340 results about "Pineapple Protease" patented technology

This invention relates to a cysteine protease inhibitor comprising casein which is a protein derived from milk, a partial peptide of casein, and/or hydrolysate of casein as an active ingredient. The cysteine protease inhibitor of the present invention can be used as preventive or therapeutic drug for osteoporosis, malignant hypercalcemia, breast cancer, prostate cancer, periodontitis or bacterial and viral infectious diseases, and food, drink, feed and the like.

PCT No. PCT/JP96/00840 Sec. 371 Date May 20, 1996 Sec. 102(e) Date May 20, 1996 PCT Filed Mar. 29, 1996 PCT Pub. No. WO96/30395 PCT Pub. Date Oct. 3, 1996A pharmaceutical composition for inhibiting cysteine protease which comprises a compound of the formula: wherein R1 is a hydrogen atom or an acyl group; R2, R3 and R4, same or different, are a bond, an amino acid residue or a group of the formula:-Y-R5-in which R5 is a group resulting from imino group removal from an amino acid residue; Y is -O-, -S- or -NR6- in which R6 is a hydrogen atom or a lower alkyl group; A is Z is a hydrogen atom, an acyl group or an optionally substituted hydrocarbon group; n is 1 or 2; provided that when n is 1, then A is and Y is -S- or -NR6-, and, at least one of R2, R3 and R4 is the formula -Y-R5-, provided that when further all Y are -NR6-, at least one of the amino acid residues is not bound to amhydrogen atom at the alpha -carbon thereof but substituted via carbon; provided that when n is 2 and Z is an aldehyde group, then R1 is an acyl group having 6 or more carbon atoms; provided that when n is 2 and A is, then at least one of R2, R3 and R4 is the formula -Y-R5-; or an ester or a salt thereof, and a pharmaceutically acceptable carrier.

Compounds having quinone and quinone analogs useful for pharmaceutical preparations have now been found which inhibit cysteine proteases, in particular, caspases and 3C-cysteine proteases. The cysteine protease inhibitors of the present invention can be identified by their mode of action in disrupting the ability of cysteine proteases and, in particular, caspases to cleave a peptide chain. These compounds are useful in inhibiting cysteine protease or cysteine protease-like proteins and for treating infections diseases or physiopathological diseases or disorders attributed to the presence of excessive or insufficient levels of cysteine proteases.

The present invention relates to a novel polypeptide which displays IgG cysteine protease activity, and in vivo and ex vivo uses thereof. Uses of the polypeptide include methods for the prevention or treatment of diseases and conditions mediated by IgG, and methods for the analysis of IgG.

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.

Activity-based probes, which are specific for certain active cysteine proteases (caspase, cathepsin and legumain) and carry radioactive labels, are disclosed. The present probes comprise an acyloxymethyketone (AOMK) “warhead” that binds only to active enzyme. The probes further comprise peptide-like structure that targets the probe to a specific cysteine protease or protease family, and a radiolabel on the probe, which is bound to the targeted enzyme. It has been found that the present probes are stable in vivo and give specific target images distinguishable over background. The preferred probes are labeled with a positron-emitting agent such as ⁶⁴Cu, ¹²⁵I (SPECT) and ^99mTc (PET). The probes show in vivo half-life and stability well suited for imaging.

A method and a product for cleaning and/or whitening of teeth. Natural human cysteine proteinases are employed for cleaning and whitening purposes and this activity can be blocked by natural cysteine protease inhibitors, which are released secondarily from the product at a later stage. The use of natural cysteine proteinases and their inhibitors provides the advantage that they are man's own proteins, and therefore the risk of allegorization is minimized. In addition, their enzyme kinetics are will known.

This invention relates to compounds of formula (I): 1 wherein: A is C(O) or CH(OH); R.sup.1 is 2 R.sup.2 is H, C.sub.1-6alkyl, C.sub.3-6cycloalkyl-C.sub.0-6alkyl, Ar-C.sub.0-6alkyl, Het-C.sub.0-6alkyl, R.sup.5C(O)--, R.sup.5C(S)--, R.sup.5S0.sub.2--, R.sup.5OC(O)--, R.sup.5R'NC(O)--, R.sup.5R'NC(S)--, adamantyl-C(O)--, or 3 R" is H, C.sub.1-6alkyl, Ar-C.sub.0-6alkyl, or Het-C.sub.0-6alkyl; R'" is H, C.sub.1-6alkyl, C.sub.3-6cycloalkyl-C.sub.0-6alkyl, Ar-C.sub.0-6alkyl, or Het-C.sub.0-6alkyl;

The present invention relates to novel cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

The present invention encompasses an oral composition containing an anti-adhesion agent, preferably a cysteine protease and most preferably ficin. In another aspect, the cysteine protease is in combination with one or more ingredients, such as antibacterial agent and surfactant. The anti-adhesion agent mitigates interaction between a subject oral cavity and plaque-forming materials.

Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.

The present disclosure provides compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the disclosure include peptidyl allyl sulfone compositions that inhibit proteases, for example cysteine proteases, either in vivo or in vitro.

The invention concerns cysteine protease capturing agents capable of highly selective and irreversible binding of the corresponding cysteine protease. Such compounds may have utility in fundamental biological research and diagnostics, e.g. involving labeled or immobilized versions of such compounds, and they may also have potential utility in therapy, based on competitive inhibition of the cysteine protease, as will be readily apparent to those skilled in the art. The present inventors have discovered that such capturing agents can be obtained by modification of a cleavage fragment of a ‘natural’ substrate for the cysteine protease of interest, said modification involving the introduction of a propargyl moiety in such a way that the terminal alkyne group is positioned to allow for interaction with the free thiol group of the cysteine residue at the active site of the protease.

The present invention provides a novel class of macrocyclic compounds, which are useful as cysteine protease inhibitors. Also provided are novel intermediates and methods of preparing the compounds. The invention also provides pharmaceutical compositions comprising the compounds. The compounds and compositions are useful in methods of treating or preventing one or more diseases associated with cysteine protease activity, particularly those associated with calpain activity.

A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: -O-Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.