公开(公告)号：US20230321123A1

公开(公告)日：2023-10-12

申请号：US18042907

申请日：2021-08-24

申请人： Helmholtz-Zentrum Für Infektionsforschung GmbH ,  Universität Des Saarlandes

发明人： Christian Ducho ,  Rolf W. Hartmann ,  Jörg Haupenthal ,  Anna K. H. Hirsch ,  Andreas Kany ,  Cansu Kaya ,  Jelena Konstantinovic ,  Katrin Voos ,  Isabell Walter ,  Samir Yahiaoui ,  Ahmed Saad Abdelsamine ,  Christian Schütz ,  Ravindra Jumde ,  Alexander Kiefer

IPC分类号： A61K31/675 ,  A61K45/06 ,  A61K31/662 ,  A61K31/428 ,  A61K31/426 ,  A61K31/381 ,  A61K31/4406 ,  A61K31/4184

CPC分类号： A61K31/675 ,  A61K45/06 ,  A61K31/662 ,  A61K31/428 ,  A61K31/426 ,  A61K31/381 ,  A61K31/4406 ,  A61K31/4184

摘要： The present invention relates to compounds of formula (Ia) and the use thereof as inhibitors of P. aeruginosa virulence factor LasB. Formula (Ia). These compounds are useful in the treatment of bacterial infections, especially caused by P. aeruginosa.

公开(公告)号：US20230146507A1

公开(公告)日：2023-05-11

申请号：US17913490

申请日：2021-03-23

申请人： Helmholtz-Zentrum Für Infektionsforschung GmbH

发明人： Rolf W. Hartmann ,  Jelena Konstantinovic ,  Jörg Haupenthal ,  Anna K. Hirsch ,  Andreas M. Kany ,  Cansu Kaya ,  Samir Yahiaoui ,  Thomas Wichelhaus ,  Eugen Proschak

IPC分类号： A61K31/196 ,  A61K31/407 ,  C07C323/41 ,  C07C311/08 ,  C07C311/46 ,  C07C311/58 ,  C07C311/64 ,  C07D295/26 ,  C07D295/135 ,  A61K31/18 ,  A61K31/167 ,  A61K31/245 ,  A61K31/64 ,  A61K31/5375 ,  A61K31/495 ,  A61P31/04

CPC分类号： A61K31/196 ,  A61K31/407 ,  C07C323/41 ,  C07C311/08 ,  C07C311/46 ,  C07C311/58 ,  C07C311/64 ,  C07D295/26 ,  C07D295/135 ,  A61K31/18 ,  A61K31/167 ,  A61K31/245 ,  A61K31/64 ,  A61K31/5375 ,  A61K31/495 ,  A61P31/04

摘要： The present invention related to novel inhibitors of metallo-β3-lactamases of formula (I)




wherein R1 is an optionally substituted aryl group of an optionally substituted heteroaryl group, and the use thereof in the treatment of bacterial infections, especially in combination with β-lactam antibiotics.

公开(公告)号：US20210353606A1

公开(公告)日：2021-11-18

申请号：US17257804

申请日：2019-07-03

申请人： HELMHOLTZ-ZENTRUM FÜR INFEKTIONSFORSCHUNG GMBH

发明人： Ahmed S.A. Ahmed ,  Martin Empting ,  Mostafa Hamed ,  Rolf W. Hartmann ,  Jörg Haupenthal ,  Thomas Hesterkamp ,  Ahmed A.M. Kamal ,  Christine K. Maurer ,  Teresa Röhrig ,  Christian Schütz ,  Samir Yahiaoui ,  Michael Zender

IPC分类号： A61K31/4439 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D405/14 ,  A61P31/04 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06

摘要： 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.