Target General Information
Target ID T68290 Target Info
Target Name Cathepsin S (CTSS)
Synonyms Cysteine protease cathepsin S
Target Type Clinical trial Target
Gene Name CTSS
Biochemical Class Peptidase
UniProt ID
Patent(s) and the Corresponding Patented Drug(s)
World Intellectual Property Organization (WIPO)
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 = 21000 nM [1]
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 = 0.009 nM [2]
Patent ID WO2010121918
Title Proline Derivatives As Cathepsin Inhibitors.
Abstract The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Patent ID WO2009136997
Title Inhibitors of Human Cathepsin L, Cathepsin B, and Cathepsin S.
Abstract The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity.
Applicant(s) The Trustes of the University of Pennsylvania
Representative Drug(s) D06XTA Drug Info IC50 = 56 nM [2]
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 [2]
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 [2]
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 = 0.009 nM [2]
Patent ID US8163793
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
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 [2]
Patent ID US20150307472
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID US20120282267
Title Cathepsin Inhibitors for The Treatment of Bone Cancer and Bone Cancer Pain.
Representative Drug(s) D06XCD Drug Info IC50 = 0.009 nM [2]
Patent ID US20110207726
Title Inhibitors of Human Cathepsin L, Cathepsin B and Cathepsin S and Therapeutic Uses Thereof.
Representative Drug(s) D06XTA Drug Info IC50 = 56 nM [2]
Patent ID US20100267722
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
European Patent Office (EPO)
Patent ID EP2888244
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID EP2421826
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
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 [2]
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 [2]
Patent ID JP5518997
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Patent ID JP201553099
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID JP2012524116
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
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 [2]
China National Intellectual Property Administration (CNIPA)
Patent ID CN104583198
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID CN102731344
Title Preparation of Hydrazine Nitrile Compounds As Cathepsin Inhibitors.
Representative Drug(s) D04VGR Drug Info Ki = 0.0031 nM [2]
Patent ID CN102405211
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
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 [2]
Russian Federal Service for Intellectual Property (Rospatent)
Patent ID RU2535479
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Portuguese Institute of Industrial Property (PINPI)
Patent ID PT2421826
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Intellectual Property Office of New Zealand (IPONZ)
Patent ID NZ595073
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Mexican Institute of Industrial Property (IMPI)
Patent ID MX2015002026
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Korean Intellectual Property Office (KIPO)
Patent ID KR2015044947
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID KR2011140136
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Patent ID KR1320790
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Intellectual Property Office in India (IP India)
Patent ID IN2015DN00962
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
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 [2]
Israel Patent Office (ILPO)
Patent ID IL237128
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID IL215065
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Spanish Patent and Trademark Office (SPTO)
Patent ID ES2436550
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Trademark and Patent Offices of Costa Rica (CRTPO)
Patent ID CR20150073
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Canadian Intellectual Property Office (CIPO)
Patent ID CA2879796
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID CA2758210
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
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 [2]
Intellectual Property Office of Australia (IP Australia)
Patent ID AU2013305102
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
Patent ID AU2010241084
Title Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor.
Representative Drug(s) D0X1AF Drug Info IC50 = 0.29 nM [2]
Argentinean National Institute of Industrial Property (AINPI)
Patent ID AR92172
Title Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation.
Representative Drug(s) D0JD5W Drug Info IC50 = 0.6 nM [2]
References
REF 1 An updated patent review of calpain inhibitors (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):17-31.
REF 2 Cathepsin B and L inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2017 Jun;27(6):643-656.

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