Substituted aminotetralines
AssigneeHoffmann-La Roche Inc.
InventorsFariborz Firooznia, Paul Gillespie, Robert Alan Goodnow, Jr., Tai-An Lin, Achyutharao Sidduri, Sung-Sau So, Jenny Tan
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Abstract
The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R4 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
Claims26
A compound of formula I:
- or a pharmaceutically acceptable salt or ester thereof, wherein:
- R1 is hydrogen, halogen, methoxy, or phenyl;
- and R2 is hydrogen, fluoro, chloro, or alkyl;
- with the proviso that R1 and R2 are not both hydrogen;
- R3 is hydrogen or methyl;
- and
- R4 is phenyl substituted by two substituents independently selected from the group consisting of:
- (1) halogen,
- (2) lower alkyl optionally substituted by halogen,
- (3) lower alkanoyl,
- (4) lower alkoxy,
- (5) lower alkylsulfanyl, lower alkylsulfinyl, or lower alkylsulfonyl, and
- (6) lower cycloalkylsulfanyl, lower cycloalkylsulfinyl, or lower cycloalkylsulfonyl;
- or alternatively,
- R4 is pyridine substituted by one or two substituents independently selected from the group consisting of:
- (1) halogen,
- (2) lower alkyl optionally substituted by halogen, and
- (3) phenyl or pyridine, wherein said phenyl or pyridine is optionally substituted by lower alkyl, lower alkylsulfanyl, lower alkylsulfonyl, lower cycloalkylsulfanyl, or lower cycloalkylsulfonyl.
Dependencies are inferred from the claim text.