Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Reexamination Certificate
2010-04-07
2011-11-01
Balasubramanian, Venkataraman (Department: 1624)
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
C514S243000
Reexamination Certificate
active
08049008
ABSTRACT:
Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
REFERENCES:
patent: 5440013 (1995-08-01), Kahn
patent: 5475085 (1995-12-01), Kahn
patent: 5618914 (1997-04-01), Kahn
patent: 5670155 (1997-09-01), Kahn
patent: 5672681 (1997-09-01), Kahn
patent: 5693325 (1997-12-01), Kahn
patent: 5710245 (1998-01-01), Kahn
patent: 5840833 (1998-11-01), Kahn
patent: 5859184 (1999-01-01), Kahn et al.
patent: 5929237 (1999-07-01), Kahn
patent: 6013458 (2000-01-01), Kahn et al.
patent: 6020331 (2000-02-01), Kahn
patent: 6117896 (2000-09-01), Qabar et al.
patent: 6184223 (2001-02-01), Kahn et al.
patent: 6245764 (2001-06-01), Kahn et al.
patent: 6294525 (2001-09-01), Stasiak et al.
patent: 6372744 (2002-04-01), Qabar et al.
patent: 6413963 (2002-07-01), Kahn et al.
patent: 6440955 (2002-08-01), Stasiak et al.
patent: 6548500 (2003-04-01), Kahn et al.
patent: 6762185 (2004-07-01), Kahn et al.
patent: 7232822 (2007-06-01), Moon et al.
patent: 7531320 (2009-05-01), Kahn et al.
patent: 7566711 (2009-07-01), Moon et al.
patent: 7576084 (2009-08-01), Moon et al.
patent: 7671054 (2010-03-01), Moon et al.
patent: 2001/0039274 (2001-11-01), Kahn et al.
patent: 2002/0022620 (2002-02-01), Kahn et al.
patent: 2002/0065416 (2002-05-01), Stasiak et al.
patent: 2002/0068695 (2002-06-01), Scolastico et al.
patent: 2003/0021773 (2003-01-01), Moroder et al.
patent: 2003/0027819 (2003-02-01), Qabar et al.
patent: 2003/0105103 (2003-06-01), Golebiowski et al.
patent: 2004/0072831 (2004-04-01), Moon et al.
patent: 2005/0059628 (2005-03-01), Kahn et al.
patent: 2007/0128669 (2007-06-01), Kahn
patent: 2007/0129353 (2007-06-01), Kahn
patent: 2384126 (2001-03-01), None
patent: WO 94/03494 (1994-02-01), None
patent: WO 97/15577 (1997-05-01), None
patent: WO 98/05333 (1998-02-01), None
patent: WO 98/49168 (1998-11-01), None
patent: WO 01/00210 (2001-01-01), None
patent: WO 01/16135 (2001-03-01), None
patent: WO 03/006447 (2003-01-01), None
patent: WO 03/031448 (2003-04-01), None
patent: WO 2004/072076 (2004-08-01), None
patent: WO 2004/072077 (2004-08-01), None
patent: WO 2004/093828 (2004-11-01), None
patent: WO 2005/116032 (2005-12-01), None
Arango, D. et al., “c-myc/p53 Interaction Determines Sensitivity of Human Colon Carcinoma Cells to 5-Fluorouracil in Vitro and in Vivo,”Cancer Research, 61:4910-4915, Jun. 15, 2001.
Batlle, E. et al., “β-Catenin and TCF Mediate Cell Positioning in the Intestinal Epithelium by Controlling the Expression of EphB/EphrinB,”Cell, 111:251-263, Oct. 18, 2002.
Behrens, J. et al., “Functional interaction of β-catenin with the transcription factor LEF-1,”Nature, 382:638-642, Aug. 15, 1996.
Bienz and Clevers, “Linking Colorectal Cancer to Wnt Signaling,”Cell, 103:311-320, Oct. 13, 2000.
Blanc-Brude, O. P. et al., “Inhibitor of apoptosis protein survivin regulates vascular injury,”Nature Medicine, 8(9):987-994, Sep. 2002.
Caca, K. et al., “β- and γ-Catenin Mutations, but not E-Cadherin Inactivation, Underlie T-Cell Factor/Lymphoid Enhancer Factor Transcriptional Deregulation in Gastric and Pancreatic Cancer,”Cell Growth&Differentiation, 10:369-376, Jun. 1999.
Cadigan and Nusse, “Wnt signaling: a common theme in animal development,”Genes&Development, 11:3286-3305, 1997.
Cecil Textbook of Medicine, edited by Bennet, J.C., and Plum F., 20th edition, vol. 1, 1004-1010, 1996.
Cheguillaume, A. et al., “New Potential Monomers for Solid Phase Synthesis of Hydrazinopeptoids: theNα-Substituted-Nβ-Protected Hydrazinoglycines and Hydrazinoglycinals,”Synlett2000, No. 3, pp. 331-334, Mar. 2000.
Chen, S. et al., “Wnt-1 Signaling Inhibits Apoptosis by Activating β-Catenin/T Cell Factor-mediated Transcription,”The Journal of Cell Biology, 152(1):87-96, Jan. 8, 2001.
Chenn and Walsh, “Regulation of Cerebral Cortical Size by Control of Cell Cycle Exit in Neural Precursors,”Science, 297:365-369, Jul. 19, 2002.
Chrivia, J.C. et al., “Phosphorylated CREB binds specifically to the nuclear protein CBP,”Nature, 365:855-859, Oct. 28, 1993.
Crawford, H.C. et al., “The metalloproteinase matrilysin is a target of β-catenin transactivation in intestinal tumors,”Oncogene, 18:2883-2891, 1999.
Daniels, D. L. et al., “β-catenin: molecular plasticity and drug design,”TRENDS in Biochemical Sciences, 26(11):672-678, Nov. 11, 2001.
DasGupta and Fuchs, “Multiple roles for activated LEF/TCF transcription complexes during hair follicle development and differentiation,”Development, 126:4557-4568, 1999.
Davis, P.D. et al., “ZD6126: A Novel Vascular-targeting Agent That Causes Selective Destruction of Tumor Vasculature,”Cancer Research, 62:7247-7253, Dec. 15, 2002.
De Ferrari and Inestrosa, “Wnt signaling function in Alzheimer's disease,”Brain Research Reviews, 33:1-12, 2000.
Dermer et al.,Bio/Technology12:320, 1994.
Dolle, R.E. “Comprehensive Survey of Combinatorial Library Synthesis: 1999,”Journal of Combinatorial Chemistry, 2(5):383-433, Sep./Oct. 2000.
Dooley and Houghten, “The use of positional scanning synthetic peptide combinatorial libraries for the rapid determination of opioid receptor ligands,”Life Sciences, 52(18):1509-1517, 1993.
Dooley, C.T. et al., “Acetalins: Opioid receptor antagonists determined through the use of synthetic peptide combinatorial libraries,”Proc. Natl. Acad. Sci. USA, 90:10811-10815, Nov. 1993.
Dooley, C.T. et al., “An All D-Amino Acid Opioid Peptide with Central Analgesic Activity from a Combinatorial Library,”Science, 266:2019-2022, Dec. 23, 1994.
Eckner, R. et al., “Molecular cloning and functional analysis of the adenovirus E1A-associated 300-kD protein (p300) reveals a protein with properties of a transcriptional adaptor,”Genes&Development, 8: 869-884, 1994.
Eguchi, M. et al., “Solid-phase synthesis and solution structure of bicyclic β-turn peptidomimetics: diversity at the i position,”Tetrahedron Letters, 42:1237-1239, 2001.
Eichler, J. et al., “Cyclic Peptide Template Combinatorial Libraries: Synthesis and Identification of Chymotrypsin Inhibitors,”Peptide Research, 7(6):300-307, 1994.
Fleisher, D. et al., “Improved Oral Drug Delivery: Solubility Limitations Overcome by the Use of Prodrugs,”Advanced Drug Delivery Reviews, 19:115-130, 1996.
Fraser, P.E. et al., “Presenilin function: connections to Alzheimer's disease and signal transduction,”Biochem. Soc. Symp., 67:89-100, 2001.
Freshney et al,Culture of Animal Cells, A Manual of Basic Technique, Alan R. Liss, Inc., 1983, New York, p4.
Fuchs, E., “Beauty is Skin Deep: The Fascinating Biology of the Epidermis and its Appendages,”The Harvey Lectures, Delivered Under the Auspices of the Harvey Society of New York, 1998-1999, Wiley-Liss, A John Wiley & Sons, Inc., Publication, Series 94, 47-48, 2000.
Fujimuro, M. et al., “A novel viral mechanism for dysregulation of β-catenin in Kaposi's sarcoma-associated herpesvirus latency,”Nature Medicine, 9(
Chung Jae Uk
Eguchi Masakatsu
Balasubramanian Venkataraman
Choongwae Pharma Corporation
Seed IP Law Group PLLC
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