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US 7,247,725 B2Granted
Gamma-aminoamide modulators of chemokine receptor activity
AssigneeMerck & Co., Inc.
InventorsGabor Butora, Alexander Pasternak, Lihu Yang, Changyou Zhou
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Abstract
The present invention is directed to compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, W, X, and n are defined herein, which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
Claims3
A compound of the formula Ib:
- wherein the dashed line represents a single or a double bond and wherein
- R1 is selected from:
- and positional and stereo isomers thereof;
- R2 is selected from:
- (C0-6alkyl)-phenyl and (C0-6alkyl)-heterocycle, where the alkyl is unsubstituted or substituted with 1–7 substituents where the substituents are independently selected from:
- (a) halo,
- (b) hydroxy,
- (c) —O—C1-3alkyl,
- (d) trifluoromethyl,
- (e) —C1-3alkyl,
- (f) —CO2R9, and
- (g) oxo;
- and where the phenyl and the heterocycle may be unsubstituted or substituted with 1–5 substituents where the substituents are independently selected from:
- (a) halo,
- (b) trifluoromethyl
- (c) trifluoromethoxy,
- (d) hydroxy,
- (e) C1-6alkyl,
- (f) C3-7cycloalkyl,
- (g) —O—C1-6alkyl,
- (h) —O—C3-7cycloalkyl,
- (i) —SCF3,
- (j) —S—C1-6alkyl,
- (k) —SO2—C1-6alkyl,
- (l) phenyl,
- (m) hetreocycle,
- (n) —CO2R9,
- (o) —CN,
- (p) —NR9R10,
- (q) —NR9—SO2—R10,
- (r) —SO2—NR9R10,
- (s) —ONR9R10, and
- (t) —O -phenyl;
- R5 is selected from:
- (a) hydrogen,
- (b) hydroxy,
- (c) C1-6alkyl,
- (d) C1-6alkyl-hydroxy,
- (e) —O—C1-3alkyl,
- (f) oxo, and
- (g) halo,
- (h) C0-4CO2R9, and
- (i) CF3,
- R15 and R16 are independently selected from:
- (a) hydrogen,
- (b) halo,
- (c) trifluoromethyl,
- (d) hydroxy,
- (e) C1-3alkyl,
- (f) —O—C1-3alkyl,
- (g) —CO2H,
- (h) –CO2C1-3alkyl,
- (i) —CN, and
- (j) heterocycle;
- and pharmaceutically acceptable salts and individual diastereomers thereof.
52 more elements
Dependencies are inferred from the claim text.