58 results about "Cystein protease" patented technology

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 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 I

in which

W—R² is selected from

and R¹, R², R^3a, R^3b, Y¹, Y², Y³, Y⁴, X, Q, m, k, R^w and R^w* 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 CR^y, or one or two of the variables Y¹ to Y⁴ are a nitrogen atom and the remaining variables are CR^y, wherein the radicals R^y may be identical or different and have the meanings mentionend in the claims.

The invention discloses a triazine compound with a structure as shown in a general formula I or pharmaceutically acceptable salt, isomer, metabolite, prodrug, solvate or hydrate, pharmaceutical composition and application thereof. The triazine compound provided by the invention overcomes the defects of single structure, lack of non-covalent high-efficiency small-molecule inhibitors and the like of the existing anti-coronavirus drugs, has good inhibitory activity on 3C-like cysteine protease, has excellent pharmacokinetic properties, and has a good treatment effect on infectious diseases.

This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3 and R4 are indicated therein, 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, osteoarthritis and rheumatoid arthritis.

The invention discloses an engineered bombyx mori baculovirus vector. The vector is obtained by replacing chitinase and cysteine protease genes in a bombyx mori baculovirus vector Bm-Bacmid with a Cm expression cassette and an egfp expression cassette which are in series connection. The egfp gene in the engineered vector is subjected to integrated expression, and can be used for monitoring cell transfection or infection and conditions after insects are infected in real time. By utilization of the vector, a bombyx mori bidensovirus nsl gene expression cassette is inserted into a transposition site, and a BmN cell or bombyx mori is infected by the prepared recombinant virus, so that expression of a targeting gene can be obtained. Results show that: the vector lacks Chitinase and Cystein Protease genes, delays cell lysis and insect liquidation, facilitates expression of an exogenous gene and inhibits digestion of a targeting protein to a certain degree, thus increasing the expression amount of the nsl gene and laying sound foundations for deep research of the structure and functions of the NS1 protein.

Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R₁, R₂, R₃, R₄, R₅, R₆, R₈, R₉ and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds

In a first aspect thereof, the present invention provides a method for treatment and/or prevention of a disease selected from the group consisting of psoriasis and squamous cell carcinoma by inhibiting the expression of squamous cell carcinoma antigen (SCCA) by cells. In another aspect thereof, the present invention provides a method for screening for substances that inhibit epidermal parakeratosis, wherein the activity of a candidate substance that inhibits cysteine protease inhibitory activity possessed by squamous cell carcinoma antigen 1 (SCCA-1) is used as an indicator.

The invention discloses a pear lignin synthesis gene PbMC1a/1b and application of the pear lignin synthesis gene PbMC1a/1b in genetic improvement of fruit quality. The PbMC1a/1b gene is a cysteine-like protease isolated and cloned from Dangshansu pear with high lignin content, an applicant names the gene as PbMC1a/1b, the sequence is shown as SEQ ID NO.1, and the corresponding amino acid sequenceis shown as SEQ ID NO.2. A gene construction over-expression vector is introduced into arabidopsis thaliana, obtained transgenic plants are verified by a biological function, the cloned PbMC1a/1b genecan promote the cell walls of fibers between ducts, lignocellulosic fibers and vascular bundles to be obviously thickened, lignin accumulation in stems is promoted and plant growth is inhibited, theexpression of genes related to lignin biosynthesis is increased, new genetic resources is provided for molecular design and breeding of fruit quality, and the PbMC1a/1b gene is an important candidategene for future genetic engineering to improve fruit quality breeding.

The invention discloses a peanut cysteine protease encoding gene AhRD21A, the construction of an overexpression vector of the peanut cysteine protease encoding gene AhRD21A and the application of the peanut cysteine protease encoding gene AhRD21A in tobacco bacterial wilt resistance genetic engineering. The gene contains a nucleotide sequence as shown in SEQ ID No. 1. The CaMV 35S promoter-driven overexpression vector agrobacterium-mediated transformation bacterial wilt susceptible variety Honghua Dajinyuan is constructed through a Gateway system, molecular detection and ralstonia solanacearum inoculation recognition are carried out on transgenic plants, and overexpression of the CaMV 35S promoter-driven overexpression vector agrobacterium-mediated transformation bacterial wilt susceptible variety Honghua Dajinyua in tobaccos can significantly improve bacterial wilt resistance of transgenic tobaccos. The result shows that the AhRD21A may participate in the resistance reaction of the plant to the bacterial wilt, which has an important gene resource for the bacterial wilt resistance genetic engineering breeding application of the plant.

of the formula (IV): where: R1=R'C(O), R'SO2, R'=a bicyclic, saturated or unsaturated, 8-12 membered ring system containing 0-4 hetero atoms selected from S, O and N, which is optionally substituted with up to four substituents independently selected from groups a), b) and c) below; or R'=a monocyclic, saturated or unsaturated, 5-7 membered ring containing 0-3 hetero atoms selected from S, O and N, which monocyclic ring bears at least one substituent selected from group a) and/or c) and which may optionally bear one or two further substituents selected from group b); R4=H, C1-7-alkyl, Ar-C1-7-alkyl, Ar, C3-7-cycloalkyl; C2-7alkenyl; R3=C1-7-alkyl, C2-C7 alkenyl, C2-C7 alkenyl, C3-7-cycloalkyl, Ar-C1-7-alkyl, Ar; R5=C1-7-alkyl, halogen, Ar-C1-7-alkyl, C1-3-alkyl-CONR3R4 or a bulky amine R6 is H, C1-7-alkyl, Ar-C1-7-alkyl, C1-3-alkyl-SO2-R<ix>, C1-3-alkyl-C(O)-NHR<ix >or CH2XAr q is 0 or 1 have utility as inhibitors of cysteine proteases such as cathepsin K and falcipain.

The invention discloses a triazine compound with a structure as shown in a general formula I or pharmaceutically acceptable salt, isomer, metabolite, prodrug, solvate or hydrate, pharmaceutical composition and application thereof. The compound disclosed by the invention overcomes the defects of single structure, lack of non-covalent and non-peptide high-efficiency small-molecule inhibitors and the like of the existing broad-spectrum antiviral drugs, and the compound disclosed by the invention has very good inhibitory activity on 3C-like cysteine protease and has a good treatment effect on infectious diseases.

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 also directed to pharmaceutical compositions comprising these compounds and processes for preparing them. The present invention is also directed to the use of these inhibitors in combination with a therapy that causes a deleterious immune response in patients receiving the therapy.

Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.

The invention discloses a heat-resistant cysteine protease, and coding genes and applications thereof. The heat-resistant cysteine protease is a protein selected from proteins: a, composed of amino acid sequences represented by SEQ ID NO.1; b, which possess protein degradation activity under high temperature conditions and are obtained via substitution and/or deletion and/or inserting of one or aplurality of amino acid residues of amino acid sequences represented by SEQ ID NO.1. The invention also discloses applications of the heat-resistant cysteine protease in degrading proteins under hightemperature conditions. The heat-resistant cysteine protease possesses high efficiency protein degrading activity as a temperature as high as 75 DEG C, and the high efficiency catalytic activity may last for 30min or longer in a solution of a temperature as high as 85 DEG C.

The invention discloses bone-strengthening probiotic formula milk powder for preventing senile osteoporosis, and every 100 g of the formula milk powder comprises the following components: desalted whey powder, inulin, calcium carbonate, 3.8-6.2 g of fructo-oligosaccharide, xylooligosaccharide, vitamin A (retinyl acetate), vitamin D (cholecalciferol), vitamin E (dl-alpha-tocopheryl acetate), ferrous sulfate, sodium selenite and the balance of water. The milk powder is prepared from the following raw materials by weight: 5g of yak bone marrow collagen peptide powder, 0.4-0.6 g of phospholipid, L-carnitine, sodium hyaluronate, milk mineral salt, hydrolyzed yolk powder, bifidobacterium lactis HN019 and the balance of skim milk powder. On the basis of the prior art, in addition to reasonable matching of calcium, phosphorus and vitamins, probiotics, angiopoietin and cysteine-inhibiting protease protein are particularly added, the bone tissue density is further improved and strengthened, and therefore the occurrence rate of osteoporosis is more effectively reduced.

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 invention provides a new application of an HUWE1 inhibitor BI8622 to inhibition of inflammasome activation. Researches discover that the HUWE1 inhibitor BI8622 can remarkably reduce activation of cysteine protease-1 (Caspase-1) and expression of interleukin 1 beta (IL-1 beta) in bone marrow derived macrophages (BMDM) of a mouse, and cell death is reduced; and meanwhile, it is proved that the BI8622 can remarkably reduce activation of the Caspase-1 and expression of the IL-1 beta in a human mononuclear macrophage line THP1 and human primary peripheral blood mononuclear cells (PBMC),and cell death is also remarkably reduced, so that the BI8622 can remarkably inhibit inflammasome activation.

The invention belongs to the technical field of biological pharmacy, and discloses an application of a medicine for inhibiting SARS-CoV-2 virus replication and an application of combination of chebulagic acid and punicalagin in any proportion in preparation of the medicine for inhibiting SARS-CoV-2 virus replication. Experiments for inhibition capacity of two broad-spectrum antiviral natural products, namely chebulagic acid and punicalagin, on SARS-CoV-2 virus replication show that chebulagic acid and punicalagin can be used as novel SARS-CoV-2 inhibitors; and under non-cytotoxic concentrations, chebulagic acid and punicalagin reduce the formation of virus-induced VERO-E6 cell monolayer plaques in a reversible and non-competitive manner by targeting the enzymatic activity of viral 3CLPro (3-chymotrypsin-like cysteine protease), and have potential application as the novel COVID-19 therapy.