Abstract: A group of heterocyclic compounds generally exhibiting central nervous system activity (such as depressant and anti-convulsant activities) and, in some cases, cardiovascular and/or anti-inflammatory activity are described. The compounds have the formula ##STR1## where A is an ethyl or propyl group which is mono-substituted by defined substituents or a di(loweralkyl)amino (loweralkoxy) carbonyl group and R is a phenyl group which may be substituted by defined substituents.
Abstract: The invention concerns novel hexahydroazepines of the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R is hydrogen, lower alkyl, benzyl or lower alkanoyl, R.sup.1 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, benzyl or cyclopropylmethyl, R.sup.2 is hydrogen, lower alkyl, lower alkenyl or lower alkynyl, R.sup.3 is lower alkyl, lower alkenyl or lower alkynyl and R.sup.4 is lower alkyl. The compounds are useful as analgesic agents.
Abstract: The invention concerns hexahydroazepines of the formula ##STR1## and the pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R.sup.4 is lower alkyl, R.sup.5 is lower alkyl, lower alkenyl, lower alkynyl or cyclopropylmethyl and R.sup.6 is a 1-adamantoyl group. The compounds are useful as analgesic agents.
Type:
Grant
Filed:
June 7, 1976
Date of Patent:
May 3, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Alan Chapman White, Richard Arthur Franklin
Abstract: Alkyl or Aralkyl N-[2-aroyl]phenylcarbamates are prepared by reacting a 3-aryl-2-indolinone with oxygen in the presence of an alkali metal alkoxide or aralkoxide.
Abstract: The invention relates to magnesium halide derivatives of tetrahydroquinolines and related compounds. These are intermediates useful in the preparation of anti-ulcer agents.
Abstract: The invention relates to novel 8-cyano-5,6,7,8-tetrahydroquinoline derivatives which are intermediates for the preparation of corresponding 8-thioamides. Some of the 8-cyano compounds are anti-ulcer agents.
Type:
Grant
Filed:
October 20, 1975
Date of Patent:
March 8, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Roger Crossley, David George Hill
Abstract: The invention relates to a compound of formula I ##STR1## or pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and represent hydrogen, or lower alkyl, and R.sup.6 represents hydrogen, alkyl or 1 to 3 carbon atoms, which may be substituted by diloweralkylamino; lower alkanoyl or aroyl.The compounds are either anti-ulcer agents or intermediates for such compounds.
Abstract: The invention relates to magnesium halide derivatives of tetrahydroquinolines and related compounds. These are intermediates useful in the preparation of anti-ulcer agents.
Abstract: The invention provides 5,6,7,8-tetrahydroquinoline derivatives which are substituted at the 8-position by an amino group. The 8-amino compounds are intermediates for corresponding thiocarbamoyl derivatives which are anti-ulcer agents.
Type:
Grant
Filed:
April 2, 1976
Date of Patent:
March 8, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Roger Crossley, David George Hill
Abstract: The invention provides a compound of formula I ##STR1## wherein R is phenylloweralkyl and R.sup.1 is loweralkyl and the pharmaceutically acceptable acid addition salts thereof. Also included are anti-ulcer compositions comprising an effective amount of a compound of formula I and a pharmaceutically acceptable carrier.
Abstract: The invention relates to novel 5,6,7,8-tetrahydroquinoline derivatives which have a group X situated at the 8-position said group X is CONHR.sup.3, or CO.sub.2 R.sup.5 wherein R.sup.3 is hydrogen lower alkyl and R.sup.5 is hydrogen, lower alkyl or a lower aralkyl radical.The compounds are intermediates for corresponding compounds where X is CSNHR.sup.3 and these are anti-ulcer agents.
Type:
Grant
Filed:
October 20, 1975
Date of Patent:
February 22, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Roger Crossley, David George Hill
Abstract: The invention provides novel indane and tetrahydronaphthalene derivatives having the general formula ##SPC1##Wherein R.sup.1 represents hydrogen or lower alkyl; R.sup.2 represents lower alkyl; R.sup.3 and R.sup.4 independently represent hydrogen or lower alkyl; and n is the integer 1 or zero; and the pharmaceutically acceptable acid addition and quaternary ammonium salts thereof; which have hypotensive activity.
Abstract: The invention relates to a process for preparing pyridine compounds which have a fused cycloalkane ring containing an amide, thioamide or nitrile group. The process involves treating a metal derivative of the pyridine compound with a silyl isocyanate or isothiocyanate and then subjecting the product to hydrolysis or alcoholysis.
Type:
Grant
Filed:
November 25, 1974
Date of Patent:
December 28, 1976
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Robin Gerald Shepherd
Abstract: This application concerns quinoline derivatives of formula I ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein X represents CSNHR.sup.1, where R.sup.1 represents hydrogen or lower alkyl, R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl, R.sup.4 represents hydrogen or single or multiple substitution by lower alkyl and n is 1, 2 or 3.These compounds are anti-ulcer agents.
Abstract: A new process for preparing 5-oxo-tetrahydroquinolines comprises condensing a compound of formula II with a ##STR1## compound of formula III to obtain a compound of formula I wherein R, R.sup.1, R.sup.2 and R.sup.3 are selected from hydrogen or alkyl, aralkyl or aryl groups, Y is NH.sub.2 or OH accompanied by an ethylenic bond or Y is oxo and the double bond is absent and A is an amino or lower alkoxy group of 1-4 carbon atoms at least one of Y or A being amino. Compounds of formula I are intermediates for pharmaceuticals.
Abstract: This invention relates to bases of the formula ##SPC1##And their acid addition salts with pharmaceutically acceptable acids. In the formula R.sup.1 represents phenyl or phenyl substituted by one or more hydroxyl, lower alkyl, lower alkoxy, haloloweralkyl or halogen atoms; R.sup.2 and R.sup.5 are hydrogen, hydroxyl, lower alkyl, lower alkoxy, haloloweralkyl or halogen and R.sup.3 and R.sup.4 are hydrogen or lower alkyl. The compounds have antidepressant activity.
Type:
Grant
Filed:
July 22, 1974
Date of Patent:
December 21, 1976
Assignee:
John Wyeth & Brother Limited
Inventors:
Alan Chapman White, Robin Michael Black
Abstract: The disclosure relates to derivatives of tetrahydro-1H-1,3-diazepine and hexahydro-1,3-diazocine of the general formula ##STR1## or pharmaceutically acceptable acid addition salts thereof wherein n represents 2 or 3, R.sup.3 and R.sup.4 which may be the same or different each represent hydrogen or lower alkyl, Ph represents phenyl, halophenyl, lower alkyl phenyl, di(lower alkyl) phenyl or lower alkoxy phenyl, R is hydroxyl, lower alkoxy or halogen, R.sup.1 is phenyl, halophenyl, lower alkyl phenyl, di(lower-alkyl phenyl, lower alkoxyphenyl or naphthyl and R.sup.6 is hydrogen or lower alkyl. The compounds have hypoglycemic activity.
Type:
Grant
Filed:
May 29, 1975
Date of Patent:
December 7, 1976
Assignee:
John Wyeth & Brother Limited
Inventors:
Alan Chapman White, Robin Michael Black
Abstract: The invention concerns a novel process for preparing 5,6,7,8-tetrahydroquinolines and related compounds substituted by a monosubstituted thioamide group in which a metal derivative of the 5,6,7,8-tetrahydroquinoline or related compound is reacted with an alkyl, aryl or aralkyl isothiocyanate and the product is treated with hydrogen ions.
Abstract: Certain novel 4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c] pyridine derivatives and their pharmacologically acceptable salts are described. These compounds provide potent and non-toxic compositions for the treatment of hypertension. Certain of the disclosed compounds also display activity as anti-tremor agents.
Type:
Grant
Filed:
April 15, 1975
Date of Patent:
November 16, 1976
Assignee:
John Wyeth & Brother Limited
Inventors:
John Leheup Archibald, Kenneth Heatherington
Abstract: A group of heterocyclic compounds useful in the treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted phenyl radical through the intermediary of a group selected from a lower-alkylene radical, a mono-keto lower alkylene radical or a hydroxy-lower-alkylene radical, or a bivalent radical of the formula ##EQU1## or --O--(lower-alkylene)-. The piperidine rings are further substituted by a benzamido, substituted benzamido or cyclohexylcarboxamido residue.
Type:
Grant
Filed:
April 2, 1975
Date of Patent:
November 16, 1976
Assignee:
John Wyeth & Brother Limited
Inventors:
John Frederick Cavalla, John Leheup Archibald