Dopamine agonists and use thereof
AssigneeNelson Research & Development Company
InventorAlan S. Horn
Life of this patent
Estimating the term…
Abstract
Compounds are disclosed having the formula: ##STR1## wherein: R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR2## R.sub.2 is H, --CH.sub.3, or ##STR3## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl; R.sub.4 is H, --CH.sub.3, --CH.sub.2 OH, --CH.sub.2 --CN, --CH.sub.2 --S--Me, CH.sub.2 --S--CN, or ##STR4## R.sub.5 is H, 1-4 carbon alkyl, alkenyl, or alkynyl, or aralkyl having a 1-4 carbon alkylene moiety; and A is --CH.sub.2 --or --CH.sub.2 CH.sub.2 --, and pharmaceutically-acceptable salts thereof. Pharmaceutical preparations using these compounds and a method for inducing a dopaminergic response by administering these compounds are also disclosed.
Claims25
A compound of the formula:
- ##STR21## wherein:
- R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR22## R.sub.2 is H, --CH.sub.3, or ##STR23## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl;
- R.sub.4 is --CH.sub.2 OH, --CH.sub.2 --CN, --CH.sub.2 --S--Me, --CH.sub.2 --S--CN, or ##STR24## R.sub.5 is H, 1-4 carbon alkyl, alkenyl, or alkynyl, or aralkyl having a 1-4 carbon alkylene moiety;
- and A is --CH.sub.2 --or --CH.sub.2 CH.sub.2 --;
- or a pharmaceutically-acceptable salt thereof.
A compound of the formula:
- ##STR28## wherein:
- R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR29## R.sub.2 is H, --CH.sub.3, or ##STR30## R.sub.3 is phenyl, benzyl, or 1-14 carbon alkyl;
- R.sub.4 is H, --CH.sub.3, --CH.sub.2 OH, --CH.sub.2 -CN, --CH.sub.2 -S-Me, --CH.sub.2 -S-CN, or ##STR31## R.sub.5 is 2-thienylethyl, or 3-thienylethyl;
- and A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --;
- or a pharmaceutically-acceptable salt thereof.
N-2-thienylethyl-9-hydroxy-2 ,3,4a,5,6,10b-hexahydro-4H-naphth-[1,2-b][1,4] oxazine or a pharmaceutically acceptable salt thereof.
N-3-thienylethyl-9-hydroxy-2,3,4a,5,6, 10b-hexahydro-4H-naphth-[1,2-b][1,4] oxazine or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition, comprising:
- an active ingredient of the formula ##STR34## wherein:
- R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR35## R.sub.2 is H, --CH.sub.3, or ##STR36## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl;
- R.sub.4 is --CH.sub.2 OH, --CH.sub.2 -CN, --CH.sub.2 -S-Me, CH.sub.2 -S-CN, or ##STR37## R.sub.5 is H, 1-4 carbon alkyl, alkenyl, or alkynyl, or aralkyl having a 1-4 carbon alkylene moiety;
- and A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, or a pharmaceutically-acceptable salt thereof;
- and
- a pharmaceutically-acceptable carrier.
A pharmaceutical composition, comprising:
- an active ingredient of the formula ##STR40## wherein:
- R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR41## R.sub.2 is H, --CH.sub.3, or ##STR42## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl;
- R.sub.4 is H, --CH.sub.3, --CH.sub.2 OH, --CH.sub.2 -CN, --CH.sub.2 -S-Me, CH.sub.2 -S-CN, or ##STR43## R.sub.5 is 2-thienylethyl, or 3-thienylethyl;
- and A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --;
- or a pharmaceutically-acceptable salt thereof;
- and
- a pharmaceutically-acceptable carrier.
A method for inducing a dopaminergic response, comprising the step of administering to a patient a dopaminergically-effective amount of a compound having the formula:
- ##STR46## wherein:
- R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR47## R.sub.2 is H, --CH.sub.3, or ##STR48## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl;
- R.sub.4 is --CH.sub.2 OH, --CH.sub.2 -CN, --CH.sub.2 -CN, --CH.sub.2 -S-Me, CH.sub.2 -S-CN, or ##STR49## R.sub.5 is H, 1-4 carbon alkyl, alkenyl, or alkynyl, or aralkyl having a 1-4 carbon alkylene moiety;
- and A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, and pharmaceutically-acceptable salts thereof.
A method for inducing a dopaminergic response, comprising the step of administering to a patient a dopaminergically-effective amount of a compound having the formula:
- ##STR50## wherein:
- R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR51## R.sub.2 is H, --CH.sub.3, or ##STR52## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl;
- R.sub.4 is H, --CH.sub.3, --CH.sub.2 OH, --CH.sub.2 -CN, --CH.sub.2 -S-Me, CH.sub.2 -S-CN, or ##STR53## R.sub.5 is 2-thienylethyl, or 3-thienylethyl;
- and A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 -;
- or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.