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US 2014/0005174 A1Published application
Indole derivatives useful as ccr2 antagonists
OwnerAnilkumar G. Nair, Joseph A. Kozlowski +2inventors
InventorsAnilkumar G. Nair, Joseph A. Kozlowski, Jose S. Duca, Stuart B. Rosenblum
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Abstract
Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salt thereof wherein R7, A, X, B, and n are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
Claims14
A compound of Formula I:
- wherein:
- Ring A is selected from the group consisting of:
- Ring B is
- X is alkylene;
- R1 and R2 independently are H, alternatively R1 and R2 together with two adjacent carbon atoms to which they are attached form cyclopentyl, cyclopentenyl, aryl, heterocyclyl, heterocyclenyl, or heteroaryl, each of which is unsubstituted or substituted by 1-3 R6 groups, wherein said heterocyclyl, heterocyclenyl, or heteroaryl rings have 1-4 heteroatoms selected from the group consisting of O, N, and S;
- R3 is 1-2 substituents independently selected from the group consisting of:
- (a) hydrogen,
- (b) C1-6alkyl,
- (c) C2-6alkenyl,
- (d) C2-6alkynyl,
- (e) cyclopropyl,
- (f) halo,
- (g) C1-6haloalkyl,
- (h) hydroxyl,
- (i) C1-6alkoxyl, and
- (j) C1-6haloalkoxyl;
- R4 is selected from the group consisting of:
- (a) hydrogen,
- (b) C1-6alkyl,
- (c) C2-6alkenyl,
- (d) C2-6alkynyl,
- (e) cyclopropyl,
- (f) halo,
- (g) C1-6haloalkyl,
- (h) hydroxyl,
- (i) C1-6alkoxyl,
- (j) C1-6haloalkoxyl, and
- (k) —CN;
- R5 is selected from the group consisting of:
- (a) hydrogen,
- (b) C1-6alkyl,
- (c) C2-6alkenyl,
- (d) C2-6alkynyl,
- (e) cyclopropyl,
- (f) C1-6haloalkyl,
- (g) aryl, and
- (h) aryl- C1-6alkyl;
- R6 is 1-3 substituents independently selected from the group consisting of:
- (a) hydrogen,
- (b) C1-6alkyl,
- (c) C1-6haloalkyl,
- (d) C1-6alkoxyl,
- (e) halo, and
- (f) aryl;
- R8 is selected from the group consisting of:
- (a) hydrogen,
- (b) C1-6alkyl,
- (c) halo,
- (d) C1-6haloalkyl, and
- (e) C1-6alkoxyl;
- R7 is 1-4 substituents independently selected from the group consisting of:
- (a) hydrogen,
- (b) C1-6alkyl,
- (c) C2-6alkenyl,
- (d) C2-6alkynyl,
- (e) hydroxyl,
- (f) halo,
- (g) C1-6haloalkyl,
- (h) —CN,
- (i) C1-6alkoxyl,
- (j) C1-6haloalkoxyl, and
- (k) —NH2;
- n is 1 or 2;
- or
- a pharmaceutically acceptable salt thereof.
62 more elements
14-17. (canceled)
Dependencies are inferred from the claim text.