Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2005-01-13
2009-10-20
Stockton, Laura L. (Department: 1626)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C546S270700, C514S286000
Reexamination Certificate
active
07605264
ABSTRACT:
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I)or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein A, B, J, K, Z, R, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
REFERENCES:
patent: 3517073 (1970-06-01), Fields
patent: 4786646 (1988-11-01), Guthrie et al.
patent: 5055468 (1991-10-01), Gray et al.
patent: 5202486 (1993-04-01), Barrish et al.
patent: 5332820 (1994-07-01), Duncia
patent: 5409932 (1995-04-01), Schwenner et al.
patent: 5411960 (1995-05-01), Schwenner et al.
patent: 5455248 (1995-10-01), DeHaven-Hudkins et al.
patent: 5514683 (1996-05-01), Kalindjian et al.
patent: 5569655 (1996-10-01), Dority, Jr. et al.
patent: 5616780 (1997-04-01), Pitteloud et al.
patent: 6214915 (2001-04-01), Avakian et al.
patent: 6262059 (2001-07-01), Pamukcu et al.
patent: 6291679 (2001-09-01), Mailliet et al.
patent: 6995181 (2006-02-01), Vaccaro
patent: 7326728 (2008-02-01), Yang
patent: 2004/0132758 (2004-07-01), Vaccaro
patent: 2005/0171136 (2005-08-01), Vaccaro
patent: 2005/0176716 (2005-08-01), Duan
patent: 2005/0176749 (2005-08-01), Yang
patent: 2005/0182082 (2005-08-01), Duan
patent: 2005/0182110 (2005-08-01), Yang
patent: 2005/0187242 (2005-08-01), Weinstein
patent: 2006/0154962 (2006-07-01), Yang
patent: 2006/0154973 (2006-07-01), Sheppeck
patent: 2006/0154975 (2006-07-01), Yang
patent: 198 678 (1982-11-01), None
patent: 197 42 014 (1999-03-01), None
patent: 0 405 436 (1995-11-01), None
patent: WO 93/16982 (1993-09-01), None
patent: WO 94/00421 (1994-01-01), None
patent: WO 95/05359 (1995-02-01), None
patent: WO 95/15947 (1995-06-01), None
patent: WO 99/15493 (1999-04-01), None
patent: WO 02/051851 (2002-07-01), None
patent: WO 03/062241 (2003-07-01), None
patent: WO 03/101932 (2003-12-01), None
patent: WO 03/104195 (2003-12-01), None
patent: WO 2004/000869 (2003-12-01), None
patent: WO 2004/005229 (2004-01-01), None
patent: WO 2004/009017 (2004-01-01), None
patent: 681802 (1968-03-01), None
Souillac, et al., Characterization of Delivery Systems, Differential Scanning Calorimetry in Encyclopedia of Controlled Drug Delivery, 1999, John Wiley & Sons, pp. 212-227.
Vippagunta et al., Advanced Drug Delivery Reviews, 48 (2001), pp. 3-26.
Alibert, S. et al., “Synthesis and Effects on Chloroquine Susceptibility inPlasmodium falciparumof a Series of New Dihydroanthracene Derivatives”, Journal of Medicinal Chemistry, vol. 45, No. 15, pp. 3195- 3209 (2002).
Compounds (by Registry Number) with no references in the Chemical Abstracts file: 500280-08-0, 496959-82-1, 332907-97-8, 331751-07-6, 331427-65-7, 312317-98-9, 312315-55-2, 311331-77-8.
El-Zanfally, S. et al., “Reactions of Aminopyridines with some Inner Anhydrides”, Egypt J. Pharm. Sci., vol. 17, No. 3, pp. 53-62 (1976).
Kotha, S. et al., “Synthesis of highly constrained unusual 60 -amino acid derivative by the Diels-Alder approach”, Indian Journal of Chemistry, vol. 41B, pp. 2330-2332 (2002).
Pradines, B. et al., “In Vitro Increase in Chloroquine Accumulation Induced by Dihydroethano- and Ethenoanthracene Derivatives inPlasmodium falciparum-Parasitized Erythrocytes”, Antimicrobial Agents and Chemotherapy, vol. 46, No. 7, pp. 2061-2068 (2002).
Baldwin, Jr., A.S., “The transcription factor NE-κB and human disease”, The Journal of Clinical Investigation, vol. 107, No. 1, pp. 3-6 (2001).
Bradsher, C.K. et al., “Acridizinium Ion Chemistry. II. The Diels-Alder Reaction”, Journal of the American Chemical Society, vol. 80, pp. 933-934 (1958).
Bradsher, C.K. et al., “Addition of Dienophiles to the Acridizinium Ion. III. Evidence for a Two-Step Reaction”, The Journal of Organic Chemistry, vol. 34, No. 6, pp. 1700-1702 (1969).
Bradsher, C.K. et al., “Cationic Polar Cycloaddition of Cyclopropenes”, J. Org. Chem., vol. 44, No. 8, pp. 1199-1202 (1979).
Bradsher, C.K. et al., “Possible Role of Charge-Transfer Complexes in Cationic Polar Cycloaddition”, J. Org. Chem., vol. 43, No. 5, pp. 822-827 (1978).
Bradsher, C.K. et al., “Stereoselectivity Due to Electrostatic Repulsion in the Polar Cycloaddition of the Acridizinium Ion”, J. Het. Chem., vol. 10, pp. 1031-1033 (1973).
Bradsher, C.K. et al., “Steric Effects in Some Cycloaddition Reactions”, Journal of the American Chemical Society, vol. 99, No. 8, pp. 2588-2591 (1977).
Bradsher, C.K. et al., “The Nature of the Addition of Dienophiles to the Acridizinium Ion”, The Journal of Organic Chemistry, vol. 33, No. 2, pp. 519-523 (1968).
Burke, J.R., “Targeting IκB kinase for the treatment of inflammatory and other disorders”, Current Opinion in Drug Discovery & Development, vol. 6, No. 5, pp. 720-728 (2003).
Burnham, W.S. et al., “6,11-Dihydroacridizinium Derivatives Having a 6,11-Etheno Bridge”, J. Org. Chem., vol. 37, No. 3, pp. 355-358 (1972).
Caldenhoven, E. et al., “Negative Cross-Talk between ReIA and the Glucocorticoid Receptor: A Possible Mechanism for the Antiinflammatory Action of Glucocorticoids”, Molecular Endocrinology, vol. 9, No. 4, pp. 401- 412 (1995).
Chakravarti, D. et al., “Role of CBP/P300 in nuclear receptor signalling”, Nature, vol. 383, pp. 99-103 (1996).
Diamond, M.I. et al., “Transcription Factor Interactions: Selectors of Positive or Negative Regulation from a Single DNA Element”, Science, vol. 249, pp. 1266-1272 (1990).
Fields, D.L., “A Novel Synthesis of 2-Naphthols, Phenanthrols, Anthracenes, and Other Polycyclic Aromatic Products”, J. Org. Chem., vol. 36, No. 20, pp. 3002-3005 (1971).
Fields, D.L. et al., “Azonia Polycyclic Quinones, o-Diazo-Oxides and Related Products”, J. Het. Chem., vol. 7, pp. 91-97 (1970).
Fields, D.L. et al., “Cleavage Reactions of Bicyclic Ketones Derived from Azoniaanthracene-Ketene Acetal Adducts”, J. Org. Chem., vol. 35, No. 6, pp. 1870-1875 (1970).
Fields, D.L. et al., “Diels-Alder Reactions Involving Azonia Polycyclic Aromatic Compounds and Nucleophilic Dienophiles”, J. Org. Chem., vol. 33, No. 1, pp. 390-395 (1968).
Fields, D.L. et al., “Overcrowded Molecules. I. Substituted 8-tert-Butyl-1-(2-pyridyl)naphthalenes, Including a Thermodynamically Stable Ketonic Tautomer”, J. Org. Chem., vol. 36, No. 20, pp. 2986-2990 (1971).
Fields, D.L. et al., “Overcrowded Molecules. II. 4,5-Bis(2-pyridyl)phenanthrene-3,6-diols”, J. Org. Chem., vol. 36, No. 20, pp. 2991-2995 (1971).
Fields, D.L. et al., “Overcrowded Molecules. III. 13,14-Bis(2- pyridyl)pentaphene and Related Compounds”, J. Org. Chem., vol. 36, No. 20, pp. 2995-3001 (1971).
Firestein, G.S. et al., “Signal Transduction and Transcription Factors in Rheumatic Disease”, Arthritis & Rheumatism, vol. 42, No. 4, pp. 609-621 (1999).
Hart, H. et al., “1,4,5,8,9-pentamethylanthracene, Synthesis and Protonation”, Tetrahedron Letters, vol. 16, No. 52, pp. 4639-4642 (1975).
Jackson, R.W. et al., “Benzobicyclooctanes as Novel Inhibitors of TNF-α Signaling”, Bioorganic & Medicinal Chemistry Letters, vol. 12, pp. 1093- 1097 (2002).
Jonat, C. et al., “Antitumor Promotion and Antiinflammation: Down-Modulation of AP-1 (Fos/Jun) Activity by Glucocorticoid Hormone”, Cell, vol. 62, pp. 1189-1204 (1990).
Kamei, Y. et al., “A CBP Integrator Complex Mediates Transcriptional Activation and AP-1 Inhibition by Nuclear Receptors”, Cell, vol. 85, pp. 403-414 (1996).
Manning, A.M. et al., “Targeting JNK for Therapeutic Benefit: From Junk to Gold”, Nature Reviews D
Gilmore John L.
Sheppeck James
Weinstein David S.
Bristol--Myers Squibb Company
Duncan Laurelee A.
Stockton Laura L.
LandOfFree
Heterocyclic modulators of the glucocorticoid receptor,... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Heterocyclic modulators of the glucocorticoid receptor,..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Heterocyclic modulators of the glucocorticoid receptor,... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4073051