Back to results
US 11,345,713 B2Granted
Compounds as modulators of TLR2 signaling
AssigneeNeuropore Therapies, Inc.
InventorsSrinivasa Reddy Natala, Wolfgang Wrasidlo
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to compounds, pharmaceutical compositions comprising such compounds, and use of such compounds in methods of treatment or in medicaments for treatment of inflammatory diseases and certain neurological disorders that are related to inflammatory signaling processes, including but not limited to misfolded proteins.
Claims16
A compound of Formula (A)
- or a tautomer, or a pharmaceutically acceptable salt of any of the foregoing, wherein
- indicates that the ring is saturated, partially unsaturated, or fully unsaturated;
- indicates that the
- is attached in either the E or Z configuration;
- G1 and G2 are each independently CRx;
- Rx is hydrogen or halogen;
- R1 is —OH;
- R2 is CHO;
- R3 is C1-C6alkoxy or halogen, wherein the C1-C6alkoxy of R3 is unsubstituted or substituted with one or more halogen;
- Y is —C(O)— or absent and R4 and R5 are each H,
- G3 is CH(X1—R6a), C(X1—R6a), N, N(X1—R6a), S, or O;
- G4 is CH(X2—R6b), C(X2—R6b), N, N(X2—R6b), S, or O;
- G5 is CH(X3—R6c), C(X3—R6c), N, N(X3—R6c), S, or O;
- G6 is CH(X4—R6d), C(X4—R6d), N, N(X4—R6d), S, O, or absent;
- G7 is N, C, or CH;
- wherein when G5 is N, at least one of (i), (ii), and (iii) applies:
- (i) at least one of G3, G4, and G6 is not CH;
- (ii) R4 and R5 come together to form —S—;
- and
- (iii) R3 is —OCH3 or halo;
- X1, X2, X3, and X4 are each independently absent,
- m is 1-6;
- R6a, R6b, R6c, and R6d are each independently hydrogen, C1-C6alkyl, C1-C6alkoxy, halo, —OH, —NRpRq, aryl, heterocyclyl, heteroaryl, —C1-C6alkyl-heterocyclyl, —OC(O)-heterocyclyl, —C(O)Rh, —S(O)2NRw1Rw2, —S(O)2Ry, or —NRz1S(O)2Rz2, wherein the C1-C6alkyl and C1-C6alkoxy of R6a, R6b, R6c, and R6d are each independently unsubstituted or substituted with one or more groups selected from the group consisting of cycloalkyl and halogen;
- the aryl and heteroaryl of R6a, R6b, R6c, and R6d are each independently unsubstituted or substituted with one or more groups selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, —OH, and C1-C6alkyl-OH;
- and the heterocyclyl, —C1-C6alkyl-heterocyclyl, and —OC(O)-heterocyclyl of R6a, R6b, R6c, and R6d are each independently unsubstituted or substituted with one or more groups selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, —OH, C1-C6alkyl-OH, ═O, and ═S;
- Rh is selected from the group consisting of H, C1-C6alkyl, C1-C6alkoxy, C3-C8cycloalkyl, and —NRrRs;
- Rp is H or C1-C6alkyl;
- Rq is C2-C3alkyl, —C(O)Rt, —C(O)ORu, or —C(O)NRv;
- Rr, Rs, Rw1, and Rz1 each independently selected from H and C1-C6alkyl;
- and
- Rt, Ru, Rv, Rw2, Ry, and Rz2 are each independently selected from H, C1-C6alkyl, unsubstituted or substituted C3-C8cycloalkyl, and unsubstituted or substituted heterocyclyl;
- or
- G5 is CH(X3—R6c) or C(X3—R6c), G6 is CH(X4—R6d) or C(X4—R6d), and R6c and R6d are taken together with the carbons to which they are attached to form a 6-membered aryl, a 6-membered heterocyclyl, or a 6-membered heteroaryl ring;
- wherein the 6-membered aryl, 6-membered heterocyclyl, and 6-membered heteroaryl rings are each independently unsubstituted or substituted;
- wherein no more than one of R6a, R6b, R6c, and R6d is C1-C6alkoxy or —OH;
- and
- wherein the compound is not a compound of Table 1X.
34 more elements
Dependencies are inferred from the claim text.