Indazole derivatives as JNK inhibitors and compositions and...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C548S362500, C548S361100, C548S305100, C548S311700, C548S266400

Reexamination Certificate

active

06897231

ABSTRACT:
Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure:wherein R1, R2and A are 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: 3541110 (1970-11-01), Bell et al.
patent: 3994890 (1976-11-01), Fujimura
patent: 4415569 (1983-11-01), Yasuo et al.
patent: 5985867 (1999-11-01), Rodgers et al.
patent: 6162613 (2000-12-01), Su et al.
patent: 6531491 (2003-03-01), Kania et al.
patent: 6534524 (2003-03-01), Kania et al.
patent: 20020161022 (2002-10-01), Reich et al.
patent: 12 66 763 (1968-04-01), None
patent: 0 494 774 (1992-07-01), None
patent: 0 518 805 (1992-12-01), None
patent: 1293557 (1970-09-01), None
patent: 2 345 486 (2000-07-01), None
patent: 2345486 (2000-07-01), None
patent: WO 9843969 (1998-10-01), None
patent: WO 9953927 (1999-10-01), None
patent: WO 0112621 (2001-02-01), None
patent: WO 02085396 (2002-10-01), None
Boehm et al., Journal of Medicinal Chemistry (Jul. 13, 2000), 43(14), pp. 2664-2674.*
Kawakami et al., Organic Letters, (Feb. 10, 2000), 2(3), pp. 413-415.*
Patel et al., Bioorganic & Medicinal Chemistry Letters (Nov. 15, 1999), 9(22), pp. 3217-3220.*
Vasilevsky et al., CA 125 :114539, 1996.*
Andronati et al., CA 122:314528, 1995.*
Buck et al., CA 120:299030, 1994.*
Rickinger et al., CA 116:235509, 1992.*
Grayshan et al., CA 112:216936, 1990.*
Fujimura et al., CA 107:198159, 1987.*
Wrzeciono et al., CA 103:123405, 1985.*
Jones et al., CA 100:51503, 1984.*
Pfoertner et al., CA 97:72295, 1982.*
Arya et al., CA 88:37692, 1978.*
Fujimura et al., CA 84:31053, 1976.*
Walser et al., CA 83:164108, 1975.*
Horner et al., CA 70:77962, 1969.*
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 ofJnk1”, 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.
Gum et al., 1997, “Regulation of 92 kDa type IV collagenase expression by thejunaminoterminal kinase-and the extracellular signal-regulated kinase-dependent signaling cascades”, Oncogene 14:1481-1493.
Han et al., 1999, “Jun N-terminal kinase in rheumatoid arthritis”, J. Pharmacol. Exp. Therap. 291:124-130.
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.
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 phosphorylated in vitro and in vivo by 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, “Impaired 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, “TheBcr-Ablleukemia 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.
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 cell 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”, J. Biol. Chem. 272:19943-19950.
Spiegelman et al., “Regulation of Adipocyte Gene Expression in Differentiation and Syndromes of Obesity/Diabetes”,J. of Biol. Chem.268:6823-6826 (1993).
Hirosumi et al., “A central role for JNK in obesity and insulin resistance”,Letters to Nature420:333-336 (2002).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Indazole derivatives as JNK inhibitors and compositions and... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Indazole derivatives as JNK inhibitors and compositions and..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Indazole derivatives as JNK inhibitors and compositions and... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3393971

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.