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US 2025/0154147 A1Published application
Novel amine-substituted phthalazines and derivatives as sos1 inhibitors
AssigneeJazz Pharmaceuticals Ireland Limited
InventorsClifford David JONES, Gayle DOUGLAS, Camille GIGNOUX, Robin Charles HUMPHREYS
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Abstract
The present disclosure provides compounds of formula (Ia) that are inhibitors of SOS1, pharmaceutical compositions thereof, and methods of treating oncological diseases using the compounds and compositions disclosed herein.
Claims57
A compound of Formula (Ia):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 and R2 are independently hydrogen, alkyl, or R1 and R2 together with the atom to which they are attached form a cycloalkyl or heterocyclyl, wherein at least one of R1 and R2 is not hydrogen;
- R3 is hydrogen, alkyl, —(C═O)—ORA, —(C═O)—N(RA)2, cycloalkyl, heterocyclyl, aryl or heteroaryl;
- wherein RA is hydrogen or alkyl;
- is a heteroaryl;
- R6 is H, alkyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl or heteroaryl;
- R7 is H, halogen, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- R8 is H, halogen, alkyl, alkoxy, alkylene-O-alkyl, cycloalkyl, or heterocyclyl;
- L1 and L2 are each independently absent or a linking group;
- and
- X is independently selected from the group consisting of C1-5alkyl, F, CF3, CHF2, CH2F, and —NH2;
- m is 1 or 2;
- and
- n is an integer from 1-5,
- provided that:
- (a)
- is not
- and
- (b) the compound of Formula (Ia) is not:
17 more elements
Dependencies are inferred from the claim text.