191 results about "Cysteine Proteinase Inhibitors" 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.

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.

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 relates to treatment of infection by enveloped viruses through the use of papain-like cysteine protease inhibitors and kits thereof. Specifically, methods for treatment of filoviruses as well as other enveloped viruses such as Nipah, in particular using cathepsin inhibitors are described.

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 relates to a biomarker for gastric cancer, CST1 (cysteine proteinase inhibitor, type 2 family), DCC1 (Defective in sister chromatid cohesion homolog 1), IFITM1 (interferon induced transmembrane protein 1) or MELK (maternal embryonic leucine zipper kinase). More particularly, the present invention relates to a diagnostic composition for gastric cancer comprising an agent measuring the expression level of CST1, DCC1, IFITM1 or MELK, a kit comprising the composition, a method for detecting the marker, and a method for screening a therapeutic agent for gastric cancer using the marker.

This invention is directed to novel oxamyl depeptide 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.

The invention discloses a preparation method of a periodic wuchereria malayi compound multivalent DNA (deoxyribonucleic acid) vaccine. The preparation method comprises the following steps of: designing a primer, amplifying BmGAPDH (reduced glyceraldehyde-phosphate dehydrogenase) and BmCPI genes by PCR (polymerase chain reaction), purifying segments of BmGAPDH and BmCPI genes, connecting and converting a T carrier, screening and identifying an I positive recombinant clone, building and identifying an I recombinant expression vector, extracting and purifying a mass of recombinant plasmid and the like. The preparation method is convenient in preparation and good in effect. The periodic wuchereria malayi which is popular in China is taken as a research object, and the periodic wuchereria malayi cysteine proteinase inhibitor / 3-phosphoglyceraldehyde dehydrogenase eukaryotic expression recombinant plasmid is built. The test result proves that the compound multivalent DNA vaccine can induce the mouse to generate the specific immune response reaction, so that a satisfied effect can be obtained, and the periodic wuchereria malayi compound multivalent DNA vaccine can be successfully prepared.

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 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.

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.

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.

The present invention discloses the tumor invasion and metastasis resisting function and application of venin cysteine proteinase inhibitor, and belongs to the field of biomedicine. Through designing and synthesizing sv-Cystatin cDNA according to 99 amino acid sequences of Chinese cobra venin Cystatin protein, cloning to pPICZ alphaA vector and transforming Pichia yeast, stable and high expression engineering bacterium GS115-sv-Cystatin is screened out. Through further inducing expression and purification, the extracorporeal bioactivity experiment shows that the recombinant sv-Cystatin protein has the functions of inhibiting the activity of papain and inhibiting the tumor cell invasion and metastasis obviously, and so do the intracorporeal experiment. The present invention also constitutes pcDNA-sv-Cystatin eukaryotic expression vector. The present invention has huge application foreground in preventing and treating tumor.

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.

There is a demand for improved turbidimetric immunoassays for human Cystatin C in biological samples, especially in human clinical samples of body fluids. The present invention provides a turbidimetric immunoassay method and reagent set enabling measurement of human Cystatin C by turbidimetric methods, resulting in a surprisingly stronger and faster turbidimetric signal than in the present state of the art. The increased and faster signal is accomplished by the use of new reagents and compositions, and enables shorter assay times and kinetic reading with a stronger signal, improving overall assay speed and quality. Improved robustness to lipid interference and improved linearity is achieved.

This invention relates to compounds of formula (I) which are cysteine protease inhibitors, in particular, 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 invention discloses a combined application of a cystatin SN and an alpha-fetoprotein (AFP), and particularly discloses the application of the cystatin SN and the AFP in preparation of a marker for diagnosis and predicting of liver cancer. The invention also discloses a capture agent of the liver cancer marker. A liver cancer detection kit is formed by combining the capture agent with conventional reagents. The obtained kit has the advantages of good specificity, high sensitivity and the like, can be used for early diagnosis of liver cancer, therapeutic effect evaluation in a therapeutic process and monitoring of metastasis and recurrence after therapy, and has test results sooner than clinical symptoms.

The present invention provides a method for diagnosis or prognosis of IgA nephropathy in a subject based on detection of the expression level of one or more biomarker genes selected from the group consisting of thymosin β4 (Tmsb4), serine or cysteine proteinase inhibitor clade E member 2 (Serpine2), secreted phosphoprotein 1 (OPN), butyrophilin-like-2 (BTNL2), S100 calcium binding protein A8 (S100A8), Cystatin C (CysC), and any combination thereof.

The invention relates to an immunoturbidimetry kit for detecting a cysteine proteinase inhibitor C and a preparation method thereof. An application liquid bottle, an antibody suspension liquid bottle and a standard substance bottle are placed in a box body; an application liquid is filled in the application liquid bottle and comprises the following components: 0.01-2% of surfactant, 0.01-1% of preservative, 0.1-20% of sodium chloride and 10-200 mmol / L of buffer solution; a latex suspension liquid coated with a monoclonal antibody of the cysteine proteinase inhibitor C is filled in the antibody suspension liquid bottle and comprises the following components: 0.05-1% of latex coated with the monoclonal antibody of the cysteine proteinase inhibitor C, 0.01-2% of surfactant, 0.01-1% of preservative and 10-200 mmol / L of buffer solution; and a standard substance of the cysteine proteinase inhibitor C is filled in the standard substance bottle. The purpose of large-batch quantitative detection on a biochemical instrument is achieved.

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.

Cathepsin S is a highly active cysteine protease belonging to the papain superfamily. It is found mainly in lymph nodes, spleen, and macrophages and this limited occurrence suggests the potential involvement of this enzyme in the pathogenesis of degenerative disease. The invention relates to novel protease inhibitors, particularly inhibitors of the cysteine proteases of the papain superfamily and more particularly to Cathepsin S. The inhibitors are Furanone derivatives of Formula (II) which have a characteristic non-hydrogen substituent R5. They are selective over other members of the family and in particular show selectivity over other members of the Cathepsin family such as L and K.

The present invention relates to a method for manufacturing a potato protein extract enriched with one or more protease inhibitors, such as potato proteinase inhibitor II, potato proteinase inhibitor I, potato cysteine protease inhibitor, and potato carboxypeptidase inhibitor, that offer a significant therapeutic benefit in controlling appetite, food intake, and body weight in mammals. In particular, the present invention relates to a method of obtaining at least one proteinase protein inhibitor from a plant material comprising the steps of extracting plant proteins from the plant material using an aqueous solvent; heating the extract to denature the plant proteins; cooling the extract to precipitate the denatured plant proteins; performing a separation process on the cooled extract to remove the denatured plant proteins; and salting-out the remaining fraction of the plant proteinase inhibitors designated as PPI fraction, and desalting the PPI fraction.

Compounds of the formula II:whereinR2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline;R3 is H, methyl or F;Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto;Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.