Patents by Inventor Alexander W. Oxford
Alexander W. Oxford 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: 5037845Abstract: A compound of formula (I) ##STR1## and its physiologically acceptable salts and solvates are described as useful in treating and/or preventing pain resulting from dilatation of the cranial vasculature in particular migraine.Type: GrantFiled: March 1, 1989Date of Patent: August 6, 1991Assignee: Glaxo Group LimitedInventor: Alexander W. Oxford
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Patent number: 5026696Abstract: 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: July 18, 1990Date of Patent: June 25, 1991Assignee: Glaxo Group LimitedInventors: Peter C. North, Alexander W. Oxford, David J. Cavalla
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Patent number: 5026722Abstract: The invention relates to indole derivatives of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl or phenylC.sub.1-3 alkyl;R.sup.2 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-7 cycloalkyl, phenyl or phenylC.sub.1-3 alkyl;X represents an oxygen atom or the group NR.sup.3 (where R.sup.3 represents a hydrogen atom or a C.sub.1-6 alkyl group);one of the groups represented by R.sup.4, R.sup.5 and R.sup.6 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;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.Type: GrantFiled: June 15, 1989Date of Patent: June 25, 1991Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Peter C. North, David J. Cavalla
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Patent number: 5019586Abstract: The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group;Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 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 p0 A is a group of the formula (a), (b), (c), (d), (e), (f) or (g): ##STR3## and when A is the group (g), the group --COCR.sup.1 R.sup.2 CH.sub.2 Im is attached at the 2- or 4- position of the indole moiety.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.Type: GrantFiled: November 24, 1989Date of Patent: May 28, 1991Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Peter C. North
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Patent number: 5013733Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.3, --COR.sup.3, --CONR.sup.3 R.sup.4 or --SO.sub.2 R.sup.3 (wherein R.sup.3 and R.sup.4, which may be the same or different each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.3 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.3 or --SO.sub.2 R.sup.3);and R.sup.2 represents a group of formula (a), (b) or (c): ##STR2## wherein R.sup.5 represents a hydrogen atom or a C.sub.1-6 alkyl, C.sub.Type: GrantFiled: February 27, 1990Date of Patent: May 7, 1991Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Alexander W. Oxford, Peter C. North, Thomas Miller, Anthony D. Baxter, Kevin I. Hammond
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Patent number: 5008272Abstract: The invention provides potent and selective antagonists of 5-HT and 5-HT.sub.3 receptors which are tricyclic lactams of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the group 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.Type: GrantFiled: August 14, 1989Date of Patent: April 16, 1991Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Alexander W. Oxford, Peter C. North
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Patent number: 5001135Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a C.sub.1-6 alkyl group;R.sub.2 represents a hydrogen atom or a C.sub.1-3 alkyl group;n represents zero or an integer from 1 to 3;and pharmaceutically acceptable salts thereof.The compounds are useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: February 9, 1990Date of Patent: March 19, 1991Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Peter C. North, Martin R. Johnson
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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: 4997841Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents H or C.sub.1-6 alkyl;R.sub.2 represents H or C.sub.1-6 alkyl;R.sub.3 represents H;R.sub.4 represents H or C.sub.1-3 alkyl; and pharmaceutically acceptable salts and solvates (for example hydrates thereof.The compounds are indicated as useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: August 12, 1988Date of Patent: March 5, 1991Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Darko Sutina, Martin R. Owen
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Patent number: 4994483Abstract: Indole derivatives are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sub.2 is a hydrogen, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl, phen(C.sub.1-4)alkyl or C.sub.5-7 cycloalkyl; R.sub.3 and R.sub.4 are hydrogen, C.sub.1-3 alkyl or propenyl groups or together form an aralkylidene group; Alk is C.sub.2 -C.sub.3 alkylene chain and A is C.sub.2 -C.sub.5 alkylene chainand its physiologically acceptable salts and solvates.The compounds may be prepared, for example, by cyclization of a compound of general formula (II): ##STR2## where Q is the group NR.sub.3 R.sub.4 or a protected derivative thereof or a leaving group and R.sub.1 l, R.sub.2, R.sub.3, R.sub.4, A and Alk are as defined for formula (I).The compounds have a selective vosoconstrictor action and are useful in treating pain such as migraine. The compounds may be formulated as pharmaceutical compositions in conventional manner, preferably for oral administration.Type: GrantFiled: November 30, 1989Date of Patent: February 19, 1991Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Brian Evans, Michael D. Dowle, Ian H. Coates
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Patent number: 4985422Abstract: Compounds which are potent and selective antagonists of the effect of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, anxiety, and nausea and vomiting, of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula (a), (b) or (c): ##STR2## 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 phenyl C.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;n represents 1 or 2;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5 ; andX represents an oxygen or a sulphur atom, and, when Im represents an imidazolyl group of formula (c), X may also represent the group NR.sup.6, where R.sup.Type: GrantFiled: April 26, 1989Date of Patent: January 15, 1991Assignee: Glaxo Group LimitedInventors: Peter C. North, Alexander W. Oxford, Ian H. Coates, Paul J. Beswick
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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: 4939144Abstract: The invention relates to ketones of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## 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 phenyl C.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;n represents 1, 2 or 3;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5, (wherein R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.Type: GrantFiled: October 21, 1988Date of Patent: July 3, 1990Assignee: Glaxo Group LimitedInventors: Ian H. Coates, David C. Humber, James A. Bell, George B. Ewan, Alexander W. Oxford, William L. Mitchell
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Patent number: 4918080Abstract: The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group; Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.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 an aromatic or heteroaromatic group as defined in the specification.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.Type: GrantFiled: April 13, 1988Date of Patent: April 17, 1990Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, David J. Cavalla, Peter C. North
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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: 4808581Abstract: The invention relates to compounds of formula (I): ##STR1## and physiologically acceptable salts or solvates thereof, wherein Im represents an imidazolyl group of formula: ##STR2## and the various substituents are defined hereinbelow. The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.Type: GrantFiled: January 22, 1988Date of Patent: February 28, 1989Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, David J. Cavalla
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Patent number: 4795756Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, phenyl optionally substituted by C.sub.1-3 alkoxy or phen(C.sub.1-4) alkyl in which the phenyl ring is optionally substituted by C.sub.1-3 alkoxy;R.sub.2 is H or C.sub.1-6 alkyl;R.sub.3 is H or C.sub.1-3 alkyl;R.sub.4 and R.sub.5 independently represents H, C.sub.1-3 alkyl or 2-propenyl; andn represents zero or 1;and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. The compounds may be formulated as pharmaceutical compositions with physiologically acceptable carrier or excipients for administration by any convenient route. Various methods for the preparation of the compounds (I) are disclosed.Type: GrantFiled: March 27, 1987Date of Patent: January 3, 1989Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Michael D. Dowle
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Patent number: 4785016Abstract: Indole derivatives are disclosed of formula (I): ##STR1## wherein R.sub.1 represents H, alkyl or alkenyl;R.sub.2 represents H, alkyl, alkenyl, cycloalkyl or phenyl or phenyl alkyl the phenyl ring being optionally substituted by halogen, alkyl, alkoxy, hydroxyl or by a group --NR.sub.a R.sub.b, or --CONR.sub.a R.sub.b, wherein R.sub.a and R.sub.b are H, alkyl, alkenyl, or with the nitrogen atom form a saturated monocyclic ring;R.sub.3 and R.sub.4 are H, alkyl or propenyl or together form an aralkylidene group;Alk represents a Cf.sub.2-3 alkyl chain optionally substituted by one or two alkyl groups; andA.sup.1 represents a C.sub.2-5 alkenyl chain and salts and solvates thereof.The compounds have selective vasoconstrictor activity and are useful in treating and/or preventing pain resulting from dilatation of the cranial vasculature, particularly migraine. The compounds may be formulated in conventional manner with pharmaceutically acceptable carriers or excipients.Type: GrantFiled: December 3, 1985Date of Patent: November 15, 1988Assignee: Glaxo Group LimitedInventors: Brian Evans, Alexander W. Oxford, Darko Butain
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Patent number: 4739072Abstract: The invention relates to a process for the preparation of a compound of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and 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.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C.sub.1-6 alkyl group;or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.Type: GrantFiled: July 23, 1986Date of Patent: April 19, 1988Assignee: SanofiInventors: Alexander W. Oxford, Colin D. Eldred, Ian H. Coates, James A. Bell, David C. Humber, George B. Ewan