Hydroxy, Bonded Diretly To Carbon, Or Ether Containing (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/276)
Abstract: Compounds, exhibiting central nervous system activity, of the formula ##STR1## wherein R.sub.1 is phenyl which is unsubstituted or substituted by at least one member selected from the group consisting of halogen, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and COOH, orR.sub.1 is ##STR2## or R.sub.1 is a heterocycle selected from the group consisting of ##STR3## R.sub.2 R.sub.3 R.sub.4 and R.sub.5, which may be identical or different, are H or CH.sub.3 ;R.sub.6 and R.sub.7, which may be identical or different, are C.sub.1 -C.sub.6 alkyl, which may be straight-chained or branched, orR.sub.7 can be H when R.sub.6 is a branched-chain alkyl, orR.sub.6 and R.sub.7 can form, with the nitrogen to which they are bonded, a heterocycle selected from the group consisting of ##STR4## R.sub.8 R.sub.9 R.sub.10 and R.sub.11, which may be identical or different, are H, halogen, CF.sub.3, hydroxy or C.sub.1 -C.sub.4 alkoxy, or two contiguous members of R.sub.8 R.sub.9, R.sub.10 and R.sub.
Type:
Grant
Filed:
February 23, 1981
Date of Patent:
June 8, 1982
Assignee:
Laboratoires Sarget
Inventors:
Marie-Helene Creuzet, Claude Feniou, Francoise Guichard, Gisele Prat
Abstract: The present invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and bioprecursors thereof in which ##STR2## represents either ##STR3## R.sup.1 represents hydrogen, halogen, C.sub.1-4 alkoxy, hydroxy, alkyl, R.sup.4 CH(OH)--, cyano or R.sup.5 CONH--, R.sup.2 and R.sup.3, which may be the same or different, each represents a straight or branched chain alkyl group or alkenyl group or R.sup.2 and R.sup.3 may, together with the nitrogen atom to which they are attached, form a saturated heterocyclic ring containing from 5 to 7 members which may optionally contain an oxygen atom; R.sup.4 represents hydrogen or alkyl; and R.sup.5 represents hydrogen, alkyl or C.sub.1-4 alkoxy. The compounds have been shown to exhibit H.sub.1 -antagonist activity in standard pharmacological tests.
Type:
Grant
Filed:
October 3, 1980
Date of Patent:
April 13, 1982
Assignee:
Glaxo Group Limited
Inventors:
John Bradshaw, Alexander W. Oxford, David I. C. Scopes
Abstract: A benzylalcohol derivative of the formula: ##STR1## wherein R is hydroxy, benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is monomethoxyphenyl, dimethoxyphenyl, trimethoxyphenyl or 3,4-methylenedioxyphenyl is prepared by reducing a compound of the formula: ##STR2## wherein R' is benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is the same as defined above, and when R' is benzyloxy, if required, further subjecting the product to catalytic hydrogenation.The compounds (I) and pharmaceutically acceptable acid addition salts thereof are used as anti-diabetic agents.
Abstract: A process for the preparation of an indolenine of the formula ##STR1## where R, X and Y are conventional substituents, by thermal rearrangement of a compound of the formula ##STR2## to give a compound of the formula ##STR3## and cyclization of this compound in the presence of an acid catalyst.
Type:
Grant
Filed:
January 30, 1979
Date of Patent:
March 10, 1981
Assignee:
BASF Aktiengesellschaft
Inventors:
Hans-Joachim Opgenorth, Horst Scheuermann, Harald Laas, Axel Nissen