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Title:
MASP-2 INHIBITORS AND METHODS OF USE
Document Type and Number:
WIPO Patent Application WO/2019/231933
Kind Code:
A3
Abstract:
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.

Inventors:
METZ MARKUS (US)
GOLDSTEIN SARA REBECCA (US)
KESHIPEDDY SANTOSH KUMAR (US)
KWON DO YEON (US)
LEMUS ROBERT HUERTA (US)
VADDELA SUDHEER BABU (US)
CUTSHALL NEIL S (US)
GAGE JENNIFER LYNN (US)
GRUSWITZ FRANZ A (US)
KHALAF JUHIENAH (US)
LITTLE THOMAS L (US)
NGUYEN JEREMIAH H (US)
NOLLERT VON SPECHT PETER KURT (US)
TSOUNG JENNIFER (US)
CICIRELLI MICHAEL (US)
Application Number:
PCT/US2019/034220
Publication Date:
July 30, 2020
Filing Date:
May 28, 2019
Export Citation:
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Assignee:
OMEROS CORP (US)
METZ MARKUS (US)
GOLDSTEIN SARA REBECCA (US)
KESHIPEDDY SANTOSH KUMAR (US)
KWON DO YEON (US)
LEMUS ROBERT HUERTA (US)
VADDELA SUDHEER BABU (US)
International Classes:
C07D207/00; C07D205/00; C07D213/00
Domestic Patent References:
WO2004032834A22004-04-22
WO2000039124A12000-07-06
Foreign References:
US20060002937A12006-01-05
Other References:
HEJA ET AL.: "Monospecific Inhibitors Show That Both Mannan-binding Lectin-associated Serine Protease-1 (MASP-1) and -2 Are Essential for Lectin Pathway Activation and Reveal Structural Plasticity of MASP-2", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. Vol. 287, no. 24, 8 June 2012 (2012-06-08), pages 20290 - 20300, XP055285722, DOI: 10.1074/jbc.M112.354332
HARMAT ET AL.: "The Structure of MBL-associated Serine Protease-2 Reveals that Identical Substrate Specificities of C1s and MASP-2 are Realized Through Different Sets of Enzyme- Substrate Interactions", JMB, vol. 342, no. 5, 14 July 2004 (2004-07-14), XP004844933
SZAKACS ET AL.: "Novel MASP-2 inhibitors developed via directed evolution of human TFPI1 are potent lectin pathway inhibitors", J. BIOL. CHEM., vol. 294, no. 20, 5 April 2019 (2019-04-05), pages 8227 - 8237, XP055727499
Attorney, Agent or Firm:
PHILLIPS, Eifion D. et al. (US)
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