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 T77350 Target Info
Target Name Proteasome beta-8 (PS beta-8)
Synonyms Y2; Really interesting new gene 10 protein; RING10; Proteasome subunit beta-5i; Proteasome subunit beta type-8; Proteasome component C13; PSMB5i; Multicatalytic endopeptidase complex subunit C13; Macropain subunit C13; Low molecular mass protein 7; LMP7
Target Type Clinical trial Target
Gene Name PSMB8
Biochemical Class Peptidase
UniProt ID
PSB8_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
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 = 4.1 nM Click to Show More [1]
2 D05MVF Drug Info IC50 = 58 nM [1]
Patent ID WO2016151483
Title Psoralen Derivatives As Non-Peptidic Inhibitors of Chymotrypsin-Like Activity of The Immunoproteasome.
Abstract This invention relates to new inhibitors of chymothrypsin-like activity of the immunoproteasome (inhibitors of gama5 or LMP7 subunit) with the general formula (I), where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of diseases where immunoproteasome activity is increased.
Applicant(s) Univerza V Ljubljani
Representative Drug(s) D0E5WC Drug Info IC50 = 13 nM Click to Show More [1]
2 D02KPK Drug Info IC50 = 90 nM [1]
3 D0J6LT Drug Info IC50 = 1600 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 IC50 = 0.09 nM Click to Show More [1]
2 D03JMZ Drug Info IC50 = 3.6 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 = 21 nM Click to Show More [1]
2 D0TU5R Drug Info IC50 = 25 nM [1]
Patent ID WO2016050359
Title Boronic Acid Derivatives.
Abstract Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmue disorder abnomality or hematological malignancies.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D04HMP Drug Info IC50 < 50 nM [1]
Patent ID WO2016050358
Title Boronic Acid Derivatives.
Abstract Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmue disorder or hematological malignancies.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D0RY9I Drug Info IC50 < 50 nM [1]
Patent ID WO2016050356
Title Boronic Acid Derivatives.
Abstract Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmue disorder or hematological malignancies.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D0RK3U Drug Info IC50 < 50 nM [1]
Patent ID WO2016050355
Title Boronic Acid Derivatives.
Abstract Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmue disorder or hematological malignancies.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D0GI4S Drug Info IC50 < 50 nM [1]
Patent ID WO2016028571
Title Dipeptidomimetics 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, R4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (la), Formula (lb ), or Formula (Ic), where the substituents R1-R4, RX, RY, X, Y, 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) D07SSU Drug Info IC50 = 6.4 nM [1]
Patent ID WO2015195950
Title Lmp7 Inhibitors.
Abstract The present disclosure provides compounds that are Large Multifunctional Protease 7 (LMP7) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of LMP7. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Applicant(s) Principia Biopharma Inc
Representative Drug(s) D0DK3R Drug Info IC50 = 5 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 = 2.72 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 = 1.82 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 = 238 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 = 212 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 = 2 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 = 14 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 = 8.5 nM [1]
Patent ID WO2006099261
Title Potent and Specific Immunoproteasome Inhibitors.
Abstract Compounds and methods of selectively inhibiting an immunoproteasome are described. Also described are methods of treating a cancer, an inflammation, and/or an autoimmune disease and methods of suppressing endogenous antigenic peptide generation by administering to a subject in need of treatment thereof a therapeutic amount of an immunoproteasome specific inhibitor.
Applicant(s) The University of North Carolina at Chapel Hill
Representative Drug(s) D0B0GG Drug Info Ki = 1030 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 = 7 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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