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US 2022/0175784 A1Published application
Isochromene derivatives as phosphoinositide 3-kinases inhibitors
AssigneeChiesi Farmaceutici S.p.A.
InventorsMatteo BIAGETTI, Paolo RONCHI, Claudio FIORELLI, Paolo BRUNO
Life of this patent
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Abstract
The invention relates to compounds of formula (I) inhibiting phosphoinositide 3-kinases (PI3K), to pharmaceutical compositions comprising them and therapeutic use thereof in the treatment of disorders associated with PI3K enzymes.
Claims24
A compound of formula (I):
- wherein:
- each R, when present, is independently selected from the group consisting of:
- OR7, halogen, and (C1-C6) alkyl;
- R1 and R2 are each independently (C1-C6) alkyl;
- R3 and R4 are each independently H or (C1-C6) alkyl;
- or
- R1 and R2 taken together with the nitrogen atom they are linked to, form a 5 or 6 membered heterocyclic radical, wherein at least one further ring carbon atom in the said heterocyclic radical is optionally replaced by at least one heteroatom selected from N, NH, S or O and optionally bears at least one -oxo (═O) substituent group;
- the said heterocyclic radical is further optionally substituted by an (C1-C6) alkyl group, and R3 and R4 are H;
- or
- R3 and R2 taken together, form a 5 or 6 membered heterocyclic radical comprising the N atom;
- the said heterocyclic radical is further optionally substituted by an (C1-C6) alkyl group, R1 is an (C1-C6) alkyl group and R4 is H;
- R5 is OR7;
- R6 is selected from the group consisting of:
- H, OR7, (C1-C6) alkyl, (C1-C6) haloalkyl, and (C1-C6) hydroxyalkyl;
- R7 is selected from the group consisting of:
- H and (C1-C6) alkyl;
- and
- p is zero or an integer ranging from 1 to 4;
- or a pharmaceutically acceptable salt of said compound.
16 more elements
(canceled)
A compound of formula (II)
- wherein
- p is zero, R3 and R4 are H, K is methoxypyridine;
- and R1 and R2 are each independently (C1-C6) alkyl, or R1 and R2 taken together with the nitrogen atom they are linked to, form a 5 or 6 membered heterocyclic radical, wherein at least one further ring carbon atom in the said heterocyclic radical is optionally replaced by at least one heteroatom and optionally bears at least one -oxo (═O) substituent group;
- the said heterocyclic radical is further optionally substituted by an (C1-C6) alkyl group.
1 more element
(canceled)
Dependencies are inferred from the claim text.