Indole carbamates as leukotriene antagonists
AssigneePfizer Inc.
InventorsMatthew F. Brown, Anthony Marfat
Life of this patent
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Abstract
Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.
Claims11
A compound of the formula ##STR8## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is CHO, CH.sub.2 F, CHF.sub.2 or CONR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are each independently selected from the group consisting of hydrogen, (C.sub.1 -C.sub.6 alkyl, (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.6)alkynyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl (C.sub.1 -C.sub.6)alkyl, ((C.sub.1 -C.sub.6)alkyl).sub.3 amino (C.sub.1 -C.sub.6)alkyl, pyridinyl and CHR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are each independently (C.sub.1 -C.sub.6)alkyl or (C.sub.6 -C.sub.10) aryl;
- or R.sup.3 and R.sup.4 together with the nitrogen to which they are attached form morpholinyl, pyrrolidinyl or a group of the formula ##STR9## wherein the broken lines represent optional double bonds;
- n is 0, 1 or 2;
- X, Y and Z are each independently CH, O, S or N;
- and
- R.sup.7 R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are each independently selected from the group consisting or hydrogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.6)alkynyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl (C.sub.1 -C.sub.6)alkyl, ((C.sub.1 -C.sub.6)alkyl).sub.2 amino (C.sub.1 -C.sub.6)alkyl, pyridinyl, CHR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are each independently (C.sub.1 -C.sub.6)alkyl or (C.sub.6 -C.sub.10)aryl;
- or
- benzhydryl optionally substituted by one to five halo;
- or R.sup.7 and R.sup.8, R.sup.8 and R.sup.9, R.sup.9 and R.sup.10, or R.sup.10 and R.sup.11 together form a benzo group;
- R.sup.2 is a group of the formula ##STR10## or a group of the formula ##STR11## wherein X is O, NH or CH.sub.2 ;
- and R.sup.12 is (C.sub.3 -C.sub.7)cycloalkyl or a group of the formula ##STR12## wherein the broken line represents an optional double bond;
- n is 0 or 1;
- m is 0, 1 or 2;
- p is 0, 1 or 2;
- Q and R.sup.3 are both CH or both CH.sub.2 ;
- with the proviso that when Q and R.sup.3 are both CH, the broken line represents a double bond;
- and
- with the proviso that when n is 1 or 2, only two of the three variables X, Y and Z can be O, S or N.
Dependencies are inferred from the claim text.