| 54 |
Titel |
TI |
[EN] SELECTIVE TMPRSS2 INHIBITORS AND MEDICAL USE THEREOF
[FR] INHIBITEURS SÉLECTIFS DE TMPRSS2 ET LEUR UTILISATION MÉDICALE |
| 71/73 |
Anmelder/Inhaber |
PA |
MAX PLANCK GESELLSCHAFT, DE
|
| 72 |
Erfinder |
IN |
KNAFF PHILIP, DE
;
LANDFESTER KATHARINA, DE
;
MAILÄNDER VOLKER, DE
;
MÜNCH JAN, DE
;
WETTSTEIN LUKAS, DE
|
| 22/96 |
Anmeldedatum |
AD |
11.06.2021 |
| 21 |
Anmeldenummer |
AN |
2021065871 |
|
Anmeldeland |
AC |
EP |
|
Veröffentlichungsdatum |
PUB |
23.12.2021 |
33
31
32 |
Priorität |
PRC
PRN
PRD |
EP
20180647
20200617
|
| 51 |
IPC-Hauptklasse |
ICM |
A61P 31/12
(2006.01)
|
| 51 |
IPC-Nebenklasse |
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-Zusatzklasse |
ICA |
|
|
IPC-Indexklasse |
ICI |
|
|
Gemeinsame Patentklassifikation |
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-Hauptklasse |
MCM |
A61P 31/12
(2006.01)
|
|
MCD-Nebenklasse |
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-Zusatzklasse |
MCA |
|
| 57 |
Zusammenfassung |
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.
[FR] L'invention concerne le composé de formule générale (I) en tant que nouveaux inhibiteurs de TMPRSS2 et l'utilisation de ces inhibiteurs pour la prophylaxie et le traitement d'une infection par le virus de la grippe ou d'une infection à coronavirus, en particulier d'une infection par le SARS-CoV2 (COVID-19). |
| 56 |
Entgegengehaltene Patentdokumente/Zitate,
in Recherche ermittelt |
CT |
WO002012162828A1
WO002016144654A1
|
| 56 |
Entgegengehaltene Patentdokumente/Zitate,
vom Anmelder genannt |
CT |
|
| 56 |
Entgegengehaltene Nichtpatentliteratur/Zitate,
in Recherche ermittelt |
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 7;
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 7;
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 7;
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 7;
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 7;
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 7;
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 7
|
| 56 |
Entgegengehaltene Nichtpatentliteratur/Zitate,
vom Anmelder genannt |
CTNP |
ABEL T, BLOOD, vol. 122, 2013, pages 2030 - 2038 1;
BELIVEAU, F. ET AL., CELL CHEM BIOL, vol. 26, no. 11, 2019, pages 1559 - 1572 1;
BERMAN, H. M ET AL.: "The Protein Data Bank", NUCLEIC ACIDS RESEARCH, vol. 28, no. 1, 2000, pages 235 - 242, XP002963358, DOI: 10.1093/nar/28.1.235 1;
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HOFFMANN ET AL., CELL, vol. 181, 2020, pages 271 - 280 1;
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KOUJI SAKAI ET AL., JOURNAL OF VIROLOGY, vol. 88, no. 10, 2014, pages 5608 - 5616 1;
MAIER, J. A. ET AL., J CHEM THEORY COMPUT, vol. 11, no. 8, 2015, pages 3696 - 71 1;
MEYER, D. ET AL., BIOCHEM J, vol. 452, no. 2, 2013, pages 331 - 43 1;
MUNCH RC, MOL THER, vol. 19, 2011, pages 686 - 693 1;
ROMAIN ZUFFEREY, NAT. BIOTECHNOL., vol. 3, 1997, pages 3 - 8 1;
STERLING, T., J CHEM INF MODEL, vol. 55, no. 11, 2015, pages 2324 - 37 1;
W-J SHIN ET AL., EXPERT OPINION ON DRUG DISCOVERY, vol. 12, no. 11, 2017, pages 1139 - 1152 1;
WATERHOUSE, A. ET AL., NUCLEIC ACIDS RES, no. 46, 2018, pages W296 - W303 1
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