1,7-naphthyridine derivatives as p38 MAP kinase inhibitors

Details 1,7-naphthyridine derivatives as p38 MAP kinase inhibitors 1,7-naphthyridine derivatives as p38 MAP kinase inhibitors

2011-03-15

2011-03-15

Fetterolf, Brandon J (Department: 1628)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S122000

Reexamination Certificate

active

07906530

ABSTRACT:
New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.

REFERENCES:
patent: 4550166 (1985-10-01), Moran et al.
patent: 57-203068 (1982-12-01), None
patent: WO 99/01449 (1999-01-01), None
patent: WO 00/63204 (2000-10-01), None
patent: WO 00/66583 (2000-11-01), None
patent: WO 01/01986 (2001-01-01), None
patent: WO 01/29042 (2001-04-01), None
patent: WO 02/02549 (2002-01-01), None
patent: WO 02/46184 (2002-06-01), None
patent: WO 02/058695 (2002-08-01), None
patent: WO 02/072576 (2002-09-01), None
patent: WO 02/072579 (2002-09-01), None
patent: WO 03/008413 (2003-01-01), None
patent: WO 03/033502 (2003-04-01), None
patent: WO 03/087087 (2003-10-01), None
patent: WO 03/097062 (2003-11-01), None
patent: WO 03/103590 (2003-12-01), None
patent: WO 2004/010995 (2004-02-01), None
patent: WO 2004/014900 (2004-02-01), None
patent: WO 2004/020438 (2004-03-01), None
patent: WO 2004/020440 (2004-03-01), None
patent: WO 2004/074290 (2004-09-01), None
patent: WO 2005/018624 (2005-03-01), None
patent: WO 2005/032551 (2005-04-01), None
patent: WO 2005/070929 (2005-08-01), None
patent: WO 2005/073219 (2005-08-01), None
patent: WO 2008/107125 (2008-09-01), None
Bao J. et al. “p38 MAP kinase inhibitors: Metabolically stabilized piperidine-substituted quinolinones and naphthyridines,”Bioorganic&Medicinal Chemistry Letters16(1): 64-68 (2006).
Gavrin, LK et al. “Inhibition of Tp12 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationships,”Bioorganic&Medicinal Chemistry Letters15(23): 5288-5292 (2005).
International Search Report mailed Oct. 18, 2007, for International Application No. PCT/EP2007/006981 (WO 2008/017461 A1).
Adams, R. H. et al. “Essential Role of p38α MAP Kinase in Placental but not Embryonic Cardiovascular Development,” Molecular Cell, 6:109-116 (2000).
Hale, K. K. et al. “Differential Expression and Activation of p38 Mitogen-Activated Protein Kinase α, β, γ, and σ in Inflammatory Cell Lineages,” The Journal of Immunology, 162:4246-4252 (1999).
Wang, X. S. et al. “Molecular Cloning and Characterization of a Novel p38 Mitogen-activated Protein Kinase,” The Journal of Biological Chemistry, 272(38):23668-23674 (1997).
U.S. Appl. No. 12/529,490, filed Sep. 1, 2009, Vidal Juan et al.
Allen, M. et al. “Deficiency of the Stress Kinase p38α Results in Embryonic Lethality: Characterization of the Kinase Dependence of Stress Responses of Enzyme-deficient Embryonic Stem Cells,”J. Exp. Med.191(5): 859-869 (2000).
Amato, JS et al. “Synthesis of 1-tert-Butyl-4-chloropiperidine: Generation of anN-tert-Butyl Group by the Reaction of a Dimethyliminium Salt with Methylmagnesium Chloride,”The Journal of Organic Chemistry, 70(5): 1930-1933 (2005).
Beardmore, VA et al. “Generation and Characterization of p38β (MAPK11) Gene Targeted Mice,”Molecular and Cellular Biology, 25(23): 10454-10464 (2005).
Brancho, D. et al. “Mechanism of p38 MAP kinase activation in vivo,”Genes&Development, 17: 1969-1978 (2003).
Cheng, C. et al. “The Friedländer Synthesis of Quinolines,”Org. Recat., Chapter 2, 37-201 (1982).
Hideshima, T. et al. “Targeting p38 MAPK inhibits multiple myeloma cell growth in the bone marrow milieu,”Blood, 101(2): 703-705 (2003).
Hildesheim, J. et al. “p38 Mitogen-Activated Protein Kinase Inhibitor Protects the Epidermis Against the Acute Damaging Effects of Ultraviolet Irradiation by Blocking Apoptosis and Inflammatory Responses,”The Journal of Investigative Dermatology, 122:497-502 (2004).
Hollenbach, E. et al. “Inhibition of RICK/Nuclear Factor-κB and p38 Signaling Attenuates the Inflammatory Response in a Murine Model of Crohn Disease,”The Journal of Biological Chemistry, 280(15): 14981-14988 (2005).
International Search Report mailed May 28, 2008, for International Application No. PCT/EP2008/001616 (WO 2008/107125 A1).
Jin, S. et al. “p38 Mitogen-Activated Protein Kinase is Activated After a Spinal Nerve Ligation in Spinal Cord Microglia and Dorsal Root Ganglion Neurons and Contributes to the Generation of Neuropathic Pain,”The Journal of Neuroscience, 23(10): 4017-4022 (2003).
Katsoulidis, E. et al. “Role of the p38 Mitogen-Activated Protein Kinase Pathway in Cytokine-Mediated Hematopoietic Suppression in Myelodysplastic Sydromes,”Cancer Research, 65(19): 9029-9037 (2005).
Kotlyarov, A. et al. “MAPKAP Kinase 2 is essential for LPS-induced TNF-α biosynthesis,”Nature Cell Biology, 1: 94-97 (1999).
Kumar, S. et al. “p38 Map Kinases: Key Signaling Molecules as Therapeutic Targets for Inflammatory Diseases,”Nature Reviews Drug Discovery, 2: 717-726 (2003).
Kyriakis, JM et al. “Mammalian Mitogen-Activated Protein Kinase Signal Transduction Pathways Activated by Stress and Inflammation,”Physiological Reviews, 81(2): 807-869 (2001).
Lee, JC et al. “A protein kinase involved in the regulation of inflammatory cytokine biosynthesis,”Nature, 372(22/29): 739-746 (1994).
Miyaura, N. et al. “Palladium-Catalyzed Cross-Coupling Reactions of Organoboron Compounds,”Chem. Rev., 95(7): 2457-2483 (1995).
Negishi, E. et al. “Novel Stereoselective Alkenyl-Aryl Coupling via Nickel-catalysed Reaction of Alkenylalanes with Aryl Halides,”J.C.S. Chem. Comm., 596-597 (1976).
Moran, DB et al. “Synthesis of (Pyridinyl)-1,2,4-triazolo[4,3-a]pyridines,” J. Heterocyclic Chem., 23: 1071-1077 (1986).
Nick, JA et al. “Selective Suppression of Neutrophil Accumulation in Ongoing Pulmonary Inflammation by Systemic Inhibition of p38 Mitogen-Activated Protein Kinase,”The Journal of Immunology, 169: 5260-5269 (2002).
Pargellis, C. et al. “Inhibitors of p38 mitogen-activated protein kinase for the treatment of rheumatoid arthritis,”Current Opinion in Investigational Drugs, 4(5): 566-571 (2003).
Sabio, G. et al. “p38γ regulates the localisation of SAP97 in the cytoskeleton by modulating its interaction with GKAP,”The EMBO Journal, 24(6): 1134-1145 (2005).
Saccani, S. et al. “p38-dependent marking of inflammatory genes for increased NF-κB recruitment,”Nature Immunology, 3(1): 69-75 (2002).
Schäfers, M. et al. “Tumor Necrosis Factor-α Induces Mechanical Allodynia After Spinal Nerve Ligation by Activation of p38 MAPK in Primary Sensory Neurons,”The Journal of Neuroscience, 23(7): 2517-2521 (2003).
See, F. et al. “p38 MAP kinase as a therapeutic target in cardiovascular disease,”Drug Discovery Today: Therapeutic Strategies, 1(2): 149-154 (2004).
Shi, Y. et al. “In the Cellular Garden of Forking Paths: How p38 MAPKs Signal for Downstream Assistance,”Biol. Chem., 383(10): 1519-1536 (2002).
Tamura, K. et al. “Requirement for p38α in Erythropoietin Expression: A Role for Stress Kinases in Erythropoiesis,”Cell, 102: 221-231 (2000).
Tsuda, M. et al. “Activation of p38 Mitogen-Activated Protein Kinase in Spinal Hyperactive Microglia Contributes to Pain Hypersensitivity Following Peripheral Nerve Injury,”GLIA, 89:89-95 (2004).
Underwood, DC et al. “SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung,”Am. J. Physiol. Lung Cell Mol. Physiol., 279: L895-L902 (2000).
Waetzig, GH et al. “p38 Mitogen-Activated Protein Kinase Is Activated and Linked to TNF-α Signaling in Inflammatory Bowel Disease,”The Journal of Immunology, 168: 5342-5351 (2002).
English Language Abstract for JP 57-203068, which published on Dec. 13, 1982.
Gilman, H. et al. “Some Substituted Isoquinolines,”Journal of American Chemical Soc

Affiliated with

Also associated with

Rating

1,7-naphthyridine derivatives as p38 MAP kinase 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 1,7-naphthyridine derivatives as p38 MAP kinase inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1,7-naphthyridine derivatives as p38 MAP kinase inhibitors will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2763718