Patents Assigned to KuDos Pharmaceuticals Limited
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Patent number: 11633396Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.Type: GrantFiled: August 24, 2022Date of Patent: April 25, 2023Assignee: Kudos Pharmaceuticals LimitedInventors: Michael Karl Bechtold, Julie Kay Cahill, Katja Maren Fastnacht, Kieran James Lennon, Bernd Harald Liepold, Claudia Bettina Packhaeuser, Benedikt Steitz
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Patent number: 11160803Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: GrantFiled: September 11, 2019Date of Patent: November 2, 2021Assignee: KUDOS PHARMACEUTICALS LIMITEDInventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
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Patent number: 10449192Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: GrantFiled: February 26, 2018Date of Patent: October 22, 2019Assignee: KUDO PHARMACEUTICALS LIMITEDInventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
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Patent number: 10034884Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: June 19, 2017Date of Patent: July 31, 2018Assignee: KuDOS Pharmaceuticals LimitedInventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Fabienne Malagu, Niall Morrison Barr Martin, Keith Menear, Graeme Cameron Murray Smith
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Patent number: 9717736Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: June 8, 2015Date of Patent: August 1, 2017Assignee: Kudos Pharmaceuticals LimitedInventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Fabienne Malagu, Niall Morrison Barr Martin, Keith Menear, Graeme Cameron Murray Smith
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Patent number: 9566276Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: GrantFiled: September 14, 2015Date of Patent: February 14, 2017Assignee: KUDOS PHARMACEUTICALS LIMITEDInventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
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Patent number: 9169235Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: GrantFiled: September 11, 2014Date of Patent: October 27, 2015Assignee: KUDOS PHARMACEUTICALS LIMITEDInventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
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Patent number: 9102670Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: April 9, 2013Date of Patent: August 11, 2015Assignee: KUDOS PHARMACEUTICALS LIMITEDInventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Fabienne Malagu, Niall Morrison Barr Martin, Keith Menear, Graeme Cameron Murray Smith
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Patent number: 8912187Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: GrantFiled: July 8, 2011Date of Patent: December 16, 2014Assignee: Kudos Pharmaceuticals LimitedInventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
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Publication number: 20140135315Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: April 9, 2013Publication date: May 15, 2014Applicant: KuDOS Pharmaceuticals LimitedInventor: KuDOS Pharmaceuticals Limited
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Patent number: 8247416Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.Type: GrantFiled: July 10, 2009Date of Patent: August 21, 2012Assignee: Kudos Pharmaceuticals LimitedInventors: Keith Allan Menear, Anthony Peter Ottridge, Derek John Londesbrough, Michael Raymond Hallett, Keith Raymond Mulholland, John David Pittam, David Dermot Patrick Laffan, Ian Woodward Ashworth, Martin Francis Jones, Janette Helen Cherryman
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Publication number: 20120142673Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: November 30, 2011Publication date: June 7, 2012Applicant: KuDOS PHARMACEUTICALS LIMITEDInventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Malagu, Niall Morrison Barr Martin, Keith Allan Menear, Graeme Cameron Murray Smith
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Patent number: 8183369Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L, methods of obtaining form L, pharmaceutical compositions comprising Form L and methods of using Form L and compositions comprising Form L.Type: GrantFiled: October 17, 2008Date of Patent: May 22, 2012Assignee: Kudos Pharmaceuticals LimitedInventors: Kathryn Anne Quigley, Ezra John Still, Leonard Jesse Chyall
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Patent number: 8143241Abstract: The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.Type: GrantFiled: October 6, 2005Date of Patent: March 27, 2012Assignees: Kudos Pharmaceuticals Limited, The Institute of Cancer ResearchInventors: Alan Ashworth, Stephen Jackson, Niall Martin, Graeme Smith, Mark O'Connor
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Patent number: 8071579Abstract: The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.Type: GrantFiled: November 30, 2004Date of Patent: December 6, 2011Assignees: The Institute of Cancer Research: Royal Cancer Hospital, Kudos Pharmaceuticals LimitedInventors: Alan Ashworth, Stephen Jackson, Niall Martin, Graeme Smith
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Patent number: 7981889Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: GrantFiled: April 24, 2008Date of Patent: July 19, 2011Assignees: Kudos Pharmaceuticals Limited, Maybridge LimitedInventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
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Publication number: 20110124638Abstract: There is provided a compound of formula I: , or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: January 26, 2011Publication date: May 26, 2011Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Heather Mary Ellen Duggan, Karine Malagu, Frederic Georges Marie Leroux, Niall Morrisson Barr Martin, Keith Allan Menear, Graeme Cameron Murray Smith
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Publication number: 20100286157Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L, methods of obtaining form L, pharmaceutical compositions comprising Form L and methods of using Form L and compositions comprising Form L.Type: ApplicationFiled: October 17, 2008Publication date: November 11, 2010Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Kathryn Anne Quigley, Ezra John Still, Leonard Jesse Chyall
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Patent number: 7750006Abstract: A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by -L-RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(?O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are aType: GrantFiled: February 10, 2006Date of Patent: July 6, 2010Assignees: Kudos Pharmaceuticals Limited, Maybridge PLCInventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Charles Richard White, Roger Frank Newton, Diane Gillian Douglas, Penny Jane Eversley, Julia Vile
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Patent number: 7732483Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(?O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(?O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groType: GrantFiled: June 5, 2008Date of Patent: June 8, 2010Assignees: Kudos Pharmaceuticals Limited, Cancer Research Technology LimitedInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Keith Allan Menear, Marc Geoffrey Hummersone, Laurent Jean Martin Rigoreau, Roger John Griffin, Bernard Thomas Golding, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Ian Robert Hardcastle, Kappusamy Saravanan