Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2010-06-29
2011-12-20
Anderson, Rebecca (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C546S272400
Reexamination Certificate
active
08080568
ABSTRACT:
This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifically in the treatment and prevention of a disease state mediated by these receptors.
REFERENCES:
patent: 7407958 (2008-08-01), Kim et al.
patent: 2003/0149277 (2003-08-01), Gaster et al.
patent: 2008/0319012 (2008-12-01), Kim et al.
patent: WO 00/61576 (2000-10-01), None
patent: WO 01/62756 (2001-08-01), None
patent: WO 02/055077 (2002-07-01), None
patent: WO 03/087304 (2003-10-01), None
patent: WO 2005/103028 (2005-11-01), None
Jordan, V. C. Nature Reviews: Drug Discovery, 2, 2003, 205.
Dorwald, F. Zaragoza. Side Reactions in Organic Synthesis: A guide to Successful Synthesis Design, Weinheim; WILEY-VCH Verlag GmbH & Co. KGaA, 2005, Preface.
Vippagunta, et al., Advanced Drug Delivery Reviews, 48, 2001, 18.
Wang, Qingjian et al.: “Reduction of bleomycin induced lung fibrosis by transforming growth factorβ soluble receptor in hamsters”,Thorax, 1999; 54, pp. 805-812.
Wahab, Nadia Abdel et al.: “Expression of extracellular matrix molecules in human mesangial cells in response to prolonged hyperglycaemia”,Biochem J., (1996), 316, pp. 985-992.
Shah, Mamta et al.: “Neutralisation of TGF-β1and TGF-β2or exogenous addition of TGF-β3to cutaneous rat wounds reduces scarring”,Journal of Cell Science, 108, 1995, pp. 985-1002.
Sanderson, Nancy et al.: “Hepatic expression of mature transforming growth factor β1 in transgenic mice results in multiple tissue lesions”,Proc. Natl. Acad. Sci. USA, vol. 92, Mar. 1995, pp. 2572-2576.
Ryu, Md, Ji-Kan et al.: “IN-1130, a Novel Transforming Growth Factor-β Type I Receptor Kinase (Activin Receptor-like Kinase 5) Inhibitor, Promotes Regression of Fibrotic Plaque and Corrects Penile Curvature in a Rat Model of Peyronie's Disease”,J Sex Med, 2009;6, pp. 1284-1296.
Rosendahl, Alexander et al.: “Activation of the TGF-β/Activin-Smad2 Pathway during Allergic Airway Inflammation”,Am J. Respir. Cell Mol. Biol., vol. 25, 2001, pp. 60-68.
Pawlowski, John E. et al.: “Stimulation of Activin A Expresssion in Rat Aortic Smooth Muscle Cells by Thrombin and Angiotensin II Correlates with Neointimal Formation in Vivo”,J. Clin. Invest., vol. 100, No. 3, Aug. 1997, pp. 639-648.
Munz, Barbara et al.: “Overexpression of activin A in the skin oftransgenic mice reveals new activites of activin in epidermal morphogenesis, dermal fibrosis and wound repair”,The EMBO Journal, vol. 18, No. 19, 1999, pp. 5205-5215.
Moon, J-A et al.: “IN-1130, a novel transforming growth factor-β type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy”,Kidney International, 2006, 70, pp. 1234-1243.
McCaffrey, Timothy A. et al.: “Decreased Type II/Type I TGF-β Receptor Ratio in Cells Derived from Human Atherosclerotic Lesions”,J. Clin. Invest., vol. 96, Dec. 1995, pp. 2667-2675.
Matzuk, M.M. et al.: “Development of cancer cachexia-like syndrome and adrenal tumors in inhibin-deficient mice”,Proc. Natl. Acad. Sci. USA, vol. 91, Sep. 1994, pp. 8817-8821.
Kim, MD, Jin Hyoung et al.: “IN-1233, an ALK-5 Inhibitor. Prevention of Granulation Tissue Formation after Bare Metallic Stent Placement in a Rat Urethal Model”,Radiology, vol. 255; No. 1, Apr. 2010, pp. 75-82.
Luo, Jian et al.: “Glia-dependent TGF-β signaling, acting independently of the TH17 pathway, is critical for initiation of murine autoimmune encephalomyelitis”,The Journal of Clinical Investigation, vol. 117, No. 11, Nov. 2007, pp. 3306-3315.
Long, MD, Phd, Lu et al.: “Altered Bone Morphogenetic Protein and Transforming Growth Factor-β Signaling in Rat Models of Pulmonary Hypertension”,Circulation, Feb. 3, 2009, pp. 566-576.
Lee, Geun Taek et al.: “Effect of IN-1130, a Small Molecule Inhibitor of Transforming Growth Factor-β Type I Receptor/Activin Receptor-Like Kinase-5, on Prostate Cancer Cells”,The Journal of Urology, vol. 180, Dec. 2008, pp. 2660-2667.
Jagirdar, Jaishree et al.: “Immunohistochemical Localization of Transforming Growth Factor Beta Isoforms in Asbestos-Related Diseases”,Environmental Health Perspectives 105, Supplement 5, Sep. 1997, 11 pages.
Hojo, Minoru et al.: “Cyclosporine induces cancer progression by a cell-autonomous mechanism”,Nature, vol. 397, Feb. 11, 1999, pp. 530-534.
Dahly, Annette J et al.: “Antihypertensive effects of chronic anti-TGF-β antibody therapy in Dahl S rats”,Am. J. Physiol. Regul. Integr. Comp. Physiol., 283: 2002, pp. R757-R767.
Cipriano, Sherry C. et al.: “Follistatin Is a Modulator of Gonadal Tumor Progression and the Activin-Induced Wasting Syndrome in Inhibin-Deficient Mice”,Endocrinology, vol. 141, No. 7, 2000, pp. 2319-2327.
Broekelmann, Thomas J. et al.: “Transforming growth factor β1is present at sites of extracellular matrix gene expression in human pulmonary fibrosis”,Proc. Natl. Acad. Sci. USA, vol. 88, Aug. 1991, pp. 6642-6646.
Domalapally Sreenu
Jin Chenghua
Kim Dae-Kee
Kota Sudhakar Rao
Maddeboina Krishnaiah
Anderson Rebecca
EWHA University - Industry Collaboration Foundation
Frommer & Lawrence & Haug LLP
Santucci Ronald R
LandOfFree
2-pyridyl substituted imidazoles as therapeutic ALK5 and/or... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4268181