Patents by Inventor David E. Bays
David E. Bays 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: 5270333Abstract: Compounds are disclosed of general formula: ##STR1## wherein R.sup.1 is H, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sup.2 is H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, aryl, ar(C.sub.1-4)-alkylene, or C.sub.5-7 cycloalkyl;R.sup.3 is H or C.sub.1-3 alkyl;R.sup.4 and R.sup.5 each represents H, C.sub.1-3 alkyl or 2-propenyl, or R.sup.4 and R.sup.5 together form an aralkylidene group;R.sup.6 represents --CO.sub.2 R.sup.7, COR.sup.7, --COCO.sub.2 R.sup.7, or --CONHR.sup.7, whereR.sup.7 represents H, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkenyl, aryl or ar(C.sub.1-4)alkylene (with the provisos that (a) R.sup.7 does not represent H or benzyl when R.sup.6 is --CO.sub.2 R.sup.7 and (b) R.sup.7 does not represent alkenyl when R.sup.6 is --CONHR.sup.7); and Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl group, and physiologically acceptable salts and solvates (e.g. hydrates) thereof.Type: GrantFiled: August 16, 1991Date of Patent: December 14, 1993Assignee: Glaxo Group LimitedInventors: David E. Bays, Alexander W. Oxford
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Patent number: 5229418Abstract: The invention relates to a salt of a basic histamine H.sub.2 -receptor antagonist of formula (I) ##STR1## and a complex of bismuth with a carboxylic acid selected from tartaric acid, citric acid and alkyl citric acids, or a solvate of such a salt, whereinR.sup.1 represents a group of formula ##STR2## where R.sup.3 represents methyl or the group (CH.sub.2).sub.2 CONR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 both represent ethyl groups;R.sup.2 represents a hydrogen atom or, when R.sup.1 is the group --C(.dbd.CHNO.sub.2)NHCH.sub.3, R.sup.2 may also represent a methyl group; andn is 3 and X is oxygen, or n is 2 and X is CH.sub.2 or sulphur;with the provisos that(i) when R.sup.1 represents ##STR3## then X is sulphur and n is 2: (ii) when R.sup.1 represents --C(.dbd.CHNO.sub.2)NHCH.sub.3 and R.sup.2 is hydrogen, then X is oxygen and n is 3 or X is CH.sub.2 and n is 2; and(iii) when R.sup.1 represents --C(.dbd.CHNO.sub.2)NHCH.sub.3 and R.sup.2 is methyl, then X is oxygen and n is 3 or X is sulphur and n is 2.Type: GrantFiled: April 25, 1991Date of Patent: July 20, 1993Assignee: Glaxo Group LimitedInventors: Eric W. Collington, John W. Clitherow, David E. Bays
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Patent number: 5114950Abstract: The invention provides amide derivatives of the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, where m represents 2, 3 or 4 or a group --X(CH.sub.2).sub.p, where p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.5, where R.sup.5 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.Type: GrantFiled: June 13, 1990Date of Patent: May 19, 1992Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, David E. Bays, David J. Cavalla, Peter C. North
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Patent number: 5045545Abstract: The invention relates to tetracyclic ketones of the general formula (I) ##STR1## wherein n represents 1, 2 or 3;Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3 -7cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Y represents a group --(CH.sub.2)m--, where m represents 2, 3 or 4, or a group --X(CH.sub.2).sub.p --, where p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule;and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.Type: GrantFiled: May 26, 1989Date of Patent: September 3, 1991Assignee: Glaxo Group LimitedInventors: David E. Bays, Ian H. Coates, John Bradshaw, William L. Mitchell
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Patent number: 4997831Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.Type: GrantFiled: August 31, 1989Date of Patent: March 5, 1991Assignee: Glaxo Group LimitedInventors: David E. Bays, Ian H. Coates, Alexander W. Oxford, Peter C. North
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Patent number: 4963546Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene chain and R.sup.3 is a hydrogen atom; orR.sup.1 and R.sup.3 together form a C.sub.2-4 alkylene chain and R.sup.2 is a hydrogen atom;A-B represents the group R.sup.4 R.sup.5 C--CH.sub.2 or R.sup.4 C.dbd.CH;R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or a C.sub.1-6 alkyl group; andIm represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.6, R.sup.7 and R.sup.8 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.Type: GrantFiled: January 31, 1989Date of Patent: October 16, 1990Assignee: Glaxo Group LimitedInventors: Peter C. North, Alexander W. Oxford, David J. Cavalla, David E. Bays
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Patent number: 4923863Abstract: Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are C.sub.1-6 alkyl or C.sub.3-6 alkenyl; or --NR.sub.1 R.sub.2 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR.sub.3 (where R.sub.6 represents C.sub.1-6 alkyl, OR.sub.4 or --NHR.sub.4, and R.sub.4 represents hydrogen, C.sub.1-6 alkyl, aryl, ar(C.sub.1-6)alkyl) or .dbd.NOR.sub.5 (where R.sub.5 represents C.sub.1-6 alkyl);X represents a direct bond, --CH.sub.2 -- or --CH.sub.2 O--;Ar represents a substituted phenyl moiety;and physiologically acceptable salts thereof.The compounds are indicated as useful for the treatment of pain and cerebral ischaemia.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: June 6, 1989Date of Patent: May 8, 1990Assignee: Glaxo Group LimitedInventors: David I. C. Scopes, David E. Bays
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Patent number: 4876267Abstract: Indole derivatives are disclosed of the formula (I): ##STR1## wherein R.sub.1 represents H, or C.sub.1-6 alkyl or C.sub.3-6 Alkenyl;R.sub.2 represents a H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl or C.sub.5-7 cycloalkyl, or a phenyl or phen(C.sub.1-4)alkyl group in which the phenyl ring is optionally substituted by halogen or C.sub.1-3 alkyl, C.sub.1-3 alkoxy or hydroxyl, or by a group NR.sup.a R.sup.b, or CONR.sup.a R.sup.b, wherein R.sup.a and R.sup.b each independently represents H or C.sub.1-3 alkyl;R.sub.3 and R.sub.4, each independently represents H or C.sub.1-3 alkyl or 2-propenyl;and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. The compounds may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers or excipients for administration by any suitable means. Various methods for the preparation of the compounds are disclosed.Type: GrantFiled: June 26, 1987Date of Patent: October 24, 1989Assignee: Glaxo Group LimitedInventors: Darko Butina, Michael D. Dowle, David E. Bays, Colin F. Webb
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Patent number: 4870096Abstract: Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one),R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl;m is zero or an integer from 1 to 4; andn is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route.Various methods for the preparation of the compounds (I) are disclosed.Type: GrantFiled: December 11, 1986Date of Patent: September 26, 1989Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Ian H. Coates, David E. Bays, Colin F. Webb
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Patent number: 4855314Abstract: Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 is halogen, a C.sub.1-3 alkoxy, R.sub.6 R.sub.7 NCO(CH.sub.2).sub.p --, R.sub.6 CONH(CH.sub.2).sub.p --, R.sub.6 R.sub.7 NSO.sub.2 (CH.sub.2).sub.p --, or R.sub.8 SO.sub.2 NH(CH.sub.2).sub.p -- (where R.sub.6 and R.sub.7 each represents hydrogen or C.sub.1-3 alkyl, R.sub.8 represents C.sub.1-3 alkyl and p is zero or 1);R.sub.2 represents hydrogen or C.sub.1-3 alkyl; R.sub.3 represents hydrogen or C.sub.1-3 alkyl;R.sub.4 and R.sub.5 each represents hydrogen, C.sub.1-3 alkyl or 2-propenyl;A represents --CO-- or --SO.sub.2 --;n represents an integer from 2 to 5; and m represents zero or an integer from 1 to 4; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine.Type: GrantFiled: January 8, 1987Date of Patent: August 8, 1989Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Ian H. Coates, David E. Bays, Colin F. Webb, Michael D. Dowle, Keith Mills, Colin D. Eldred
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Patent number: 4839377Abstract: Compounds are disclosed of general formula (I) ##STR1## wherein R.sub.1 represents a group CHO, COR.sub.8, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, CSNR.sub.9 R.sub.10 or SO.sub.2 NR.sub.9 R.sub.10,where R.sub.8 represents an alkyl, cycloalkyl, aryl or aralkyl group,R.sub.9 represents a hydrogen atom or an alkyl group, andR.sub.10 represents a hydrogen atom or an alkyl, cyclo-alkyl, aryl or aralkyl group;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-3 alkyl group;R.sub.5 represents a hydrogen atom or an alkyl, cycloalkyl, alkenyl or an aralkyl group orR.sub.4 and R.sub.5 together form an aralkylidene group orR.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a saturated monocyclic 5- to 7-membered ring; andAlk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl groups;with the provisos that when R.sub.Type: GrantFiled: August 6, 1987Date of Patent: June 13, 1989Assignee: Glaxo Group LimitedInventors: David E. Bays, Colin F. Webb, Michael D. Dowle
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Patent number: 4672067Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents CHO, COR.sub.8, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, CSNR.sub.9 R.sub.10 or SO.sub.2 NR.sub.9 R.sub.10, whereR.sub.8 represents alkyl, cycloalkyl, aryl or aralkyl,R.sub.9 represents hydrogen or alkyl, andR.sub.10 represents hydrogen or alkyl, cycloalkyl, aryl or aralkyl;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7 each independently represents hydrogen or C.sub.1-3 alkyl;R.sub.5 represents hydrogen, or alkyl, cycloalkyl, alkenyl or aralkyl, orR.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the attached nitrogen atom form a saturated monocyclic 5- to 7-membered ring; andAlk represents C.sub.2-3 alkylene chain optionally substituted by not more than two C.sub.1-3 alkyl groups;and physiologically acceptable salts and solvates thereof.Type: GrantFiled: June 28, 1984Date of Patent: June 9, 1987Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Keith Mills, Colin F. Webb, Michael D. Dowle, David E. Bays
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Patent number: 4670448Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined in the detailed description.The compounds show pharmaceutical activity as selective histamine H.sub.2 -antagonists.Type: GrantFiled: February 10, 1983Date of Patent: June 2, 1987Assignee: Glaxo Group LimitedInventors: John W. Clitherow, John Bradshaw, John W. M. Mackinnon, Duncan B. Judd, David E. Bays, Roger Hayes, Andrew Pearce
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Patent number: 4650810Abstract: Compounds are disclosed of general formula (I): ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.6 and R.sub.7, which may be the same or different, each represents a hydrogen atom or an alkyl group;R.sub.2 represents a hydrogen atom or an alkyl, aryl, aralkyl, cycloalkyl or alkenyl group;or R.sub.1 and R.sub.2, together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7-membered ring which may optionally contain a further hetero function;R.sub.5 represents a hydrogen atom or an alkyl or alkenyl group;or R.sub.4 and R.sub.5 together form an aralkylidene group;Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl groups; andX represents an oxygen or sulphur atom; and physiologically acceptable salts, solvates and bioprecursors thereof.Type: GrantFiled: January 26, 1983Date of Patent: March 17, 1987Assignee: Glaxo Group LimitedInventors: David E. Bays, Colin F. Webb, Michael D. Dowle
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Patent number: 4636521Abstract: Compounds are disclosed of general formula (I) ##STR1## wherein R.sub.1 represents an alkyl, cycloalkyl, aryl or aralkyl group;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-3 alkyl group;R.sub.5 represents a hydrogen atom or an alkyl, cycloalkyl, alkenyl or an aralkyl group; or R.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a saturated monocyclic 5- to 7-membered ring; Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl groups; and physiologically acceptable salts, solvates and bioprecursors thereof. The compounds are described as potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using one or more pharmaceutically acceptable carriers or excipients.Type: GrantFiled: June 29, 1984Date of Patent: January 13, 1987Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Keith Mills, Colin F. Webb, Michael D. Dowle, David E. Bays
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Patent number: 4571394Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichQ represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4- positions:Z represents one of the groups ##STR2## where X represents NCN, NSO.sub.2 Methyl, NSO.sub.2 Phenyl or CHNO.sub.2. The compounds show pharmacological activity as selective histamine H.sub.2 -antagonists.Type: GrantFiled: July 23, 1982Date of Patent: February 18, 1986Assignee: Glaxo Group LimitedInventors: Roger Hayes, David E. Bays, John W. M. MacKinnon
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Patent number: 4518598Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, and hydrates thereof. The substituents are defined in the specification.The compounds show pharmacological activity as selective histamine H.sub.2 -antagonists.Type: GrantFiled: January 9, 1984Date of Patent: May 21, 1985Assignee: Glaxo Group LimitedInventors: Roger Hayes, David E. Bays, John W. M. Mackinnon, Linda Carey, Philip Blatcher
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Patent number: 4507296Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts or hydrates thereof, in which the substituents are defined later in the specification.The compounds show pharmacological activity as selective histamine H.sub.2 -antagonists.Type: GrantFiled: January 9, 1984Date of Patent: March 26, 1985Assignee: Glaxo Group LimitedInventors: Roger Hayes, David E. Bays, John W. M. Mackinnon, Linda Carey
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Patent number: 4485104Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof have been found to show pharmacological activity as selective histamine H.sub.2 -antagonists. The substituents in the compounds of formula (I) are defined in the main body of the disclosure.Type: GrantFiled: February 24, 1983Date of Patent: November 27, 1984Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Barry J. Price, Roger Hayes, David E. Bays
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Patent number: 4481199Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined later.The compounds show pharmacological activity as selective histamine H.sub.2 -antagonists.Type: GrantFiled: July 6, 1983Date of Patent: November 6, 1984Assignee: Glaxo Group LimitedInventors: Linda Carey, Barry J. Price, John W. Clitherow, John Bradshaw, Michael Martin-Smith, David E. Bays, Philip Blatcher