Target General Information
Target ID T11388 Target Info
Target Name Cathepsin K (CTSK)
Synonyms Cathepsin X; Cathepsin O2; Cathepsin O; CTSO2; CTSO
Target Type Clinical trial Target
Gene Name CTSK
Biochemical Class Peptidase
UniProt ID
Patent(s) and the Corresponding Patented Drug(s)
World Intellectual Property Organization (WIPO)
Patent ID WO2015161928
Title 3-Oxo-Tetrahydro-Furo[3,2-B]Pyrrol-4(5H)-Yl) Derivatives I.
Abstract The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Applicant(s) Gruenenthal Gmbh
Representative Drug(s) D0MR9V Drug Info Ki = 12 nM [1]
Patent ID WO2013163567
Title Novel Alpha-Helical Peptidomimetic Inhibitors and Methods Using Same.
Abstract The present invention includes a novel class of highly specific protease inhibitors. In one embodiment, the inhibitors of the invention are a-helical in structure. In another embodiment, the present invention represents the first demonstration of a highly specific cysteine protease inhibitor. The invention includes a composition comprising a peptide, or a salt thereof, having at least one a-helix, wherein the peptide inhibits a protease. In one embodiment, the peptide comprises at least two cysteine residues, wherein the at least two cysteine residues occupy i,i+4 positions in the peptide and are covalently connected through a linker. In another embodiment, the linker comprises alpha, alpha' -meta-xylylene.
Applicant(s) The Trustes of the University of Pennsylvania
Representative Drug(s) D06LLT Drug Info Ki > 100000 nM [2]
Patent ID WO2012151319
Title Cathepsin Inhibitors for The Treatment of Bone Cancer and Bone Cancer Pain.
Abstract The present invention is directed to methods of using compounds that are inhibitors of cysteine proteases, in particular, of both cathepsins S and K and optionally further cathepsins B and/or L in treating bone cancer. The present invention is directed to pharmaceutical compositions comprising these compounds for treating bone cancer and bone cancer pain, especially the pain associated with metastasis. A single compound can be used to ameliorate the pain, the injury to bone, while also reducing tumor growth, the risk of metastasis and/or invasiveness of the cancer.
Applicant(s) Virobay, Inc. Booth, Robert
Representative Drug(s) D06XCD Drug Info IC50 = 2.3 nM [1]
Patent ID WO2010142650
Title Novel Cyclopentane Derivatives.
Abstract The invention relates to compounds of formula (I) wherein A1, R1, R2, R3, R4 and R5 are defined in the description and in the claims, which are preferential inhibitors of the cysteine protease cathepsin, in particular of the cysteine protease cathepsin S or L, making them useful as medicaments, particularly in the treatment of diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease or diabetic nephropathy.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D00KGL Drug Info IC50 >= 0.135 nM [1]
Patent ID WO2009112839
Title Compounds.
Abstract A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.
Applicant(s) Amura Therapeutics Limited
Representative Drug(s) D0QM0D Drug Info Ki = 38 nM [1]
Patent ID WO2010056877
Title Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S.
Representative Drug(s) D05OIU Drug Info Ki < 100 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US8680152
Title Cathepsin Inhibitors for The Treatment of Bone Cancer and Bone Cancer Pain.
Representative Drug(s) D06XCD Drug Info IC50 = 2.3 nM [1]
Patent ID US7893099
Title Novel Cyclopentane Derivatives As Cysteine Protease Cathepsin Inhibitors and Their Preparation Use In The Treatment of Diseases.
Representative Drug(s) D00KGL Drug Info IC50 >= 0.135 nM [1]
Patent ID US20150307507
Title 3-Oxo-Tetrahydro-Furo[3,2-B]Pyrrol-4(5H)-Yl Derivatives I As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0MR9V Drug Info Ki = 12 nM [1]
Patent ID US20120282267
Title Cathepsin Inhibitors for The Treatment of Bone Cancer and Bone Cancer Pain.
Representative Drug(s) D06XCD Drug Info IC50 = 2.3 nM [1]
Patent ID US20100317647
Title Novel Cyclopentane Derivatives As Cysteine Protease Cathepsin Inhibitors and Their Preparation Use In The Treatment of Diseases.
Representative Drug(s) D00KGL Drug Info IC50 >= 0.135 nM [1]
European Patent Office (EPO)
Patent ID EP2440521
Title Novel Cyclopentane Derivatives As Cysteine Protease Cathepsin Inhibitors and Their Preparation Use In The Treatment of Diseases.
Representative Drug(s) D00KGL Drug Info IC50 >= 0.135 nM [1]
Patent ID EP2361243
Title Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S.
Representative Drug(s) D05OIU Drug Info Ki < 100 nM [1]
Japan Patent Office (JPO)
Patent ID JP5540004
Title Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S.
Representative Drug(s) D05OIU Drug Info Ki < 100 nM [1]
Patent ID JP2012508758
Title Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S.
Representative Drug(s) D05OIU Drug Info Ki < 100 nM [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN103086923
Title Hydrazine Nitriles As Cathepsin K Inhibitor and Their Preparation Use In The Treatment of Osteoporosis.
Representative Drug(s) D0BR6D Drug Info IC50 = 0.64 nM [1]
Patent ID CN102731344
Title Preparation of Hydrazine Nitrile Compounds As Cathepsin Inhibitors.
Representative Drug(s) D04VGR Drug Info Ki = 0.0031 nM [1]
Patent ID CN102264695
Title Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S.
Representative Drug(s) D05OIU Drug Info Ki < 100 nM [1]
Korean Intellectual Property Office (KIPO)
Patent ID KR2012034727
Title Novel Cyclopentane Derivatives As Cysteine Protease Cathepsin Inhibitors and Their Preparation Use In The Treatment of Diseases.
Representative Drug(s) D00KGL Drug Info IC50 >= 0.135 nM [1]
Intellectual Property Office in India (IP India)
Patent ID IN2011KN02004
Title Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S.
Representative Drug(s) D05OIU Drug Info Ki < 100 nM [1]
Canadian Intellectual Property Office (CIPO)
Patent ID CA2762619
Title Novel Cyclopentane Derivatives As Cysteine Protease Cathepsin Inhibitors and Their Preparation Use In The Treatment of Diseases.
Representative Drug(s) D00KGL Drug Info IC50 >= 0.135 nM [1]
Patent ID CA2743749
Title Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S.
Representative Drug(s) D05OIU Drug Info Ki < 100 nM [1]
Intellectual Property Office of Australia (IP Australia)
Patent ID AU2010257586
Title Novel Cyclopentane Derivatives As Cysteine Protease Cathepsin Inhibitors and Their Preparation Use In The Treatment of Diseases.
Representative Drug(s) D00KGL Drug Info IC50 >= 0.135 nM [1]
References
REF 1 Cathepsin B and L inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2017 Jun;27(6):643-656.
REF 2 An updated patent review of calpain inhibitors (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):17-31.

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