Patents by Inventor Stephen John Gregson
Stephen John Gregson 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: 11370801Abstract: A compound of formula I and salts and solvates thereof, wherein: R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, NRN2 (where RN2 is H or C1-4 alkyl), and/or aromatic rings, e.g. benzene or pyridine; Y and Y? are selected from O, S, or NH; R6, R7, R9 are selected from the same groups as R6, R7 and R9 respectively; R11b is selected from OH, ORA, where RA is C1-4 alkyl; and RL is a linker for connection to a cell binding agent.Type: GrantFiled: April 18, 2018Date of Patent: June 28, 2022Assignee: MEDIMMUNE LIMITEDInventors: Philip Wilson Howard, Stephen John Gregson
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Patent number: 10799595Abstract: A compound of formula (I): (I) and its conjugates.Type: GrantFiled: October 13, 2017Date of Patent: October 13, 2020Assignee: MedImmune LimitedInventors: Philip Wilson Howard, Stephen John Gregson
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Publication number: 20200115390Abstract: A compound of formula I and salts and solvates thereof, wherein: R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, NRN2 (where RN2 is H or C1-4 alkyl), and/or aromatic rings, e.g. benzene or pyridine; Y and Y? are selected from O, S, or NH; R6, R7, R9 are selected from the same groups as R6, R7 and R9 respectively; R11b is selected from OH, ORA, where RA is C1-4 alkyl; and RL is a linker for connection to a cell binding agent.Type: ApplicationFiled: April 18, 2018Publication date: April 16, 2020Inventors: Philip Wilson Howard, Stephen John Gregson
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Patent number: 10420777Abstract: A conjugate comprising a PBD dimer linked from the tether joining the two PBD units, wherein the linker is of formula (A1):(Formula (A1)) wherein RN1 is selected from H and C1-4 alkyl; L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; Q is: (Formula (Q)), where Qx is such that Q is an amino-acid residue, a dipeptide residue or a tripeptide residue.Type: GrantFiled: September 11, 2015Date of Patent: September 24, 2019Inventors: Philip Wilson Howard, Stephen John Gregson, Jean-Noel Levy
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Publication number: 20190282705Abstract: A compound of formula (I): (I) and its conjugates.Type: ApplicationFiled: October 13, 2017Publication date: September 19, 2019Inventors: Philip Wilson HOWARD, Stephen John GREGSON
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Publication number: 20170239365Abstract: A conjugate comprising a PBD dimer linked from the tether joining the two PBD units, wherein the linker is of formula (A1): (Formula (A1)) wherein RN1 is selected from H and C1-4 alkyl; L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; Q is: (Formula (Q)), where Qx is such that Q is an amino-acid residue, a dipeptide residue or a tripeptide residue.Type: ApplicationFiled: September 11, 2015Publication date: August 24, 2017Inventors: Philip Wilson HOWARD, Stephen John GREGSON, Jean-Noel LEVY
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Patent number: 9624227Abstract: A compound with the formula I:Type: GrantFiled: December 22, 2014Date of Patent: April 18, 2017Assignee: MEDIMMUNE LIMITEDInventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
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Publication number: 20150111880Abstract: A compound with the formula I: wherein: R2 is of formula II: where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N?C?O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; either: (a) R10 is H, and RType: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Inventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
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Patent number: 8940733Abstract: The present invention is directed to novel pyrrolobenzodiazepine dimers and methods of using the dimers in the treatment of proliferative diseases.Type: GrantFiled: November 13, 2013Date of Patent: January 27, 2015Assignee: Spirogen SARLInventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
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Publication number: 20140142090Abstract: The present invention is directed to novel pyrrolobenzodiazepine dimers and methods of using the dimers in the treatment of proliferative diseases.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Applicant: SPIROGEN SARLInventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
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Patent number: 8633185Abstract: Compounds of the formula I: or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2?, R6?, R7?, R9?, X? and M? are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M? may together represent a divalent pharmaceutically acceptable cation.Type: GrantFiled: November 2, 2009Date of Patent: January 21, 2014Assignee: Spirogen SarlInventors: Philip Wilson Howard, Zhizhi Chen, Stephen John Gregson
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Patent number: 8592576Abstract: Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N?C?O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.Type: GrantFiled: October 16, 2009Date of Patent: November 26, 2013Assignee: Spirogen SarlInventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
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Patent number: 8501934Abstract: Methods of preparing ZC-423 (I) which result in varying enantiomeric ratios.Type: GrantFiled: July 22, 2009Date of Patent: August 6, 2013Assignee: Spirogen SARLInventors: Philip Wilson Howard, Stephen John Gregson, Zhizhi Chen, Arnaud Charles Tiberghien, Luke Masterson
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Patent number: 8487092Abstract: The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R2 is CHR2A, and R2A is independently selected from H, R, CO2R, COR, CHO, CO2H, and halo; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R8 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R is independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R7 groups or R8 groups of each monomer form together a dimer bridge having the formula —X—R?—X— linking the monomers; wherein R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g.Type: GrantFiled: October 16, 2009Date of Patent: July 16, 2013Assignee: Spirogen Developments SARLInventors: Philip Wilson Howard, Stephen John Gregson, ZhiZhi Chen, Arnaud Charles Tiberghien, Luke Masterson
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Publication number: 20110201803Abstract: The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R2 is CHR2A, and R2A is independently selected from H, R, CO2R, COR, CHO, CO2H, and halo; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R8 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R is independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R7 groups or R8 groups of each monomer form together a dimer bridge having the formula —X—R?—X— linking the monomers; wherein R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g.Type: ApplicationFiled: October 16, 2009Publication date: August 18, 2011Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Stephen John Gregson, Zhizhi Chen, Arnaud Charles Tiberghien, Luke Masterson
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Publication number: 20110196148Abstract: Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N?C?O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)m—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.Type: ApplicationFiled: October 16, 2009Publication date: August 11, 2011Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
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Publication number: 20110162227Abstract: Methods of preparing ZC-423 (I) which result in varying enantiomeric ratios.Type: ApplicationFiled: July 22, 2009Publication date: July 7, 2011Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Stephen John Gregson, Zhizhi Chen, Arnaud Charles Tiberghien, Luke Masterson
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Patent number: 7741319Abstract: The present inventors have developed a key intermediate for the production of C2 substituted PBDs, which has a leaving group at the C2 position, a carbamate protecting group at the N10 position and a protected hydroxy group at the C11 position. In a first aspect, the present invention comprises a compound with a the formula (I), wherein: R10 is a carbamate-based nitrogen protecting group; R11 is an oxygen protecting group; and R2 is a labile leaving group. In a further aspect, the present invention comprises a method of synthesising a compound of formula (III), or a solvate thereof, from a compound of formula (I) as defined in the first aspect, R16 is either O—R11, wherein R11 is as defined in the first aspect, or OH, or R10 and R16 together form a double bond between N10 and C11; and R15 is R. The other substituents are defined in the claims.Type: GrantFiled: March 1, 2005Date of Patent: June 22, 2010Assignee: Spirogen LimitedInventors: Philip Wilson Howard, Stephen John Gregson
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Publication number: 20100113425Abstract: Compounds of the formula I: or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2?, R6?, R7?, R9?, X? and M? are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M? may together represent a divalent pharmaceutically acceptable cation.Type: ApplicationFiled: November 2, 2009Publication date: May 6, 2010Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Zhizhi Chen, Stephen John Gregson
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Patent number: 7612062Abstract: Compounds of the formula: (I) or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2?, R6?, R7?, R9?, X? and M? are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M? may together represent a divalent pharmaceutically acceptable cation.Type: GrantFiled: April 21, 2006Date of Patent: November 3, 2009Assignee: Spirogen LimitedInventors: Stephen John Gregson, Philip Wilson Howard, Zhizhi Chen