公开(公告)号：US20240173332A1

公开(公告)日：2024-05-30

申请号：US18547244

申请日：2022-02-24

Applicant: Pfizer Inc.

Inventor： Matthew Barrett ,  Alexandre Bedernjak ,  George Stuart Cockerill ,  James Good

IPC: A61K31/5513 ,  A61K9/00 ,  A61K9/08 ,  A61K9/20 ,  A61K45/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/22 ,  A61K47/26 ,  A61K47/69 ,  A61P31/14 ,  C07D487/04

CPC classification number: A61K31/5513 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2059 ,  A61K45/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/22 ,  A61K47/26 ,  A61K47/6951 ,  A61P31/14 ,  C07D487/04

Abstract: Pharmacuetical Compounds Benzodiazepine derivatives of formula (I): wherein: R1 is H or F; R2 is selected from formula (II) and formula (III) R3 is C1-C6 alkyl which is unsubstituted or substituted by CF3, or is a monocyclic 4- to 6-membered heterocyclic group containing 1 or 2 heteroatoms selected from O, N and S; R4 is H or a group selected from —X, -alk-X, —CONR6R7, C═NNR6R7, —SO2R6 and —SO2NR6R7; R4 is a group selected from —X, -alk-X, —CONR6R7, —C═NNR6R7, —SO2R6 and —SO2R6R7; X is OH or a derivative of an OH group selected from α-amino carboxylic acid esters, carboxylic acid esters, carbonates, carbamates, ethers and phosphates: alk is C1-C6 alkylene which is unsubstituted or substituted by C3-C6 cycloalkyl; and R6 and R7 are each independently C1-C6 alkyl or C3-C6 cycloalkyl; and the pharmaceutically acceptable salts thereof are inhibitors of respiratory syncytial virus (RSV) and can therefore be used to treat or prevent an RSV infection.

公开(公告)号：US12227507B2

公开(公告)日：2025-02-18

申请号：US17636510

申请日：2020-08-20

Applicant: Pfizer Inc.

Inventor： George Stuart Cockerill ,  James Good ,  Craig Alex Avery ,  Andrew Joseph Warner ,  Edward James Cochrane

IPC: A61K31/5513 ,  A61K45/06 ,  A61P31/14 ,  C07D487/04 ,  C07D519/00

Abstract: Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, and are bonds, and and are absent; or (ii) T is C, Z is N, and are bonds, and and are absent; each of R3 and R4 is independently halo, —OR6, —NR6R7, —COR8, —C(O)OR8, —CON(R8)2 or —R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.