118 results about "Caspase inhibitors" patented technology

The present invention relates to trans-capsularly administering into a diseased joint a high specificity antagonist selected from the group consisting of: i) an inhibitor of a pro-inflammatory interleukin; ii) an inhibitor of TNF-α synthesis; iii) an inhibitor of membrane-bound TNF-α; iv) an inhibitor of a natural receptor of TNF-α; v) an inhibitor of NO synthase,

• • vi) an inhibitor of PLA₂ enzyme; vii) an anti-proliferative agent; viii) an anti-oxidant; ix) an apoptosis inhibitor selected from the group consisting of EPO mimetic peptides, EPO mimetibodies, IGF-I, IGF-II, and caspase inhibitors, and x) an inhibitor of MMPs; and xi) an inhibitor of p38 kinase.

A collection container and a method for collecting a biological sample, particularly whole blood, includes at least one stabilizing agent in an amount effective to inhibit apoptosis. The stabilizing agent comprises or consists of one or more caspase inhibitors.

Described herein are compounds that are useful as caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CN, CHN2, R, or CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, or an aralkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; and R3 is hydrogen, an optionally substituted aryl group, an optionally substituted aralkyl group, or an optionally substituted C1-6 aliphatic group, R4 is an optionally substituted group selected from an aryl group or a heterocyclyl group, or R3 and R4 taken together with the nitrogen to which they are attached optionally form a substituted or unsubstituted monocyclic, bicyclic or tricyclic ring.

Disclosed are compositions and methods for treating cancer that contain caspase inhibitors and/or antioxidant compositions. Formulations containing noncaspase inhibitor anti-cancer agents are also disclosed.

The invention relates to the discovery that the proliferation and survival of pancreatic progenitor cells can be enhanced by contacting the cells with, (1) a caspase inhibitor sufficient to reduce apoptosis in the pancreatic endocrine cells; and, (2) a growth factor in an amount sufficient to increase the level of activated Akt in the pancreatic endocrine cells.

This invention provides caspase inhibitors of formula I:

wherein Z is oxygen or sulfur; R¹is hydrogen, —CHN₂, R, CH₂OR, CH₂SR, or —CH₂Y; Y is an electronegative leaving group; R² is CO₂H, CH₂CO₂H, or esters, amides or isosteres thereof; R³ is a group capable of fitting into the S2 subsite of a caspase enzyme; R⁴ and R⁵ are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.

The invention discloses an organic rare earth bacteria inhibitor, mainly, a binary or ternary compound of lanthanon and 8-Hydroxyquinoline with other organic ligand. The invention also discloses the application of the organic rare earth bacteria inhibitor in preventing the plant bacteria and pests. The plant bacteria and pests include the rice bacteria and pests, the cotton bacteria and pests, the corn bacteria and pests, the vegetable bacteria and pests, and the like. The invention widens the application range of the rare earth to the pesticide filed; secondly, the invention comprehensively takes the advantage of the bacteriostatic function of the organic ligands and the rare earth, can perform double bacteriostatic effect with high bacteriostatic effect; in addition, the dosage of the organic rare earth bacteria inhibitor is less, the toxicity is low, the effective duration is long, the medicine resistance cannot be produced, and the production cost is low.

The invention relates to the use of at least one caspase inhibitor, in particular a caspase-3 inhibitor, for preparing a pharmaceutical composition for the prophylaxis and/or therapy of a viral infection, in particular an infection with an RNA negative-strand virus, preferably an influenza infection, and to a test system for identifying suitable active substances.

Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I: wherein R1 is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R2 is preferably a P2-P4 moiety of a caspase inhibitor. Key intermediates include the azidolactones III and VIII:

Described here are novel, highly selective inhibitors and activity based probes (ABPs) for caspases 3, 7, 8, and 9 and legumain. The compounds selectively inhibit only certain caspases. A positional scanning combinatorial library (PSCL) approach was used to screen pools of peptide acyloxymethyl ketones (AOMKs) containing both natural and non-natural amino acids for activity against a number of purified recombinant caspases. These screens were used to identify structural elements at multiple positions on the peptide scaffold that could be modulated to control inhibitor specificity towards target caspases. Further disclosed are individual optimized covalent inhibitors that could also be equipped with various tags for use as activity based probes, as well as labeled substrates.

This invention provides caspase inhibitors having the formula:

wherein R¹ is CO₂H, CH₂CO₂H, or esters, amides or isosteres thereof; R² and R³ are each independently selected from hydrogen or an optionally substituted C₁–C₆ aliphatic group; and R⁴ and R⁵ are each independently selected from hydrogen, an optionally substituted C₁–C₆ aliphatic group, or R⁴ and R⁵ taken together with the ring to which they are attached form an optionally substituted bicyclic ring. The caspase inhibitors are useful for treating a number of diseases such as cancer, acute inflammatory and autoimmune disorders, ischemic diseases and certain neurodegenerative disorders.

The present invention relates to compounds of formula I:

useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the compounds, and methods of using the compounds and compositions in the treatment of various diseases, conditions, or disorders.

The present invention provides a compound of formula

wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.

The invention relates to a new combination of an anti-MAdCAM antibody with an anti-fibrotic agent, such as a protease inhibitor, preferably a caspase inhibitor. The invention also relates to pharmaceutical compositions comprising the combination of the invention, and the use of the combination for the treatment of liver fibrosis.

This invention provides novel caspase inhibitors useful for prophylaxis or treatment of a number of pathologies, including, for example, Huntington's disease. In certain embodiments the inhibitors include inhibitors of casepase-3 and/or casepase-6.

The present invention relates to compounds of Formula I, II, IVC, VIIIC, IXC, or XC and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, II, IVC, VIIIC, IXC, or XC are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases). Processes for synthesizing tripeptides are provided.