284 results about "Cysteine protease" patented technology

The present invention relates to new compounds that act as specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I). Those compounds are represented by the general formula and the pharmaceutical salts thereof, in which R is an acyl-residue including urethane and peptide, or a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 carbocyclic, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, all of the above residues may be optionally substituted, or is H, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R' is a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 cycloalkenyl, C2-C9 heterocycloalkyl, C3-C9 heterocycloalkenyl, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues my be optionally substituted, or is H.

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.

In one aspect, the invention relates to an immunogenic composition that includes a mutant Clostridium difficile toxin A and / or a mutant Clostridium difficile toxin B. Each mutant toxin includes a glucosyltransferase domain having at least one mutation and a cysteine protease domain having at least one mutation, relative to the corresponding wild-type C. difficile toxin. The mutant toxins may further include at least one amino acid that is chemically crosslinked. In another aspect, the invention relates to antibodies or binding fragments thereof that binds to said immunogenic compositions. In further aspects, the invention relates to isolated nucleotide sequences that encode any of the foregoing, and methods of use of any of the foregoing compositions.

PCT No. PCT / GB96 / 01707 Sec. 371 Date Feb. 26, 1998 Sec. 102(e) Date Feb. 26, 1998 PCT Filed Jul. 17, 1996 PCT Pub. No. WO97 / 04004 PCT Pub. Date Feb. 6, 1997The invention provides compounds for use in the treatment of allergic diseases including juvenile asthma and eczema. The compounds can inhibit IgE mediated reaction to major environmental and occupational allergens and can also have a prophylactic effect against allergic disease by preventing allergic sensitization to environmental and occupational allergens when administered to at-risk individuals (e.g., those at genetic risk of asthma and those exposed to occupational allergens in the workplace). The compounds are also useful for inactivation or attenuation of the allergenicity of allergens in situ. The invention provides compounds and ligands per se, pharmaceutical compositions containing the compounds, processes for producing the compounds and pharmaceutical compositions, and methods for using the compounds and compositions in treatment or prophylaxis of IgE mediated allergic diseases and in inactivation or attenuation of allergens in situ. The invention also enables the reduction or destruction of the viability of allergy-causing organisms.

The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I), which can be used in the treatment of malignant cell degeneration, immune deseases impaired wound healing and metabolic diseases of humans and are represented by the general formula in which R is a peptide or a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 carbocyclic, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R′ is a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 cycloalkenyl, C2-C9 heterocycloalkyl, C3-C9 heterocycloalkenyl, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues may be optionally substituted, or is H.

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.

In one aspect, the invention relates to an immunogenic composition that includes a mutant Clostridium difficile toxin A and / or a mutant Clostridium difficile toxin B. Each mutant toxin includes a glucosyltransferase domain having at least one mutation and a cysteine protease domain having at least one mutation, relative to the corresponding wild-type C. difficile toxin. The mutant toxins may further include at least one amino acid that is chemically crosslinked. In another aspect, the invention relates to antibodies or binding fragments thereof that binds to said immunogenic compositions. In further aspects, the invention relates to isolated nucleotide sequences that encode any of the foregoing, and methods of use of any of the foregoing compositions.

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 modified Fc-containing molecules including modified antibodies characterized by increased resistance to host and pathogen-derived proteases, ability to interact with FcγR receptors except with FcγRI, and lack of induction of IL-10 secretion by macrophages, and methods of using and making them.

The present invention relates to modified Fc-containing molecules including modified antibodies characterized by increased resistance to host and pathogen-derived proteases, ability to interact with FcγR receptors except with FcγRI, and lack of induction of IL-10 secretion by macrophages, and methods of using and making them.

This invention relates to the therapeutic, diagnostic and pharmacogenetic use of nucleic acids and proteins involved in human proteolytical system such as serine and cysteine proteases and their inhibitors and pharmaceutical agents and other therapies affecting these. This invention discloses methods for the treatment and prevention of cardiovascular diseases such as coronary heart disease (CHD), acute myocardial infarction (AMI), chronic CHD, arterial hypertension (HT) and cerebrovascular stroke and metabolic disorders such as the metabolic syndrome (MBO) and obesity and methods for detecting or diagnosing a risk of, or predisposition to the said diseases in a subject, for selecting treatment in a subject and for selecting subjects for studies testing cardiovascular, anti-diabetic and anti-obesity drugs, as well as to transgenic animals.

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.

The invention provides a cysteine protease inhibitor C test kit, wherein the kit comprises a reagent R1 and a reagent R2, the reagent R2 is a reaction solution for promoting specific binding of an antigen and an antibody, the reagent R2 is a polystyrene latex particle mixture coated by an anti-human cystatin C antibody and is put in a proper buffer solution. The polystyrene latex particle mixture in the reagent R2 is a mixture of large-diameter polystyrene latex particles and small-diameter polystyrene latex particles. The kit is high in detection sensitivity, high in accuracy, good in linearity within the test range, good in stability and low in production cost.

This invention is directed to novel oxamyl dipeptide ICE / ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

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.

Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.

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.

In some embodiments, the present disclosure relates to an avian-free egg white composition comprising 45-63% Ovalbumin, 9-15% Ovotransferrin, 0-15% Ovomucoid, 3- 5% Ovoglobulin G2, 3-5% Ovoglobulin G3, 2.5-5% Ovomucin, 3-5% Lysozyme, 1-2% Ovoinhibitor, 0.8-1.5% Ovoglycoprotein, 0.6-1.0% Flavoprotein, 0.3-0.8% Ovomacroglobulin, 0.02-0.1% Avidin, and 0.02-0.1% Cystatin. In some embodiments, the composition comprises an edible yeast and one or more of the preceding proteins. In some embodiments, the avian-free egg white further comprises one or more of: flavor enhancers, calcium supplements, added vitamins, and a gelling agent. In some embodiments, the present disclosure pertains to a non-allergenic egg-white composition for human consumption. In some embodiments, the present disclosure pertains to methods of making the avian-free egg-white composition.

This invention relates to 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. They have the following structure: Formula (I)

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 invention relates to a triazine compound with a structure represented by a formula A, or a stereoisomer, a prodrug, an active metabolite or a pharmaceutically acceptable salt, a solvate or a crystal form thereof, a pharmaceutical composition of the triazine compound, the stereoisomer, the prodrug, the active metabolite or the pharmaceutically acceptable salt, the solvate or the crystal form, and a use method of the triazine compound. In addition, the invention also relates to a method for preparing a 3C-like cysteine protease inhibitor or a medicine for treating and / or preventing virus infectious diseases. In particular, the present invention relates to the use for treating viral infectious diseases such as Middle East Syndrome Related Coronavirus (MERS-CoV), Severe Acute Respiratory Syndrome Related Coronavirus (SARS-CoV), Influenza A virus, Influenza B virus, Novel Coronavirus Pneumonia (COVID-19) and the like.

The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

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.