Patents Assigned to Cyclacel Limited
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Patent number: 8497291Abstract: The present invention relates to a pharmaceutical formulation which comprises (i) a capsule, and (ii) a core comprising crystalline 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosylcytosine and a liquid carrier.Type: GrantFiled: December 22, 2006Date of Patent: July 30, 2013Assignee: Cyclacel LimitedInventors: Robert Westwood, Alistair Selkirk
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Patent number: 8404692Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR11, NHCO, NHSO2, NHCH2, CH2, CH2CH2, or CH?CH; X is a hydrocarbyl group optionally substituted by one or more R12 groups; R10 and R11 are each independently II or alkyl; R1-R4 are each independently II or (CII2)mR12, where m is O, 1, 2, or 3; each R12 is independently (CH2)aR16, where each R16 is independently selected from O(CH2)bR13, R13, COR13, COOR13, CN, CONR13R14, NR13R14, NR13COR14, SR13, SOR13, SO2R13, NR13SO2R14, SO2OR13, SO2NR13R14, halogen, CF3, and NO2, and wherein each a is 0, 1, 2, or 3 and b is 0, 1, 2, or 3; R13 and R14 are each independently H or (CH2)aR15, where n is 0, 1, 2, or 3; and each R15 is independently selected from alkyl, cycloalkyl, heteroaryl, aralkyl, aryl and heterocycloalkyl, each of which may be optionally substituted by one or more substituents selected from halogen, OH, CN, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(Type: GrantFiled: October 9, 2006Date of Patent: March 26, 2013Assignee: Cyclacel LimitedInventors: Stuart Jones, Robert Westwood, Mark Thomas, Janice McLachlan, Kenneth Duncan, Fred Scaerou, Daniella I. Zheleva
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Publication number: 20130072504Abstract: The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.Type: ApplicationFiled: January 24, 2011Publication date: March 21, 2013Applicant: CYCLACEL LIMITEDInventors: Benjamin Mark Skead, Christopher Peter Worrall, Jonathan Charles Christian Atherton, Julian Scott Northen, Philippe Fernades
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Patent number: 8349792Abstract: A first aspect of the invention relates to a combination comprising 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof. A second aspect relates to a pharmaceutical product comprising (i) 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and (ii) a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof, as a combined preparation for simultaneous, sequential or separate use in therapy.Type: GrantFiled: December 19, 2007Date of Patent: January 8, 2013Assignee: Cyclacel LimitedInventors: Simon R. Green, Ian Neil Fleming
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Publication number: 20130005747Abstract: The present invention provides a method for determining whether or not a cancer subject is suitable for treatment with a purine-based roscovitine-like inhibitor, which method comprises the step of determining the ras status of the cancer, wherein a determination that the subject has mutant ras status is indicative that the subject is suitable for treatment with a purine-based roscovitine-like inhibitor.Type: ApplicationFiled: December 21, 2011Publication date: January 3, 2013Applicants: Cyclacel Limited, The General Hospital Corporation d/b/a Massachusetts General Hospital, The Trustees of Dartmouth CollegeInventors: Simon Richard GREEN, Judy H. CHIAO, Jeffery SETTLEMAN, Ethan DMITROVSKY, Fabrizio Vittorio GALIMBERTI
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Publication number: 20120309723Abstract: The present invention relates to the use of an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating a disease associated with antinuclear antibodies, wherein the inhibitor of CDK2 and/or CDK7 and/or CDK9 or pharmaceutically acceptable salt thereof is administered in an amount sufficient to down-regulate the levels of antinuclear antibodies. A further aspect of the invention relates to a combination comprising an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, and methylprednisolone, and its use in the treatment of diseases associated with antinuclear antibodies, such as SLE.Type: ApplicationFiled: May 4, 2012Publication date: December 6, 2012Applicant: CYCLACEL LIMITEDInventors: Ariela BENIGNI, Carla ZOJA, Giuseppe REMUZZI, Athos GIANELLA-BORRADORI
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Patent number: 8124593Abstract: A first aspect of the invention relates to a method of treating leukaemia or myelodysplastic syndromes (MDS), said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days or 14 consecutive days every 21 days.Type: GrantFiled: November 5, 2008Date of Patent: February 28, 2012Assignee: Cyclacel LimitedInventors: Athos Gianella-Borradori, Judy Chiao
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Publication number: 20110224421Abstract: The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2? into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.Type: ApplicationFiled: May 8, 2009Publication date: September 15, 2011Applicant: CYCLACEL LIMITEDInventors: Gavin Wood, Robert Westwood
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Publication number: 20110207692Abstract: A first aspect of the invention relates to a combination comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.Type: ApplicationFiled: June 5, 2009Publication date: August 25, 2011Applicant: CYCLACEL LIMITEDInventors: Simon Richard Green, Ruth Mackay, Ian Neil Fleming
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Patent number: 7902361Abstract: The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj?) or a hydrocarbyl group optionally substituted by one or more R6 groups; R2, R3, and R4 are each independently H, alkyl or alkenyl, each of which may be optionally substituted with one or more R7 groups; R6 and R7 are each independently halogen, NO2, CN, (CH2)mORa, O(CH2)nORb, (CH2)pNRcRd, CF3, COORe, CONRfRg, CORh, SO3H, SO2Ri, SO2NRjRk, (CH2)qNRa?CORg?, Rf?, (CH2)rNRb?SO2Rh?, SO2NRd?Ri?, SO2NRe?(CH2)sORc?, heterocycloalkyl or heteroaryl, wherein said heterocycloalkyl and heteroaryl may be optionally substituted by one or more substituents selected from aralkyl, sulfonyl, Rm and CORn; Rg?, Rh?, Ri? and Rj? are each independently selected from alkyl, aryl, aralkyl and heteroaryl, each of which may be optionally substituted with one or more substituents selected from halogen, OH, NO2, NH2 CF3 and COOH; m, p, q and r are each independently 0, 1, 2 or 3; nType: GrantFiled: April 21, 2006Date of Patent: March 8, 2011Assignee: Cyclacel LimitedInventors: Shudong Wang, Gavin Wood, Kenneth Duncan, Christopher Meades, Darren Gibson, Janice McLachlan, Alex Perry, David Blake, Daniella I. Zheleva, Peter Martin Fischer
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Patent number: 7897605Abstract: The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.Type: GrantFiled: July 29, 2008Date of Patent: March 1, 2011Assignee: Cyclacel LimitedInventors: Shudong Wang, Christopher Meades, Gavin Wood, Janice O'Boyle, Campbell McInnes, Peter Martin Fischer
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Publication number: 20110046093Abstract: The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4? each independently H alkyl; or R4 and R4? together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.Type: ApplicationFiled: September 29, 2008Publication date: February 24, 2011Applicant: CYCLACEL LIMITEDInventors: Jonathan James Hollick, Stuart Donald Jones, Claire June Flynn, Michael George Thomas
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Patent number: 7772207Abstract: A first aspect of the invention relates to a combination comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.Type: GrantFiled: December 3, 2004Date of Patent: August 10, 2010Assignee: Cyclacel LimitedInventors: Simon Richard Green, Roger Neil Sleigh
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Publication number: 20100143350Abstract: The present invention relates to combination comprising (i) an ErbB inhibitor; and (ii) a CDK inhibitor, or a pharmaceutically acceptable salt thereof, selected from: (a) roscovitine; (b) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-2-methyl-pentan-2-ol; (c) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-pentan-2-ol; and (d) (2R,3S-3-(6-((4,6-dimethylpyridin-3-ylmethylamino)-9-isopropyl-9H-purin-2-ylamino)pentan-2-ol. Further aspects of the invention relate to pharmaceutical products and pharmaceutical compositions comprising combinations according to the invention, and methods of treatment using the same.Type: ApplicationFiled: October 5, 2009Publication date: June 10, 2010Applicant: CYCLACEL LIMITEDInventors: Simon GREEN, Sheelagh FRAME, Ian FLEMING
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Publication number: 20100125084Abstract: One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL).Type: ApplicationFiled: April 24, 2008Publication date: May 20, 2010Applicant: CYCLACEL LIMITEDInventor: Judy Chiao
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Publication number: 20100093769Abstract: The present invention relates to compounds of formula (I) wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl or cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and each R9 is other than H. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula (I), and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.Type: ApplicationFiled: October 5, 2009Publication date: April 15, 2010Applicants: CYCLACEL LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Peter William SHELDRAKE, Butrus ATRASH, Simon GREEN, Edward MCDONALD, Sheelagh FRAME
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Publication number: 20100069291Abstract: A first aspect of the invention relates to a combination comprising 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof. A second aspect relates to a pharmaceutical product comprising (i) 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and (ii) a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof, as a combined preparation for simultaneous, sequential or separate use in therapy.Type: ApplicationFiled: December 19, 2007Publication date: March 18, 2010Applicant: CYCLACEL LIMITEDInventors: Simon Green, Ian Fleming
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Publication number: 20100035870Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR11, NHCO, NHSO2, NHCH2, CH2, CH2CH2, or CH?CH; X is a hydrocarbyl group optionally substituted by one or more R12 groups; R10 and R11 are each independently II or alkyl; R1-R4 are each independently II or (CII2)mR12, where m is O, 1, 2, or 3; each R12 is independently (CH2)aR16, where each R16 is independently selected from O(CH2)bR13, R13, COR13, COOR13, CN, CONR13R14, NR13R14, NR13COR14, SR13, SOR13, SO2R13, NR13SO2R14, SO2OR13, SO2NR13R14, halogen, CF3, and NO2, and wherein each a is 0, 1, 2, or 3 and b is 0, 1, 2, or 3; R13 and R14 are each independently H or (CH2)nR15, where n is 0, 1, 2, or 3; and each R15 is independently selected from alkyl, cycloalkyl, heteroaryl, aralkyl, aryl and heterocycloalkyl, each of which may be optionally substituted by one or more substituents selected from halogen, OH, CN, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO— alkyl, CO-aryl, NH2, NH-alkyl, NType: ApplicationFiled: October 9, 2006Publication date: February 11, 2010Applicant: Cyclacel LimitedInventors: Stuart Jones, Robert Westwood, Mark Thomas, Janice McLachlan, Kenneth Duncan, Fred Scaerou, Daniella I. Zheleva
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Publication number: 20090325983Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.Type: ApplicationFiled: June 23, 2009Publication date: December 31, 2009Applicants: CYCLACEL LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Peter Martin FISCHER, Michael JARMAN, Edward MCDONALD, Bernard NUTLEY, Florence RAYNAUD, Stuart WILSON, Paul WORKMAN
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Publication number: 20090318446Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof. The present invention seeks to provide further substituted heteroaryl-substituted pyrimidine derivatives. More specifically, the invention relates to compounds that have broad therapeutic applications in the treatment of a number of different diseases and/or that are capable of inhibiting one or more protein kinases.Type: ApplicationFiled: January 11, 2006Publication date: December 24, 2009Applicant: Cyclacel LimitedInventors: Peter Martin Fischer, Shudong Wang, Christopher Meades, Matin J.I. Andrews, Darren Gibson, Kenneth Duncan