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121 results about "Cathepsin K" patented technology
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Cathepsin K, abbreviated CTSK, is an enzyme that in humans is encoded by the CTSK gene.
Method of Improving Treatments in Rheumatic and Arthritic Diseases
Improved treatments of joint diseases, such as, e.g. osteoarthritis and rheumatoid arthritis, and pain, wherein a strontium-containing compound is administered alone or in combination with one or more second therapeutically and / or prophylactically active substances, selected from the group consisting of bisphosphonates, glucosamine, pallitative agents, analgesic agents, disease modifying anti-rheumatic compounds (DMARDs), selective estrogen receptor modulators (SERMs), aromatase inhibitors, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, COX-3 inhibitors, opioids, inhibitors / antagonists of IL-1, inhibitors / antagonists of TNF-alpha, inhibitors of matrix metallo-proteinases (MMPs), cathepsin K inhibitors, inhibitors / antagonists of RANK-ligand, statins, glucocorticoids, chondroitin sulphate, NMDA receptor antagonists, inhibitors of interleukin-I converting enzyme, Calcitonin gene related peptide antagonists, glycine antagonists, vanilloid receptor antagonists, inhibitors of inducible nitric oxide synthetase (iNOS), N-acetylcholine receptor agonists, neurokinin antagonists, neuroleptic agents, PAR2 receptor antagonists and anabolic growth factors acting on joint tissue components. Pharmaceutical compositions comprising a strontium-containing compound and a second therapeutically and / or prophylactically active substance as defined above.
Owner:OSTEOLOGIX AS
Cathepsin cysteine protease inhibitors
ActiveUS20060111440A1Avoid adjustmentImprove bioavailabilityBiocideSenses disorderDiseaseCathepsin O
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.
Owner:MERCK CANADA
Cathepsin cysteine protease inhibitors
ActiveUS20050240023A1Treating and preventing cathepsin dependent conditionBiocideOrganic chemistryCathepsin KCathepsin
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.
Owner:AXYX PHARMA INC +1
Cyanoalkylamino derivatives as protease inhibitors
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.
Owner:AXYX PHARMA INC +1
Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
InactiveUS20050054819A1BiocideCarbamic acid derivatives preparationCathepsin KCombinatorial chemistry
Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.
Owner:SMITHKLINE BECKMAN CORP
Method of inhibiting cathepsin K
InactiveUS6274336B1High specificity and stabilityInhibit synthesisHydrolasesPeptide/protein ingredientsProteinase activityCathepsin K
Owner:SMITHKLINE BECKMAN CORP
Cathepsin cysteine protease inhibitors
Owner:AXYX PHARMA INC +1
Cathepsin cysteine protease inhibitors
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)
Owner:MERCK CANADA INC
Bone Densifying Agent Characterized By Use Of Cathepsin K Inhibitor With Pth
InactiveUS20070238769A1Increased more efficientlyIncrease bone densityBiocideOrganic chemistryCathepsin KBone formation
The present invention relates to an agent for increasing BMD characterized by use of a cathepsin K inhibitor as a bone resorption inhibitor in combination with a type of PTH as a bone formation stimulator. This agent for increasing BMD is useful for the treatment of osteoporosis, bone fracture, arthritis, rheumatoid arthritis, osteoarthritis, hypercalcemia, osteometastasis of carcinoma, periodontal disease, bone Paget's disease and other bone metabolic diseases. For example, as the cathepsin K inhibitor, there can be mentioned a compound of formula (W) and a salt thereof, etc.
Owner:ONO PHARMA CO LTD
Methods of diagnosing synovial disease in a mammal by detecting bacterial DNA in synovial tissues from dogs with inflammatory knee arthritis and degenerative anterior cruciate ligament rupture
Method of diagnosing persistent, chronic synovitis and progressive joint degradation in the joint of a mammal. The method including providing a test sample comprising synovial fluid, cell or tissue from the joint of a mammal; detecting the presence of bacterial DNA, measuring the concentration of one or more biomarkers being cathepsin K, MMP-2 and -9, cathepsin S, tartrate-resistant acid phosphatase, invariant chain, CD4+ T-lymphocytes, CD8+ T-lymphocytes, CD44+ mononuclear cells, Toll-like receptor-2, Toll-like receptor-9, or a combination thereof; and, comparing the concentration of the biomarker from the test sample to a corresponding biomarker concentration in a control sample from healthy dogs, or an internal PBMC control sample, wherein a statistically significant elevated concentration of the biomarker in the test sample indicates that the mammal's joint is diseased.
Owner:WISCONSIN ALUMNI RES FOUND
4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis
InactiveUS20060166966A1Treating and preventing cathepsin dependent conditionBiocideOrganic chemistryCathepsin KCathepsin Y
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.
Owner:MERCK FROSST CANADA INC
Method for screening small-molecule inhibitors by taking cathepsin D as target point
InactiveCN107346379AImprove efficiencyOrganic active ingredientsBioinformaticsCathepsin KCathepsin O
The invention belongs to the technical field of medical chemistry, and relates to a drug screening method, in particular to a method for establishing a virtual screening model and an in vitro testing model of small-molecule inhibitors by taking cathepsin D as a target point. The method comprises the following steps: (1) acquiring, analyzing and processing a three-dimensional structure of cathepsin D protein; (2) establishing and processing a small-molecule database; (3) establishing a computer virtual screening system; (4) applying the computer virtual screening system obtained in the step (3) to screen a small-molecule ligand library obtained in the step (2); (5) predicting absorption, distribution, metabolism, excretion and toxicity (ADME-T). After the method for screening the cathepsin D inhibitors is adopted, six seedling compounds having cathepsin D inhibition activity are finally screened out; the method has the advantages of being rapid, economical and efficient, greatly increases the efficiency and provides a basis for finding the cathepsin D small-molecule inhibitors. The compounds, which are obtained by using the method and have the cathepsin D inhibition activity, can be further used for developing novel anti-cancer drugs.
Owner:FUDAN UNIV
Novel Superactive IL-33 Fragments, and Uses Thereof
The present invention discloses novel active polypeptide fragments of human IL-33 corresponding to natural forms generated by the proteases of human neutrophils (cathepsin G, elastase 2, proteinase 3), as well as the use thereof as a drug, in particular for the treatment of infectious diseases, inflammatory diseases, atherosclerosis, cardiovascular diseases, obesity, or cancer.
Owner:CENT NAT DE LA RECHERCHE SCI
Cathepsin inhibitors
InactiveCN1842515AReduce chargeInhibition is effectiveOrganic compound preparationAntipyreticDiseaseCathepsin K
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.
Owner:MERCK FROSST CANADA INC
Inhibitors of cathepsin B
Owner:VIROBAY INC
Cathepsin K inhibitors
Owner:F HOFFMANN LA ROCHE & CO AG
Cysteine protease inhibitors
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.
Owner:MEDIVIR AB
Hydrazine cathepsin K inhibitor and application thereof in treating osteoporosis
InactiveCN103086923AHigh selectivityHigh yieldOrganic chemistryAntipyreticCathepsin KHydrazine compound
The invention provides a hydrazine cathepsin K inhibitor and an application of the inhibitor in treating osteoporosis, which belong to the technical field of cathepsin inhibitors. The inhibitor does not include a P2-P3 connection part but have different P3 locus structures. The structure is represented by the following formula, and in the formula, P3 is aryl and comprises para-biphenyl, para-phenyl-pyridine, para-phenyl thiophene, para-terphenyl and meta-terphenyl. The non-peptide hydrazine cathepsin inhibitor designed and synthesized in the invention has the advantages of being relatively simple in structure, easy to get in materials, convenient to synthesize and high in yield; the design and the synthesis of the matrix structure greatly facilitate the synthesis of subsequent final products. By adopting the inhibitor, the inhibiting effect to the cathepsin K is higher than sub-nano-mole level, and the inhibiting effect to B and S is on micro-mole level, and the difference of inhibiting effects of cathepsin K and cathepsin L with extremely high homology is increased, thus the possibility of developing the inhibitor as the medicine for treating osteoporosis is increased.
Owner:JILIN UNIV
Cathepsin K inhibitors
The present invention provides a compound of the Formula: a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, wherein m, n, Ar1, R1, R2, R3, R4, and R5 are those defined herein. The present invention also provides methods for using and preparing compounds of Formula I.
Owner:F HOFFMANN LA ROCHE & CO AG
Prenylflavonoids from jackfruit and their new use in anti-osteoporosis
The invention relates to a kind of prenylflavonoids and their application in the preparation of anti-osteoporosis drugs. The invention isolated 7 prenylflavonoids from Jackfruit moraceae plants of the genus artocarpus (I) (Artocarpus / I) (I) (heterophyllus / I), were 5'HydroxycudraflavoneA, artochaminB, artelastoxanthone, artoindonesianinQ, kuwanonT, artoheteroidA and artoheteroidB. Activity tests showed that the prenylflavonoids of the invention has strong inhibitory activity on important therapeutic target for osteoporosis -- protease K, the prenylflavones' IC50 is 0.88 - 93.9mM, can be used for preparing drugs for treating osteoporosis.
Owner:JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
Protease inhibitors
The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.
Owner:GLAXO SMITHKLINE LLC
Cathepsin E as a Marker of Colon Cancer
Owner:UNIV OF NOTRE DAME DU LAC
Protease inhibitors
Compounds of the formula II:whereinR1 and R2 are independently H, F or CH3; orR1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo;R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and / or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro;R4 is methyl or fluoro; m is 0, 1 or 2;E is a bond, or thiazolyl, optionally substituted with methyl or fluoro;A1 is CH or N,A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N;R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F;R7 is H, C1-C4 alkyl or For a pharmaceutically acceptable salt, N-oxide or hydrate thereof, 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.
Owner:MEDIVIR AB
Cathepsin cysteine protease inhibitors
ActiveUS20160244417A1Treating and preventing cathepsin dependent conditionTreating and preventing and disease stateOrganic chemistrySkeletal disorderDiseaseCathepsin K
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.
Owner:MERCK SHARP & DOHME LLC
Cysteine protease inhibitors
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.
Owner:MEDIVIR AB
Serpin and minimum functional fragment and immunosuppression effect thereof
ActiveCN110330564AReduce manufacturing costSmall molecular weightPeptide/protein ingredientsAntipyreticDiseaseCathepsin K
The invention discloses a serpin and a minimum functional fragment and immunosuppression effect thereof. The serpin SA from haemaphysalis longicornis has activity restraining effects on cathepsin B, cathepsin G, papain and blood coagulation X factors, a minimum functional fragment SA-RCL having the immunosuppression activity is determined and has restraining activity on the cathepsin G, the immunosuppression effects of the SA and the SA-CRL to immunocyte are verified, and the treatment effects of the SA and the SA-CRL in a mouse arthritis model are verified. In the manner, the preparation costof the SA is low, the minimum functional fragment SA-RCL is small in molecular weight, stable in nature, easy to absorb, poor in immunogenicity and not liable to neutralize and degrade by hosts, theSA and the SA-RCL can be used for development of vaccines for resisting tick-borne diseases and treatment of anti-inflammation diseases.
Owner:上海景晗生物科技有限公司
Cycloalkane Carboxamide Derivatives and Production Process of Same
InactiveUS20090156805A1Reduce usageUseful in treatmentCarbamic acid derivatives preparationOrganic compound preparationMethyl groupPhenyl group
Novel cycloalkane carboxamide derivatives having an action that selectively inhibits cathepsin K, and a production process thereof, are provided.A cycloalkane carboxamide derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof:(wherein R1 and R2 represent (substituted) alkyl groups, (substituted) alkenyl groups, (substituted) alkynyl groups, (substituted) aromatic hydrocarbon groups or (substituted) heterocyclic groups, ring A represents an alkylidene group having 5 to 7 carbon atoms, and ring B represents a formyl group or a hydroxymethyl group).
Owner:SEIKAGAKU KOGYO CO LTD
Use of cathepsin k inhibitors for the treatment of glaucoma
InactiveUS20060020001A1Improve the level ofSuitable for useOrganic active ingredientsBiocideCathepsin KCathepsin
Owner:ALCON INC
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