公开(公告)号：US20240239767A1

公开(公告)日：2024-07-18

申请号：US18539471

申请日：2023-12-14

Applicant: AstraZeneca AB

Inventor： Gavin Donal O’MAHONY ,  Olaf PANKNIN ,  Andrey FROLOV ,  Anna TOMBERG ,  Mateusz Piotr PLESNIAK ,  Jens Peter BRANDT ,  Erik WEIS ,  Jens Patrik JOHANSSON ,  Emma BRATT

IPC: C07D401/14 ,  A61P9/00 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D401/14 ,  A61P9/00 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: A compound with the Formula (I):






wherein A is of the following formula:








and



X1 is selected from O, S or NH;
X2 is either N or C—H
X3 is either N or C—RA3;
wherein if X1 is NH and X2 is C—H then X3 is C—RA3;
B is of formula (B-1) or (B-2)










C is selected from the group consisting of optionally substituted C6-10 carboaryl, C5-6 heteroaryl or C5-10 heterocyclyl, and their use as PCSK9 inhibitors.

公开(公告)号：US20240217951A1

公开(公告)日：2024-07-04

申请号：US18470521

申请日：2023-09-20

Applicant: AstraZeneca AB

Inventor： Gavin Donal O’MAHONY ,  Olaf PANKNIN ,  Andrey FROLOV ,  Anna TOMBERG ,  Mateusz Piotr PLESNIAK ,  Jens Peter BRANDT ,  Jan Åke LINDBERG ,  Jens Patrik JOHANSSON

IPC: C07D401/14 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/501 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048

CPC classification number: C07D401/14 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/501 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048

Abstract: A compound with the Formula (I):


A-B—C  (I)



wherein A is of the following formula:










where X1 is C—RA1;
B is of formula (B-1) or (B-2)










and C is selected from the group consisting of optionally substituted C6-10 carboaryl, C5-6 heteroaryl and C5-10 heterocyclyl and their use as PCSK9 inhibitors.

公开(公告)号：US20240228469A1

公开(公告)日：2024-07-11

申请号：US18470548

申请日：2023-09-20

Applicant: AstraZeneca AB

Inventor： Gavin Donal O’MAHONY ,  Olaf PANKNIN ,  Andrey FROLOV ,  Anna TOMBERG ,  Erik WEIS ,  Hans Frederik BERGSTRÖM ,  Karl Thomas ANTONSSON ,  Jan Åke LINDBERG ,  Jens Patrik JOHANSSON

IPC: C07D403/14 ,  A61K31/53 ,  A61K31/675 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07F9/6558

CPC classification number: C07D403/14 ,  A61K31/53 ,  A61K31/675 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07F9/65583

Abstract: A compound with the Formula (I):


A-B-C  (I)

wherein A is of the following formula:




where X1 is N

B is of formula (B-1) or (B-2)





and C is selected from the group consisting of optionally substituted C6-10 carboaryl, C5-6 heteroaryl and C5-10 heterocyclyl and their use as PCSK9 inhibitors.