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US 2021/0267989 A1Published application
Novel Compounds for the Treatment, Alleviation or Prevention of Disorders Associated with Tau Aggregates
AssigneeAC Immune SA
InventorsSreenivasachary Nampally, Emanuele Gabellieri, Jerome Molette
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Abstract
The present invention relates to novel compounds of formula (I) that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
Claims25
A compound of formula (I):
- or stereoisomers, racemic mixtures, tautomers, pharmaceutically acceptable salts, thereof;
- wherein
- A is selected from the group consisting of
- wherein
- can be attached to the N atom at any available position, and wherein
- is substituted by one or more substituents Rj;
- B is selected from the group consisting of O and NRa;
- E and V are independently selected from the group consisting of N, NR5, O and S;
- G is selected from the group consisting of a benzene ring and a pyridine ring;
- J is selected from the group consisting of O, N—R1 and CH2 or J is selected from the group consisting of CH or C if J is attached to R2;
- Y, Y1, Y2 and Y3 are CZ;
- Z is independently selected from the group consisting of H, halogen, O-alkyl, alkyl and CN;
- R is independently selected from the group consisting of
- and —NR3R4;
- Ra is selected from the group consisting of H and alkyl;
- Rd, Re, Rf, and Rg are independently selected from the group consisting of H and alkyl, or any two of Rd, Re, Rf, and Rg may be joined to form a 3 to 8-membered ring;
- Rj is independently selected from the group consisting of -halogen, —O-alkyl, —NR3R4, —CN,
- wherein a C1-2 carbon atom-containing bridge or a bond can be present between the a carbon atom and the c or d carbon atom or wherein a C1-2 carbon atom-containing bridge or a bond can be present between the b carbon atom and the c or d carbon atom;
- R1 is selected from the group consisting of H and alkyl;
- R2 is independently selected from the group consisting of alkyl, or —O-alkyl and wherein if two R2 are geminal they can be joined to form a 3 to 6-membered ring;
- R3 and R4 are independently selected from the group consisting of H and alkyl;
- R5 is selected from the group consisting of H and alkyl;
- n is 0, 1, 2, 3 or 4;
- r and s are independently 0, 1, 2 or 3;
- and
- t and u are independently 1, 2 or 3.
23 more elements
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A compound of the formula:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.