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Bibliographic data

Document EP000003925667A1 (Pages: 114)

Bibliographic data Document EP000003925667A1 (Pages: 114)
INID Criterion Field Contents
54 Title TI [DE] SELEKTIVE TMPRSS2-INHIBITOREN UND MEDIZINISCHE VERWENDUNG DAVON
[EN] SELECTIVE TMPRSS2 INHIBITORS AND MEDICAL USE THEREOF
[FR] INHIBITEURS SÉLECTIFS DE LA TMPRSS2 ET LEUR UTILISATION MÉDICALE
71/73 Applicant/owner PA MAX PLANCK GESELLSCHAFT, DE
72 Inventor IN
22/96 Application date AD Jun 17, 2020
21 Application number AN 20180647
Country of application AC EP
Publication date PUB Dec 22, 2021
33
31
32
Priority data PRC
PRN
PRD


51 IPC main class ICM A61P 31/12 (2006.01)
51 IPC secondary class ICS A61K 38/05 (2006.01)
A61K 38/06 (2006.01)
A61K 38/07 (2006.01)
A61P 31/16 (2006.01)
C07K 5/072 (2006.01)
C07K 5/078 (2006.01)
C07K 5/083 (2006.01)
C07K 5/093 (2006.01)
C07K 5/09 (2006.01)
C07K 5/103 (2006.01)
C07K 5/113 (2006.01)
C07K 5/11 (2006.01)
IPC additional class ICA
IPC index class ICI
Cooperative patent classification CPC A61K 38/00
A61K 45/06
A61P 31/12
A61P 31/16
C07K 5/06095
C07K 5/06113
C07K 5/06147
C07K 5/0806
C07K 5/0817
C07K 5/0819
C07K 5/1008
C07K 5/1019
C07K 5/1021
MCD main class MCM A61P 31/12 (2006.01)
MCD secondary class MCS A61K 38/05 (2006.01)
A61K 38/06 (2006.01)
A61K 38/07 (2006.01)
A61P 31/16 (2006.01)
C07K 5/072 (2006.01)
C07K 5/078 (2006.01)
C07K 5/083 (2006.01)
C07K 5/093 (2006.01)
C07K 5/09 (2006.01)
C07K 5/103 (2006.01)
C07K 5/113 (2006.01)
C07K 5/11 (2006.01)
MCD additional class MCA
57 Abstract AB [EN] The invention relates to the compound of general formula (I) as novel inhibitors of TMPRSS2 and their use for the prophylaxis and treatment of influenza virus infection or coronavirus infection, in particular, SARS-CoV2 (COVID-19) infection.
56 Cited documents identified in the search CT WO002012162828A1
WO002016144654A1
56 Cited documents indicated by the applicant CT
56 Cited non-patent literature identified in the search CTNP ALEXANDER MAIWALD ET AL: "Changing the selectivity profile - from substrate analog inhibitors of thrombin and factor Xa to potent matriptase inhibitors", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 31, no. sup1, 11 May 2016 (2016-05-11), GB, pages 89 - 97, XP055748134, ISSN: 1475-6366, DOI: 10.3109/14756366.2016.1172574 0;
COLOMBO ELOÏC ET AL: "Design and synthesis of potent, selective inhibitors of matriptase", ACS MEDICINAL CHEMISTRY LETTERS, AMERICAN CHEMICAL SOCIETY, US, vol. 3, no. 7, 12 July 2012 (2012-07-12), pages 530 - 534, XP008173043, ISSN: 1948-5875, [retrieved on 20120411], DOI: 10.1021/ML3000534 0;
DOMINIC DUCH?NE ET AL: "Analysis of Subpocket Selectivity and Identification of Potent Selective Inhibitors for Matriptase and Matriptase-2", JOURNAL OF MEDICINAL CHEMISTRY, VOL. 57, N.23, 11 November 2014 (2014-11-11), pages 10198 - 10204, XP055429365, Retrieved from the Internet [retrieved on 20171128], DOI: 10.1021/jm5015633 0;
HOFFMANN MARKUS ET AL: "SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor", CELL, ELSEVIER, AMSTERDAM NL, vol. 181, no. 2, 5 March 2020 (2020-03-05), pages 271, XP086136225, ISSN: 0092-8674, [retrieved on 20200305], DOI: 10.1016/J.CELL.2020.02.052 0;
KWON HONGMOK ET AL: "Structure-based design, synthesis, and biological evaluation of Leu-Arg dipeptide analogs as novel hepsin inhibitors", BIORGANIC & MEDICINAL CHEMISTRY LETTERS,, vol. 26, no. 2, 8 December 2015 (2015-12-08), pages 310 - 314, XP029380287, ISSN: 0960-894X, DOI: 10.1016/J.BMCL.2015.12.023 0;
WILLIAM C RIPKA: "New thrombin inhibitors in cardiovascular disease", CURRENT OPINION IN CHEMICAL BIOLOGY, vol. 1, no. 2, 1 August 1997 (1997-08-01), GB, pages 242 - 253, XP055748161, ISSN: 1367-5931, DOI: 10.1016/S1367-5931(97)80016-6 0;
ZHENFU HAN ET AL: "Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer", ACS MEDICINAL CHEMISTRY LETTERS, vol. 5, no. 11, 10 October 2014 (2014-10-10), US, pages 1219 - 1224, XP055748199, ISSN: 1948-5875, DOI: 10.1021/ml500254r 0
56 Cited non-patent literature indicated by the applicant CTNP ABEL T, BLOOD, vol. 122, 2013, pages 2030 - 2038 1;
DEMAISON C, HUM GENE THER., vol. 13, 2002, pages 803 - 813 1;
HOFFMANN ET AL., CELL, vol. 181, 2020, pages 271 - 280 1;
HURET JLAHMAD MARSABAN MBERNHEIM ACIGNA JDESANGLES FGUIGNARD JCJACQUEMOT-PERBAL MCLABARUSSIAS MLEBERRE V, NUCLEIC ACIDS RES., vol. 41, January 2013 (2013-01-01) 1;
KOUJI SAKAI ET AL., JOURNAL OF VIROLOGY, vol. 88, no. 10, 2014, pages 5608 - 5616 1;
MUNCH RC, MOL THER, vol. 19, 2011, pages 686 - 693 1;
ROMAIN ZUFFEREY, NAT. BIOTECHNOL., vol. 3, 1997, pages 3 - 8 1;
W-J SHIN ET AL., EXPERT OPINION ON DRUG DISCOVERY, vol. 12, no. 11, 2017, pages 1139 - 1152 1;
XIA S: "A pan-coronavirus fusion inhibitor targeting the HR1 domain of human coronavirus spike", SCI ADV, vol. 5, 2019, pages eaav4580 1
Citing documents Determine documents
Sequence listings
Search file IPC ICP A61P 31/12
A61P 31/16
C07K 5/072
C07K 5/078
C07K 5/083
C07K 5/093
C07K 5/09
C07K 5/103
C07K 5/113
C07K 5/11