Patents by Inventor Francis D. King
Francis D. King 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: 5637611Abstract: Use of a compound of general formula (I): ##STR1## wherein: R.sup.1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, arylC.sub.1-6 alkoxy, --CO.sub.2 R.sup.4, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n CONR.sup.5 R.sup.6, --(CH.sub.2).sub.n SO.sub.2 NR.sup.5 R.sup.6, C.sub.1-6 alkanoylamino (CH.sub.2).sub.n, or C.sub.1-6 alkylsulphonylamino (CH.sub.2).sub.n ;R.sup.4 represents hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl;R.sup.5 and R.sup.6 each independently represent hydrogen or C.sub.1-6 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a ring;n represents 0, 1 or 2; andR.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1-6 alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring;or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT.sub.Type: GrantFiled: May 15, 1995Date of Patent: June 10, 1997Assignee: SmithKline Beecham p.l.c.Inventors: Francis D. King, Laramie M. Gaster, Alberto J. Kaumann, Rodney C. Young
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Patent number: 5620992Abstract: A compound of formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X.sub.1, X.sub.2, x, Y and Z are as defined in the specification are useful in the treatment or prophylaxis of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: March 10, 1995Date of Patent: April 15, 1997Assignee: SmithKline Beecham plcInventors: Francis D. King, Laramie M. Gaster, Keith R. Mulholland
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Patent number: 5580885Abstract: The use of a compound of formula (I) or pharmaceutically acceptable salt thereof, in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein: X.sub.1 is O or S; X.sub.2 is O, S, NR or NRCO wherein R is hydrogen or C.sub.1-6 alkyl; x is 1, 2 or 3; Y is O or NH; Z is sub-formula (a), (b) or (c) in the manufacture of a medicament for use in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1994Date of Patent: December 3, 1996Assignee: SmithKline Beecham p.l.c.Inventors: Francis D. King, Laramie M. Gaster, Keith R. Mulholland, Shirley K. Rahman, Paul A. Wyman, Gareth J. Sanger, Kay A. Wardle, Gordon S. Baxter, Guy A. Kennett, Alberto J. Kauman
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Patent number: 5552398Abstract: Compounds of formula (I), ##STR1## wherein L is N or CR.sub.c, wherein R.sub.c is hydrogen, alkoxy, halo, alkyl or cyano; Q is NR.sub.1, CH.sub.2, O, or S; R.sub.a is hydrogen, halo, alkyl, amino, nitro or alkoxy; R.sub.b is hydrogen, halo, alkyl or alkoxy; R.sub.1 is hydrogen, alkyl, alkenyl, aralkyl, alkanoyl, or alkanoylalkyl; R.sub.2 is alkoxy; R.sub.3 is hydrogen, chloro or fluoro; R.sub.4 is hydrogen, alkyl, amino optionally substituted by alkyl, halo, hydroxy or alkoxy; R.sub.5 is hydrogen, halo, alkyl, alkoxy, nitro, amino or alkylthio; R.sub.6 is hydrogen, halo, alkyl, alkoxy or amino; n is 0, 1, 2, 3, or 4; p and m are independently 0, 1 or 2; and R.sub.q is hydrogen or C.sub.1-6 are 5-HT.sub.4 receptor antagonists.Type: GrantFiled: November 14, 1994Date of Patent: September 3, 1996Assignee: SmithKline Beecham p.l.c.Inventors: Francis D. King, Laramie M. Gaster, Paul A. Wyman
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Patent number: 5492919Abstract: The invention provides the use of a compound of formula (I) ##STR1## wherein A, E, F, U, X, Y, Z, are as defined in the specification, or a pharmaceutically acceptable salt thereof, for the treatment of diarrhea predominant irritable bowel syndrome.Type: GrantFiled: July 6, 1994Date of Patent: February 20, 1996Assignee: SmithKline Beecham p.l.c.Inventors: Gareth J. Sanger, Francis D. King, Gordon S. Baxter, Laramie M. Gaster, Alberto J. Kaumann, Guy A. Kennett, Keith R. Mulholland, Mythily Vimal, Kay A. Wardle, Paul A. Wyman, Rodney C. Young
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Patent number: 5464864Type: GrantFiled: December 23, 1993Date of Patent: November 7, 1995Assignee: SmithKline Beecham P.L.C.Inventors: Francis D. King, Laramie M. Gaster, Alberto J. Kaumann, Rodney C. Young
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Patent number: 5322951Abstract: An intermediate compound of Formula (V): ##STR1## wherein G is COQ.sub.1 and Q.sub.1 represents chloro, bromo, C.sub.1-4 alkoxy, PhO--, Cl.sub.5 C.sub.6 O--, Cl.sub.3 CO--, succinimidyloxy or imidazolyloxy; the remainder of the terms R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and Y are defined in the specification. The intermediates of Formula V are useful for preparing 1-(2,3-dihydro-1-carboxamide final products wherein said final products possess 5-HT M-receptor antagonist activity.Type: GrantFiled: November 13, 1992Date of Patent: June 21, 1994Assignee: Beecham Group, p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 5200413Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.Type: GrantFiled: August 5, 1991Date of Patent: April 6, 1993Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 5049556Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.Type: GrantFiled: August 2, 1989Date of Patent: September 17, 1991Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 5034398Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH or O, or X is NH and Y is CO;Z is CH.sub.2, O, S or NR.sub.3 wherein R.sub.3 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and R.sub.a is not present; orZ is CH or N and R.sub.a is as defined for R.sub.3 above;R.sub.b is present when X--Y--R.sub.2 is attached at the phenyl ring and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.1 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.Type: GrantFiled: October 3, 1989Date of Patent: July 23, 1991Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4959367Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is N or CH;R.sub.1 and R.sub.2 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-7 acyl, C.sub.1-7 acylamino, or amino, aminocarbonyl or aminosulphonyl, optionally substituted by one or two C.sub.1-6 alkyl or C.sub.3-8 cycloalkyl groups, or by C.sub.4-5 polymethylene or by phenyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsuphinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro; or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy;Z is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; andR.sub.3 or R.sub.4 is C.sub.1-4 alkyl;having 5-HT.sub.3 receptor antagonist activity, a process for their preparation and their use as pharmaceuticals.Type: GrantFiled: November 2, 1988Date of Patent: September 25, 1990Assignee: Beecham Group P.L.C.Inventor: Francis D. King
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Patent number: 4946966Abstract: A process for the preparation of a compound of formula (I): ##STR1## which comprises the reactive of a methylating agent with a compound of formula (IV): ##STR2## in a polar solvent in which is dissolved an alkali metal alkoxide, in an inert atmosphere.Type: GrantFiled: December 20, 1988Date of Patent: August 7, 1990Assignee: Beecham Group P.L.C.Inventors: Francis D. King, Thomas W. Ramsay
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Patent number: 4937247Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CH or N;Y is NH or O;R.sub.1 is hydrogen or halogen;R.sub.2 is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p and q are independently 1 to 3; and R.sub.4 or R.sub.5 is C.sub.1-4 alkyl;R.sub.3 i s C.sub.1-10 acyl, C.sub.1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl or benzyloxycarbonyl, or R.sub.6 R.sub.7 NCO or R.sub.6 R.sub.7 NS(O).sub.m wherein m is 1 or 2 and R.sub.6 and R.sub.7 are independently C.sub.1-6 alkyl groups or together are C.sub.4-6 polymethylene; having 5-HT.sub.3 antagonist activity, a process for their preparation and their use as pharmaceuticals.Type: GrantFiled: September 25, 1987Date of Patent: June 26, 1990Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4920127Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;R.sub.1 is hydrogen, fluoro or chloro;R.sub.2 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl or together are a bond; orR.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5, together are C.sub.2-7 polymethylene or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.x -- where m and x. are 1 to 5 such that m+x is 2 to 6;R.sub.4 is C.sub.1-7 acyl, C.sub.1-6 alkoxycarbonyl, hydroxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups, CF.sub.3, C.sub.1-6 alkyl substituted by C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or by C.sub.1-6 alkoxycarbonyl, or R.sub.4 is phenyl or phenyl-C.sub.1-4 alkyl optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;Z is a group of formula (a), (b) or (c).Type: GrantFiled: February 16, 1988Date of Patent: April 24, 1990Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 4918079Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein the various substituents are defined hereinbelow, having 5-HT.sub.3 receptor antagonist activity, processes for their preparation and their use as pharmaceuticals.Type: GrantFiled: September 30, 1988Date of Patent: April 17, 1990Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4886808Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH;Z is NR.sub.3 wherein R.sub.3 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and R.sub.a is not present; orZ is N and R.sub.a is as defined for R.sub.3 above;R.sub.b is present when X-Y-R.sub.2 is attached at the phenyl ring and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.1 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.Type: GrantFiled: March 16, 1988Date of Patent: December 12, 1989Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4883874Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen;either R.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylithio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.Type: GrantFiled: February 8, 1989Date of Patent: November 28, 1989Assignee: Beecham Group plc. of Beecham HouseInventors: Francis D. King, Michael S. Hadley, Roger T. Martin
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Patent number: 4882327Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof:Y-CO-L-Z (I)whereinL is NH or O; Y is a group of formula (a), (b) or (c): ##STR1## wherein R.sub.1 and R.sub.2, R.sub.5 and R.sub.6, R.sub.9 and R.sub.10, are independently selected from hydrogen or halogen;X is N or CR.sub.3whereinR.sub.3 is hydrogen or C.sub.1-6 alkoxy;R.sub.4 is hydrogen, halogen, CH.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;one of R.sub.7 and R.sub.8 is C.sub.Type: GrantFiled: April 22, 1988Date of Patent: November 21, 1989Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4871744Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof; ##STR1## wherein L is NH or O;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl), hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.Type: GrantFiled: June 3, 1988Date of Patent: October 3, 1989Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 4857647Abstract: A compound of formula (XXII): ##STR1## or a compound of formula (XXIII): ##STR2## wherein in formula (XXIII), J.sup.1 -1 is 1 to 4; and Q.sub.6 and Q.sub.7 are on the same carbon atom; and wherein, in formulae (XXII) and (XXIII), Q.sub.6 is NH.sub.2 and Q.sub.7 is H and p is 0 to 2; q is 0 to 3; and one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen; and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl.Type: GrantFiled: June 4, 1987Date of Patent: August 15, 1989Assignee: Beecham Group p.l.c.Inventor: Francis D. King