1,2,4-oxadiazole derivatives as immunomodulators
AssigneeAuirgene Discovery Technologies Limited
InventorsPottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
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Abstract
The present invention relates to 1,2,4-oxadiazole and 1,2,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
Claims47
A compound of formula (I)
- wherein,
- Q is S or O;
- R1 represents —CH2OH or —CH(CH3)OH, optionally substituted with alkyl or acyl;
- R2 is hydrogen or —CO-Aaa;
- Aaa is an amino acid residue selected from Thr and Ser;
- wherein the C-terminus thereof is a free terminus, is amidated, or is esterified;
- R3 represents —CH2C(O)NH2, —CH2C(O)OH, —CH2CH2C(O)NH2, or —CH2CH2C(O)OH;
- ----- is an optional bond;
- R4 and R5 independently are hydrogen or absent;
- R6 is hydrogen, alkyl, or acyl;
- or a pharmaceutically acceptable salt or a stereoisomer thereof.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient and at least one compound of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof,
- wherein,
- Q is S or O;
- R1 represents —CH2OH or —CH(CH3)OH, optionally substituted with alkyl or acyl;
- R2 is hydrogen or —CO-Aaa;
- Aaa is an amino acid residue selected from Thr and Ser;
- wherein the C-terminus thereof is a free terminus, is amidated, or is esterified;
- R3 represents —CH2C(O)NH2, —CH2C(O)OH, —CH2CH2C(O)NH2, or —CH2CH2C(O)OH;
- ----- is an optional bond;
- R4 and R5 independently are hydrogen or absent;
- and
- R6 is hydrogen, alkyl, or acyl.
Dependencies are inferred from the claim text.