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1. WO2020007938 - PqsR INVERSE AGONISTS

Publication Number WO/2020/007938
Publication Date 09.01.2020
International Application No. PCT/EP2019/067899
International Filing Date 03.07.2019
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72
Nitrogen atoms
74
Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
C07D 213/74 (2006.01)
C07D 401/12 (2006.01)
C07D 413/12 (2006.01)
C07D 417/12 (2006.01)
A61K 31/506 (2006.01)
A61K 31/4439 (2006.01)
CPC
A61P 31/00
C07D 213/74
C07D 401/12
C07D 413/12
C07D 417/12
Applicants
  • HELMHOLTZ-ZENTRUM FÜR INFEKTIONSFORSCHUNG GMBH [DE/DE]; Inhoffenstrasse 7 38124 Braunschweig, DE
Inventors
  • AHMED, Ahmed S. A.; DE
  • EMPTING, Martin; DE
  • HAMED, Mostafa; DE
  • HARTMANN, Rolf W.; DE
  • HAUPENTHAL, Jörg; DE
  • HASTERKAMP, Thomas; DE
  • KAMAL, Ahmed A. M.; DE
  • MAURER, Christine K.; DE
  • RÖHRIG, Teresa; DE
  • SCHÜTZ, Christian; DE
  • YAHIAOUI, Samir; DE
  • ZENDER, Michael; DE
Agents
  • FORSTMEYER, Dietmar; BOETERS & LIECK Oberanger 32 80331 München, DE
  • PAUSTIAN, Othmar; DE
  • LIECK, H.-Peter; DE
Priority Data
18181475.703.07.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PqsR INVERSE AGONISTS
(FR) AGONISTES INVERSES DE PQSR
Abstract
(EN)
The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.
(FR)
La présente invention concerne un composé de formule générale (I), qui agit en tant qu'inhibiteur de PqsR (le seul récepteur connu actuellement pour le signal de quinolone de Pseudomonas (PQS)) ; une composition pharmaceutique contenant un ou plusieurs composés selon l'invention ; une préparation combinée contenant au moins un composé selon l'invention et au moins un autre ingrédient pharmaceutique actif ; et des utilisations dudit(desdits) composé(s), y compris l'utilisation en tant que médicament, par exemple l'utilisation dans le traitement ou la prophylaxie d'une infection bactérienne, en particulier d'une infection par Pseudomonas aeruginosa ou Burkholderia.
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