Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Reexamination Certificate
2006-11-15
2011-11-15
Lewis, Patrick (Department: 1623)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
C514S043000
Reexamination Certificate
active
08058258
ABSTRACT:
The present invention relates to a method of inducing apoptosis in a tumour cell as well as modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of general formula (I). In general formula A is C or N. R1, R4and R5are, independently selected, H or aliphatic, cycloaliphatic aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0-3 heteroatoms being N, O, S, or Si. R4and R5may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2is H or a halogen, such as F or Cl. R3is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms being N, O, S, Si, or a halogen such as Cl or F. Also provided is a pharmaceutical composition for inducing apoptosis in a tumour cell and/or modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The pharmaceutical composition comprises a compound as defined above or a pharmaceutically acceptable salt thereof and a carrier or diluent.
REFERENCES:
patent: 510260 (1893-12-01), Higham
patent: 4968690 (1990-11-01), Marquez et al.
patent: 5843780 (1998-12-01), Thomson
patent: 6090622 (2000-07-01), Gearhart et al.
patent: 2005/0176142 (2005-08-01), Nakorn et al.
patent: 2005/0244417 (2005-11-01), Ashkenazi et al.
patent: 2005/0245559 (2005-11-01), Koul et al.
patent: 2005/0266093 (2005-12-01), Mohapatra
patent: 2006/0147456 (2006-07-01), Lebecque et al.
patent: WO-90/09177 (1990-08-01), None
patent: WO-2004046312 (2004-06-01), None
Oxenrider et al. FEBS Letters (1993), vol. 316, pp. 273-277.
Moon et al. Bioorganic & Medicinal Chemistry Letters (2004), vol. 14, pp. 5641-5644.
Beisel, et al, Histone methylation by theDrosophilaepigenetic transcriptional regulator Ash1, Nature, Oct. 2002, vol. 419, pp. 857-862.
Boyer, et al., “Polycomb complexes repress developmental regulators in murine embryonic stem cells,” Nature, vol. 441, May 18, 2006, doi:10.1038, pp. 349-353.
Bracken, et al, EXH2 is downstream of the pRB-E2F pathway, essential for proliferation and amplified in cancer, The EMBO Journal, 2003, vol. 22 No. 20, pp. 5323-5335.
Bracken, Genes Dev. 2006,20 1123-1136.
Bray, et al., “3-Deazaneplanocin A induces massively increased interferon-χ production in Ebola virus-infected mice,” Antiviral Research, 55 (2002), pp. 151-159.
Brown, R, Trends in Molecular Medicine (2002), 8,4,S43-S48.
Cao, et al, SUZ12 Is Required for Both the Histone Methyltransferase Activity and the Silencing Function of the EED-EZH2 Complex, Molecular Cell, Jul. 2, 2004, vol. 15, pp. 57-67.
Cao, et al., Role of Histone H3 Lysine 27 Methylation in Polycomb-Group Silencing, Science, 2002, 298, pp. 1039-1043.
Chambers, I. Smith, Oncogene 2004, 23, 7150-7160.
Chen, et al, Down-regulation of Human DAB2IP Gene Expression Mediated by Polycomb Ezh2 Complex and Histone Deacetylase in Prostate Cancer, The Journal of Biological Chemistry, vol. 280 No. 23, Jun. 10, 2005, pp. 22437-22444, USA.
Chiang, Journal of Biological Chemistry, vol. 267, No. 7 (1992) pp. 4988-4991.
Collins, et al., “Stem Cell Function, Self-Renewal and Behavioral Heterogeneity of Cells from the Adult Muscle Saellite Cell Niche,” Cell, vol. 122, Jul. 29, 2005, pp. 289-301.
Costa, Non-coding RNAs: New players in eukaryotic biology, Gene, 2005, vol. 357, pp. 83-94.
De Clercq, Erik, “Vaccinia Virus Inhibitors as a Paradignm for Chemotherapy of Poxvirus Infections,” Clinical Microbiology Review, Apr. 2001, pp. 382-397.
De Clercq, et al., “Broad-Spectrum Antiviral and Cytocidal Activity of Cyclopentenylcytosine, A Carbocyclic Nucleoside Targeted at CTP Synthetase,” Biochemical Pharmacology, 1999, vol. 41, No. 12 pp. 1821-1829.
De Clercq, Biochemical Pharmacology, vol. 41, No. 12 (1991) p. 1821-1829.
Driscoll, Stem Cells vol. 12 No. 1 (1994) pp. 7-12.
Feinberg, A.P., Nature Review Genetics (2006) pp. 7, 21-33.
Glazer, et al., “3-Deazaneplanocin: A new and potent inhibitor of S-Adenosylhomocysteine Hydrolase and its effects on human promyelocytice leukemia cell line HL-60,” Biochemical and Biophysical Research Communications, Mar. 13, 1986, vol. 135 No. 2, pp. 688-694.
Hayashi, M. Nucleic Acids Symposium Series No. 8 (1980 65-67.
Holden, Gene-Srppressing Proteins Reveal Secrets of Stem Cells, Science, Apr. 21, 2006, vol. 312, p. 349.
Kalantry, et al, The Polycomb group protein Eed protects the inactive X-chromosome from differentiation-induced reactivation, Nature Cell Biology, Feb. 2006, vol. 8 No. 2, pp. 195-202.
Kamminga, et al, The Polycomb group gene Ezh2 prevents hematopoietic stem cell exhaustion, Blood Journal, Mar. 1, 2006, vol. 107 No. 5, pp. 2170-2179.
Kim, et al, Korean Journal of Biochemistry vol. 20 No. 2 (1988) p. 85-92.
Kirmizis, et al, Identification of the Polycomb Group Protein SU(Z)12 as a Potential Molecular Target for Human Cancer Therapy, Molecular Cancer Therapeutics, Jan. 2003, vol. 2, pp. 113-121.
Kirmizis, et al, Silencing of human polycomb target genes is associated with methylation of histone H3 Lys 27, Genes & Development, 2004, vol. 18, pp. 1592-1605.
Krivtsov, et al., “Transformation from committed progenitor to leukemia stem cell initiated by MLL-AF9” Nature, Aug. 2006, vol. 442, pp. 818-822.
Kuzmichev, Andrei, “Composition and histone substrates of polycomb repressive group complexes change during cellular differentiation,” PNAS, Feb. 8, 2005, vol. 102, No. 6, 1859-1864.
Kusmichev, “Different Ezh2-containing complexes target methylation of histone H1 or nucleosomal Histone H3”, Molecular Cell, 2004, 14, 2, 382-397.
Lee, et al, Control of Developmental Regulators by Polycomb in Human Embryonic Stem Cells, Cell, Apr. 21, 2006, pp. 301-313.
Levine, et al., Division of labor in Polycomb group repression, TRENDS in Biochemical Sciences, Sep. 2004, vol. 29, pp. 478-485.
Lund, et al., Polycomb complexes and silencing mechanisms, Science Direct, 2004, pp. 239-246
Maitra, Nature Genetics (2005) 37, 18, 1099-1103.
Milne, et al., MLL Targets SET Domain Methyltransferase Activity toHoxGene Promoters, Molecular Cell, Nov. 2002, vol. 10, pp. 1107-1117.
Mitsui, et al, The Homeoprotein Nanog Is Required for Maintenance of Pluripotency in Mouse Epiblast and ES Cells, Cell, May 30, 2003, vol. 113, pp. 631-642.
Moon et al, Bioorganic & Medicinal Chemistry Letters vol. 14, No. 22 (2004) pp. 5641-5644.
Morrissey, et al, Potent and persistent in vivo anti-HBV activity of chemically modified siRNAs, Nature Biotechnology, Aug. 2005, vol. 23 No. 8, pp. 1002-1007.
Muller, et al., Histone Methyltransferase Activity of aDrosophilaPolycomb Group Repressor Complex, Cell Press, Oct. 2002, vol. 111, pp. 197-208.
Nichols, et al, Formation of Pluripotent Stem Cells in the Mammalian Embryo Depends on the POU Transcription Factor Oct4, Cell, Oct. 30, 1998, vol. 95, pp. 379-391.
Pasini, et al., “Suz12 is essential for mouse development and for EZH2 histone methyltransferase activity,” The EMBO Journal (2004) 23, 4061-4071.
Passegue, Proc. Natl. Acad. Sci. USA (2003), 100, 11842-11849.
Patzel, Design of siRNAs producing unstructured guide-RNAs results in improved RNA interference efficiency, Nature Biotechnology, Nov. 2005, vol. 23 No. 11, pp. 1440-1444.
Peedicayil, Epigenetic therapy—a new development in pharmacology, Indian J Med Res, Jan. 2006, vol. 123, pp. 17-24.
Rando, Thomas A., “The adult muscle stem cell comes of age,” Nature Medicine, Aug. 2005, pp. 829-831.
Reynolds, et al, Tumor Suppressor p16INK4A Regulates Polycomb-mediated DNA Hypermethylation in Human Mammary Epithelial Cells, The Journal of Biological Chemistry, Aug. 25, 2006, vol. 281 No. 32, pp. 24790-24802, USA.
Santos, F. Reproduction (2004) vol. 127, pp. 643-651.
Saramaki, et al, The Gene for Polycomb Group Protein Enhancer of Zeste Homolog 2 (EZH2) is Amplified in Late-Stage Prostate Cancer, Genes, Chromosomes & Cancer, 2006, vol. 45, pp. 639-645.
Schoeft
Tan Jing
Yang Xiao Jing
Yu Qiang
Agency for Science Technology and Research
Choate Hall & Stewart LLP
Lewis Patrick
LandOfFree
Methods for cancer therapy and stem cell modulation does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Methods for cancer therapy and stem cell modulation, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Methods for cancer therapy and stem cell modulation will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4273188