Invention Grant
- Patent Title: Pyrrole derivatives as PLK1 inhibitors
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Application No.: US17453959Application Date: 2021-11-08
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Publication No.: US11884656B2Publication Date: 2024-01-30
- Inventor: Robert George Boyle , David Winter Walker , Richard Justin Boyce
- Applicant: SENTINEL ONCOLOGY LIMITED
- Applicant Address: GB Cambridge
- Assignee: SENTINEL ONCOLOGY LIMITED
- Current Assignee: SENTINEL ONCOLOGY LIMITED
- Current Assignee Address: GB Cambridge
- Agency: Heslin Rothenberg Farley & Mesiti P.C.
- Priority: GB 06806.5 2017.04.28
- Main IPC: C07D413/14
- IPC: C07D413/14 ; C07D207/32 ; C07D231/12 ; C07D261/08 ; C07D401/04 ; C07D403/10 ; C07D405/14 ; C07D409/04 ; A61P35/00 ; C07D207/325 ; C07D401/14 ; C07D403/12 ; C07D413/12

Abstract:
The invention provides compounds of the formula (3):
or a pharmaceutically acceptable salt or tautomer thereof, wherein:
Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O;
ring X is a benzene or pyridine ring;
ring Y is a benzene, pyridine, thiophene or furan ring;
Ar1 is an optionally substituted benzene, pyridine, thiophene or furan ring;
m is 0, 1 or 2;
n is 0, 1 or 2;
R1 is selected from various substituents:
R2 is selected from hydrogen and a C1-4 hydrocarbon group;
R3 is selected from hydrogen and a C1-4 hydrocarbon group;
R4 is selected from various substituents;
R5 is selected from various substituents;
Ar2 is an optionally substituted phenyl, pyridyl or pyridone group;
R6 is a group Q1-Ra—Rb;
Q1 is absent or is a C1-3 saturated hydrocarbon linker;
Ra is selected from O; C(O); C(O)O; CONRc; N(Rc)CO; N(Rc)CONRc, NRc; and SO2NRc;
Rb is selected from hydrogen and various substituents;
and Rb is selected from R4.
The compounds are useful in the treatment of cancers.
or a pharmaceutically acceptable salt or tautomer thereof, wherein:
Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O;
ring X is a benzene or pyridine ring;
ring Y is a benzene, pyridine, thiophene or furan ring;
Ar1 is an optionally substituted benzene, pyridine, thiophene or furan ring;
m is 0, 1 or 2;
n is 0, 1 or 2;
R1 is selected from various substituents:
R2 is selected from hydrogen and a C1-4 hydrocarbon group;
R3 is selected from hydrogen and a C1-4 hydrocarbon group;
R4 is selected from various substituents;
R5 is selected from various substituents;
Ar2 is an optionally substituted phenyl, pyridyl or pyridone group;
R6 is a group Q1-Ra—Rb;
Q1 is absent or is a C1-3 saturated hydrocarbon linker;
Ra is selected from O; C(O); C(O)O; CONRc; N(Rc)CO; N(Rc)CONRc, NRc; and SO2NRc;
Rb is selected from hydrogen and various substituents;
and Rb is selected from R4.
The compounds are useful in the treatment of cancers.
Public/Granted literature
- US20220135552A1 PYRROLE DERIVATIVES AS PLK1 INHIBITORS Public/Granted day:2022-05-05
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