or 2′-positions is bonded to the biphenyl skeleton via a thiocarbonyl group, forming compounds with thioamide functionality. The present invention also encompasses any of the conformational isomers (atropisomers) of said compound of formula I. The compounds of formula I have application in the preventive or therapeutic treatment of a degenerative disease.

The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and / or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds.The carboxamide compounds are compounds of the general formula Iin whichW—R2 is selected fromand R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y1, Y2, Y3 and Y4 are CRy, or one or two of the variables Y1 to Y4 are a nitrogen atom and the remaining variables are CRy, wherein the radicals Ry may be identical or different and have the meanings mentionend in the claims.