US 11,987,569 B2
Substituted imidazoquinolines as agonists of TLR7
Christophe Henry, Munich (DE)
Assigned to BIONTECH SE, Mainz (DE)
Filed by BIONTECH SE, Mainz (DE)
Filed on Feb. 10, 2022, as Appl. No. 17/669,117.
Application 17/669,117 is a continuation of application No. 16/644,079, granted, now 11,279,684, previously published as PCT/EP2018/073485, filed on Aug. 31, 2018.
Claims priority of application No. PCT/EP2017/072353 (WO), filed on Sep. 6, 2017.
Prior Publication US 2022/0242845 A1, Aug. 4, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61P 35/00 (2006.01); C07D 401/04 (2006.01); C07D 471/04 (2006.01)
CPC C07D 401/04 (2013.01) [A61P 35/00 (2018.01); C07D 471/04 (2013.01)] 16 Claims
 
1. A compound having the general Formula (I):

OG Complex Work Unit Chemistry
wherein
R1 is selected from the group consisting of C1-6-alkyl, C1-3-alkoxy-C1-3-alkyl, and C1-3-alkylamino-C1-3-alkyl, wherein each said C1-6-alkyl, C1-3-alkoxy-C1-3-alkyl, and C1-3-alkylamino-C1-3-alkyl is optionally substituted by one or more groups independently selected from the group consisting of OH and halogen;
R2 is selected from the group consisting of —CO—R5, —CONH—R5, and
—COO—R5;
R3 is 1,1-dioxothietan-3-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 4; and
R5 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-C1-3-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.