Troponyl-oxamic acid derivatives
AssigneeAyerst McKenna and Harrison Ltd.
InventorsJehan F. Bagli, Tibor Bogri
Life of this patent
Estimating the term…
Abstract
Tropone derivatives characterized by having a derivative of oxamic acid at positions 2 and/or 5 are disclosed. In addition, the tropone nucleus can be optionally further substituted. The foregoing compounds are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of said compounds are disclosed.
Claims26
A compound of formula I ##STR4## in which R.sup.1 and R.sup.4 are the same or different selected from the group consisting of hydrogen, halo, trifluoromethyl, lower alkoxy, lower alkyl, phenyl, hydroxy, phenoxy, mercapto, (2-carboxyphenyl)thio, NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 each is hydrogen or lower alkyl or R.sup.7 is lower alkyl and R.sup.8 is p-toluenesulfonyl, and a radical of formula NR.sup.9 COCOOR.sup.10 wherein R.sup.9 and R.sup.10 each is hydrogen or lower alkyl;
- and R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are the same or different selected from the group consisting of hydrogen, halo, trifluoromethyl, lower alkoxy, lower alkyl, phenyl, hydroxy, phenoxy, mercapto, (2-carboxyphenyl)thio and NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 each is hydrogen or lower alkyl or R.sup.7 is lower alkyl and R.sup.8 is p-toluenesulfonyl;
- with the proviso that at least one of R.sup.1 and R.sup.4 must be a radical of formula NR.sup.9 COCOOR.sup.10 wherein R.sup.9 and R.sup.10 are as defined herein;
- or a therapeutically acceptable salt thereof.
A compound of formula 1 ##STR5## in which a. R.sup.1 is a radical of formula NR.sup.9 COCOOR.sup.10 in which R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy;
- b. R.sup.4 is a radical of formula NR.sup.9 COCOOR.sup.10 in which R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy;
- or
- c. R.sup.1 and R.sup.4 are a radical of formula NR.sup.9 COCOOR.sup.10 wherein R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy;
- or a therapeutically acceptable salt thereof.
A compound of formula 1 ##STR6## in which a. R.sup.1 is a radical of formula NR.sup.9 COCOOR.sup.10 in which R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least three of R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are hydrogen;
- b. R.sup.4 is a radical of formula NR.sup.9 COCOOR.sup.10 in which R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least three of R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are hydrogen;
- or
- c. R.sup.1 and R.sup.4 are a radical of formula NR.sup.9 COCOOR.sup.10 wherein R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least two of R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are hydrogen, or a therapeutically acceptable salt thereof.
A compound of formula 1 ##STR7## in which a. R.sup.1 is a radical of formula NR.sup.9 COCOOR.sup.10 in which R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are hydrogen;
- or
- b. R.sup.1 and R.sup.4 are a radical of formula NR.sup.9 COCOOR.sup.10 in which R.sup.9 and R.sup.10 each is hydrogen or lower alkyl, and R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are hydrogen, or a therapeutically acceptable salt thereof.
Dependencies are inferred from the claim text.