Target General Information
Target ID T61746 Target Info
Target Name Cathepsin B (CTSB)
Synonyms Ctsb; Cathepsins B; Cathepsin-B; Cathepsin B1; CPSB; APPS; APP secretase
Target Type Patented-recorded Target
Gene Name CTSB
Biochemical Class Peptidase
UniProt ID
Patent(s) and the Corresponding Patented Drug(s)
World Intellectual Property Organization (WIPO)
Patent ID WO2014164844
Title Cathepsin Inhibitors.
Abstract The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.
Applicant(s) Virobay, Inc
Representative Drug(s) D0A2NA Drug Info Ki < 1 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 = 0.33 nM [1]
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 [1]
Patent ID WO2009100225
Title Inhibitors of Cathepsin B.
Abstract The present invention is directed to a method of using compounds of Formula (I) to inhibit Cathepsin B. Specifically the compounds of the present invention are useful as therapeutic agents for the treatment of tumor invasion, metastasis, Alzheimer's Disease, arthritis, inflammatory diseases such as chronic and acute pancreatitis, inflammatory airway disease, and bone and joint disorders, including osteoporosis, osteoarthritis, rheumatoid arthritis, psoriasis, and other autoimmune disorders, liver fibrosis, including liver fibrosis associated with HCV, all types of steatosis (including non-alcoholic steatohepatitis) and alcohol-associated steatohepatitis, non-alcoholic fatty liver disease, forms of pulmonary fibrosis including idiopathic pulmonary fibrosis, pathological diagnosis of interstitial pneumonia following lung biopsy, renal fibrosis, cardiac fibrosis, retinal angiogenesis and fibrosis/gliosis in the eye, schleroderma, and systemic sclerosis. The compopunds of Formula (I) are also useful for treating subjects with both HCV and fibrosis in a mammal, particularly liver fibrosis, and subjects affirmatively diagnosed or at risk for bopth HCV and liver fibrosis.
Applicant(s) VIROBAY, INC
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
Patent ID WO2008037072
Title Cathepsin B Inhibitors.
Abstract Compounds of formula ( I ) : are found to be selective inhibitors of cathepsin B, and hence useful in treating a variety of pathological conditions.
Applicant(s) Merck Frosst Canada Ltd
Representative Drug(s) D0E2AF Drug Info IC50 < 1000 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 = 0.33 nM [1]
Patent ID US8211897
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
Patent ID US20150191459
Title Preparation of Substituted 2-(1-Phenylethylamino)-3-Phenylpropanamide Derivatives As Cathepsin Inhibitors.
Representative Drug(s) D0A2NA Drug Info Ki < 1 nM [1]
Patent ID US20140256698
Title Preparation of Substituted 2-(1-Phenylethylamino)-3-Phenylpropanamide Derivatives As Cathepsin Inhibitors.
Representative Drug(s) D0A2NA Drug Info Ki < 1 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 = 0.33 nM [1]
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 [1]
Patent ID US2010004871
Title Preparation of Diarylalkynyltrifluoroethyl Sulfonylalaninamides As Cathepsin B Inhibitors.
Representative Drug(s) D0E2AF Drug Info IC50 < 1000 nM [1]
Patent ID US20090203629
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
European Patent Office (EPO)
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]
Patent ID EP2353599
Title 8-Hydroxyquinolines As Inhibitors of Cathepsin B.
Representative Drug(s) D0KG9M Drug Info Ki = 37700 nM [1]
Patent ID EP2237793
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
Patent ID EP2076490
Title Preparation of Diarylalkynyltrifluoroethyl Sulfonylalaninamides As Cathepsin B Inhibitors.
Representative Drug(s) D0E2AF Drug Info IC50 < 1000 nM [1]
Japan Patent Office (JPO)
Patent ID JP5718647
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
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 JP2015051985
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 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]
Patent ID JP2011511089
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN103006621
Title Cathepsin B Inhibitors.
Representative Drug(s) D0WO4T Drug Info IC50 = 3240 ng/ml [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]
Patent ID CN101969973
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
Patent ID CN103330708
Title 2-(3,5-Dimethoxybenzylidene) Cyclopentanone, A Novel Synthetic Small-Molecule Compound, Provides Effectes Against Ischemic Stroke.
Representative Drug(s) D0UX4J Drug Info N.A. [1]
Mexican Institute of Industrial Property (IMPI)
Patent ID MX2010008371
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 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 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]
Patent ID CA2713108
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 nM [1]
Brazilian Patent and Trademark Office (BRPTO)
Patent ID BR200900772
Title Preparation of Peptides As Inhibitors of Cathepsin B.
Representative Drug(s) D0L1PP Drug Info IC50 = 19 nM; Ki = 19 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.

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