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US 2010/0137371 A1Published application
Novel Pharmaceutical Compounds
OwnerCarl Berthelette, Claude Dufresne +2inventors
InventorsCarl Berthelette, Claude Dufresne, Lianhai Li, zhaoyin Wang
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Abstract
The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents.
Claims21
A compound of structural Formula I
- and the pharmaceutically acceptable salts, esters and solvates thereof wherein:
- is selected from the group consisting of
- wherein the numbers “1” and “2” indicate the points of attachment within structural Formula I;
- A is selected from the group consisting of —Cl and phenyl optionally mono- or di-substituted with a substituent independently selected at each occurrence from the group consisting of (i) —F (ii) —Cl, (iii) —C1-3alkyl optionally substituted with one or more of halo, (iv) —OC1-3alkyl optionally substituted with one or more of halo, (v) —OC3-6cycloalkyl, (vi) —C3-6cycloalkyl, (vii) —CH2OH, (viii) —COOR5, (ix) —CN and (x) —NR5R5a;
- n is an integer selected from zero, 1 and 2;
- R1 is selected from the group consisting of (i) —H, (ii) —Br, (iii) —Cl, (iv) —COC1-6alkyl, (v) —COOC1-6alkyl, (vi) —COOC3-6cycloalkyl, (vii) —SO2C1-6alkyl, (viii) —SO2NR5R5, (ix) —CONR5R5, (x) —CN, (xi) —C1-6alkyl optionally mono- or di-substituted with a substituent independently selected at each occurrence from the group consisting of —OH and —F, (xii) phenyl optionally mono- or di-substituted with a substituent independently selected at each occurrence from the group consisting of —OH and —F, (xiii) tetrazolyl optionally substituted with methyl, (xiv) 1,2,4-oxadiazolyl optionally substituted with methyl, and (xv) pyridinyl optionally substituted with methyl;
- R2 is selected from the group consisting of —H, —OH, —F, —C1-3alkyl, —OC1-3alkyl and —OC(O)—C1-3alkyl;
- R3 is selected from the group consisting of —H, —C1-6alkyl, —C1-6alkyl substituted with one or more of fluoro, —C1-6alkyl substituted with R6, phenyl, —C2-6alkenyl, —C3-6cycloalkyl and —C5-7cycloalkenyl;
- R4 is selected from the group consisting of —H, —C1-6alkyl, —C1-6alkyl substituted with one or more of fluoro, —C1-6alkyl substituted with R6, phenyl, —C2-6alkenyl, —C3-6cycloalkyl and —C5-7cycloalkenyl;
- R5 is independently selected at each occurrence from the group consisting of —H, —C1-6 alkyl and —C3-6cycloalkyl;
- R5a is independently selected at each occurrence from the group consisting of —H, —C1-6 alkyl, —C3-6cycloalkyl and —COOR5;
- and
- R6 is independently selected at each occurrence from the group consisting of —COOR5, —C(O)H, —CN, —CR5R5OH, —OR5, —S—C1-6alkyl and —S—C3-6 cycloalkyl.
10 more elements
-26. (canceled)
Dependencies are inferred from the claim text.