Patents Assigned to John Wyeth & Brother Limited
  • Anti-ulcer treatment method
    Patent number: 4288439
    Abstract: A method for treating ulcers or hypersecretion is described employing an anti-ulcer agent of formula I. Accordingly the invention provides a method for treating ulcers or hypersecretion in a mammal which comprises administering to said mammal an effective amount of an anti-ulcer agent of formula I ##STR1## wherein R is alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 12 carbon atoms, R.sup.1 is hydrogen or alkyl of 1 to 6 carbon atoms, Z.sup.- is an anion selected from halide, lower alkyl- and arylsulphonate and the R and R.sup.1 radicals may be the same or different, and A represents a methylene or ethylene radical optionally substituted by alkyl of 1 to 6 carbon atoms, oxo or hydroxy and S is sulphur.Anti-ulcer compositions comprising a compound of formula I and a pharmaceutical carrier are also described.
    Type: Grant
    Filed: November 29, 1979
    Date of Patent: September 8, 1981
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Piperidino ureas and thioureas
    Patent number: 4281132
    Abstract: Compounds of formula ##STR1## in which X represents oxygen or sulphur;Y represents --CHOH-- or ##STR2## Z represent ##STR3## or a direct bond; R represents cycloalkyl group having 5 to 7 carbon atoms or an optionally substituted aryl or heteroaryl radical, or when --Z-- is a direct bond R also represents hydrogen;R.sup.1 represents hydrogen or lower alkyl;R.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy; andR.sup.3 represents hydrogen or lower alkyl, and a pharmaceutically acceptable acid addition or quarternary ammonium salts thereof, are disclosed which possess hypotensive activity.
    Type: Grant
    Filed: October 24, 1978
    Date of Patent: July 28, 1981
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Amide derivatives
    Patent number: 4278685
    Abstract: Novel amides of formula ##STR1## wherein R.sup.1 and R.sup.2 are each halogen, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl, R.sup.5 and R.sup.6 are each hydrogen or lower alkyl and n is an integer of from 1 to 3 inclusive, are anti-ulcer agents which possess anti-secretory activity.
    Type: Grant
    Filed: November 8, 1978
    Date of Patent: July 14, 1981
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Novel pyridine derivatives
    Patent number: 4272628
    Abstract: New 4-pyridinamine derivatives having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, [wherein one of R.sup.1 and R.sup.2 is aryl or heteroaryl, the other of R.sup.1 and R.sup.2 is lower alkyl, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl, and n is 0 or 1] are described. They show CNS activity and may used as antidepressant drugs. N-([.alpha.-Phenyl]-n-propyl)-4-pyridinamine also shows anti-ulcer activity.
    Type: Grant
    Filed: June 22, 1979
    Date of Patent: June 9, 1981
    Assignee: John Wyeth & Brother Limited
    Inventors: Edwin T. Edington, Alan C. White
  • 4-Pyridinamine derivatives
    Patent number: 4243808
    Abstract: Novel 4-pyridinamine derivatives having the formula ##STR1## and their pharmaceutically acceptable acid addition salts (wherein A is C.sub.1 to C.sub.4 alkylene, each of B.sub.1 and B.sub.2, together with the two carbon atoms joined thereto, forms arylene or heteroarylene, R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl and n is 0 or 1) are described. They show CNS activity and may be used as anti-depressant drugs.
    Type: Grant
    Filed: June 22, 1979
    Date of Patent: January 6, 1981
    Assignee: John Wyeth & Brother Limited
    Inventors: Edwin T. Edington, Alan C. White
  • .beta.Adrenergic blocking piperidino ureas and thioureas
    Patent number: 4235915
    Abstract: Compounds of formula ##STR1## in which X represents oxygen or sulphur;Y represents --CHOH-- or ##STR2## Z represents ##STR3## or a direct bond; R represents cycloalkyl group having 5 to 7 carbon atoms or an optionally substituted aryl or heteroaryl radical, or when --Z-- is a direct bond R also represents hydrogen;R.sup.1 represents hydrogen or lower alkyl.andR.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy;ora pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which reduce heart rate or have hyperglycaemic activity.
    Type: Grant
    Filed: December 5, 1977
    Date of Patent: November 25, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward
  • Benzoquinolizines having blood pressure lowering activity, and in some instances, anti-secretory activity
    Patent number: 4235910
    Abstract: The invention concerns 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 and R represents --CXNHR.sup.3 (where X is O, S or .dbd.NH and R.sup.3 is hydrogen or lower alkyl) or --(CH.sub.2).sub.n R.sup.4 (where n is 0 or 1 and R.sup.4 is aryl). These compounds lower blood pressure. Some are also anti-ulcer agents. The compounds in which R.sup.1, R.sup.2 and R are as defined above, with the proviso that when R is phenyl, R.sup.1 and R.sup.2 are not both lower alkoxy, are novel.
    Type: Grant
    Filed: May 10, 1979
    Date of Patent: November 25, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. White, Terence J. Ward
  • 4-Aminoquinoline derivatives, useful as anti-inflammatory agents
    Patent number: 4235908
    Abstract: New 4-aminoquinoline derivatives having the formula ##STR1## wherein X is halogen or trifluoromethyl at the designated 7- or 8-position; Z is hydrogen, halogen, lower alkyl, lower alkoxy, nitro, di(lower alkyl)amino or trifluoromethyl, n is from 1 to 4, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl and A is lower alkylene, and their pharmaceutically acceptable acid addition salts show anti-inflammatory activity.
    Type: Grant
    Filed: April 9, 1979
    Date of Patent: November 25, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: John T. A. Boyle
  • 1H-Pyrrole-1-acetamide compounds and their pharmaceutical compositions
    Patent number: 4225613
    Abstract: Pyrrole derivatives of general formula (II) ##STR1## wherein R.sup.7 and R.sup.8 are the same or different and each represent hydrogen or lower alkyl, R.sup.13 and R.sup.14 are each hydrogen, lower alkyl or halogen with the proviso that at least one or R.sup.13 and R.sup.14 is halogen or (lower)alkyl, R.sup.15 and R.sup.16 are each hydrogen or lower alkyl and R.sup.17 is aryl or aryl(lower)alkyl are useful as hypotensive or antihypertensive agents.
    Type: Grant
    Filed: April 30, 1979
    Date of Patent: September 30, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Slow release pharmaceutical compositions containing 3-[2-(4-benzamido-1-piperidyl)ethyl]indole, embonate
    Patent number: 4223008
    Abstract: The invention provides a pharmaceutical composition in tablet form having an enteric coating and comprising 3-[2-(4-benzamido-1-piperidyl)ethyl]indole, embonate and a pharmaceutically acceptable carrier useful as a prolonged release antihypertensive formulation.
    Type: Grant
    Filed: May 14, 1979
    Date of Patent: September 16, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: George K. E. Gregory
  • Anti-depressant indole derivatives
    Patent number: 4209521
    Abstract: The invention concerns a compound of formula II ##STR1## or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof wherein R.sup.5 represents hydrogen, hydroxy, lower alkoxy or lower alkyl, R.sup.6 represents hydrogen or lower alkyl, and R.sup.7 represents phenyl, lower alkoxy phenyl, halophenyl, or thenyl and X represents oxygen or sulphur. These indole derivatives exhibit psychotropic activity. The invention includes a method of alleviating depression in a warm blooded animal afflicted with depression which method comprises administering to said animal an effective amount of a compound of formula II or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: November 8, 1978
    Date of Patent: June 24, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward
  • Piperidino ureas and thioureas
    Patent number: 4199590
    Abstract: Compounds of formula ##STR1## in which hal represents halogen;R represents hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sup.2 represents a subsituted or unsubstituted monocyclic heterocyclic group;and X represents oxygen or sulphur; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which have hypotensive and/or antihypertensive activity.
    Type: Grant
    Filed: August 24, 1978
    Date of Patent: April 22, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Hexahydroazepine, piperidine and pyrrolidine derivatives
    Patent number: 4197239
    Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine of formula I ##STR1## where n is 2,3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.1 is lower alkyl. The compounds may be aromatized and the aromatized compounds converted to 3,3-disubstituted-hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: April 8, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. Cavalla, Alan C. White, Robin G. Shepherd
  • Hexahydroazepine, piperidine and pyrrolidine derivatives
    Patent number: 4197241
    Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) ##STR1## where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: April 8, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. Cavalla, Alan C. White
  • Process for preparing oxazoles
    Patent number: 4190584
    Abstract: (4,5-Diaryloxazol-2-yl)propionic and butyric acids having anti-inflammatory activity had previously been prepared by esterification of aroylarylcarbinols with a reactive derivative of butanedioic and pentanedioic acids, for instance, succinic or glutaric anhydride, isolation of the keto ester so formed and cyclization of the keto ester with a nitrogen-donating cyclizing agent, for instance, ammonium acetate in acetic acid. It has now been found that the omission of the isolation of the keto ester intermediate improves the purity of the oxazole product.
    Type: Grant
    Filed: July 17, 1978
    Date of Patent: February 26, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: George O. Weston
  • Blood pressure lowering benzoquinolizines
    Patent number: 4183937
    Abstract: The invention concerns novel benzoquinolizines 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 or halogen, R.sup.3 and R.sup.4 which may be the same or different each represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or R.sup.3 and R.sup.4 together represent a tetra- or penta-methylene chain.The novel compounds of the invention lower blood pressure in warm-blooded animals.
    Type: Grant
    Filed: November 22, 1978
    Date of Patent: January 15, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Thiazole compound
    Patent number: 4183854
    Abstract: The invention relates to pharmaceutical compositions for use in treating ulcers or hypersecretion in mammals comprising a compound of formula Ia ##STR1## where Hal is a halogen atom, R.sup.1 is hydrogen or alkyl of 1-6 carbon atoms, R is hydrogen, alkyl of 1-5 carbon atoms (which may be substituted by two or more chlorine or bromine atoms), alkenyl of 2 to 5 carbon atoms, perfluoroalkyl of 1-5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms, R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or COR.sup.4 where R.sup.4 is as defined for R and R and R.sup.4 may be the same or different, and a pharmaceutically acceptable carrier.Methods of treatment of affected mammals and some novel compounds are also described.
    Type: Grant
    Filed: July 28, 1978
    Date of Patent: January 15, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Amino pyridine derivatives
    Patent number: 4180670
    Abstract: Novel 4-pyridinamine derivatives having the formula ##STR1## [where R.sup.1 and R.sup.2 are aryl or heteroaryl (optionally linked together by a lower alkylene bridge) or one of R.sup.1 and R.sup.2 is aryl or heteroaryl and the other of R.sup.1 and R.sup.2 is lower alkyl or ar(lower)alkyl, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl and n is 0 or 1] and their non-toxic acid addition salts are described. They show CNS activity and may be used as antidepressant drugs. Some also show stimulant activity.Novel intermediates having the formula ##STR2## are also described.
    Type: Grant
    Filed: January 30, 1978
    Date of Patent: December 25, 1979
    Assignee: John Wyeth & Brother Limited
    Inventors: Edwin T. Edington, Alan C. White
  • Process for preparing 3-[(benzamidopiperid-1-yl)alkyl] indoles
    Patent number: 4162252
    Abstract: The invention provides a new process for preparing indoles in which a 4-acylamido-1-[3-indolyl-alylene] pyridinium compound or a corresponding tetrahydropyridine compound is reduced with alkali metal borohydride in special solvents to give a corresponding piperidine compound.
    Type: Grant
    Filed: February 28, 1977
    Date of Patent: July 24, 1979
    Assignee: John Wyeth & Brother Limited
    Inventor: George O. Weston
  • Tetrahydroquinoline derivatives
    Patent number: 4160094
    Abstract: The invention relates to new tetrahydroquinoline derivatives which are intermediates useful in the preparation of anti-ulcer agents. The new derivatives have formula (I) ##STR1## wherein M is sodium, potassium or lithium, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or a lower alkyl, or a phenyl radical, and any of R.sup.4, R.sup.5 and R.sup.6 may be a gem-di-lower alkyl radical.
    Type: Grant
    Filed: February 18, 1975
    Date of Patent: July 3, 1979
    Assignee: John Wyeth & Brother Limited
    Inventors: Adrian C. W. Curran, Roger Crossley, David G. Hill