Patents Assigned to Wyeth
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Patent number: 4337259Abstract: The invention relates to a pharmaceutical composition comprising an anti-ulcer effective amount of a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl, or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or lower alkoxy, R.sup.2 represents hydrogen, chlorine or trifluoromethyl and n is 1 or 2, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable carrier.A method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula I is also disclosed. Some compounds of formula I are novel and within the scope of the invention.Type: GrantFiled: February 9, 1981Date of Patent: June 29, 1982Assignee: John Wyeth & Brother LimitedInventor: Roger Crossley
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Patent number: 4332822Abstract: Novel cyanoguanidine derivatives having the formula ##STR1## wherein Ar is a phenyl or pyrrol-1-yl group substituted by one or more substituents selected from halogen, trifluoromethyl, lower alkyl, lower alkoxy and nitro and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen or lower alkyl or R.sub.1 and R.sub.2 taken together form dimethylene or trimethylene, lower blood pressure and, in some cases are also anti-ulcer agents.Type: GrantFiled: January 30, 1981Date of Patent: June 1, 1982Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4331673Abstract: The invention concerns compounds of formula ##STR1## wherein the sulphur is bonded to the pyridinium ring at position 2 or 4, Y is --S-- or --CH.sub.2 --, R represents hydrogen, or a lower alkyl group, or other carboxylic protecting group; R.sup.1 represents hydrogen or lower alkyl; R.sup.2 represents lower alkyl, aryl of 6 to 10 carbon atoms or aralkyl of 7 to 11 carbon atoms; R.sup.3 represents hydrogen or a substituent selected from lower alkyl, halogen and lower alkoxy; q and r are each 1 or 2; and X.sup..crclbar. represents a halide ion or an organosulphonate ion, which are antihypertensive agents and are useful as intermediates to captopril and analogous compounds.Type: GrantFiled: April 16, 1981Date of Patent: May 25, 1982Assignee: John Wyeth & Brother LimitedInventor: Roger Crossley
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Patent number: 4330546Abstract: 3-Aryl-3-aryloxyalkylamines of the general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl or benzyl, Ar is phenyl optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups, and Ar.sup.1 is methylsulphinyl, methylsulphonyl- or cyano-substituted phenyl, 2- or 4-pyridyl, 2-pyrazinyl, 2-quinolinyl, 2-thienyl or 2-thiazolyl exhibit activity on the central nervous system, e.g. as antidepressants.Type: GrantFiled: September 3, 1980Date of Patent: May 18, 1982Assignee: John Wyeth & Brother LimitedInventor: Robin G. Shepherd
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Patent number: 4328232Abstract: The invention concerns benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein the ##STR2## linkage represents a single bond linkage of formula ##STR3## or a double bond linkage of formula ##STR4## 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, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, di(lower)alkylamino or trifluoromethyl and X is O, S or NH. The compounds possess anti-secretory activity.Type: GrantFiled: October 27, 1980Date of Patent: May 4, 1982Assignee: John Wyeth & Brother LimitedInventors: Terence J. Ward, John F. White
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Patent number: 4327102Abstract: The invention provides a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or fluorine, R.sup.2 represents hydrogen, fluorine, chlorine or trifluoromethyl, n is 1 or 2 or pharmaceutically acceptable acid addition salt thereof.Pharmaceutical compositions containing the compounds are also covered as are methods of treating ulcers or hypersecretion using the compounds. Corresponding thiocompounds, useful as intermediates, are also disclosed.Type: GrantFiled: February 9, 1981Date of Patent: April 27, 1982Assignee: John Wyeth & Brother LimitedInventor: Roger Crossley
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Patent number: 4325953Abstract: 4-Aryl-4-aryloxypiperidines of the general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl or benzyl, Ar is phenyl optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups and Ar.sup.1 is a phenyl radical optionally substituted by one or more cyano, methylsulphinyl, methylsulphonyl, lower alkoxy, trifluoromethyl, lower alkyl, lower alkenyl, halogen, nitro, amino or acylamino groups or an aromatic heterocyclic mono- or di-cyclic radical, exhibit activity on the central nervous system, e.g. as antidepressants.Type: GrantFiled: September 3, 1980Date of Patent: April 20, 1982Assignee: John Wyeth and Brother LimitedInventor: Robin G. Shepherd
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Patent number: 4318909Abstract: Novel benzoxazocines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 represents hydrogen, or one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro, amino acylamino, mono- or di- (lower)alkyl-amino or cyano substituents, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together represent --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, R.sup.5 represents hydrogen, lower alkyl, phenyl (lower)alkyl or cycloalkyl (lower)alkyl, and Ar is a phenyl radical optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups exhibit activity on the central nervous system, particularly as antidepressants. The compounds can be prepared from novel alcohols of formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Ar are as defined above and X is fluorine, chlorine or bromine.Type: GrantFiled: December 8, 1980Date of Patent: March 9, 1982Assignee: John Wyeth & Brother LimitedInventors: Alan C. White, Robin G. Shepherd
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Patent number: 4305502Abstract: The invention relates to packages containing shaped articles carrying chemicals, particularly to pharmaceutical dosage forms carrying pharmaceuticals. The shaped articles, which disintegrate rapidly in water are contained in depressions in sheets of filmic material and are enclosed by a covering sheet adhering to the filmic material. The shaped articles may be formed in the depressions by a sublimation process.Type: GrantFiled: July 14, 1978Date of Patent: December 15, 1981Assignee: John Wyeth & Brother LimitedInventors: George K. E. Gregory, David S. S. Ho
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Patent number: 4304781Abstract: The invention concerns the treatment of ulcers and hypersecretion in a mammal using compounds of the formula IAr--A--S--Y Iwhere Ar is phenyl, which may be substituted or cycloalkyl of 5 to 7 carbon atoms, A is saturated or unsaturated lower alkylene which may be substituted by lower alkyl, oxo or hydroxy, S is sulphur and Y is an optionally substituted pyridine, pyridinium, tetrahydropyridine or tetrahydropyridinium radical. Certain novel compounds and pharmaceutical compositions are also disclosed.Type: GrantFiled: July 21, 1980Date of Patent: December 8, 1981Assignee: John Wyeth & Brother LimitedInventor: Roger Crossley
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Patent number: 4296029Abstract: 2-Oxo-hexahydroazepine, -piperidine or pyrrolidines of formula ##STR1## wherein n is 2,3 or 4, R is hydrogen, lower alkyl, aryl(lower)alkyl, loweralkenylmethyl or cycloalkylmethyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl are prepared by a novel process involving reaction of an anion of a lactam of formula ##STR2## where R.sup.3 is lower alkyl, aryl(lower)alkyl, trialkyl-, triaryl- or triarylalkyl-silyl with a benzyne of formula ##STR3## where R.sup.4 is lower alkyl, aryl(lower)alkyl or trialkyl-, triaryl- or triarylalkyl-silyl. The products are useful as intermediates for preparing pharmacologically active 2-unsubstituted -hexahydroazepine, -piperidine and pyrrolidine derivatives.Type: GrantFiled: June 23, 1980Date of Patent: October 20, 1981Assignee: John Wyeth & Brother LimitedInventors: Brian J. Bushell, John F. Cavalla, Robin G. Shepherd, Alan C. White
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Patent number: 4291042Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable acid addition or quaternary ammonium salts thereof wherein the piperidine ring is substituted in the 3 or 4 position; X represents .dbd.CH-- or .dbd.N--; Y represents --NR.sup.5 --, --O-- or --S-- wherein R.sup.5 is hydrogen or lower alkyl; A is lower alkylene or hydroxy lower alkylene, Z and Z.sup.1 independently represent ##STR2## Z may also represent --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CHMe-- or --CMe.sub.2 --; R.sup.1, R.sup.2, R.sup.3 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, trifluoromethyl, lower-alkanoylamino, hydroxy or aryl lower alkoxy; or R.sup.1 and R.sup.2 when adjacent together with the carbons to which they are attached form a six membered carbocyclic ring; and R.sup.4 represents hydrogen or lower alkyl, are disclosed which possess psychotropic activity and are useful as anti-depressants.Type: GrantFiled: January 21, 1980Date of Patent: September 22, 1981Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4288439Abstract: 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: GrantFiled: November 29, 1979Date of Patent: September 8, 1981Assignee: John Wyeth & Brother LimitedInventor: Roger Crossley
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Patent number: 4281132Abstract: 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: GrantFiled: October 24, 1978Date of Patent: July 28, 1981Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4278685Abstract: 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: GrantFiled: November 8, 1978Date of Patent: July 14, 1981Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4272628Abstract: 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: GrantFiled: June 22, 1979Date of Patent: June 9, 1981Assignee: John Wyeth & Brother LimitedInventors: Edwin T. Edington, Alan C. White
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Patent number: 4271304Abstract: Pyridine derivatives having the formula ##STR1## and their N-oxides and pharmaceutically acceptable acid addition salts, wherein R.sup.1 and R.sup.2 are independently aryl, R.sup.3 is hydrogen or lower alkyl and n is 0, 1 or 2, have CNS activity and may be used as antidepressants.Type: GrantFiled: May 9, 1979Date of Patent: June 2, 1981Assignee: John Wyeth & Brother, Ltd.Inventors: Edwin T. Edington, Alan C. White
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Patent number: 4248876Abstract: The invention concerns novel piperidine derivatives of the formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 represents (lower)alkyl, R.sup.2 represents a phenyl group optionally substituted by one or more (lower)alkyl, (lower)alkoxy, halogen, amino, (lower)alkylamino, di(lower)alkylamino or trifluoromethyl substituents and X represents=O; ##STR2## [where R.sup.3 and R.sup.4 both represent hydrogen, both represent the same (lower)alkyl or one is hydrogen and the other is (lower)alkyl or R.sup.3 and R.sup.4 together represent an alkylene group such that the ##STR3## is a cyclic ketal group containing 2 or 3 carbon atoms]; or ##STR4## [where OR is hydroxy, etherified hydroxy or esterified hydroxy]. The compounds possess anti-depressant activity.Type: GrantFiled: January 3, 1978Date of Patent: February 3, 1981Assignee: John Wyeth & Brother Ltd.Inventor: Alan C. White
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Patent number: 4249012Abstract: The invention relates to the use of thiazoles in the treatment of ulcers and/or hypersecretion in mammals. The invention also provides in a preferred aspect a pharmaceutical composition for use in the treatment of ulcers or hypersecretion comprising a compound of formula I ##STR1## where R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, or phenyl, R is hydrogen, n-alkyl of 1-4 carbon atoms (which may be substituted by chlorine), or cyclopropyl, R.sup.3 is hydrogen 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.Type: GrantFiled: May 15, 1978Date of Patent: February 3, 1981Assignee: John Wyeth & Brother Ltd.Inventor: Roger Crossley
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Patent number: 4243808Abstract: 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: GrantFiled: June 22, 1979Date of Patent: January 6, 1981Assignee: John Wyeth & Brother LimitedInventors: Edwin T. Edington, Alan C. White