Patents by Inventor Barry E. Ayres
Barry E. Ayres 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: 5057496Abstract: There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 (where R.sup.6 is a hydrogen atom or a hydroxyl group and R.sup.7 is a pyridinyl ring);X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4, and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency.Type: GrantFiled: December 6, 1988Date of Patent: October 15, 1991Assignee: Glaxo Group LimitedInventors: Peter C. Cherry, Michael W. Foxton, Barry E. Ayres, Andrew D. Searle
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Patent number: 4985407Abstract: There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 is a hydrogen atom and R.sup.7 is a phenyl group, or R.sup.6 is a methyl group and R.sup.7 is a hydrogen atom or a methyl or ethyl group;X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.Type: GrantFiled: December 6, 1988Date of Patent: January 15, 1991Assignee: Glaxo Group LimitedInventors: Michael W. Foxton, Barry E. Ayres, Anthony W. J. Cooper
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Patent number: 4621081Abstract: Cephalosporin antibiotics of general formula: ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group, and Y.sup..sym. represents a C-linked 5- or 6-membered heterocyclic ring containing at least one C.sub.1-4 alkyl-substituted quaternary nitrogen atom, which ring may also contain one or more sulphur atoms) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties, is (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxycyclobut-1-oxyimino)ace tamido]-3-[(1-methylpyridinium-4-yl)-thiomethyl]ceph-3-em-4-carboxylate.Type: GrantFiled: September 27, 1982Date of Patent: November 4, 1986Assignee: Glaxo Group LimitedInventors: Cynthia H. O'Callaghan, Barry E. Ayres, David G. H. Livermore, Christopher E. Newall, Niall G. Weir
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Patent number: 4504477Abstract: Cephalosporin antibiotics of general formula ##STR1## (wherein Y.sup..sym. represents a C-attached 1-C.sub.1-4 alkylpyridinium group) exhibit broad spectrum antibiotic activity with unusually high activity against strains of Pseudomonas organisms as well as high activity against various members of the Enterobacteriaceae. The invention also includes the non-toxic salts, non-toxic metabolically labile esters and 1-oxides of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of the antibiotics.Type: GrantFiled: July 21, 1981Date of Patent: March 12, 1985Assignee: Glaxo Group LimitedInventors: Cynthia H. O'Callaghan, Barry E. Ayres, David G. H. Livermore, Christopher E. Newall, Niall G. Weir
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Patent number: 4464368Abstract: Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group, or together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group and R.sup.1 represents a C.sub.1-4 alkyl group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.Particularly effective compounds of formula (I) are (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetami do]-3-(2-methylpyrazolium-1-ylmethyl)ceph-3-em-4-carboxylate and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-[(1-carboxycyclobut-1-oxyimino)ac etamido]-3-(2-methylpyrazolium-1-ylmethyl)]ceph-3-em-4-carboxylate.Type: GrantFiled: July 23, 1981Date of Patent: August 7, 1984Assignee: Glaxo Group LimitedInventors: Cynthia H. O'Callaghan, Barry E. Ayres, Christopher E. Newall, David G. H. Livermore, Derek R. Sutherland
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Patent number: 4427675Abstract: Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group, or together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group). These compounds exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.Particularly effective compounds of formula (I) are (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetami o]-3-(pyridazinium-1-ylmethyl)ceph-3-em-4-carboxylate and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(t-carboxycyclobut-1-oxyimino)ace tamido]-3-(pyridazinium-1-ylmethyl)ceph-3-em-4-carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I), compositions containing the antibiotic compounds of the invention and a method of combatting bacterial infection utilizing the antibiotics.Type: GrantFiled: September 29, 1981Date of Patent: January 24, 1984Assignee: Glaxo Group LimitedInventors: Barry E. Ayres, Cynthia H. O'Callaghan, David G. H. Livermore, Christopher E. Newall
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Patent number: 4315005Abstract: Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.1 and R.sup.b, which may be the same or different, each represent a C.sub.1-2 alkyl group, or together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkylidene group and Y.sup..sym. represents a 1-carbamoylmethylpyridinium group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.Particularly effective compounds of formula (I) are (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetami do]-3-[(1-carbamoylmethylpyridinium-4-yl)thiomethyl]ceph-3-em-4-carboxylate and (6R,7R)-[(Z)-2-(2-aminothiazol-4-yl)-2-[(1-carboxycyclobut-1-oxyimino)acet amido]-3-[(1-carbamoylmethylpyridinium-4-yl)thiomethyl]-ceph-3-em-4-carboxy late.Type: GrantFiled: March 21, 1980Date of Patent: February 9, 1982Assignee: Glaxo Group LimitedInventors: Barry E. Ayres, Niall G. Weir
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Patent number: 4192871Abstract: Pregnanes and androstanes are described which essentially possess a 3.alpha.-hydroxy group, a 5.alpha.-hydrogen atom or a 4.5- or 5,6-double bond, a 17.alpha.-hydrogen atom and an 11.beta.-aminoester group. Other optional substituents or double bonds may be present. The compounds have anaesthetic activity.Type: GrantFiled: May 22, 1978Date of Patent: March 11, 1980Assignee: Glaxo Laboratories LimitedInventors: Gordon H. Phillipps, Peter J. May, Barry E. Ayres
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Patent number: 4168309Abstract: Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; m or n are each 0 or 1 such that the sum of m and n is 0 or 1; and R.sup.Type: GrantFiled: September 30, 1977Date of Patent: September 18, 1979Assignee: Glaxo Laboratories LimitedInventor: Barry E. Ayres
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Patent number: 4132849Abstract: A process for the preparation of a 3-hydroxymethyl cephalosporin compound which comprises selectively hydrolyzing a 3-formyloxymethyl cephalosporin compound under acidic conditions in the presence of a protic solvent whereby a 3-hydroxymethyl cephalosporin is produced.Type: GrantFiled: October 7, 1977Date of Patent: January 2, 1979Assignee: Glaxo Laboratories LimitedInventor: Barry E. Ayres