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US 5,670,509 AGranted
Tocolytic oxytocin receptor antagonists
AssigneeMerck & Co., Inc.
InventorsBen E. Evans, Douglas W. Hobbs, Joseph M. Pawluczyk, Douglas J. Pettibone, Kenneth E. Rittle, Peter D. Williams
Life of this patent
Estimating the term…
Abstract
Compounds of the formula X-Y-Z-R.sup.1 wherein: X is ##STR1## Y is --CO-- or --SO.sub.2 --; Z is an optional substituent selected from --NH--, --O--, --CHR--, --CH.dbd.CH--, --CH.dbd., --(CH.sub.2).sub.m -- or--CHCHOH--; and R.sup.1 is --CH.sub.3 --, --CH(CH.sub.3).sub.2, or substituted phenyl are tocolytic oxytocin antagonists useful in the treatment of pre-term labor, stripping labor preparatory to Caesarean delivery and dysmenorrhea.
Claims11
A compound or a pharmaceutically acceptable salt thereof, of the formula X-Y-Z-R.sup.1, wherein
- X is ##STR134## Y is --CO--, or --SO.sub.2 --;
- Z is an optional substituent that, when present, is --NH--, --O--, --CHR--, --CH.dbd.CH--, --CH.dbd., --(CH.sub.2).sub.m -- or --CHCHOH--;
- R is C.sub.1-5 alkyl or C.sub.1-5 alkoxycarbonylamino,
- R.sup.1 is --CH.sub.3, --CH(CH.sub.3).sub.2, --NR.sup.4 R.sup.5, --NCOR.sup.6 or ##STR135## R.sup.2 is acetyl, O-Het where Het is imidazole or benzimidazole or azimidobenzene, or where R.sup.2 is further defined as --COR.sup.6, --(CH.sub.2).sub.m -- NHCOR.sup.7, --(CH.sub.2).sub.m --NHCOOR.sup.7, --(CH.sub.2).sub.m --NR.sup.8 R.sup.9, --(CH.sub.2).sub.m --NHCO--(CH.sub.2).sub.m R.sup.7, --(CH.sub.2).sub.m --NHCO--CHR.sup.7 R.sup.7, --(CH.sub.2).sub.m --NHCO--CH.dbd.CHR.sup.7, --NHSO.sub.2 R-- where R is as defined above, NHSO.sub.2 R.sup.7, --SO.sub.2 R.sup.10, --COR.sup.11, ##STR136## R.sup.3 is hydrogen, or hydroxyl;
- R.sup.4 is hydrogen, C.sub.1-5 alkyl, or C.sub.6-10 cycloalkyl;
- R.sup.5 is hydrogen or acetyl;
- R.sup.6 is ##STR137## R.sup.7 is ##STR138## hydrogen, C.sub.1-4 alkyl, NSO.sub.2 R.sup.12 or NHO--C.sub.1-4 alkyl;
- R.sup.8 is hydrogen or C.sub.1-5 alkyl;
- R.sup.9 is hydrogen or C.sub.1-5 alkyl;
- R.sup.10 is --CH.sub.3, ##STR139## R.sup.11 is --CH.sub.3, ##STR140## R.sup.12 is hydrogen, C.sub.1-5 alkyl or C.sub.1-5 alkoxy;
- and m is an integer of from 0 to 5.
8 more elements
Dependencies are inferred from the claim text.