Patents by Inventor John L. Archibald
John L. Archibald has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5212179Abstract: The invention concerns the preparation of 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 a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 25, 1990Date of Patent: May 18, 1993Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 5068337Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A represents a group of formula --XR.sup.3 whereinX is (i) a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q --or (ii) a group of formula --(CHR.sup.6).sub.r --O--(CHR.sup.7).sub.qin which formulae: Y represents --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 providing that p and q do not both represent 0, 1 or 2 and the other is zero; R.sup.6, R.sup.7 and R.sup.8 independently represent hydrogen or lower alkyl, and R.sup.Type: GrantFiled: November 13, 1986Date of Patent: November 26, 1991Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 5064842Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein:.alpha. and .beta. together represent a bond and additionally when B is an electron withdrawing group .alpha. can also represent OH and .beta. can represent hydrogen;Ar is an optionally substituted aryl or heteroaryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optioanlly substituted aryl or heteroaryl;A represents a group of formula --XR.sup.3 wherein X is a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q -- in which formula: Y represents --O--, --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: June 25, 1990Date of Patent: November 12, 1991Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 4985438Abstract: The invention concerns the preparation of 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 a substitutent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 19, 1988Date of Patent: January 15, 1991Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4900750Abstract: This invention concerns compounds of formula ##STR1## or salts thereof, wherein: Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl, aralkyl, or aryl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A and B independently represent a group of formula --XR.sup.3 whereinX is a group of formula --(CHR.sup.6).sub.p Y(CHR.sup.7).sub.q --whereinY represents --O--, --S--, --NR.sup.8 -- or a direct bond; p and q each represent 0, 1 or 2 providing that p and q do not both represent O when Y is a direct bond; and R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or alkyl; and R.sup.Type: GrantFiled: August 3, 1987Date of Patent: February 13, 1990Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 4866075Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydoxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity whilst exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.Type: GrantFiled: August 12, 1988Date of Patent: September 12, 1989Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward, Janet C. White
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Patent number: 4806552Abstract: The invention concerns the preparation of 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 --NM.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 a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: November 12, 1986Date of Patent: February 21, 1989Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4801595Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydroxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity while exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.Type: GrantFiled: December 15, 1986Date of Patent: January 31, 1989Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Janet C. White
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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: 4772617Abstract: The invention concerns indole derivatives of formula I ##STR1## in which R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy,R.sub.2, R.sub.3 and R.sub.4 independently represent hydrogen or lower alkyl,A represents an alkylene, oxoalkylene or hydroxyalkylene chain each having 2 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity while exhibiting reduced CNS depressant properties.Also disclosed are methods for preparing the compounds of formula I and pharmaceutical compositions containing them.Type: GrantFiled: December 15, 1986Date of Patent: September 20, 1988Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4722930Abstract: The invention concerns the preparation of 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 a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: September 30, 1985Date of Patent: February 2, 1988Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4694012Abstract: This invention concerns a method of treatment using 1,4-dihydropyridine derivatives having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl;Y is --(CH.sub.2).sub.n --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, CN, --N(R.sup.3).sub.2, (CH.sub.2).sub.m CO.sub.2 H, (CH.sub.2).sub.m CO.sub.2 (C.sub.1 -C.sub.4 alkyl) or (CH.sub.2).sub.m CON(R.sup.3).sub.2 groups wherein each R.sup.3 is independently H or C.sub.1 -C.sub.4 alkyl and m is 0 or 1;and n is 1 to 3 when X is linked by a ring carbon atom or 2 or 3 when X is linked by a ring nitrogen atom.Type: GrantFiled: July 30, 1985Date of Patent: September 15, 1987Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 4563466Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammoniun 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 a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 26, 1983Date of Patent: January 7, 1986Inventors: John L. Archibald, Terence J. Ward
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Patent number: 4454139Abstract: The invention concerns benzoquinolizines of formula ##STR1## and their acid addition salts. In the formula R.sup.7 is lower alkyl or a phenyl or naphthyl radical optionally substituted with specified substituents and R.sup.8 is methyl or ethyl. The compounds possess high .alpha..sub.2 (presynaptic) adrenoceptor antagonistic activity and a good .alpha..sub.2 /.alpha..sub.1 antagonistic selectivity.Type: GrantFiled: September 9, 1982Date of Patent: June 12, 1984Assignee: John Wyeth & Brother, LimitedInventors: Terence J. Ward, John L. Archibald
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Patent number: 4447604Abstract: Thiazolotriazine derivatives having the formula I ##STR1## their pharmaceutically acceptable salts, pharmaceutically acceptable triazolotriazinium compounds containing the cation having formula II ##STR2## and their zwitterionic forms and pharmaceutically acceptable acid addition salts [where A is hydroxy whilst B is hydrogen or A and B together represent a direct bond; R.sup.1 is aryl; R.sup.2 and R.sup.3 are independently lower alkyl or ar(lower)alkyl] are novel compounds useful as anti-cancer agents.Type: GrantFiled: April 1, 1982Date of Patent: May 8, 1984Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, John T. A. Boyle
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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: 4357333Abstract: The disclosure describes new 4-aminoquinoline derivatives of general formula ##STR1## and their pharmaceutically acceptable acid addition salts, where X is trifluoromethyl or halogen, Z is hydrogen or a defined substituent and R is a group having one of the formulae ##STR2## where 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. The new 4-aminoquinoline derivatives show analgesic activity and, in some cases, anti-inflammatory activity.Type: GrantFiled: August 11, 1980Date of Patent: November 2, 1982Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, John T. A. Boyle
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Patent number: 4235915Abstract: 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: GrantFiled: December 5, 1977Date of Patent: November 25, 1980Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4209521Abstract: 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: GrantFiled: November 8, 1978Date of Patent: June 24, 1980Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4177279Abstract: 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: GrantFiled: July 21, 1975Date of Patent: December 4, 1979Assignee: John Wyeth & Brother Ltd.Inventors: John L. Archibald, John L. Jackson