A

COMPOUNDS AND USES

Espacenet Family 88093322

Abstract

There is provided herein compound of formula (I) as defined in Formula (I), wherein Ra, Rb, Rc, A and p have meanings given in the description, and pharmaceutically-acceptable salts and solvates thereof, which compounds are useful in the treatment of diseases in which pan-immunoproteasome inhibition is desired or required, and particularly in the treatment of cancer.

Inventors 6

  1. Elmer Maurits Aachen author as filed: Maurits, Elmer
  2. Patrick M. Dekker Aachen author as filed: Dekker, Patrick Mark
  3. Herman S. Overkleeft Aachen author as filed: Overkleeft, Herman Steven
  4. Bogdan I. Florea Aachen author as filed: Florea, Bogdan Iulius
  5. Groll, Michael
  6. Huber, Eva

Inventors are linked to an Aachen author when surname and first name match exactly one author.

Applicants

  • UNIVERSITEIT LEIDEN GBS Leiden
  • TECHNISCHE UNIVERSITÄT MÜNCHEN
  • Univ Muenchen Tech

Cited papers 5 in the database

Non-patent literature as cited (12)
  • - COUX, O.TANAKA, K.GOLDBERG, A. L.: "Structure and functions of the 20S and 26S proteasomes", ANNU. REV. BIOCHEM., vol. 65, 1996, pages 801 - 47, XP000925558, DOI: 10.1146/annurev.bi.65.070196.004101
  • - KNIEPERT, A.GROETTRUP, M.: "The unique functions of tissue-specific proteasomes", TRENDS IN BIOCHEMICAL SCIENCES, vol. 39, no. 1, 2014, pages 17 - 24
  • - MANASANCH, E. E.ORLOWSKI, R. Z.: "Proteasome inhibitors in cancer therapy", NAT REV CLIN ONCOL, vol. 14, no. 7, 2017, pages 417 - 433, XP037922981, DOI: 10.1038/nrclinonc.2016.206
  • - JOHNSON, H. W. B. ET AL.: "Required Immuno-proteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616", J MED CHEM, vol. 61, no. 24, 2018, pages 11127 - 11143
  • - MUCHAMUEL, T. ET AL.: "A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis", NAT. MED., vol. 15, no. 7, 2009, pages 781 - 7, XP037922221, DOI: 10.1038/nm.1978
  • - B. M. TROSTI. FLEMING: "Comprehensive Organic Synthesis", 1991, PERGAMON PRESS
  • - A. R. KATRITZKYC. W. REESE. F. V. SCRIVEN: "Comprehensive Heterocyclic Chemistry II", 1996, PERGAMON PRESS
  • - "Hetarenes and Related Ring Systems", vol. 9-17, 2006, GEORG THIEME VERLAG, article "Science of Synthesis"
  • - A. R. KATRITZKYO. METH-COHNC. W. REES: "Comprehensive Organic Functional Group Transformations", 1995, PERGAMON PRESS
  • - T.W. GREENEP.G.M. WUTZ: "Protective Groups in Organic Synthesis", 1999, WILEY-INTERSCIENCE
  • - MICHAEL BASLER ET AL: "Amelioration of autoimmunity with an inhibitor selectively targeting all active centres of the immunoproteasome", BRITISH JOURNAL OF PHARMACOLOGY, WILEY-BLACKWELL, UK, vol. 175, no. 1, 29 November 2017 (2017-11-29), pages 38 - 52, XP071056809, ISSN: 0007-1188, DOI: 10.1111/BPH.14069
  • - GERJAN DE BRUIN ET AL: "Structure-Based Design of &bgr;1i or &bgr;5i Specific Inhibitors of Human Immunoproteasomes", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 14, 24 July 2014 (2014-07-24), pages 6197 - 6209, XP055176679, ISSN: 0022-2623, DOI: 10.1021/jm500716s

Cited patents 2