Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T49031 Target Info
Target Name Proteasome beta-5 (PS beta-5)
Synonyms Proteasome subunit beta type-5; Proteasome subunit X; Proteasome subunit MB1; Proteasome epsilon chain; Proteasome chain 6; Multicatalytic endopeptidase complex epsilon chain; Macropain epsilon chain; MB1; LMPX
Target Type Patented-recorded Target
Gene Name PSMB5
Biochemical Class Peptidase
UniProt ID
PSB5_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2017156471
Title Immunoproteasome Inhibitor Analogs.
Abstract The disclosure provides for compounds having immunoproteasome inhibitory activity, and pharmaceutical compositions made thereof. The disclosure further provides for the use of the compounds and compositions in treating various diseases and disorders in a subject that are associated with immunoproteasome activity, including inflammatory disorders, autoimmune disorders, hematological disorders, and neurodegenerative disorders.
Applicant(s) The Regents of the University of California
Representative Drug(s) D0DY3A Drug Info Ki = 280 nM Click to Show More [1]
2 D01GON Drug Info Ki = 910 nM [1]
3 D00GGB Drug Info Ki = 1220 nM [1]
Patent ID WO2017066763
Title Proteasome Inhibitors and Uses Thereof.
Abstract The compounds of the present invention are represented by the following compounds having Formula (I) where the substituents R, R1 -R5, k, m, n, and q are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders, infectious disease, or for providing immunosuppression for transplanted organs or tissues.
Applicant(s) Cornell University
Representative Drug(s) D06OXO Drug Info IC50 = 106 nM Click to Show More [1]
2 D05MVF Drug Info IC50 = 326 nM [1]
Patent ID WO2015106200
Title Dipeptides As Inhibitors of Human Immunoproteasomes.
Abstract The compounds of the present invention are represented by the following compounds having Formula (I) where the substituents R1-R10, X, Y, k, m, n, q, and s are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.
Applicant(s) Cornell University
Representative Drug(s) D02SYR Drug Info LD50 = 34 nM Click to Show More [1]
2 D03JMZ Drug Info LD50 = 2040 nM [1]
Patent ID WO2014086701
Title Substituted Thiazole Compounds.
Abstract The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0K0GJ Drug Info IC50 = 1075 nM Click to Show More [1]
2 D0TU5R Drug Info IC50 = 20000 nM [1]
Patent ID WO2014152134
Title Tripeptide Epoxy Ketone Protease Inhibitors.
Abstract Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.
Applicant(s) Onyx Therapeutics, Inc
Representative Drug(s) D0E6ED Drug Info IC50 = 17.44 nM [1]
Patent ID WO2014152127
Title Dipeptide and Tripeptide Epoxy Ketone Protease Inhibitors.
Abstract Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases.
Applicant(s) Onyx Therapeutics, Inc
Representative Drug(s) D0AR6B Drug Info IC50 = 5.72 nM [1]
Patent ID WO2014114603
Title Substituted Thiazole Compounds.
Abstract The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0C2MH Drug Info IC50 = 587 nM [1]
Patent ID WO2014086697
Title Substituted Thiazole Compounds.
Abstract The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0NE8M Drug Info IC50 = 17488 nM [1]
Patent ID WO2014086664
Title Substituted Triazole Boronic Acid Compounds.
Abstract The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D01VMN Drug Info IC50 = 20 nM [1]
Patent ID WO2014086663
Title Substituted Triazole and Imidazole Compounds.
Abstract The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D03CMD Drug Info IC50 = 20000 nM [1]
Patent ID WO2011109355
Title Compounds for Immunoproteasome Inhibition.
Abstract One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
Applicant(s) Onyx Therapeutics, Inc
Representative Drug(s) D0L1TT Drug Info EC50 = 155.8 nM [1]
Patent ID WO2006045066
Title Labeled Compounds for Proteasome Inhibition.
Abstract Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and/or dosing purposes.
Applicant(s) PROTEOLIX, INC. BENNETT, Mark, K. BUCHHOLZ, Tonia, J. DEMO, Susan LAIDIG, Guy, J. LEWIS, Evan, R. SMYTH, Mark, S.
Representative Drug(s) D01OOO Drug Info IC50 = 5 nM [1]
References  Top
REF 1 A patent review of immunoproteasome inhibitors.Expert Opin Ther Pat. 2018 Jul;28(7):517-540.

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