Patents Assigned to John Wyeth & Brother Ltd.
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Patent number: 4783455Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl or a mono- or bicyclic aryl or heteroaryl radical, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino, X represents--CH.sub.2 CR.sup.3 R.sup.4 CH.sub.2 --or --(CH.sub.2).sub.4 --where R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached represent a 5, 6 or 7 membered carbocyclic ring and R.sup.5 represents acyl and R.sup.6 represents hydrogen or R.sup.5 and R.sup.6 each independently represent hydrogen or lower alkyl, are useful as hypoglycaemics.Type: GrantFiled: May 22, 1987Date of Patent: November 8, 1988Assignee: John Wyeth and Brother Ltd.Inventor: Ian A. Cliffe
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Patent number: 4778802Abstract: The invention relates to compounds of formula ##STR1## or a salt thereof, wherein .dbd.X-- is .dbd.CH-- or .dbd.N--, R and R.sup.1 independently represent hydrogen, halogen or lower alkoxy and R.sup.2 is hydrogen or a substituent selected from halogen, lower alkyl, lower alkoxy or halolower alkyl which compounds exhibit psychotropic activity and are useful as antidepressants.Type: GrantFiled: November 12, 1986Date of Patent: October 18, 1988Assignee: John Wyeth & Brother, Ltd.Inventors: John L. Archibald, Terence J. Ward
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Patent number: 4758598Abstract: Solid shaped articles, particularly pharmaceutical dosage forms, are prepared by freezing in a mould a composition comprising a predetermined amount of chemical (e.g. pharmaceutical) and a solution of carrier material and then subliming solvent from the frozen composition. The side wall or walls of the mould make an angle with the vertical of at least 5.degree. at the surface of the composition. This enables shaped articles of constant thickness to be produced with minimum sublimation times.Type: GrantFiled: April 8, 1986Date of Patent: July 19, 1988Assignee: John Wyeth & Brother Ltd.Inventor: George K. E. Gregory
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Patent number: 4754597Abstract: Solid shaped articles, particularly rapidly dissolving pharmaceutical dosage forms, carrying predetermined unit quantities of chemicals are prepared by a novel process involving the addition of the predetermined amount of chemical in a solvent to a placebo article which contains a network of carrier material. The placebo article is prepared by freezing a composition of carrier material in a solvent and subliming the solvent from the frozen composition.Type: GrantFiled: March 30, 1987Date of Patent: July 5, 1988Assignee: John Wyeth & Brother Ltd.Inventors: Ian R. Buxton, Harold Feldman
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Patent number: 4666900Abstract: This invention relates to compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 independently represent hydrogen or a substituent selected from lower alkyl, lower alkoxy, halogen, alkanoyl of 2 to 7 carbon atoms, lower alkoxycarbonyl, halolower alkyl, hydroxy, cyano, amino, mono- or diloweralkyl amino, C.sub.2 -C.sub.7 alkanoylamino, carboxy, carboxylower alkyl, hydroxyloweralkyl, carbamoyl, carbamoyloxy, lower alkyl- or aryl-carbonyl, (lower alkoxy)-lower alkoxy, phenyl or a phenyl group itself optionally substituted by a substituent as hereinbefore defined excepting phenyl, or an adjacent pair of R.sup.1-4 together with the carbon atoms to which they are attached complete a six membered unsaturated carbocyclic or nitrogen containing heterocyclic ring, optionally substituted by one or more of the substituents listed above for R.sup.1 ; m represents 0 or 1; and R.sup.5, R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: March 12, 1986Date of Patent: May 19, 1987Assignee: John Wyeth & Brother Ltd.Inventors: Roger Crossley, Peter J. Meade
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Patent number: 4614663Abstract: The invention relates to novel, edible fat-containing food products adapted for human infant nutrition containing a novel fat composition. The fat composition comprises (a) palm oil; (b) an oil selected from olive oil and oleic oil; (c) an oil selected from coconut oil, babassu oil and palm kernel oil; (d) an oil selected from soybean oil, corn oil, sunflower seed oil, cotton seed oil and safflower oil, and, if desired, (e) up to 2% calculated on the weight of the fat composition, of a lecithin such as soy lecithin. The amounts of the oils are so chosen that the composition contains defined quantities of linoleic acid, oleic acid, lauric and myristic acids and palmitic and stearic acids.Type: GrantFiled: May 3, 1985Date of Patent: September 30, 1986Assignee: John Wyeth & Brother Ltd.Inventor: Arthur W. T. Rule
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Patent number: 4609748Abstract: The invention provides novel silyl reagents of Formula IR.sup.b R.sup.c R.sup.d SiNCYwherein R.sup.b is a branched chain alkyl of 3-10 carbon atoms, cycloalkyl of 4-8 carbon atoms or branched chain aralkyl of 8-12 carbon atoms and R.sup.c and R.sup.d are selected from alkyl of 1-10 carbon atoms, cycloalkyl of 4-8 carbon atoms, aralkyl of 7-12 carbon atoms or aryl with the proviso that R.sup.c and R.sup.d are not the same group as R.sup.b, and Y is oxygen or sulphur. A further novel compound tri-isopropylsilyl isothiocyanate is also included. These silyl reagents are useful in preparing tetrahydroquinoline 8-nitriles, amides and thioamides as described in Ser. No. 506,279.Type: GrantFiled: April 16, 1985Date of Patent: September 2, 1986Assignee: John Wyeth & Brother, Ltd.Inventor: Robin G. Shepherd
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Patent number: 4609655Abstract: The invention provides a compound of formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,Ar is a phenyl or naphthyl group which may be substituted or unsubstituted,R.sup.1 and R.sup.2 are the same or different and are hydrogen, alkyl, alkoxy, alkoxyalkyl, hydroxyalkyl, hydroxy, halogen, nitro, carboxy, a carboxylic alkyl ester, carbamoyl, carbamoyloxy, cyano, acyl, acylamino or trifluoromethyl, or an acid addition salt thereof.The compounds are useful for the treatment of ulcers or hypersecretion in mammals. Pharmaceutical compositions containing the novel compounds and processes for their preparation are described.Type: GrantFiled: September 6, 1985Date of Patent: September 2, 1986Assignee: John Wyeth & Brother, Ltd.Inventor: Roger Crossley
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Patent number: 4607042Abstract: This invention concerns the use in the treatment or prevention of atherosclerotic disorders and/or coronary heart disease of compounds of formula ##STR1## represents a ring system of formula ##STR2## wherein R.sup.1 represents hydrogen, methyl or benzyl, R.sup.2 represents hydrogen or methyl, R.sup.3 represents hydrogen or methoxy, R.sup.5 represents phenyl, 3-indolyl, 2-furyl, diphenylmethyl, benzyloxy, or phenyl monosubstituted by chlorine, bromine, lower alkyl, carboxy, methylenedioxy, trifluoromethyl or phenyl, or represents phenyl substituted up to three times by lower alkoxy, A represents an ethylene or a 1-oxoethylene biradical, and Z is an oxo- group or, when A is ethylene and R.sup.5 is phenyl, may also represent two hydrogen atoms, and X is an anion of a pharmaceutically acceptable acid.Type: GrantFiled: February 25, 1985Date of Patent: August 19, 1986Assignee: John Wyeth & Brother Ltd.Inventor: Vanessa Pierce
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Patent number: 4593111Abstract: The invention concerns novel compounds of formula IIIAR.sub.x.sup.a Si(NCS).sub.4-x IIIAwherein R.sup.a is selected from electron donating substituents consisting of alkoxy of 1-10 carbon atoms, cycloalkoxy of 4-8 carbon atoms, aralkoxy of 7-12 carbon atoms, phenoxy which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, the group R.sup.b R.sup.c N-wherein R.sup.b and R.sup.c are selected from alkyl of 1-6 carbon atoms, cycloalkyl of 4-6 carbon atoms, phenyl which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, and aralkyl of 7-12 carbon atoms or R.sup.b and R.sup.Type: GrantFiled: May 24, 1985Date of Patent: June 3, 1986Assignee: John Wyeth & Brother Ltd.Inventor: Roger Crossley
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Patent number: 4577022Abstract: The invention provides new silyl derivatives of 5,6,7,8-tetrahydroquinolines and related compounds. The tetrahydroquinolines are substiuted at the 8-position by the group SiR.sub.3 where R may be one of various hydrocarbon groups or an electron donating substituent. The 8-position may also carry a lithium, sodium or potassium atom. The new silyl derivatives may be prepared by treating a corresponding 8-lithio, sodio or potassio tetrahydroquinoline with a silyl halide R.sub.3 SiHal followed by a metal compound R*M where M is sodium, potassium or lithium and R* is alkyl, cycloalkyl, aralkyl or aryl or an amine residue. The new silyl derivatives are useful intermediates for the preparation of known 5,6,7,8-tetrahydroquinline-8-nitriles, amides and thioamides employing an alkyl silyl isothiocyanate or cyanate. The nitriles and thioamides are anti-ulcer agents. The related compounds may be made by analogous methods.Type: GrantFiled: June 21, 1983Date of Patent: March 18, 1986Assignee: John Wyeth & Brother, Ltd.Inventors: Roger Crossley, Robin G. Shepherd
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Patent number: 4576955Abstract: The invention provides a compound of the formula I ##STR1## wherein Y is a heterocyclic radical of formula ##STR2## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkoxy, halogen, formyl, phenyl, phenylalkyl, halophenyl, or acetal [CH(OR.sup.4).sub.2 where R.sup.4 is lower alkyl or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, the dotted lines in formula V represent an optional double bond in one of the indicated positions, A is a saturated or unsaturated alkylene radical having from 1 to 6 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and R.sup.3 is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms and Z.sup.- is an anion, and acid addition salts thereof, with the provisos that (1) when more than one R.sup.1 radical is present in the molecule then the R.sup.Type: GrantFiled: October 13, 1983Date of Patent: March 18, 1986Assignee: John Wyeth & Brother, Ltd.Inventors: Roger Crossley, Kay H. Dickinson
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Patent number: 4547510Abstract: This invention concerns compounds of formula ##STR1## and acid addition salts thereof, wherein R represents lower alkoxy, alkanoyloxy of 2 to 7 carbon atoms or hydroxy;R.sup.1 and R.sup.2 independently represent hydrogen, lower alkoxy, alkanoyloxy of 2 to 7 carbon atoms, hydroxy or lower alkyl;R.sup.3, R.sup.4 and R.sup.5 each represent hydrogen or lower alkyl with the proviso that at least one of R.sup.3, R.sup.4 and R.sup.5 is lower alkyl;and R.sup.6 and R.sup.7 each represent hydrogen or lower alkyl which possess anti-ulcer activity.Type: GrantFiled: April 12, 1984Date of Patent: October 15, 1985Assignee: John Wyeth & Brother Ltd.Inventor: Roger Crossley
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Patent number: 4474782Abstract: Morpholine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts possess analgesic and/or opiate antagonistic activity. In the formula R.sup.1 represents lower alkyl; R.sup.2 represents hydrogen, lower alkyl or (lower)alkoxymethyl; R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R.sup.4 represents a lower alkenyl or lower alkynyl group containing at least 3 carbon atoms and in which there is no unsaturated bond in the 1-position.Type: GrantFiled: February 24, 1984Date of Patent: October 2, 1984Assignee: John Wyeth & Brother, Ltd.Inventors: Alan C. White, Edwin T. Edington
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Patent number: 4451465Abstract: 2,3,4,10-Tetrahydro-3,3-dimethyl-10-phenylpyrimido[1,2-a]indol-10-ol and the pharmaceutically acceptable acid addition salts thereof are useful in treatment or preventing obesity in mammals. The compounds may be administered in pharmaceutical compositions, optionally with one or more vitamins.Type: GrantFiled: June 22, 1982Date of Patent: May 29, 1984Assignee: John Wyeth & Brother Ltd.Inventors: Alan C. White, Michael G. Wyllie
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Patent number: 4427676Abstract: The invention provides novel thiomorpholines of the formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts wherein n represents 0 or 1, R.sup.1 represents (lower)alkyl, R.sup.2 represents hydrogen or (lower)alkyl, R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R.sup.4 represents hydrogen, hydroxy, acyloxy or a protected hydroxy group, with the proviso that when n is 0, R.sup.4 is other than hydrogen. The compounds in which n is 0 and R.sup.4 is lower alkoxy, hydroxy or acyloxy are analgesics and/or opiate antagonists and the compounds in which n is 1 and R.sup.4 is hydrogen are hypotensives or anti-hypertensives. The other compounds of formula (I) are intermediates for the pharmacologically active compounds.Type: GrantFiled: December 14, 1981Date of Patent: January 24, 1984Assignee: John Wyeth & Brother Ltd.Inventors: Alan C. White, Michael M. Hann
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Patent number: 4426387Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.Type: GrantFiled: April 7, 1982Date of Patent: January 17, 1984Assignee: John Wyeth & Brother Ltd.Inventors: John L. Archibald, Terrence J. Ward
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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: 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: 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