公开(公告)号：US20190194213A1

公开(公告)日：2019-06-27

申请号：US16331920

申请日：2017-07-25

Applicant: Universite de Liege

Inventor： Cécile Oury ,  Patrizio Lancellotti

IPC: C07D487/04 ,  A61L27/54 ,  A61P31/04

CPC classification number: C07D487/04 ,  A01N43/90 ,  A61L27/54 ,  A61L2300/404 ,  A61L2300/406 ,  A61L2430/20 ,  A61P31/04

Abstract: Triazolo(4,5-d)pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or use as inhibitor of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers.

公开(公告)号：US10905691B2

公开(公告)日：2021-02-02

申请号：US16688961

申请日：2019-11-19

Applicant: Universite de Liege

Inventor： Cécile Oury ,  Patrizio Lancellotti

IPC: A61K31/519 ,  C07D487/04 ,  A61P31/04 ,  A61L2/00 ,  A61L2/16

Abstract: A method for treatment of a bacterial infection in a host mammal in need of such treatment or a method of administering to the host mammal an effective amount of a Triazolo(4,5-d)pyrimidine of formula(I): wherein R1 is C3-5 alkyl optionally substituted by one or more halogen atoms; R2 is a phenyl group, optionally substituted by one or more halogen atoms; R3 and R4 are both hydroxyl; R is XOH, wherein X is CH2, OCH2CH2, or a bond, and wherein when X is a bond, R is OH; or a pharmaceutical acceptable salt, provided that when X is CH2 or a bond, R1 is not propyl; when X is CH2 and R1 is CH2CH2CF3, butyl or pentyl, the phenyl group at R2 must be substituted by fluorine; when X is OCH2CH2 and R1 is propyl, the phenyl group at R2 must be substituted by fluorine.

公开(公告)号：US11434241B2

公开(公告)日：2022-09-06

申请号：US16958023

申请日：2019-02-14

Applicant: UNIVERSITE DE LIEGE

Inventor： Patrizio Lancellotti ,  Cécile Oury ,  Bernard Pirotte

IPC: C07D473/40 ,  A61K9/00 ,  C07D473/28

Abstract: Pyrimidine derivatives of formula (I): optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. Pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. Pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.

公开(公告)号：US20200093826A1

公开(公告)日：2020-03-26

申请号：US16688961

申请日：2019-11-19

Applicant: Universite de Liege

Inventor： Cécile Oury ,  Patrizio Lancellotti

IPC: A61K31/519 ,  A61P31/04 ,  A61L2/16 ,  A61L2/00

Abstract: A method for treatment of a bacterial infection in a host mammal in need of such treatment or a method of administering to the host mammal an effective amount of a Triazolo(4,5-d)pyrimidine of formula(I): wherein R1 is C3-5 alkyl optionally substituted by one or more halogen atoms; R2 is a phenyl group, optionally substituted by one or more halogen atoms; R3 and R4 are both hydroxyl; R is XOH, wherein X is CH2, OCH2CH2, or a bond, and wherein when X is a bond, R is OH; or a pharmaceutical acceptable salt, provided that when X is CH2 or a bond, R1 is not propyl; when X is CH2 and R1 is CH2CH2CF3, butyl or pentyl, the phenyl group at R2 must be substituted by fluorine; when X is OCH2CH2 and R1 is propyl, the phenyl group at R2 must be substituted by fluorine.