Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2006-10-10
2006-10-10
Stockton, Laura L. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S406000, C548S358500, C548S357100
Reexamination Certificate
active
07119114
ABSTRACT:
Compounds having activity as selective inhibitors of JNK are disclosed The compounds of this invention are pyrazoloanthrone and derivatives thereof having the following structure:wherein R1and R2are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
REFERENCES:
patent: 4198518 (1980-04-01), Tzikas
patent: 4202827 (1980-05-01), Tzikas
patent: 4556654 (1985-12-01), Showalter et al.
patent: 6162613 (2000-12-01), Su et al.
patent: 146895 (1972-02-01), None
patent: 1257149 (1967-12-01), None
patent: 0 208 211 (1987-01-01), None
patent: 1293557 (1970-09-01), None
patent: 1404969 (1973-08-01), None
patent: 1576217 (1977-07-01), None
patent: WO 99/53927 (1999-10-01), None
patent: WO 00/35909 (2000-06-01), None
patent: WO 01/12609 (2001-02-01), None
patent: WO 01/12621 (2001-02-01), None
patent: WO 02/085396 (2002-10-01), None
STN International® CAPLUS Database, Accession No. 1997:491798; Ivanova et al., Poverkhnost (1997), (4-5), 193-201.
STN International® CAPLUS Database, Accession No. 1994:30709, Sokolyuk et al., Zh. Org. Khim. (1992), 28(10), 2193-200.
STN International® CAPLUS Database, Accession No. 1973:406796, Arient, Patent No. CS146895 (1973).
STN International® CAPLUS Database, Accession No. 1989:185177, Showalter et al. (1988).
Laakso et al., CA 51:76969, 1957.
Mosby et al., CA 54:80551, 1960.
Akamatsu, CA 58:27252, 1963.
Ames et al., 1987, “An integrated concept of amebicidal action: electron transfer and oxy radicals”, Free Radical Biol. Med. 3:85-96.
Aspenström et al., 1996, “Two GTPases, Cdc42 and Rac, bind directly to a protein implicated in the immunodeficiency disorder Wiskott-Aldrich syndrome”, Curr. Biol. 6:70-75.
Chen et al., 1996, “Activation and inhibition of the AP-1 complex in human breast cancer cells”, Mol. Carcinogenesis 15:215-226.
Dong et al., 1998, “Defective T cell differentiation in the absence of Jnk1”, Science 282:2092-2095.
Faris et al., 1996, “Regulation of interleukin-2 transcription by inducible stabile expression of dominant negative and dominant active mitogen-activated protein kinase kinase kinase in Jurkat T cells”, J. Biol. Chem. 271:27366-27373.
Galushko and Dokunikhin, 1977, “Pyrazoloanthrone derivatives I. Reactivity of 3-aminopyrazoloanthrone”, Khimiya Geterotsiklicheskikh Soedinenii, 7:956-961.
Gum et al., 1997, “Regulation of 92 kDa type IV collagenase expression by the jun aminoterminal kinase- and the extracellular signal-regulated kinase- dependent signaling cascades”, Oncogene 14:1481-1493.
Gvon et al., 1994, “Amino-imino tautomerism and intramolecular cyclization of 4, 9-diamino-1, 10-anthraquinone-1-tosylimines” Dokl. Akad. Nauk, 334:465-468 (in Russian with English abstract).
Han et al., 1999, “Jun N-terminal kinase in rheumatoid arthritis”, J. Pharmacol. Exp. Therap. 291:124-130.
Hartley et al., 1988, “Characteristics of the interaction of anthrapyrazole anticancer agents with deoxyribonucleic acids: structural requirements for DNA binding, intercalation, and photosensitization”, Mol. Pharmacol. 33:265-271.
Hibi et al., 1993, “Identification of an oncoprotein- and UV-responsive protein kinase that binds and potentiates the c-Jun activation domain”, Genes Dev. 7:2135-2148.
Ishizuka et al., 1997, “Mast cell tumor necrosis factor α production is regulated by MEK kinases”, Proc. Natl. Acad. Sci. USA 94:6358-6363.
Ivanova et al., 1997, “XPS investigation of electronic structure of pyrazolanthrone and its derivatives” Poverkhnost, 4-5:193-201.
Judson, 1992, “The anthrapyrazoles: a new class of compounds with clinical activity in breast cancer”, Semin. Oncol. 19:687-694.
Karin et al., 1997, “AP-1 function and regulation”, Curr. Opin. Cell. Biol. U9:240-246.
Lange-Carter et al., 1993, “A divergence in the MAP kinase regulatory network defined by MEK kinase and Raf”, Science 260:315-319.
Li et al., 1996, “Blocked signal transduction to the ERK and JNK protein kinases in anergic CD4+T cells”, Science 271:1272-1276.
Li et al., 1996, “The Ras-JNK pathway is involved in shear-induced gene expression”, Mol. Cell. Biol. 16:5947-5954.
Lin et al., 1995, “Identification of a dual specificity kinase that activates the Jun kinases and p38-Mpk2”, Science 268:286-290.
Manning and Mercurio, 1997, “Transcription inhibitors in inflammation”, Exp. Opin. Invest. Drugs 6:555-567.
Milne et al., 1995, “p53 is phosphorylatedin vitroandin vivoby an ultraviolet radiation-induced protein kinase characteristic of the c-Jun kinase, JNK1”, J. Biol. Chem. 270:5511-5518.
Mohit et al., 1995, “p493F12kinase: a novel MAP kinase expressed in a subset of neurons in the human nervous system”, Neuron 14:67-78.
Nishina et al., 1997, “Imparied CD28-mediated interleukin 2 production and proliferation in stress kinase SAPK/ERK1 kinase (SEK1)/mitogen-activated protein kinase kinase 4 (MKK4)-deficient T lymphocytes”, J. Exp. Med. 186:941-953.
Okamoto et al., 1997, “Selective activation of the JNK/AP-1 pathway in Fas-mediated apoptosis of rheumatoid arthritis synoviocytes”, Arthritis & Rheumatism 40:919-926.
Pombo et al., 1994, “The stress-activated protein kinases are major c-Jun amino-terminal kinases activated by ischemia and reperfusion”, J. Biol. Chem. 269:26546-26551.
Raitano et al., 1995, “The Bcr-Abl leukemia oncogene activates Jun kinase and requires Jun for transformation”, Proc. Natl. Acad. Sci. USA 92:11746-11750.
Sabapathy et al., 1999, “JNK2 is required for efficient T-cell activation and apoptosis but not for normal lymphocyte development”, Curr. Biol. 9:116-125.
Showalter et al., 1987, “Anthrapyrazole anticancer agents. Synthesis and structure-activity relationships against murine leukemias”, J. Med. Chem. 30:121-131.
Showalter et al., 1984, “5-[(Aminoalkyl)amino]-substituted anthral[1,9-cd]pyrazol-6(2H)-ones as novel anticancer agents. Synthesis and biological evaluation”, J. Med. Chem. 27:253-255.
Singh and Shah, 1978, “Reactions of 2,2′-ethylene-bis-anthrapyrazolone”, Indian J. -Chem. 16B:100-102.
Sokolyuk et al., 1992, “Synthesis and photochemical properties of peri-phenoxy derivatives of 6H-anthra[1,9-cd]-6-pyrazolone (pyrazolanthrone)”, Zhurnal Organicheskoi Khimii 28:2193-200.
Su et al., 1994, “JNK is involved in signal integration during costimulation of T lymphocytes”, Cell 77:727-736.
Swantek et al., 1997, “Jun N-terminal kinase/stress-activated protein kinase (JNK/SAPK) is required for lipopolysaccharide stimulation of tumor necrosis factor alpha (TNF-α) translation: glucocorticoids inhibit TNF-α translation by blocking JNK/SAPK”, Mol. Cell. Biol. 17:6274-6282.
Szabo et al., 1996, “Altered cJUN expression: an early event in human lung carcinogenesis”, Cancer Res. 56:305-315.
Tournier et al., 1997, “Mitogen-activated protein kinase kinase 7 is an activator of the c-Jun NH2-terminal kinase”, Proc. Natl. Acad. Sci. USA 94:7337-7342.
Whitmarsh and Davis, 1996, “Transcription factor AP-1 regulation by mitogen-activated protein kinase signal transduction pathways”, Mol. Med. 74:589-607.
Yan et al., 1994, “Activation of stress-activated protein kinase by MEKK1 phosphorylation of its activator SEK1”, Nature 372:798-800.
Yang et al., 1998, “Differentiation of CD4+T cells to Th1 cells requires MAP kinase JNK2”, Immunity 9:575-585.
Yin et al., 1997, “Tissue-specific pattern of stress kinase activation in ischemic/reperfused heart and kidney”
Bennett Brydon L.
Bhagwat Shripad S.
Manning Anthony M.
Murray Brion W.
O'Leary Eoin C.
Signal Pharmaceuticals LLC
Stockton Laura L.
LandOfFree
Pyrazoloanthrone and derivatives thereof as JNK inhibitors... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pyrazoloanthrone and derivatives thereof as JNK inhibitors..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyrazoloanthrone and derivatives thereof as JNK inhibitors... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3618694