Abstract: Compounds of formula 1 ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different selected from the group consisting of hydrogen, halogen, nitro, trifluoromethyl, lower alkyl and lower alkoxy, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 together form a CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 chain and R.sup.3 and R.sup.4, R.sup.1 and R.sup.4 and R.sup.1 and R.sup.2, respectively, are as defined above, R.sup.5 is hydrogen, lower alkyl or a radical of formula -Alk-OR.sup.6 wherein Alk is an alkylene selected from the group consisting of CR.sup.7 R.sup.8, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 and CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 CR.sup.13 R.sup.14 wherein each of R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is hydrogen or lower alkyl and R.sup.6 is hydrogen or lower alkyl; R.sup.15 is hydrogen or lower alkyl; X is O, S, SO or SO.sub.2 ; and Y is O or NR.sup.
Abstract: Disclosed is a process for preparing (4a,13b-trans)-1,2,4,4a,8,9,13b,14-octahydro-3H-benzo[6,7]cyclohepta[1,2,3 -de]-pyrido[2,1-a]isoquinolin-3-one involving a 1,3-cycloaddition of a 4-halo-1-butene to 1,7,8,12b-tetrahydrobenzo[1,2]cyclohepta-[3,4,5-de]isoquinoline N-oxide.
Abstract: Disclosed are methods and compositions for the prevention of painful conditions in an animal subject comprising the use of (+)(4a,13b-trans)-(3-hydroxy,13b-trans)-3-isopropyl-2,3,4,4a,8,9,13b,14-oc tahydro-1H-benzo[6,7]cyclohepta[1,2,3-de]pyrido[2,1-a]isoquinolin-3-ol, or a therapeutically acceptable acid addition salt thereof, alone or in a potentiating amount in combination with a suitable analgesic agent.
Abstract: Phthalimidopiperidines of the formula ##STR1## are described where R.sub.1 is hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, phenyl(lower)alkyl, pyridyl(lower)alkyl, furyl(lower)alkyl or thienyl(lower)alkyl and R.sub.2 and R.sub.3 are hydrogen or various substituents. The compounds are useful pharmaceutically, particularly as anti-convulsants, and also in some cases as anti-arrhythmic agents and anti-inflammatory agents, and in some cases useful as intermediates for the preparation of 4-aminoquinoline derivatives having anti-malarial activity.
Type:
Grant
Filed:
January 21, 1976
Date of Patent:
October 11, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
John Terence Arnott Boyle, John Christopher Saunders
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 quinoline derivatives of the formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts of those compounds capable of forming acid addition salts. In formula (I), R.sup.1 and R.sup.2 which may be the same of different each represent hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halogen, R.sup.3 and R.sup.4 which may be the same or different each represent lower alkyl and X represents hydroxy, halogen, hydrazino, or a radical of formula -NR.sup.5 R.sup.6 where R.sup.5 and R.sup.6 which may be the same or different each represent hydrogen or lower alkyl or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring containing 5 to 7 ring atoms. The compounds possess hypotensive activity.
Abstract: The invention provides 5,6,7,8-tetrahydroquinoline derivatives which are substituted at the 8-position by the group NHCSNHR.sup.5 where R.sup.5 is lower alkanoyl or aroyl. These compounds are intermediates for corresponding compounds where R.sup.5 is hydrogen, such compounds being anti-ulcer agents.This application is a continuation-in-part of our copending U.S. application Ser. No. 554,259 filed Feb. 28, 1975, now U.S. Pat. No. 3,991,065.
Type:
Grant
Filed:
April 2, 1976
Date of Patent:
September 13, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Roger Crossley, David George Hill
Abstract: Novel piperidine compounds and their use in 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 cycloalkyl or a substituted or unsubstituted phenyl radical through the intermediary of a lower-alkylene radical. The piperidine ring is further substituted by an acylamino residue.
Type:
Grant
Filed:
June 16, 1976
Date of Patent:
September 6, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
John Frederick Cavalla, John Leheup Archibald
Abstract: The invention provides a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent hydrogen or alkyl of 1-6 carbon atoms, R.sup.3 represents hydrogen, alkyl of 1-6 carbon atoms, or phenyl, X is Na, K, Li, or CSNHR.sup.4 wherein R.sup.4 is hydrogen or alkyl of 1-6 carbon atoms and n is 3, 4 or 5 or a pharmaceutically acceptacle acid addition salt of a compound where X is CSNHR.sup.4.The compounds of formula I wherein X is CSNHR.sup.4 are anti-ulcer agents. Those in which X is Na, K or Li are intermediates.
Type:
Grant
Filed:
January 23, 1976
Date of Patent:
September 6, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Robin Gerald Shepherd
Abstract: A group of heterocyclic compounds useful in the treatment of disorders and diseases of the cardiovascular system is described. These compounds are piperidine compounds linked by the nitrogen atom to a methylenedioxyphenyl or an ethylenedioxyphenyl radical through the intermediary of a group selected from a mono-keto lower alkylene radical or a hydroxy-lower-alkylene radical or a bivalent radical of the formula ##STR1## or --O--(lower alkylene). The piperidine rings are further substituted by a benzamido residue.
Type:
Grant
Filed:
April 20, 1976
Date of Patent:
August 30, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
John Frederick Cavalla, John Leheup Archibald
Abstract: This invention relates to compounds having the general formula: ##STR1## wherein W represents a phenyl or indolyl radical, either of which radicals may be unsubstituted or substituted by halogen, lower alkyl, lower alkoxy or hydroxy; A represents a lower alkylene radical an oxo lower alkylene radical or a hydroxy lower alkylene radical; R represents a phenyl radical optionally substituted by halogen, lower alkyl, lower alkoxy or hydroxy, or a cycloalkyl radical of 5 to 7 carbon atoms; R.sup.1 represents hydrogen or a lower alkyl radical or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof; which possess hypotensive activity.
Type:
Grant
Filed:
April 14, 1976
Date of Patent:
August 30, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
John Leheup Archibald, John Lambert Jackson
Abstract: 2-Morpholinol derivatives characterized by having an aryloxymethyl radical attached to the 6 position and an alkyl or alkynyl radical attached to the nitrogen at the 4 position are disclosed. The derivatives may be optionally substituted at the 2 position with an alkyl or aryl group and the hydroxyl function at position 2 may be replaced with an alkoxy group. The 2-morpholinol derivatives of this invention are useful .beta.-adrenergic blocking and antifungal agents. Methods for the preparation and use of these derivatives are also described.
Abstract: The invention relates to pharmaceutical compositions containing 5,6,7,8-tetrahydroquinoline-8-thioamides and nitriles and related tricyclic compounds and methods of treating ulcers using said compounds.
Type:
Grant
Filed:
October 24, 1975
Date of Patent:
August 23, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Roger Crossley, David George Hill
Abstract: The invention relates to novel cyclopenteno[b]pyridine derivatives which have a thioamide group in the 7-position and related tricyclic compounds. The compounds are anti-ulcer agents.
Type:
Grant
Filed:
October 20, 1975
Date of Patent:
June 21, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Roger Crossley, David George Hill
Abstract: Pharmaceutical compositions containing a group of heterocyclic compounds and their use in treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds used in the composition and/or methods are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted cycloalkyl, aryl or heterocyclic radical through the intermediary of a group selected from a lower-alkylene radical, a monoketo lower-alkylene radical or a hydroxy-lower-alkylene radical, or a bivalent radical of the formula --NH.CO.(CH.sub.2).sub.n -- where n is 1, 2 or 3, ##STR1## or --0-(lower-alkylene)--. The piperidine ring is further substituted by an acylamino residue.
Type:
Grant
Filed:
April 2, 1975
Date of Patent:
June 14, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
John Frederick Cavalla, John Leheup Archibald
Abstract: The invention relates to thioureas which are derivatives of organic nitrogen compounds containing a pyridine ring to which is fused a saturated nitrogen containing ring which carries on its nitrogen atom a thioamide or substituted thioamide group. The compounds are anti-ulcer agents or intermediates therefor.
Abstract: Lactone esters of formula ##STR1## in which X is chloro, bromo or lower alkyl and Y is ##STR2## are disclosed. The lactone esters possess antihyperlipoproteinemic activity. Methods for the preparation and use, as well as pharmaceutical compositions of the lactone esters, also are disclosed.
Abstract: A group of benz[g]indolyl compounds useful in the treatment of disorders and diseases of the cardiovascular system is described. These are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted benz[g]indolyl radical through the intermediary of a lower-alkylene radical. The piperidine rings are further substituted by an acylamino residue.
Type:
Grant
Filed:
November 15, 1974
Date of Patent:
June 7, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
John Frederick Cavalla, John Leheup Archibald
Abstract: A group of heterocyclic compounds useful in the treatment of disorders and diseases of the cardiovascular system is described. These compounds are piperidine compounds linked by the nitrogen atom to a halogen-substituted or unsubstituted phenyl radical through the intermediary of a ##STR1## GROUP WHEREIN N IS AN INTEGER FROM 1 TO 4, AND Ar represents phenyl or halophenyl. The piperidine rings are further substituted by a benzamido residue.
Type:
Grant
Filed:
April 20, 1976
Date of Patent:
June 7, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
John Frederick Cavalla, John Leheup Archibald
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.