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US 2020/0317663 A1Published application
Substituted imidazoquinolines
AssigneeBioNTech SE
InventorChristophe HENRY
Life of this patent
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Abstract
The invention relates to imidazoquinoline derivatives and to pharmaceutical compositions containing the imidazoquinoline derivatives. The imidazoquinoline derivatives of the invention are useful as toll-like receptor agonists, in particular agonists of TLR7, and promote induction of certain cytokines.
Claims13
A compound having the general Formula (I):
- wherein
- R1 is selected from the group consisting of —H, C1-6-alkyl, C1-6-alkoxy, C1-3-alkoxy-C1-3-alkyl, C1-6-alkylthio, C1-3-alkylthio-C1-3alkyl, C1-3-alkylamino-C1-3-alkyl, 4- to 10-membered heterocycloalkyl, C3-10-cycloalkyl, C6-10-aryl, C6-10-aryl-C1-2-alkyl and 5- to 10-membered heteroaryl, wherein said C1-6-alkyl, C1-6-alkoxy, C1-3-alkoxy-C1-3-alkyl, C1-6-alkylthio, C1-3-alkylthio-C1-3-alkyl C1-3-alkylamino-C1-3-alkyl, C6-10-aryl, 4- to 10-membered heterocycloalkyl, C3-10-cycloalkyl, C6-10-aryl-C1-2-alkyl and 5- to 10-membered heteroaryl is optionally substituted by one or more groups independently selected from the group consisting of C1-4-alkyl, —OH, halogen, —CO—N(R4)2, —N(R4)2, —CO—R4, —COO—R4, —N3, —NO2, and —CN;
- R2 is selected from the group consisting of —CO—R5, —CONH—R5, and —COO—R5;
- R3 is tetrahydropyran-4-yl, which is optionally substituted by one or more groups independently selected from the group consisting of C1-4-alkyl, —OH, and halogen;
- R4 is each independently selected from the group consisting of H and C1-4-alkyl;
- n is an integer from 3 to 6;
- and
- R5 is selected from the group consisting of —H, C1-6-alkoxy, C1-6-alkoxy, C1-3-alkoxy-C1-3-alkyl, C1-6-alkylthio, C1-6-alkylthio-C1-3-alkyl, C1-3-alkylamino-C1-3-alkyl, C6-10-aryl, 4- to 10-membered heterocycloalkyl, C3-10-cycloalkyl and 5- to 10-membered heteroaryl, wherein said C1-6-alkyl, C1-6-alkoxy, C1-3-alkoxy-C1-3-alkyl, C1-6-alkylthio, C1-3-alkylthio-C1-3-alkyl, C1-3-alkylamino-C1-3-alkyl, C6-10-aryl, 4- to 10-membered heterocycloalkyl, C3-10-cycloalkyl and 5- to 10-membered heteroaryl is optionally substituted by one or more groups independently selected from the group consisting of C1-4-alkyl, —OH, halogen, —CO—N(R4)2, —N(R4)2, —CO—R4, —COO—R4, —N3, —NO2, and —CN;
- or a physiologically functional derivative, solvate or salt thereof.
6 more elements
9-10. (canceled)
Dependencies are inferred from the claim text.