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Cathepsin patents

      

This page is updated frequently with new Cathepsin-related patent applications.




 Hydroxystatin derivatives for the treatment of arthrosis patent thumbnailHydroxystatin derivatives for the treatment of arthrosis
The present invention relates to compounds of the formula (i) and in particular to medicaments comprising at least one compound of the formula (i) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin d is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries arthritis, pain, allodynia or hyperalgesia.. .
Merck Patent Gmbh


 Novel substituted spirocycles patent thumbnailNovel substituted spirocycles
Wherein a and cy have one of the meanings as indicated in the specification and their use as inhibitors of cathepsin c, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase i activity, e.g. Respiratory diseases..

 Formulations for cathepsin k inhibitors patent thumbnailFormulations for cathepsin k inhibitors
The instant invention relates to pharmaceutical compositions containing cathespin k inhibitors. Also disclosed are processes for making said pharmaceutical compositions..

 Methods for detection and treatment of neurodegenerative diseases patent thumbnailMethods for detection and treatment of neurodegenerative diseases
Provided herein are methods for detecting an increased probability or risk of neurodegeneration in a subject. In some embodiments the method comprises assaying a sample from the subject for lysozyme and/or cathepsin s and detecting the lysozyme and/or cathepsin s from the sample, wherein an increased lysozyme and/or cathepsin s compared to levels in a control subject sample indicate an increased probability or risk of neurodegeneration.

 Novel assay for early detection of a disease using a magnetic nanoparticle biosensor patent thumbnailNovel assay for early detection of a disease using a magnetic nanoparticle biosensor
A multiplex hand-held diagnostic biosensor, using two inflammatory salivary biomarkers, human neutrophil elastase (hne) and cathepsin-g, was constructed made to potentially detect periodontitis at an early stage is described. The use of magnetic nanoparticle biosensor method used as a device was based on the measurement of proteolytic activity using specific proteases probes.
Alfaisal University


 Protease-resistant mutants of stromal cell derived factor-1 in the repair of tissue damage patent thumbnailProtease-resistant mutants of stromal cell derived factor-1 in the repair of tissue damage
The present invention features mutant stromal cell derived factor-1 (sdf-1) peptides that have been mutated to make them resistant to digestion by, for example, the proteases dipeptidyl peptidase iv (dppiv), matrix metalloproteinase-2 (mmp-2), matrix metalloproteinase-9 (mmp-9), leukocyte elastase, cathepsin g, carboxypeptidase m, and carboxypeptidase n, but which retain chemoattractant activity.. .
Mesoblast International Sàrl


 Compositions and methods for inhibition of cathepsins patent thumbnailCompositions and methods for inhibition of cathepsins
This invention is directed to compound of formula i and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin k or cathepsin l, will be therapeutically useful.. .

 Furo[3, 2-b] pyrr0l-3-ones as cathespin s inhibitors patent thumbnailFuro[3, 2-b] pyrr0l-3-ones as cathespin s inhibitors
Compounds of formula (i) exhibit surprisingly high efficacies for human cathepsin s, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, sjogrens syndrome, grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.. .

 Cathepsin cysteine protease inhibitors patent thumbnailCathepsin cysteine protease inhibitors
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..
Merck Sharp & Dohme Corp.


 Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity patent thumbnailTemplate-fixed beta-hairpin peptidomimetics with protease inhibitory activity
Wherein z is a chain of 11 α-amino acid residues which, depending on their positions in the chain (counted starting from the n-terminal amino acid) are gly, or pro, or pro(4nhcophe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially cathepsin g or elastase or tryptase. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy..

Cathepsin cysteine protease inhibitors

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..
Merck Sharp & Dohme Corp.

3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals

Wherein ht, g, r10, r30, r40, r50 and r60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin a, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example.

Aminostatin derivatives for the treatment of arthrosis

The present invention relates to compounds of the formula (i) and in particular medicaments comprising at least one compound of the formula (i) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which cathepsin d is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.. .
Merck Patent Gmbh

Nitrogen-containing bicyclic aromatic heterocyclic compound

On the basis of a cathepsin s inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. It was found that a nitrogen-containing bicyclic heterocyclic compound has an excellent cathepsin s inhibitory effect, thereby completing the invention.
Astellas Pharma Inc.

Peptide for suppressing osteoclast differentiation and use thereof

The peptide of the present invention performs a function, which is the same as or similar to that of natural interleukin (il)-3, and has superior skin permeability due to the small size thereof. In addition, the peptide of the present invention suppresses the activation of nf-κb and nuclear transition by inhibiting the receptor activator of nuclear factor kappa-b ligand (rankl)-rank signaling pathway, and suppresses the expression of a rankl or an inflammatory cytokine-induced tartrate-resistant acid phosphatase (trap), cathepsin k, or tnf receptor type 1 or type 2, thereby inhibiting osteoclast differentiation depending on the treatment concentration.

Formulations for cathepsin k inhibitors with vitamin d

The instant invention relates to pharmaceutical compositions comprising cathespin k inhibitors and vitamin d. Also disclosed are processes for making said pharmaceutical compositions,.
Merck Sharp & Dohme Corp.

Hydroxy-ethylene derivatives for the treatment of arthrosis

The present invention relates to compounds of the formula i and in particular medicaments comprising at least one compound of the formula i for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin d is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.. .
Merck Patent Gmbh

Materials for positive cathepsin b modulation and methods of use for treating mild cognitive impairment (mci), early dementia, a-synucleinopathy, traumatic brain injury, cardiomyopathy, eye disease and skin damage

The present invention provides methods for treating a subject afflicted with i) mild cognitive impairment (mci), ii) early dementia, iii) early α-synucleinopathy, iv) traumatic brain injury, v) cardiomyopathy, vi) eye disease, or vii) skin damage, comprising administering to the subject at least one compound that increases the level of active cathepsin b in cells of the subject, or a pharmaceutically acceptable salt or ester thereof, in an amount that is effective to treat the subject. The present invention also provides compositions for treating a subject afflicted with i) mild cognitive impairment (mci), ii) early dementia, iii) early α-synucleinopathy, iv) traumatic brain injury, v) cardiomyopathy, vi) eye disease, or vii) skin damage..
University Of North Carolina At Pembroke

Compositions and methods for inhibiting bacterial and viral pathogens

Compositions and methods including amodiaquine (aq) or n-desethy amodiaquine (deaq) are provided for treating, inhibiting, or preventing cathepsin b dependent pathogens and toxins in a host cell or infected subject. Compositions and methods also include aq or deaq in combination with an antibiotic for more effective clearance of the pathogen and/or toxins..
Keck Graduate Institute Of Applied Life Sciences

Method of inhibiting angiogenesis, tumorigenesis and cathepsin activity

Insulin-like growth factor binding proteins (igfbps) and variants thereof, including igfbp-1, igfbp-2, igfbp-3, igfbp-4, igfbp-5, igfbp-8 and the c-terminal fragments thereof, inhibit angiogenesis, tumorigenesis and cathepsin activity, particularly cathepsin b activity.. .
National Research Council Of Canada

Methods for treating pulmonary emphysema using substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c

And their use as inhibitors of cathepsin c, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase i activity, e.g. Respiratory diseases..

Novel substituted spirocycles

Wherein a and cy have one of the meanings as indicated in the specification and their use as inhibitors of cathepsin c, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase i activity, e.g. Respiratory diseases..

Protease inhibitors

Or 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.. .

Amidopyridinol derivative or pharmaceutically acceptable salt thereof and pharmaceutical composition comprising same as active component

The present invention relates to an amidopyridinol derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including an amidopyridinol derivative or a pharmaceutically acceptable salt thereof as an active component. An amidopyridinol derivative represented by chemical formula 1 or a pharmaceutically acceptable salt thereof has an excellent antiangiogenic effect in a chorioallantoic membrane model, and thus is useful as an agent for preventing or treating diseases associated with angiogenesis, such as macular degeneration or arthritis, and also has an excellent colitis-inhibitory effect in a model of inflammatory bowel diseases, and thus is useful as an agent for preventing or treating inflammatory bowel diseases.
Research Cooperation Foundation Of Yeungnam University

Substituted oxetanes and their use as inhibitors of cathepsin c

And their use as inhibitors of cathepsin c, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase i activity, e.g. Respiratory diseases..

Furo [3, 2-b] pyrr0l-3-0nes as cathespin s inhibitors

Compounds of formula (i) exhibit surprisingly high efficacies for human cathepsin s, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, sjogrens syndrome, grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.. .

2 amino-3,4-dihydrcquinazoline derivatives and the use thereof as cathepsin d inhibitors

The present invention relates to compounds of the formula (i) and in particular to medicaments comprising at least one compound of the formula (i) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin d is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.. .
Merck Patent Gmbh

Acylguanidines for treating osteoarthritis

The present invention relates to compounds of the formula (i) and in particular to medicaments comprising at least one compound of the formula i for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin d is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.. .
Merck Patent Gmbh

Cathepsin l inhibitors and probes comprising vinyl sulfonate moiety and methods of using same

Human cathepsin l inhibitors and probes containing a vinyl sulfonate ester moiety are described. The inhibitors are highly potent (low nm affinity), selective, and cell permeable, and can inhibit ultra-low concentration of active cathepsin l.
Research Foundation Of The City University Of New York

Methods for diagnosing and/or treating sterility

The present invention concerns a polypeptide comprising the n-terminal fragment of a cystatin, and/or a cystatin expression inducer for use for the treatment of sterility and/or infertility, and a method of diagnosing and/or predicting sterility and/or infertility of a subject and/or of a couple of subjects, which method comprises measuring the level of at least one cystatin in a biological sample of a male subject and/or measuring the level of at least one cystatin in a biological sample of a female subject, and optionally measuring further the level of at least one cathepsin in a biological sample of said male of female subject.. .
Bioquanta Corp

Diaromatic amino acid substrate for cathepsin detection

The present invention relates to a diaromatic amino acid substrate for cathepsin detection. When the substrate used for cathepsin detection is a polymer resulting from the binding of a protease-preferred amino acid and quencher to a diaromatic amino acid, cathepsin can be detected sensitively and accurately by fluorescence because cathepsin causes the protease-preferred amino acid and quencher to dissociate from the diaromatic amino acid, and fluorescence is recovered during this time..

Composition for inhibition of cathepsin k

The present invention relates to the a method of inhibiting bone resorption in a mammal in need thereof with an oral pharmaceutical composition comprising a cathepsin k inhibitor, or a pharmaceutically acceptable salt thereof, or a mixture thereof, according to a continuous schedule having a dosage interval of once weekly, biweekly, twice monthly or once monthly.. .
Merck Sharp & Dohme Corp.

Hydroxystatin derivatives for the treatment of arthrosis

The present invention relates to compounds of the formula (i) and in particular to medicaments comprising at least one compound of the formula (i) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin d is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries arthritis, pain, allodynia or hyperalgesia.. .
Merck Patent Gmbh

Cathepsin inhibitors

The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.. .
Virobay, Inc.

Furo[3, 2-b] pyrr0l-3-ones as cathespin s inhibitors

Compounds of formula (i) exhibit surprisingly high efficacies for human cathepsin s, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, sjogrens syndrome, grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.. .

Methods for inhibiting viruses by targeting cathepsin-l cleavage sites in the viruses' glycoproteins

The disclosure provides methods and compositions useful for inhibiting virus requiring membrane fusion for viral entry, specifically for inhibiting severe acute respiratory syndrome coronavirus (sars-cov), ebola virus (ebov), hendra (hev) and nipah (niv) viruses by targeting cathepsin-l (catl) cleavages sites in the viruses' glycoproteins.. .
The Board Of Trustees Of The University Of Illinois

Nitrogen-containing bicyclic aromatic heterocyclic compound

[means for solution] it was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin s inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin s inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like..

Methods for treating pulmonary emphysema using substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c

And their use as inhibitors of cathepsin c, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase i activity, e.g. Respiratory diseases..

Cathepsin cysteine protease inhibitors

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..
Merck Sharp & Dohme Corp.

Method for preparing virus-like particle and recombinant baculovirus used therein

A recombinant baculovirus is provided for preparing picornavirus virus-like particles (vlp), wherein chitinase a (chia) and cathepsin v (v-cath) genes of the recombinant baculovirus are functionally disrupted and the recombinant baculovirus includes a picornavirus capsid protein gene under control of a strong promoter, and includes a protease gene configured for encoding a protease for hydrolyzing the capsid protein under control of a weak promoter. The recombinant baculovirus of the present invention may adopt high five or sf-9 cells for manufacturing enterovirus virus-like particles with improved stability and higher yields in comparison with the conventional arts.
National Tsing Hua University

Conformationally constrained, fully synthetic macrocyclic compounds

The conformationally restricted, spatially defined macrocyclic ring system of formula (i) is constituted by three distinct molecular parts: template a, conformation modulator b and bridge c. Macrocycles described by this ring system i are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase.
Polyphor Ag

Simukunin

The present invention includes a novel protein, also referred to herein as simukunin, that inhibits the function of several physiologically important enzymes. Simukunin is a potent inhibitor of the blood coagulation cascade, inhibiting factor xa and functioning as an efficient anticoagulant.
University Of Georgia Research Foundation, Inc.

Compositions and methods for inhibition of cathepsins

This invention is directed to compound of formula i and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin k or cathepsin l, will be therapeutically useful.. .
Baylor University

Cysteine protease inhibitors

For the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin s.. .

Method of using substituted 2-aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c

And their use as inhibitors of cathepsin c, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase i activity, e.g. Respiratory diseases..

Methods and compositions for diagnosis and prognosis of renal injury and renal failure

The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in sepsis patients. In particular, the invention relates to using assays that detect one or more biomarkers selected from the group consisting of insulin-like growth factor-binding protein 7, beta-2-glycoprotein 1, metalloproteinase inhibitor 2, alpha-1 antitrypsin, leukocyte elastase, serum amyloid p component, c-x-c motif chemokine 6, immunoglobulin a, immunoglobulin g subclass i, c-c motif chemokine 24, neutrophil collagenase, cathepsin d, c-x-c motif chemokine 13, involucrin, interleukin-6 receptor subunit beta, hepatocyte growth factor, cxcl-1, -2, -3, immunoglobulin g subclass ii, metalloproteinase inhibitor 4, c-c motif chemokine 18, matrilysin, c-x-c motif chemokine 11, and antileukoproteinase as diagnostic and prognostic biomarker assays of renal injury in the sepsis patient..
Astute Medical, Inc.

Identification of two novel biomarkers for niemann-pick disease type c

This invention provides novel biomarkers for niemann-pick disease, type c (npc). In an exemplary embodiment, the invention provides methods for identifying a subject as having npc.
The Usa , As Represented By The Secretary, Department Of Health & Human Services

Cathepsin c inhibitors

Disclosed are 4-amino-2-butenamides of formula (i) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin c enzyme such as chronic obstructive pulmonary disease.. .

Radiolabeled biomarkers for osteoclast activation and related methods thereof

The present invention provides biomarkers that find use as imaging agents within nuclear medicine applications (e.g., pet imaging and spect imaging). In particular, the present invention provides methods for identifying and characterizing osteoclast activation within subjects with radiolabeled cathepsin k inhibitors..

Procathepsin l and cathepsin l as biomarkers for ischemia

The present invention relates to procathepsin l, cathepsin l or a fragment thereof as a biomarker for ischemia. The present invention further relates to methods for diagnosing, predicting, prognosticating and/or monitoring ischemia based on measuring said biomarker, and to related kits, devices and uses thereof..



Cathepsin topics:
  • Protease Inhibitor
  • Protease Inhibitors
  • Atherosclerosis
  • Recombinant
  • Osteoarthritis
  • Rheumatoid Arthritis
  • Steoporosis
  • Osteoporosis
  • Polypeptide
  • Nanoparticle
  • Fluorescence
  • Inflammatory Disease
  • Liver Diseases
  • Enterovirus
  • Virus Like Particle


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    This listing is a sample listing of patent applications related to Cathepsin for is only meant as a recent sample of applications filed, not a comprehensive history. There may be associated servicemarks and trademarks related to these patents. Please check with patent attorney if you need further assistance or plan to use for business purposes. This patent data is also published to the public by the USPTO and available for free on their website. Note that there may be alternative spellings for Cathepsin with additional patents listed. Browse our RSS directory or Search for other possible listings.


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