US 5,684,151 A · 1-arylsulphonyl, arylcarbonyl and 1-arylphosphonyl-3-phenyl-1,4,5,6-tetrahydropyridazines

Abstract

Disclosed are progestin agonists having the following formula: ##STR1## W is absent or --CH.dbd.CH--; R.sup.1 are independently selected from the group consisting of halogen, --CF.sub.3, and NO.sub.2, or both R.sup.1 may be joined to form a bi-radical which is --CH.dbd.CHCH.dbd.CH--; R.sup.3 are independently selected from the group consisting of hydrogen, C.sub.1-6 branched or linear alkyl, halogen and --CF.sub.3, with the proviso that R.sup.3 at the 3-position must be H where R.sup.3 at the 4-position is H, or both R.sup.3 may be joined to form a bi-radical selected from the group consisting of --CH.dbd.CHCH.dbd.CH--, --C(NC.sub.1-4 alkyl.sub.2)=CHCH.dbd.CH-- and --(CH.sub.2).sub.4 --; R.sup.5 is selected from the group consisting of H and Me; with the proviso that only one of R.sup.1 and R.sup.3 forms the fused bi-radical; and the stereoisomers.

Claims12

Dependent claims

Compounds effective as progestin agonists and having the formula:

##STR27## W is absent or --CH.dbd.CH--;
R.sup.1 are independently selected from the group consisting of halogen, --CF.sub.3, and NO.sub.2, or both R.sup.1 may be joined to form a bi-radical which is --CH.dbd.CHCH.dbd.CH--;
R.sup.3 are independently selected from the group consisting of hydrogen, C.sub.1-6 branched or linear alkyl, halogen and --CF.sub.3, with the proviso that R.sup.3 at the 3-position must be H when R.sup.3 at the 4-position is H, or both R.sup.3 may be joined to form a bi-radical selected from the group consisting of --CH.dbd.CHCH.dbd.CH--, --C(NC.sub.1-4 alkyl.sub.2).dbd.CHCH=CH-- and --(CH.sub.2).sub.4 --;
R.sup.5 is selected from the group consisting of H and Me;
with the proviso that only one of R.sup.1 and R.sup.3 forms the fused bi-radical;
and the stereoisomers thereof.

3 more elements

Compounds effective as progestin antagonists and having the formula:

##STR28## W is absent or --CH.dbd.CH--;
R.sup.1 is selected from the group consisting of halogen, --CF.sub.3 and --NO.sub.2, or both R.sup.1 may be joined to form a bi-radical which is --CH.dbd.CHCH.dbd.CH--;
R.sup.3 is hydrogen, halogen, --CF.sub.3, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy C.sub.1-4 alkyl and C.sub.1-4 alkoxy carbonyl C.sub.1-4 alkoxy with the proviso that R.sup.3 at the 2-position is not hydrogen, or R.sup.3 may be joined to form a bi-radical which is --CH.dbd.CHCH.dbd.CH-- attached at the 2- and 3-positions;
R.sup.a are independently selected from hydrogen or halogen with the proviso that each may be halogen when R.sup.3 is selected only from halogen;
R.sup.5 is selected from the group consisting of hydrogen and methyl, or alternatively, R.sup.5 may be joined with the 6-position to form a bi-radical which is
(5)-CH.sub.2 CH.dbd.CH-(6);
with the proviso that only one of R.sup.1, R.sup.3 and R.sup.5 forms the fused bi-radical;
and the steroisomers and pharmaceutically acceptable salts or esters thereof.

5 more elements

Dependencies are inferred from the claim text.

1-arylsulphonyl, arylcarbonyl and 1-arylphosphonyl-3-phenyl-1,4,5,6-tetrahydropyridazines

Life of this patent

1-arylsulphonyl, arylcarbonyl and 1-arylphosphonyl-3-phenyl-1,4,5,6-tetrahydropyridazines

Life of this patent

Abstract

Claims12