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US 8,044,088 B2Granted
1-acetic acid-indole derivatives with PGD2 antagonist activity
AssigneeOxagen Limited
InventorsRichard Edward Armer, Edward Andrew Boyd, Philip Andrew Hay
Life of this patent
Estimating the term…
Abstract
Compounds of general formula (I) wherein R1 is halo or cyano; R2 is C1-C4 alkyl; and R3 is phenyl substituted with one or more substituents chosen from C1-C6 alkyl, halo or —SO2(C1-C6 alkyl); or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof; are useful in the treatment of diseases and conditions mediated by the action of PGD2 at the CRTH2 receptor.
Claims21
A compound of general formula (II):
- wherein R1 is halo or cyano;
- R2 is C1-C4 alkyl;
- R3 is phenyl substituted with one or more substituents chosen from C1-C6 alkyl, halo or —SO2(C1-C6 alkyl);
- R4 is hydrogen, C1-C6 alkyl, aryl, (CH2)mOC(═O)C1-C6alkyl, (CH2)mN(R5)2, or CH((CH2)mO(C═O)R6)2;
- m is 1 or 2;
- R5 is hydrogen or methyl;
- and
- R6 is C1-C18 alkyl;
- or a pharmaceutically acceptable salt thereof.
6 more elements
[3-(1-Benzenesulfonyl-1H-pyrrol-2-ylmethyl)-5-fluoro-2-methyl-indol-1-yl]-acetic acid;
- {5-Fluoro-2-methyl-3-[1-(toluene-4-sulfonyl)-1H-pyrrol-2-ylmethyl]-indol-1-yl}-acetic acid;
- or
- {3-[1-(2,4-Difluoro-benzenesulfonyl)-1H-pyrrol-2-ylmethyl]-5-fluoro-2-methylindol-1-yl}-acetic acid;
- or the C1-C6 alkyl, aryl, (CH2)mOC(═O)C1-C6alkyl, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2 ester thereof, wherein R5 is hydrogen or methyl and R6 is C1-C18 alkyl, or a pharmaceutically acceptable salt thereof.
1 more element
Dependencies are inferred from the claim text.