Patents Represented by Attorney Arthur E. Wilfond
  • Patent number: 4127660
    Abstract: New thiazolotriazines having the formula ##STR1## (where R.sup.1 is aryl and R.sup.2 is ar(lower)alkyl, lower alkyl or lower alkenyl) and their pharmaceutically acceptable acid addition salts are described. The corresponding thiazolotriazinium compounds comprising a cation having the formula ##STR2## (where R.sup.1 and R.sup.2 are as explained above and R.sup.3 is ar(lower)alkyl, lower alkyl or lower alkenyl) and a pharmaceutically acceptable anion are also described. The compounds are indicated for use as anti-ulcer agents.
    Type: Grant
    Filed: December 16, 1977
    Date of Patent: November 28, 1978
    Assignee: John Wyeth & Brother Limited
    Inventor: John T. A. Boyle
  • Patent number: 4126683
    Abstract: The invention concerns novel fused ring indole derivatives of the formula ##STR1## and the pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein n represents 1 or 2 and R.sup.1 represents hydrogen, hydroxyl, lower alkyl, lower alkoxy, trifluoromethyl, halogen, amino or mono- or di-(lower)alkylamino. The compounds are useful as anti-depressant agents.
    Type: Grant
    Filed: June 8, 1977
    Date of Patent: November 21, 1978
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Robert F. Sugden
  • Patent number: 4105778
    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 ; Y is O or NR.sup.
    Type: Grant
    Filed: September 8, 1977
    Date of Patent: August 8, 1978
    Assignee: Ayerst, McKenna & Harrison, Ltd.
    Inventors: Adolph H. Philipp, Ivo L. Jirkovsky
  • Patent number: 4105666
    Abstract: (Aroylamino)-1-(aroyloxyalkyl)piperidines having the formula ##STR1## WHERE Ar.sup.1 and Ar.sup.2 are aryl (including heteroaryl) groups and n is from 2 to 6, and their pharmaceutically acceptable acid addition salts are described. The piperidine derivatives show hypotensive activity.
    Type: Grant
    Filed: July 13, 1977
    Date of Patent: August 8, 1978
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Patent number: 4105773
    Abstract: The invention provides a compound of formula I, ##STR1## wherein R is hydrogen, alkyl of 1-6 carbon atoms, or COR.sup.3 where R.sup.3 is hydrogen, alkyl of 1-5 carbon atoms, alkenyl of 2 to 5 carbon atoms, alkynyl of 2 to 5 carbon atoms, or cycloalkyl of 3 to 5 carbon atoms, R.sup.1 is hydrogen or alkyl of 1-6 carbon atoms, R.sup.2 is alkyl of 1-6 carbon atoms and R.sup.3 is as above defined.The compounds are intended for use in the treatment of ulcers or hypersecretion in mammals.
    Type: Grant
    Filed: May 23, 1977
    Date of Patent: August 8, 1978
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, David G. Hill
  • Patent number: 4105771
    Abstract: This invention relates to compounds having the formula ##STR1## and the pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R represents phenyl or phenyl substituted by halogen, lower alkyl, hydroxy, trifluoromethyl or lower alkoxy; n represents 0 or 1 and m represents 2 or 3 with the proviso that n plus m equals 3; and R.sup.1 represents phenyl, thienyl, pyridyl, furyl, indolyl or phenyl substituted by halogen, lower alkyl, lower alkoxy, trifluoromethyl or hydroxy, which exhibit antihypertensive activity in warm blooded animals.
    Type: Grant
    Filed: June 9, 1977
    Date of Patent: August 8, 1978
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Wart
  • Patent number: 4095025
    Abstract: The invention concerns diarylpyrazole lower alkanoic acids and derivatives which are pharmacologically efficacious as anti-inflammatory agents. The said compounds can be represented by the formula ##STR1## in which one of D, E, F and G represents hydrogen, one is a lower aliphatic acid radical or derivative thereof and the remaining two of D, E, F and G are aryl or heteroaryl radicals.
    Type: Grant
    Filed: November 30, 1971
    Date of Patent: June 13, 1978
    Assignee: John Wyeth & Brother Limited
    Inventor: Robert Anthony Newberry
  • Patent number: 4092320
    Abstract: The invention relates to N-acyl thioureas which are derivatives of 1,5-Naphthyridines. The compounds are intermediates for anti-ulcer agents.
    Type: Grant
    Filed: April 7, 1977
    Date of Patent: May 30, 1978
    Assignee: John Wyeth & Brother Limited
    Inventor: Adrian Charles Ward Curran
  • Patent number: 4092317
    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 and lower alkyl. Compounds of formula I are intermediates for pharmaceuticals.
    Type: Grant
    Filed: September 5, 1975
    Date of Patent: May 30, 1978
    Assignee: John Wyeth & Brother Limited
    Inventor: Adrian Charles Ward Curran
  • Patent number: 4092418
    Abstract: The invention relates to thioureas which are derivatives of 1,5-Naphthyridines. The compounds are anti-ulcer agents or intermediates therefor.
    Type: Grant
    Filed: April 7, 1977
    Date of Patent: May 30, 1978
    Assignee: John Wyeth & Brother Limited
    Inventor: Adrian Charles Ward Curran
  • Patent number: 4085110
    Abstract: The invention relates to novel cyclopentena[b,e]pyridine derivatives which have a thioamide group in the 7-position. The compounds are anti-ulcer agents.
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: April 18, 1978
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: Adrian Charles Ward Curran, Roger Crossley, David George Hill
  • Patent number: 4085215
    Abstract: The invention relates to novel pyridine derivatives which have a fused 5,6, or 7-membered saturated hydrocarbon ring adjacent to the nitrogen of the pyridine ring, and a group X situated on said hydrocarbon ring and separated by one carbon atom from the pyridine nitrogen atom, said group X is cyano, CONHR.sup.3, CSNHR.sup.3 or CO.sub.2 R.sup.5 wherein R.sup.3 is selected from hydrogen, lower alkyl and lower aralkyl radicals and R.sup.5 is selected from hydrogen, lower alkyl and lower aralkyl radicals which may be substituted by alkyl, alkoxy, halogen, nitro or trifluoromethyl; other substituents may be present. Compounds wherein X is CSNHR.sup.3 are anti-ulcer agents and the other compounds are intermediates therefor.
    Type: Grant
    Filed: July 30, 1975
    Date of Patent: April 18, 1978
    Assignee: John Wyeth & Brother Ltd.
    Inventors: Adrian Charles Ward Curran, Roger Crossley, David George Hill
  • Patent number: 4085108
    Abstract: The invention relates to novel silicon derivatives of tetrahydroquinolines, which are intermediates in a process for preparing 5,6,7,8-tetrahydroquinoline-8-carboxamides and thiocarboxamides.
    Type: Grant
    Filed: September 8, 1976
    Date of Patent: April 18, 1978
    Assignee: John Wyeth & Brother Ltd.
    Inventors: Adrian Charles Ward Curran, Robin Gerald Shepherd
  • Patent number: 4076820
    Abstract: The invention relates to novel benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 and R.sup.2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents hydrogen, lower alkyl or aryl and R.sup.4 represents --SO.sub.2 R.sup.5 (where R.sup.5 is lower alkyl or aryl, --CONH.sub.2 or --CXNHR.sup.6 (where X is oxygen or sulphur and R.sup.6 is aryl or aryl.CO.--). The compounds have hypotensive activity.
    Type: Grant
    Filed: May 13, 1976
    Date of Patent: February 28, 1978
    Assignee: John Wyeth & Brother, Limited
    Inventors: John Leheup Archibald, John Lambert Jackson
  • Patent number: 4073906
    Abstract: The invention relates to pyrimido 1,2-b!isoquinolines of the formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula, R.sup.1 and R.sup.2 each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, trifluoromethyl, halogen, amino or mono- or di-(lower)alkylamino and R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl. The compounds have utility as anti-gastric ulcer agents.
    Type: Grant
    Filed: November 5, 1975
    Date of Patent: February 14, 1978
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Robin M. Black
  • Patent number: 4062869
    Abstract: A process for preparing tryptophol derivatives comprises reducing a 3-indolylglyoxylic acid ester or acid halide using an alkali metal borohydride in the presence of an alcohol or ether solvent. The tryptophol derivatives prepared are useful as intermediates to pharmacologically active compounds.
    Type: Grant
    Filed: June 3, 1976
    Date of Patent: December 13, 1977
    Assignee: John Wyeth & Brother Limited
    Inventor: George Oliver Weston
  • Patent number: 4061641
    Abstract: The invention provides compounds of general formula I ##STR1## and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R represents hydrogen or lower alkyl, R.sup.1 represents hydrogen or lower alkyl, R.sup.2 represents hydrogen or lower alkyl, R.sup.3 represents hydrogen, halogen, lower alkoxy, hydroxy, or lower alkyl, R.sup.4 represents hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, thienyl, furyl, phenyl; phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy or trifluoromethyl; or benzoyl, halobenzoyl, lower alkanoyl, cycloalkanoyl of 6 to 8 carbon atoms, or thienoyl, A represents an alkylene, mono- or diketo- or hydroxy-alkylene radical having from 1 to 5 carbon atoms and X is oxygen or sulphur.The compounds exhibit action on the cardiovascular system particularly hypotensive and/or anti-hypertensive activity.
    Type: Grant
    Filed: July 15, 1976
    Date of Patent: December 6, 1977
    Assignee: John Wyeth & Brother Limited
    Inventors: John Leheup Archibald, John Lambert Jackson
  • Patent number: 4061758
    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 monosubstituted by defined substituents or a di(loweralkyl) amino (loweralkoxy) carbonyl group and R is a phenyl group which may be substituted by defined substituents. Pharmaceutical compositions having hypotensive activity or central nervous system activity comprise a non-toxic carrier and an effective amount of such a compound.
    Type: Grant
    Filed: February 24, 1977
    Date of Patent: December 6, 1977
    Assignee: John Wyeth & Brother Limited
    Inventor: John Leheup Archibald
  • Patent number: 4061640
    Abstract: Compounds of the formula ##STR1## in which W is quinolyl or lower alkyl quinolyl;A is alkylene of 1 to 6 carbon atoms;R is phenyl, halophenyl, lower alkoxy phenyl or lower alkyl phenyl;Or a pharmaceutically acceptable acid addition salt thereof, are hypotensive and bradycardial agents.
    Type: Grant
    Filed: July 29, 1976
    Date of Patent: December 6, 1977
    Assignee: John Wyeth & Brother Limited
    Inventors: John Frederick Cavalla, John Leheup Archibald
  • Patent number: 4061754
    Abstract: The invention relates to imidazo[1,2-a]quinolines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts. In formula I R.sup.1 and R.sup.2 which may be the same or 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 R.sup.5 represents hydrogen, lower alkyl, aryl or arylloweralkyl. The compounds possess hypotensive activity.
    Type: Grant
    Filed: January 7, 1976
    Date of Patent: December 6, 1977
    Assignee: John Wyeth & Brother Limited
    Inventor: Robin Michael Black