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US 11,447,482 B1Granted
Imidazopyridine and oxazolopyridine derivatives and analogs thereof, methods of preparation thereof, methods of HIF-2A pathway inhibition, and induction of ferroptosis
AssigneeKuda Therapeutics, Inc.
InventorsXiaohui Liu, Mei Yee Koh
Life of this patent
Estimating the term…
Abstract
Novel substituted imidazopyridine and oxazolopyridine compounds that are useful as inhibitors of HIF-2α and inducers of ferroptosis through perturbations in iron metabolism, synthetic methods for making said compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and compositions to treat disorders associated with dysfunction of HIF-2α or iron metabolism.
Claims20
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- X1 is NH;
- X2 is O;
- Z is NH;
- each of C1, C2, C3, and C4, (C1-4) as independently, C or N, wherein at least one of C1-4 is N;
- when C1 is N, then R1 is not present;
- when C2 is N, then R2 is not present;
- when C3 is N, then R3 is not present;
- when C4 is N, then R4 is not present;
- when C1 is C, then R1 is H, CH3,
- when C2 is C, then R2 is H, Cl, CF3, OCH3, or
- when C3 is C, then R3 is H, OCH3, CF3,
- when C4 is C, then R4 is H, OCH3, or
- Ca, Cc, Cd, and Ce are each C;
- Cb is C or N;
- Ra is H or OCH3;
- when Cb is C, then Rb is H, F, or OCH3, or together with Rc forms a methylenedioxy;
- when Cb is N, then Rb is not present;
- Rc is H, F, Cl, CH3, OCH3, CN, CF3, OCF3, SCH3, N(CH3), OCH(CH3)2
- C(CH3)3
- or together with Rb forms a methylenedioxy;
- and
- Rd and Re are each H.
20 more elements
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- X1 is NH;
- X2 is O;
- Z is NH;
- each of C1, C2, C3, and C4, (C1-4) is, independently, C or N,
- wherein at least one of C1-4 is N;
- each of Ca, Cb, Cc, Cd, and Ce (Ca-e) is, independently, C or N;
- each of R1, R2, R3, and R4, (R1-4) and each of Ra, Rb, Rc, Rd, and Re (Ra-e):
- (i) is, independently, selected from H, F, Cl, CH3, OCH3, CN, CF3, OCF3, SCH3, N(CH3)2, OCH(CH3)2
- or, when the respective C1-4 or Ca-e to which the respective R1-4 or Ra-e is attached is N, then the said R1-4 or Ra-e is not present;
- or
- (ii) together with an adjacent one of R1-4 or Ra-e forms methylenedioxy.
9 more elements
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- X1 is O or NH;
- X2 is O or S or NH;
- Z is CH2 or O or S or NRA, where RA is H or C1-4 alkyl;
- each of C1, C2, C3, and C4, (C1-4) and each of Ca, Cb, Cc, Cd, and Ce (Ca-e) is, independently, C or N,
- wherein at least one of C1-4 is N;
- and
- each of R1, R2, R3, and R4, (R1-4) and each of Ra, Rb, Rc, Rd, and Re (Ra-e):
- (i) is, independently, selected from H, F, Cl, CH3, OCH3, CN, CF3, OCF3, SCH3, N(CH3)2, OCH(CH3)2
- or, when the respective C1-4 or Ca-e to which the respective R1-4 or Ra-e is attached is N, then the said R1-4 or Ra-e is not present;
- or
- (ii) together with an adjacent one of R1-4 or Ra-e forms a methylenedioxy.
9 more elements
Dependencies are inferred from the claim text.