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US 5,684,046 AGranted
Hydrogenated naphthalenes and related LTB.sub.4 antagonists
AssigneePfizer Inc.
InventorKevin Koch
Life of this patent
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Abstract
Described herein are Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.
Claims13
A compound of the formula ##STR18## wherein A is CH.sub.2, NH or N(C.sub.1 -C.sub.6 alkyl);
- n is 1
- R.sup.1 is a substituent at position b or c of the formula ##STR19## R.sup.2, R.sup.8, R.sup.9, and R.sup.10 are hydrogen or each independently are one or any two of the following:
- fluoro, chloro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.4 perfluoroalkyl, C.sub.1 -C.sub.4 perfluoroalkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl or C.sub.1 -C.sub.6 alkylsulfonyl;
- R.sup.3 is --(CH.sub.2).sub.q CHR.sup.11 R.sup.12, --(CH.sub.2).sub.q R.sup.12,--O(CH.sub.2).sub.p CHR.sup.11 R.sup.12, or --O(CH.sub.2).sub.p R.sup.12, wherein p is 0, 1, or 2 and q is 0, 1, 2, or 3;
- R.sup.4 is carboxy, tetrazolyl or R.sup.13 SO.sub.2 NHCO;
- R.sup.11 is hydrogen, C.sub.1 -C.sub.6 alkyl or R.sup.8 -substituted phenyl wherein R.sup.8 is as defined above;
- R.sup.12 and R.sup.13 are hydrogen or each independently are C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.8 cycloalkyl;
- or phenyl, thienyl, pyridyl, furyl, naphthyl, quinolyl, isoquinolyl, pyrimidinyl, or pyrazinyl, each of which is optionally substituted by phenyl, R.sup.9, or R.sup.9 -substituted phenyl wherein R.sup.9 is as defined above;
- or a salt or esters of those compounds of formula I containing a carboxy group, wherein the esters contain ester groups selected from the group consisting of C.sub.1 -C.sub.6 alkyl, phenyl(C.sub.1 -C.sub.6)alkyl, C.sub.3 -C.sub.7 cycloalkyl, and phenyl and benzyl substituted by fluoro, chloro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy.
6 more elements
A process for preparing a compound of the formula ##STR20## wherein A is CH.sub.2 NH or N(C.sub.1 -C.sub.6)alkyl
- n is 1;
- R.sup.1 is a substituent at position b or c of the formula ##STR21## R.sup.1, R.sup.8, R.sup.9, and R.sup.10 are hydrogen or each independently are one or any two of the following:
- fluoro, chloro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.4 perfluoroalkyl, C.sub.1 -C.sub.4 perfluoroalkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl or C.sub.1 -C.sub.6 alkylsulfonyl;
- R.sup.3 is --(CH.sub.2).sub.q CHR.sup.11 R.sup.12, --(CH.sub.2).sub.q R.sup.12, --O(CH.sub.2).sub.p CHR.sup.11 R.sup.12, or --O(CH.sub.2).sub.p R.sup.12, wherein p is 0, 1, or 2 and q is 0, 1,2, or 3;
- R.sup.4 is carboxy, tetrazolyl or R.sup.13 SO.sub.2 NHCO;
- R.sup.11 is hydrogen, C.sub.1 -C.sub.6 alkyl or R.sup.8 -substituted phenyl wherein R.sup.8 is as defined above;
- R.sup.12 and R.sup.13 are hydrogen or each independently are C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.8 cycloalkyl;
- or phenyl, thienyl, pyridyl, furyl, naphthyl, quinolyl, isoquinolyl, pyrimidinyl, or pyrazinyl, each of which is optionally substituted by phenyl, R.sup.9, or R.sup.9 -substituted phenyl wherein R.sup.1 is as defined above;
- or a salt or ester of those compounds of formula I containing a carboxy group, wherein the esters contain ester groups selected from the group consisting of C.sub.1 -C.sub.6 alkyl, phenyl(C.sub.1 -C.sub.6)alkyl, C.sub.3 -C.sub.7 cycloalkyl, and phenyl and benzyl substituted by fluoro, chloro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy, by reducing a compound of the formula ##STR22##
6 more elements
Dependencies are inferred from the claim text.