Thiophene derivatives for up-regulating HLA-DM activity
AssigneesDana-Farber Cancer Institute, Inc., The Brigham and Women's Hospital, Inc.
InventorsLi-An Yeh, Gregory D. Cuny, Melissa Call, Kai Wucherpfennig, Ross L. Stein
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I), compositions, methods and kits are provided. The compounds and compositions may be particularly useful for modulating immunological responses. Formula (I) wherein, R1 is alkyl, aryl, or heterocyclyl; R2 is H, alkyl, aryl, heterocyclyl, OR3 or N(R3)2, R3 is H, alkyl, aryl, or heterocyclyl; R4 is H, CN, halogen, CF3, CO2R3, or C(O)N(R3)2; X is S, SO2, O, or NR3; and Y is S, O, or NR3.
Claims25
A compound of the formula:
- wherein,
- R1 is alkyl, aryl, or heterocyclyl;
- R2 is H, alkyl, aryl, heterocyclyl, OR3, or N(R3)2;
- R3 is H, alkyl, aryl, or heterocyclyl;
- R4 is H, CN, halogen, CF3, CO2R3, or C(O)N(R3)2;
- X is S, SO2, O, or NR3;
- and
- Y is S, O, or NR3.
6-11. (canceled)
15-23. (canceled)
25-28. (canceled)
30-44. (canceled)
46-67. (canceled)
69-100. (canceled)
An assay comprising:
- providing isolated MHC class II molecule bound to CLIP;
- contacting the isolated MHC class II molecule with a test compound;
- contacting the isolated MHC class II molecule with HLA-DM and with a peptide that binds the isolated MHC class II molecule;
- measuring the kinetics of binding of the peptide to the isolated MHC class II molecule;
- and
- determining whether the test compound enhances binding of the peptide to the isolated MHC class II molecule as compared to a control.
103-109. (canceled)
A kit comprising:
- a first container containing isolated MHC class II bound to CLIP;
- and
- a second container containing a peptide that binds the isolated MHC class II.
(canceled)
Dependencies are inferred from the claim text.