Abstract: Compounds of formula ##STR1## wherein: R.sub.1 is phenyl, naphthyl, phenyl substituted from one to five times by R.sub.6, or naphthyl substituted from one to five times by R.sub.6 ; R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyl substituted at least once by halogen, C.sub.1 -C.sub.3 alkoxy and/or by C.sub.3 -C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, phenyl, phenyl mono- to tri-substituted by halogen, C.sub.1 -C.sub.3 alkoxy and/or by C.sub.1 -C.sub.3 alkyl, benzyl, or benzyl mono- to tri-substituted by halogen, C.sub.1 -C.sub.3 alkoxy and/or by C.sub.1 -C.sub.3 alkyl; R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or the radical CO-R.sub.7 ; R.sub.4 is C.sub.3 -C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 cycloalkyl mono- to tri-substituted by halogen and/or by methyl, C.sub.1 -C.sub.4 alkyl substituted at least once by halogen, hydroxy and/or by cyano, C.sub.2 -C.sub.5 alkynyl, C.sub.1 -C.sub.4 alkylthio or the radical CH.sub.2 XR.sub.8 ; R.sub.5 is hydrogen, C.sub.
Abstract: A pharmaceutical preparation for treating menopausal symptoms, estrogen deficiency and hormone-dependent tumors, and for use as a contraceptive, comprises a compound of formula I ##STR1## wherein R.sub.1 is hydrogen, methyl, a tetrahydropyranyl group or an acyl group andR.sub.2 is hydrogen or methyl.
Type:
Grant
Filed:
December 7, 1988
Date of Patent:
December 11, 1990
Assignee:
Schering Aktiengesellschaft
Inventors:
Peter Jungblut, Rudolf Wiechert, Dieter Bittler
Abstract: This invention relates to benzoxazine and benzoxazepine carboxamide compounds which exhibit 5-HT.sub.3 antagonist properties including CNS, anti-emetic and gastric prokinetic activity and which are void of any significant D.sub.2 receptor binding affinity. This invention also relates to pharmaceutical compositions and methods for the treatment of gastrointestinal and mental disorders using said compounds.
Type:
Grant
Filed:
September 26, 1989
Date of Patent:
June 19, 1990
Assignee:
Rorer Pharmaceutical Corporation
Inventors:
Raymond D. Youssefyeh, Jeffrey C. Pelletier, Henry F. Campbell