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US 2023/0143470 A1Published application
Small molecule inhibitors of influenza hemagglutinin
AssigneeThe Scripps Research Institute
InventorsDennis W. WOLAN, Ian A. WILSON, Yao YAO, Seiya KITAMURA, Nicholas C. WU, Rameshwar U. KADAM, Chang-Chun LEE
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Abstract
Disclosed are small molecule inhibitors of influenza HA, and methods of using them to treat or prevent HA-mediated diseases and conditions.
Claims48
A compound of formula (I) or (II):
- wherein
- R1 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R2 is substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclyl;
- R3 is selected from absent H, alkyl, -alkylene-(heterocyclyl), -alkylene-(aryl), -alkylene-(cycloalkyl), -alkylene-O—R5, -alkylene-C(O)N(R5)2, -alkylene-C(O)R5, -alkylene-C(O)2R5, -alkylene-N(R5)2, -alkylene-N(R)C(OR5), -alkylene-N(R5)C(O)N(R5)—, -alkylene-N(R5)SO2—R5, -alkylene-S—R5, -aryl, -arylene-(heterocyclyl), -arylene-alkyl, -arylene-(cycloalkyl), -arylene-O—R5, -arylene-C(O)N(R5)2, -arylene-C(O)R5, -arylene-C(O)2R5, -arylene-N(R5)2, -arylene-N(R)C(OR5), -arylene-N(R5)C(O)N(R5)—, -arylene-N(R5)SO2—R5, -arylene-S—R5, -heterocyclyl, -heterocyclylene-(alkyl), -heterocyclylene-(aryl), -heterocyclylene-(cycloalkyl), -heterocyclylene-(cycloalkyl), -heterocyclylene-O—R5, -heterocyclylene-C(O)N(R5)2, -heterocyclylene-C(O)R5, -heterocyclylene-C(O)2R5, -heterocyclylene-N(R5)2, -heterocyclylene-N(R)C(OR5), -heterocyclylene-N(R5)C(O)N(R5)—, -heterocyclylene-N(R5)SO2—R5, -heterocyclylene-S—R5, -cycloalkyl, -cycloalkylene-(alkyl), -cycloalkylene-(aryl), -cycloalkylene-(cycloalkyl), cycloalkylene(heterocycloalkyl), -cycloalkylene —O—R5, -cycloalkylene-C(O)N(R5)2, -cycloalkylene-C(O)R5, -cycloalkylene-C(O)2R5, -cycloalkylene-N(R5)2, -cycloalkylene-N(R)C(OR5), -cycloalkylene-N(R5)C(O)N(R5)—, -cycloalkylene-N(R5)SO2—R5, -alkylene-N(H)-alkylene-C(O)OR5, -alkylene-C(O)OR5, -arylene-alkylene-aryl, —C(O)R5, —C(O)2R5, -alkylene-S-alkyl, -alkylene-S—S—R5, —C(O)-alkyl, —C(O)-alkylene-N(R5)2, —C(O)2R5, -aryl-alkylene-N(R5)C(O)—R5, -cycloalkylene-N(R5)S(O)(F)—R5;
- —SO2—NR5, —S(O)(F)—NR5;
- R4 is selected from alkyl, -alkylene-(heterocyclyl), -alkylene-(aryl), -alkylene-(cycloalkyl), -alkylene-O—R5, -alkylene-C(O)N(R5)2, -alkylene-C(O)R5, -alkylene-C(O)2R5, -alkylene-N(R5)2, -alkylene-N(R)C(OR5), -alkylene-N(R5)C(O)N(R5)—, -alkylene-N(R5)SO2—R5, -alkylene-S—R5, -aryl, -arylene-(heterocyclyl), -arylene-alkyl, -arylene-(cycloalkyl), -arylene-O—R5, -arylene-C(O)N(R5)2, -arylene-C(O)R5, -arylene-C(O)2R5, -arylene-N(R5)2, -arylene-N(R)C(OR5), -arylene-N(R5)C(O)N(R5)—, -arylene-N(R5)SO2—R5, -arylene-S—R5, -heterocyclyl, -heterocyclylene-(alkyl), -heterocyclylene-(aryl), -heterocyclylene-(cycloalkyl), -heterocyclylene-(cycloalkyl), -heterocyclylene-O—R5, -heterocyclylene-C(O)N(R5)2, -heterocyclylene-C(O)R5, -heterocyclylene-C(O)2R5, -heterocyclylene-N(R5)2, heterocyclylene-N(R)C(OR5), -heterocyclylene-N(R5)C(O)N(R5)—, -heterocyclylene-N(R5)SO2—R5, -heterocyclylene-S—R5, -cycloalkyl, -cycloalkylene-(alkyl), -cycloalkylene-(aryl), -cycloalkylene-(cycloalkyl), cycloalkylene(heterocycloalkyl), -cycloalkylene —O—R5, -cycloalkylene-C(O)N(R5)2, -cycloalkylene-C(O)R5, -cycloalkylene-C(O)2R5, -cycloalkylene-N(R5)2, -cycloalkylene-N(R)C(OR5), -cycloalkylene-N(R5)C(O)N(R5)—, -cycloalkylene-N(R5)SO2—R5, -alkylene-N(H)-alkylene-C(O)OR5, -alkylene-C(O)OR5, -arylene-alkylene-aryl, —C(O)R5, —C(O)2R5, -alkylene-S-alkyl, -alkylene-S—S—R5, —C(O)-alkyl, —C(O)-alkylene-N(R5)2, —C(O)2R5, -aryl-alkylene-N(R5)C(O)—R5, -cycloalkylene-N(R5)S(O)(F)—R5;
- —SO2—NR5, —S(O)(F)—NR5;
- or
- R3 and R4 can be taken together to form a substituted of unsubstituted heterocyclyl, and
- R5 is H or alkyl or aryl or -alkylene-aryl.
7 more elements
Dependencies are inferred from the claim text.