Heteroaryl compounds and uses thereof
AssigneeAprinoia Therapeutics Limited
InventorsMing-Kuei JANG, Paul TEMPEST
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Abstract
Described herein are compounds of formula (I), and pharmaceutically acceptable salts, solvates, hydrates, isotopically labeled derivatives and radiolabeled derivative thereof, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for detecting and imaging Tau aggregates in the brain for detection of Alzheimer's disease (AD) in a subject.
Claims16
A heteroaryl compound having a structure of formula (I), or a pharmaceutically acceptable salt, a solvate, a hydrate, an isotopically labeled derivative or a radiolabeled derivative thereof,
- wherein the structural unit
- is
- Ra is selected from the group consisting of H, OH, halogen, C1-3 alkyl, C1-3 alkoxy, NH2, C1-3 alkylamino and C1-6 alkoxycarbonyl, wherein said C1-3 alkyl, said C1-3 alkoxy, said C1-3 alkylamino, and said C1-6 alkoxycarbonyl are optionally substituted with OH, halogen, C2-6 heterocycloalkyloxy or toluenesulfonyloxy;
- Rb is selected from the group consisting of
- H, C1-6 alkyl, C1-6 alkoxycarbonyl, C1-3 alkylcarbonyl, benzyl and benzoyl;
- wherein said C1-6 alkyl, said C1-6 alkoxycarbonyl, and said C1-3 alkylcarbonyl are optionally substituted with halogen, OH, C1-3 alkoxy, C2-6 heterocycloalkyloxy or toluenesulfonyloxy;
- Q is CH or N;
- X is CH or N;
- Y is CR6 or N;
- R6 is selected from the group consisting of H, NH2, OH, —N(CH3)2, C1-6 alkoxy,
- wherein said NH2 and said C1-6 alkoxy are optionally mono-substituted with C1-3 alkyl or halogen;
- J is CH or N;
- K is CH or N;
- and
- provided that X and Y are not N simultaneously, and J and Y are not N simultaneously;
- R′ is halogen, OH, C1-6 alkyl, or C1-6 alkoxy;
- R″ is Br, I, OH, NH2,
- C1-6 alkylamino or C3-6 heterocycloalkyl;
- wherein said C1-6 alkylamino and said C3-6 heterocycloalkyl are optionally substituted with a substituent selected from the group consisting of oxo, OH, halogen, C3-6 cycloalkyl, C1-4 alkoxy carbonyl, C3-6 heterocycloalkyloxy, toluenesulfonyloxy, and phenyl which is further optionally substituted with OH and/or C1-3 alkoxy;
- m is 0, 1, 2;
- and
- n is 0, 1, or 2;
- provided that:
- when Y is N or CH, then n is 1 or 2;
- and
- when Y is CR6, wherein R6 is NH2 or C1-6 alkoxy, and wherein said NH2 and said C1-6 alkoxy are optionally mono-substituted with C1-3 alkyl or halogen, then n is 0.
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A heteroaryl compound having a structure of formula (I), or a pharmaceutically acceptable salt, a solvate, a hydrate, an isotopically labeled derivative or a radiolabeled derivative thereof, which is selected from the group consisting of
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Dependencies are inferred from the claim text.