Patents by Inventor Stuart Cockerill
Stuart Cockerill 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: 12227507Abstract: Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, and are bonds, and and are absent; or (ii) T is C, Z is N, and are bonds, and and are absent; each of R3 and R4 is independently halo, —OR6, —NR6R7, —COR8, —C(O)OR8, —CON(R8)2 or —R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: GrantFiled: August 20, 2020Date of Patent: February 18, 2025Assignee: Pfizer Inc.Inventors: George Stuart Cockerill, James Good, Craig Alex Avery, Andrew Joseph Warner, Edward James Cochrane
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Publication number: 20240173332Abstract: Pharmacuetical Compounds Benzodiazepine derivatives of formula (I): wherein: R1 is H or F; R2 is selected from formula (II) and formula (III) R3 is C1-C6 alkyl which is unsubstituted or substituted by CF3, or is a monocyclic 4- to 6-membered heterocyclic group containing 1 or 2 heteroatoms selected from O, N and S; R4 is H or a group selected from —X, -alk-X, —CONR6R7, C?NNR6R7, —SO2R6 and —SO2NR6R7; R4 is a group selected from —X, -alk-X, —CONR6R7, —C?NNR6R7, —SO2R6 and —SO2R6R7; X is OH or a derivative of an OH group selected from ?-amino carboxylic acid esters, carboxylic acid esters, carbonates, carbamates, ethers and phosphates: alk is C1-C6 alkylene which is unsubstituted or substituted by C3-C6 cycloalkyl; and R6 and R7 are each independently C1-C6 alkyl or C3-C6 cycloalkyl; and the pharmaceutically acceptable salts thereof are inhibitors of respiratory syncytial virus (RSV) and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: February 24, 2022Publication date: May 30, 2024Applicant: Pfizer Inc.Inventors: Matthew Barrett, Alexandre Bedernjak, George Stuart Cockerill, James Good
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Publication number: 20230365585Abstract: Benzodiazepine derivatives of formula (Ib) wherein: R1 is H or halo; Y is selected from O, S, SO, SO2 and NR; one or two of V, W and X is or are N or CH and the other one or two is or are CH; R2 is a group selected from C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 haloalkyl, halo, —OR, —NHR?, —SOmNR2, —SOmR, nitro, —CO2R, —CN, —CONR2, —NHCOR and —NR11R12; each R is independently H or C1-C6 alkyl; R11 and R12 are each independently H or C1-C6 alkyl; or R11 and R12 form, together with the N atom to which they are attached, either (a) a morpholine ring which is optionally bridged by a —CH2— group linking two ring carbon atoms that are positioned para to each other, or (b) a spiro group of the following formula (b): R? is C3-C6 cycloalkyl; m is 1 or 2; n is 0, 1 or 2; and each of R3 to R10 is independently selected from H, C1-C6 alkyl, halo, —OR, -NR2,—NHR?, —SOmNR2, —SOmR, nitro, —CO2R, —CN, —CONR2, —NHCOR, —NR13R 4 whereinR13 and R14 form, together with the N atom to which they are attached, a morpholine ring, and thType: ApplicationFiled: July 7, 2021Publication date: November 16, 2023Inventors: Matthew BARRETT, George Stuart COCKERILL, James GOOD, Craig Alex AVERY, Edward James COCHRANE, Stuart Thomas ONIONS, Andrew Joseph WARNER
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Publication number: 20230270751Abstract: Benzodiazepine derivatives of formula (Ie) wherein one R1 and R2 is a benzodiazepinyl-containing group of formula (II) in which R8 is H or halo; the other of R1 and R2 is a group Z selected from H, C3-C6 cycloalkyl, halo, —NHR9, benzyl, phenyl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, wherein phenyl, heterocyclyl and heteroaryl are unsubstituted or substituted by one or two substituents selected from 4- to 10-membered heterocyclyl which is unsubstituted or substituted by OR, and from C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, halo, —OR, —(CH2)mOR, —NR2, —(CH2)mNR2, —NHR?, —SOmNR2, —SOmR, —SR, nitro, —CO2R, —CN, —CONR2, —NHCOR, —CH2NR10R11 and —NR10R11, in which each R is independently H or C1-C6 alkyl, R? is C3-C6 cycloalkyl and m is 1 or 2; R9 is selected from phenyl and 4- to 10-membered heteroaryl wherein phenyl and heteroaryl are unsubstituted or substituted by halo; R10 and R11 are each independently H or C1-C6 alkyl; or R10 and R11 form, together with theType: ApplicationFiled: July 7, 2021Publication date: August 31, 2023Inventors: Matthew BARRETT, George Stuart COCKERILL, James GOOD, Craig Alex AVERY, Edward James COCHRANE, Stefan Paul JONES, Stuart Thomas ONIONS, Andrew Joseph WARNER
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Patent number: 11634425Abstract: Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, -a- and -c- are bonds, and -b- and -d- are absent; or (ii) T is C, Z is N, -b- and -d- are bonds, and -a- and -c- are absent; each of R3 and R4 is independently halo, —OR6, —NR6R7—COR8, —C(O)OR8, —CON(R8)2 or —R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: GrantFiled: June 21, 2022Date of Patent: April 25, 2023Assignee: PFIZER INC.Inventors: George Stuart Cockerill, James Good, Edward James Cochrane
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Publication number: 20220409629Abstract: Benzodiazepine derivatives of formula (I): wherein: each of R1 and R2 is independently H or halo; R3 is H, C1-C6 alkyl, —NHR8 or —OR?; either (i) a, c, and e are all bonds, with b, d and f absent; orb, d and f are all bonds, with a, c and e absent; R4 is H or a group selected from C1-C6 alkyl, C3-C6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R5 is H or halo; R6 is —OR8, —NR8R9 or —R8; R7 is H or halo; each of R8 and R9 is independently H or a group selected from C1-C6 alkyl, C3-C6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R? is H or C1-C6 alkyl; and one of V and W is CH and the other is N or CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: October 22, 2020Publication date: December 29, 2022Inventors: MATTHEW BARRETT, GEORGE STUART COCKERILL, JAMES GOOD, CRAIG ALEX AVERY, EDWARD JAMES COCHRANE
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Publication number: 20220380349Abstract: Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; R3 is H, C1-C6 alkyl or —NHR8; either (i), a, c and c are all bonds, with, b, d and f absent; orb, d, and f are all bonds, with a, c, and c absent; R4 is H or a group selected from C1-C6 alkyl, C3-C6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R5 is H or halo; R6 is —OR8, —NR8R9 or —R8; R7 is H or halo; each of R8 and R9 is independently H or a group selected from C1-C6 alkyl, C3-C6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; n is 1 or 2; and one of V, W and X is N or CH and the other two are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infectionType: ApplicationFiled: November 2, 2020Publication date: December 1, 2022Inventors: MATTHEW BARRETT, GEORGE STUART COCKERILL, JAMES GOOD
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Publication number: 20220324873Abstract: Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, —a— and —c— are bonds, and —b— and —d— are absent; or (ii) T is C, Z is N, —b— and —d— are bonds, and —a— and —c— are absent; each of R3 and R4 is independently halo, —OR6, —NR6R7—COR8, —C(O)OR8, —CON(R8)2 or —R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C-6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: June 21, 2022Publication date: October 13, 2022Inventors: GEORGE STUART COCKERILL, JAMES GOOD, CRAIG ALEX AVERY, EDWARD JAMES COCHRANE, ANDREW JOSEPH WARNER
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Publication number: 20220306639Abstract: Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, and are bonds, and and are absent; or (ii) T is C, Z is N, and are bonds, and and are absent; each of R3 and R4 is independently halo, —OR6, —NR6R7, —COR8, —C(O)OR8, —CON(R8)2 or —R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: August 20, 2020Publication date: September 29, 2022Inventors: George Stuart COCKERILL, James GOOD, Craig Alex AVERY, Edward James COCHRANE, Andrew Joseph WARNER
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Patent number: 11247973Abstract: The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesising the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.Type: GrantFiled: August 15, 2017Date of Patent: February 15, 2022Assignee: The University of DurhamInventor: Stuart Cockerill
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Publication number: 20210017138Abstract: The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesising the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.Type: ApplicationFiled: August 15, 2017Publication date: January 21, 2021Inventor: Stuart Cockerill
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Patent number: 10603319Abstract: Pyrimidine derivatives of formula (I) wherein: Z is a direct bond or —(CH2)n— wherein n is 1 or 2; one of X and Y is N, CH or CF, and the other of X and Y is CH; one of R1 and R2 is selected from —NHR, —NR2, —OR, —SR, —S(O)R, —S(O)2R and a group of the following formula (A) and the other of R1 and R2 is selected from —NHR?, —OH, —OR? and a group of the above formula (A); R is unsubstituted C1-C6 alkyl; R? is a group selected from C1-C6 alkyl, 5- to 12-membered aryl and C3-C6 cycloalkyl, which group is unsubstituted or substituted; W is —(CH2)m—, —CH2—O—CH2—, —CH2—S—CH2— or —CH2—S(O)2—CH2—; p is 1, q is an integer of 1-6 and V is N; or p is 1, q is 0 and V is CH; or p is 0, q is 0 and V is N; r is 0 or 1; and R3 is —(CH2)s—NH2 or —(CH2)s—OH wherein s is 0 or an integer of 1 to 4; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: GrantFiled: August 3, 2017Date of Patent: March 31, 2020Assignee: REVIRAL LIMITEDInventors: Stuart Cockerill, Matthew Barrett
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Patent number: 10406166Abstract: The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesizing the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.Type: GrantFiled: April 15, 2016Date of Patent: September 10, 2019Assignee: The University of DurhamInventors: Stuart Cockerill, Jonathan Harburn
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Publication number: 20190167683Abstract: Pyrimidine derivatives of formula (I) wherein: Z is a direct bond or —(CH2)n— wherein n is 1 or 2; one of X and Y is N, CH or CF, and the other of X and Y is CH; one of R1 and R2 is selected from —NHR, —NR2, —OR, —SR, —S(O)R, —S(O)2R and a group of the following formula (A) and the other of R1 and R2 is selected from —NHR?, —OH, —OR? and a group of the above formula (A); R is unsubstituted C1-C6 alkyl; R? is a group selected from C1-C6 alkyl, 5- to 12-membered aryl and C3-C6 cycloalkyl, which group is unsubstituted or substituted; W is —(CH2)m—, —CH2—O—CH2—, —CH2—S—CH2— or —CH2—S(O)2—CH2—; p is 1, q is an integer of 1-6 and V is N; or p is 1, q is 0 and V is CH; or p is 0, q is 0 and V is N; r is 0 or 1; and R3 is —(CH2)s—NH2 or —(CH2)s—OH wherein s is 0 or an integer of 1 to 4; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: August 3, 2017Publication date: June 6, 2019Inventors: Stuart Cockerill, Matthew Barrett
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Patent number: 10106539Abstract: Benzimidazoles of formula (I): wherein: one of X and Y is an N atom or a substituted C atom, and the other is CH; L is a single bond, C1-3 alkylene, C2-3 alkenylene or C2-3 alkynylene; R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, 3- to 10-membered cycloalkyl, 5- to 10-membered heterocyclyl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Z is halo, C1-6 haloalkyl, nitro, —CN, —N(R2)2, —OR2, —SR2, —S(=0)R2, or —S(=0)2R2; each R2 is independently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; and m is 0 or 1; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: GrantFiled: October 6, 2015Date of Patent: October 23, 2018Assignee: REVIRAL LIMITEDInventors: Stuart Cockerill, Neil Mathews, Simon Ward, Graham Lunn, Michael Paradowski, Jose Miguel Gascon Simorte
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Publication number: 20180085378Abstract: The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesising the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.Type: ApplicationFiled: April 15, 2016Publication date: March 29, 2018Inventors: Stuart Cockerill, Jonathan Harburn
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Patent number: 9809575Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C?O, >S(?O), >S(?O)2, —O—C(?O)—, —C(?O)—O—, N(R2)—C(?O)—, or —C(?O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(?O)R2, —S(?O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: GrantFiled: November 12, 2012Date of Patent: November 7, 2017Assignee: ReViral LimitedInventors: Stuart Cockerill, Christopher Pilkington, James Lumley, Richard Angell, Neil Mathews
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Publication number: 20170305908Abstract: Benzimidazoles of formula (I): wherein: one of X and Y is an N atom or a substituted C atom, and the other is CH; L is a single bond, C1-3 alkylene, C2-3 alkenylene or C2-3 alkynylene; R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, 3- to 10-membered cycloalkyl, 5- to 10-membered heterocyclyl or 5- to 12- membered heteroaryl, each of which is unsubstituted or substituted; Z is halo, C1-6 haloalkyl, nitro, —CN, —N(R2)2, —OR2, —SR2, —S(?0)R2, or —S(?0)2R2; each R2 is independently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; and m is 0 or 1; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: October 6, 2015Publication date: October 26, 2017Applicant: REVIRAL LIMITEDInventors: Stuart Cockerill, Neil Mathews, Simon Ward, Graham Lunn, Michael Paradowski, Jose Miguel Gascon Simorte
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Publication number: 20160339027Abstract: A pharmaceutical formulation comprising the compound of formulaType: ApplicationFiled: August 3, 2016Publication date: November 24, 2016Applicant: NOVARTIS AGInventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey, Stephen Barry Guntrip, Kathryn Jane Smith
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Publication number: 20160051551Abstract: A pharmaceutical formulation comprising the compound of formulaType: ApplicationFiled: October 20, 2015Publication date: February 25, 2016Applicant: NOVARTIS AGInventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey, Stephen Barry Guntrip, Kathryn Jane Smith