Patents by Inventor Robert Southgate
Robert Southgate 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: 4820701Abstract: Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.3 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R.sup.4 is hydrogen or formamido, R.sup.5 is hydrogen, C.sub.1-6 alkyl, substituted alkyl, aryl or aralkyl, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, C.sub.1-6 alkyl, substituted alkyl, halogen, amino, phenyl, substituted phenyl, hydroxyl or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 form the residue of an optionally substituted 5- or 6-membered carbocyclic ring or a 5- or 6- membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphr or nitrogen, and X represents ##STR2## or tautomers thereof wherein R.sup.8 and R.sup.9 are the same or different and each represents hydroxy, or protected hydroxy.Type: GrantFiled: October 21, 1987Date of Patent: April 11, 1989Assignee: Beecham Group p.l.c.Inventors: Robert Southgate, Colin H. Frydrych
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Patent number: 4521337Abstract: A process for the preparation of a compound of the formulae (Ia) and/or (Ib): ##STR1## wherein R.sup.1 and R.sup.2 are independently substituted or unsubstituted hydrocarbon groups or are joined together so as to form a carbocyclic or heterocyclic ring, and R.sup.3 is a substituted or unsubstituted hydrocarbon group; which process comprises the ring-closing cyclization of a compound of the formula (II): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in relation to formulae (Ia) and (Ib).Type: GrantFiled: March 14, 1983Date of Patent: June 4, 1985Assignee: Beecham Group p.l.c.Inventors: Robert Southgate, Pamela Brown
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Patent number: 4446146Abstract: The compounds of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt or ester thereof; R.sub.2 is a group of the sub-formula (a) or (b):--CR.sub.4 .dbd.C(R.sub.5) NH.CO.sub.n R.sub.6 (a)--CR.sub.7 .dbd.C(R.sub.8)R.sub.9 (b)wherein R.sub.4 is a hydrogen atom or a lower alkyl group; R.sub.5 is a hydrogen atom or a lower alkyl group; R.sub.6 is a lower alkyl, phenyl, fluorophenyl, chlorophenyl, bromophenyl or benzyl group; and n is 1 or 2; R.sub.7 is a hydrogen or a lower alkyl group; R.sub.8 is a hydrogen atom or a lower alkyl group; R.sub.9 is a hydrogen atom or a lower alkyl or phenyl group; R.sub.3 is a group of the sub-formula (c):CR.sub.10 R.sub.11 R.sub.12 (c)wherein R.sub.10 is a hydrogen atom or a hydroxyl or O.CO.R.sub.13 or O.CO.OR.sub.13 group where R.sub.13 is a lower alkyl, phenyl, benzyl, fluorobenzyl, chlorobenzyl, bromobenzyl, lower alkoxybenzyl or nitrobenzyl group; R.sub.11 is a hydrogen atom or a lower alkyl group; R.sub.Type: GrantFiled: July 20, 1979Date of Patent: May 1, 1984Assignee: Beecham Group LimitedInventors: Robert Southgate, Terence C. Smale, Roger J. Ponsford
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Patent number: 4438036Abstract: The present invention provides a process for inversion of the absolute stereochemistry at the .alpha.-carbon atom of a C-6 substituent of a bicyclic carbapenem antibiotic via a phosphorus - azodicarboxylate mediated reaction. Novel azides, amines and formates are described as useful intermediates and as antibacterial agents.Type: GrantFiled: October 13, 1981Date of Patent: March 20, 1984Assignee: Beecham Group LimitedInventors: David F. Corbett, Robert Southgate, Steven Coulton
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Patent number: 4431587Abstract: Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.Type: GrantFiled: December 14, 1981Date of Patent: February 14, 1984Assignee: Beecham Group LimitedInventors: Kay H. Dickinson nee Berryman, Terence C. Smale, Robert Southgate
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Patent number: 4428961Abstract: The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 is a group such that COOR.sup.1 is a carboxyic acid group or a salt or ester thereof;R.sup.3 is hydrogen or an organic radical;n is zero or 1;R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.3 alkyl;X is C.sub.1 -C.sub.6 alkylene optionally substituted by hydroxy or a carboxylic acid group or a salt or ester thereof;Y is an amino, or substituted amino, wherein the substituent is carboxylic acyl, C.sub.1 -C.sub.6 alkyl or a group .dbd.C(R.sup.14)NR.sup.15 R.sup.16 wherein R.sup.15 and or C.sub.1 -C.sub.6 alkyl and R.sup.14 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a group --NR.sup.A R.sup.B wherein R.sup.A and R.sup.B are independently hydrogen or C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: January 23, 1981Date of Patent: January 31, 1984Assignee: Beecham Group LimitedInventors: Robert Southgate, Terence C. Smale, Roger J. Ponsford
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Patent number: 4405637Abstract: Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.Type: GrantFiled: September 28, 1981Date of Patent: September 20, 1983Assignee: Beecham Group LimitedInventors: Kay H. Dickinson nee Berryman, Terence C. Smale, Robert Southgate
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Patent number: 4401595Abstract: Compounds are provided of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group and A.sub.1 is a hydrogen atom or a methyl group. These compounds possess antibacterial activity. The preparation of these compounds is described.Type: GrantFiled: October 19, 1981Date of Patent: August 30, 1983Assignee: Beecham Group LimitedInventors: Andrew J. G. Baxter, Patricia M. Roberts, Robert Southgate
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Patent number: 4387051Abstract: The present invention provides the compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts and esters thereof wherein R.sup.3 is a hydrogen atom, a group HO.sub.3 S-- or a group R.sup.5 CO wherein R.sup.5 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, aryl, aryl(C.sub.1-6)alkyl or aryloxy(C.sub.1-6)alkyl; and R.sup.4 is an organic group other than methyl bonded to the --CO--NH-- moiety via a carbon atom; with the proviso that when R.sup.3 is a hydrogen atom or a group R.sup.5 CO the stereochemical configuration at the .alpha.-carbon atom of the C-6 substituent is S, and with the further proviso that when R.sup.3 is a group HO.sub.3 S-- the hydrogen atoms at C-5 and C-6 are cis. Their use is described as are processes for their preparation. Compounds wherein the R.sup.4 CO-- moiety is replaced by a hydrogen atom are also prepared.Type: GrantFiled: October 28, 1980Date of Patent: June 7, 1983Assignee: Beecham Group LimitedInventors: David F. Corbett, Robert Southgate, Alfred J. Eglington
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Patent number: 4350703Abstract: Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.Type: GrantFiled: January 5, 1981Date of Patent: September 21, 1982Assignee: Beecham Group LimitedInventors: Kay H. Dickinson, Terence C. Smale, Robert Southgate
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Patent number: 4293501Abstract: The present invention relates to sodium, thallium, silver or lithium salts of the compoundHS--CH=CHNHC(O).sub.n R.sub.6wherein n is 1 or 2, R.sub.6 is alkyl, phenyl or substituted phenyl. The salts are useful as reagents for the preparation of sulfur containing Clavulanic acid derivatives.Type: GrantFiled: December 14, 1979Date of Patent: October 6, 1981Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Andrew J. G. Baxter, Robert Southgate
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Patent number: 4263314Abstract: The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt thereof or is a group of the formula CO.sub.2 R.sub.1.sup.1 wherein R.sub.1.sup.1 is a group such that CO.sub.2 R.sub.1.sup.1 is an ester group, R.sub.2 is a hydrogen atom or a lower alkyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a phenyl group or a phenyl group substituted by one or two groups selected from fluorine, chlorine, OR.sub.5, NH.CO.R.sub.5, NH.CO.sub.2 R.sub.5 or CO.sub.2 R.sub.5 where R.sub.5 is a lower alkyl or benzyl group.A process for their preparation and their use in pharmaceutical compositions is also described.Type: GrantFiled: January 19, 1979Date of Patent: April 21, 1981Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Robert Southgate, Patricia M. Roberts
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Patent number: 4255441Abstract: The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt thereof or is a group of the formula CO.sub.2 R.sub.1.sup.1 wherein R.sub.1.sup.1 is a group such that CO.sub.2 R.sub.1.sup.1 is an ester group, R.sub.2 is a hydrogen atom or a lower alkyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a NH. CO.sub.n R.sub.6 group where R.sub.6 is a lower alkyl group, a phenyl group or a phenyl group substituted by one or two halogen atoms, lower alkyl or lower alkoxyl groups; and n is 1 or 2.A process for their preparation and their use in pharmaceutical compositions is also described.Type: GrantFiled: January 19, 1979Date of Patent: March 10, 1981Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Andrew J. G. Baxter, Robert Southgate
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Patent number: 4245089Abstract: Compounds of the formula (III): ##STR1## wherein R.sub.1 is alkyl of up to 3 carbon atoms and R.sub.2 is alkyl of up to 3 carbon atoms optionally joined to R.sub.1 so that R.sub.1 and R.sub.2 and the carbon atom to which they are attached form a spiro-cyclopentyl or spiro-cyclohexyl ring, and wherein the configuration about the .beta.-lactam ring is trans, are useful in the preparation of antibacterial .beta.-lactam compounds.A process for the preparation of the compounds of the formula (III), is also desired.Type: GrantFiled: January 25, 1979Date of Patent: January 13, 1981Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Robert Southgate
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Patent number: 4210661Abstract: This invention provides synthetic .beta.-lactam antibacterial compounds, a process for their preparation and pharmaceutical compositions containing them.The compounds are those of the formula (II): ##STR1## wherein: R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt or ester thereof; and R.sub.2 is a phenyl group or a phenyl group substituted by one to four groups selected from lower alkyl, fluorine, chlorine, bromine, CN, NO.sub.2, COR.sub.3, OR.sub.3, SR.sub.3, NH.sub.2, NHCOR.sub.3, NHCO.sub.2 R.sub.3, CO.sub.2 R.sub.3 or CO.sub.2 R.sub.10 where R.sub.3 is lower alkyl, benzyl, fluorobenzyl, chlorobenzyl, bromobenzyl or nitrobenzyl and CO.sub.2 R.sub.10 is carboxyl or a salt thereof, not more than three such groups being selected from fluorine, chlorine, bromine, CN, NO.sub.2, NH.sub.2, COR.sub.3 or CO.sub.2 R.sub.3 and not more than two such groups being selected from CN, NO.sub.2 and NH.sub.2.Type: GrantFiled: August 2, 1978Date of Patent: July 1, 1980Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Robert Southgate, Patricia M. Roberts
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Patent number: 3975383Abstract: Substituted ceph-3-ems having a substituted amino side chain in the 7-position, carboxylic acid or a salt or ester thereof in the 4-position and a benzyl or monohalobenzyl group in the 3-position.Type: GrantFiled: August 29, 1974Date of Patent: August 17, 1976Assignee: Beecham Group LimitedInventors: John Herbert Charles Nayler, Michael John Pearson, Robert Southgate
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Patent number: 3974154Abstract: 3-BENZYL-7-AMINO-3-CEPHEM-4-CARBOXYLIC ACID AND ESTERS AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF.Type: GrantFiled: April 24, 1974Date of Patent: August 10, 1976Assignee: Beecham Group LimitedInventors: John Herbert Charles Nayler, Michael John Pearson, Robert Southgate
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Patent number: 3959267Abstract: This invention relates to novel substituted ceph-3-ems some of which are of value as intermediates in the synthesis of antimicrobially active cephalosporin analogues whilst others are useful as antimicrobial agents in their own right. The invention is described in Part D of this specification. Parts A, B, C and E relate to starting materials and processes necessary for the preparation of the novel cephems.Type: GrantFiled: August 30, 1974Date of Patent: May 25, 1976Assignee: Beecham Group LimitedInventors: John Herbert Charles Nayler, Michael John Pearson, Robert Southgate
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Patent number: 3939157Abstract: Antimicrobially active ceph-3-ems having in the 3-position a benzyl or mono-halobenzyl group, preferably with the mono-halo group in the para-position of the phenyl part of the benzyl group.Type: GrantFiled: July 31, 1974Date of Patent: February 17, 1976Assignee: Beecham Group LimitedInventors: John Herbert Charles Nayler, Michael John Pearson, Robert Southgate