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 T19947 Target Info
Target Name Immunoproteasome complex (IP)
Synonyms i-proteasome complex
Target Type Clinical trial Target
Gene Name NO-GeName
UniProt ID
NOUNIPROTAC
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2018005781
Title Process of Preparing A Peptide Epoxyketone Immunoproteasome Inhibitor, and Precursors Thereof.
Abstract Disclosed herein are methods for preparing [(2S,3R)-N-[(2S)-3-(cyclopent- 1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound "G"): and precursors thereof.
Applicant(s) Kezar Life Sciences
Representative Drug(s) D0WJ3T Drug Info N.A. [1]
Patent ID WO2018005772
Title Crystalline Salts of Peptide Epoxyketone Immunoproteasome Inhibitor.
Abstract Provided herein is a peptide epoxyketone immunoproteasome inhibitorhaving a structure: Formula (I) wherein X- is a counterion, crystal forms, salts, and processes for making the same, and formulations thereof.
Applicant(s) Kezar Life Sciences
Representative Drug(s) D0WJ3T Drug Info N.A. [1]
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) D0JK0Y Drug Info N.A. [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) D0B0VK Drug Info N.A. [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) D0A0VU Drug Info N.A. [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) D0HV3N Drug Info N.A. [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) D0P9YR Drug Info N.A. [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) D06SJU Drug Info N.A. [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) D01NCJ Drug Info N.A. [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) D0DU4H Drug Info N.A. [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) D0WF1F Drug Info N.A. [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) D0O9YJ Drug Info N.A. [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) D0HM4V Drug Info N.A. [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) D0D2PS Drug Info N.A. [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) D09EGD Drug Info N.A. [1]
Patent ID WO2014056954
Title Macrocyclic Ketoamide Immunoproteasome Inhibitors.
Abstract The invention is concerned with the compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R3 and R3 are defined in the detailed description and claims. 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) D0X4HJ Drug Info N.A. [1]
Patent ID WO2014056748
Title Ketoamide Immunoproteasome Inhibitors.
Abstract The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R1 R2, R2 R3, R4, R4and R5 are defined in the detailed description and claims. 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) D0UZ4S Drug Info N.A. [1]
Patent ID WO2013092979
Title Alpha-Amino Boronic Acid Derivatives, Selective Immunoproteasome Inhibitors.
Abstract The present invention provides compounds of Formula (I) as inhibitors of LMP7 for the treatment of autoimmune and inflammatory diseases. In formula (I), Rb and Rc are independently selected from one another from H or C1-C6-alkyl; whereby Rb and Rc may be linked to form a 5 or 6 membered-ring containing the oxygen atoms to which they are linked; Q denotes Ar, Het or cycloalkyl; R1 R2 independently from each other denotes H, ORa, Hal, C1-C6-alkyl wherein 1 to 5 H atoms may be independently replaced by OH or Hal; Y denotes CR 3R4, preferably CH2 or C(CH3)2; R 3, R4 independently of one another denote H or C1-C6-alkyl; L denotes L1 or L2 or alkyl; n is an integer selected from 0 to 3; L 1 is Q1-CO-M- wherein Q 1 is Ar or Het, preferably, phenyl, naphthyl or pyridine, optionally substituted with 1 to 5 groups independently selected from ORa, Hal, phenyl, and C1-C6-alkyl wherein 1 to 5 H atoms may be independently replaced by OH or Hal; L2 is Q2-M- wherein Q 2 is a fused bicyclic system containing 1 nitrogen atom and 1 to 3 additional groups independently selected from O, S, N, or CO, and wherein at least one of the rings is aromatic whereby the fused bicyclic system is optionally substituted with 1 to 5 groups independently selected from ORa, Hal, phenyl, and C1-C6-alkyl wherein 1 to 5 H atoms may be independently replaced by OH or Hal; or Q 2 is unsaturated or aromatic 5 membered-ring system containing 1 to 3 heteroatoms selected from N, O, S and CO, and optionally substituted with a phenyl ring or pyridine ring whereby phenyl ring and pyridine ring are optionally substituted with 1 to 4 groups independently selected from ORa, Hal, phenyl, and C1-C6-alkyl wherein 1 to 5 H atoms may be independently replaced by OH or Hal; M is a linear or branched alkylene having 1 to 5 carbon atoms wherein 1 or 2 H atoms may be replaced by OR a or a phenyl ring optionally substituted with 1 to 5 groups independently selected from Hal, ORa, and C1-C6-alkyl optionally substituted with 1 to 5 groups independently selected from OH, and Hal; or M denotes a cycloalkylene having 3 to 7 carbon atoms; or M denotes a thiazolidinyl group; R a is H or C1-C6-alkyl wherein 1 to 5 H atom may be independently replaced by OH or Hal; Ar denotes a 6 membered-aromatic carbocyclic ring optionally fused with another carbocyclic saturated, unsaturated or aromatic ring having 5 to 8 carbon atoms; Het denotes a 5- or 6-membered saturated, unsaturated or aromatic heterocyclic ring having 1 to 3 heteroatoms independently selected from N, N+O-, O, S, SO, and SO 2, and optionally fused with another saturated, unsaturated or aromatic ring having 5 to 8 atoms and optionally containing 1 to 3 heteroatoms selected from N, O, and S; Hal denotes CI, Br, I of F; preferably CI or F.
Applicant(s) Ares Trading Sa
Representative Drug(s) D0JI5X Drug Info N.A. [1]
Patent ID WO2011136905
Title Crystalline Peptide Epoxyketone Immunoproteasome Inhibitor.
Abstract The invention relates to crystalline peptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.
Applicant(s) Onyx Therapeutics, Inc
Representative Drug(s) D0NO3H Drug Info N.A. [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) D06GDM Drug Info N.A. [1]
Patent ID WO2010108172
Title Crystalline Tripeptide Epoxy Ketone Protease Inhibitors.
Abstract The invention relates to crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.
Applicant(s) Onyx Therapeutics, Inc
Representative Drug(s) D0C4JQ Drug Info N.A. [1]
Patent ID WO2007149512
Title Peptide Epoxyketones for Pr0Teas0Me 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) Proteolix, Inc
Representative Drug(s) D0NO3H Drug Info N.A. [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) D0R5FU Drug Info N.A. [1]
Patent ID WO2006092326
Title Mimetic Peptides and The Use Thereof In The form of 20S, 26S and Immunoproteasome Inhibitors.
Abstract The invention relates to mimetic peptide compounds, to the synthesis and use thereof for inhibiting proteasomes and inducing apoptosis in tumoral cells. Pharmaceutical compositions containing said compounds and the use of said compounds for treating diseases, in particular cancer and neurogenerative diseases are also disclosed.
Applicant(s) UNIV DARMSTADT TECH [DE]; CHARITE UNIVERSITAETSMEDIZIN [DE]
Representative Drug(s) D04HPR Drug Info N.A. [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) D01OBB Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20160332998
Title Selective Immunoproteasome Inhibitors with Non-Peptide Scaffolds.
Applicant(s) University of Kentucky Research Foundation
Representative Drug(s) D01VHD Drug Info N.A. Click to Show More [1]
2 D03JWM Drug Info N.A. [1]
3 D0RF5E Drug Info N.A. [1]
4 D0ZH3O Drug Info N.A. [1]
Patent ID US20080064659
Title Epoxyketone-Based Immunoproteasome Inhibitors.
Applicant(s) University of Kentucky Research Foundation
Representative Drug(s) D0FJ8E Drug Info N.A. [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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