Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid...

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

C546S114000

Reexamination Certificate

active

11206707

ABSTRACT:
Disclosed are compounds of formula (I):wherein R1and R2are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

REFERENCES:
patent: 5350748 (1994-09-01), Boschelli et al.
patent: 5656638 (1997-08-01), Gaeta et al.
patent: 5852046 (1998-12-01), Lang et al.
patent: 6232320 (2001-05-01), Stewart et al.
patent: 6313301 (2001-11-01), Miki et al.
patent: 6358978 (2002-03-01), Ritzeler et al.
patent: 6579882 (2003-06-01), Stewart et al.
patent: 6964956 (2005-11-01), Cywin et al.
patent: 6974870 (2005-12-01), Cywin et al.
patent: 7119102 (2006-10-01), Chen et al.
patent: 7291733 (2007-11-01), Cywin et al.
patent: 2001/0020030 (2001-09-01), Stewart et al.
patent: 2005/0038104 (2005-02-01), Chen et al.
patent: 2005/0282866 (2005-12-01), Ritzeler et al.
patent: 2006/0019976 (2006-01-01), Karp et al.
patent: 2006/0270671 (2006-11-01), Chen et al.
patent: 194198 (2005-07-01), None
patent: WO 92/03427 (1992-03-01), None
patent: 34548 (1995-12-01), None
patent: WO 00/61586 (2000-10-01), None
patent: WO 00/75145 (2000-12-01), None
patent: 00610 (2001-01-01), None
patent: 30774 (2001-05-01), None
patent: WO 01/30774 (2001-05-01), None
patent: 58890 (2001-08-01), None
patent: WO 01/58890 (2001-08-01), None
patent: 68648 (2001-09-01), None
patent: WO 01/68648 (2001-09-01), None
patent: 41843 (2002-05-01), None
patent: 051849 (2002-07-01), None
patent: 037886 (2003-05-01), None
patent: WO 03/037886 (2003-05-01), None
patent: 072561 (2003-09-01), None
patent: 103661 (2003-12-01), None
patent: WO 01/00610 (2004-01-01), None
patent: 030031 (2006-03-01), None
patent: 043145 (2006-04-01), None
U.S. Appl. No. 11/836,590, filed Aug. 9, 2007; Substituted Tricyclic Heterocycles and Their Uses.
M-J Yin, et al., “The Anti-Inflammatory agents aspirin and salicylate inhibit the activity of IkB Kinase-B”, Nature, vol. 396, p. 77, 1998.
G. Warner, et al., “Synthese neuer Pyrido[3′,2′:4,5]thieno[3,2-d]1,2,3-triazin-Derivate als Antianaphylaktika”, Pharmazie, 1993, v48, p. 514.
K. Takeda, et al., “Limb and Skin Abnormalities in Mice Lacking IKKalpha”, Science, vol. 284, p. 313, 1999.
A. O. Stewart, et al., “Discovery of Inhibitors of Cell Adhesion Molecule Expression in Human Endothelial Cells, 1. Selective Inhibition of ICAM-1 and E-Selectin Expression”, J. Med. Chem., vol. 44, p. 988, 2001.
U. Siebenlist, et al., “Structure, Regulation, and Function of NF-kB”, Ann. Rev. Cel.l Biol. vol. 10, p. 405, 1994.
A.M. Shestopalov, et al., “Synthesis Based on 2-Aryl-3-Aroyl-1,1-Dicyanopropanes”, J. Org. Chem USSR Eng Trns, v20, p. 1382, 1984.
Y. Sharanin, et al., “Cyclizations of Nitriles. LVI. * Synthesis and Transformations of Substituted 6-Aryl-3-cyano-4-(2-thienyl)-pyridine-2(1H)-thiones”, J. Org. Chem USSR. Eng TRNS, v32, No. 8, p. 1207, 1996 Translated from Zhurnal Organicheskoi Khimii vol. 32, No. 8, 1996, pp. 1251.
U. Senftleben, et al., “Activation by IKKalpha of a Second, Evolutionary Conserved, NF-kB Signaling Pathway”, Science, vol. 293, p. 1495, 2001.
R. Seetharaman, et al., “Essential Role of T Cell NF-kB Activation in Collagen-Induced Arthitis”, J. Immunology, vol. 163, p. 1577, 1999.
V.J. Palombella, et al., “The Ubiquitin-Proteasome Pathway is Required for Processing the NF-kB1 Precursor Protein and the Activation of NF-kB”, Cell, vol. 78, p. 773, 1994.
A. Pahl, et al., “Asthma Therapy in the New Millennium”, Inflammation Research, vol. 51, p. 273, 2002.
P. Libby, “Atherosclerosis: The New View”, Scientific American, p. 46, 2002.
Q. Li, et al., “Severe Liver Degeneration in Mice Lacking the IkB Kinase 2 Gene”, Science, vol. 284, p. 321, 1999.
I. Lavon, et al., “High Susceptibility to Bacterial Infection, But no Liver Dysfunction, in Mice Compromised for Hepatocyte NF-kB activation”, Nature Medicine, vol. 6, No. 5, p. 573, 2000.
A. Krauze, et al., “Derivatives of 3-cyano-6-phenyl-4-(3′-pyridyl)-pyridine-2(1H)-Thione and their Neurotropic Activity”, Eur. J. Med. Chem, vol. 34, p. 301, 1999.
M. Karin, et al., “The IkB Kinase (IKK) and NF-kB: key elements of Proinflammatory Signalling”, Seminars in Immunology, vol. 12, p. 85, 2000.
M. Karin, et al., “NF-kB in Cancer: From Innocent Bystander to Major Culprit”, Nature Reviews Cancer, vol. 2, p. 301, 2002.
C. Jobin, et al., “Inhibition of Proinflammatory Molecule Production by Adenovirus-Mediated Expression of a Nuclear Factor kB Super-Repressor in Human Intestinal Epithelial Cells”, J. Immunology, vol. 160, p. 410, 1998.
Y. Hu et al., “Abnormal Morphogenesis but Intact IKK Activation in Mice Lacking the IKKalpha Subunit of IkB Kinase”, Science, vol. 284, p. 316, 1999.
B. Haefner, “NF-kB: Arresting a Major Culprit in Cancer”, Drug Discovery Today, vol. 7, No. 12, p. 653, 2002.
A. Gause, et al., “Role of B Cells in the Pathogenesis of Rheumatoid Arthritis”, Biodrugs, vol. 15, No. 2, p. 73, 2001.
A. Distefano, et al., “Increased Expression of Nuclear Factor-kB in Bronchial Biopsies from Smokers and Patients with COPD”, Eur. Respir. J., vol. 20, p. 556, 2002.
O.T.M. Chan, et al., “The Central and Multiple roles of B Cells in Lupus Pathogenesis”, Immunological Review, vol. 169, p. 107, 1999.
Y. Cao, et al., “IKKalpha Provides an Essential Link between Rank Signaling and Cyclin D1 Expression during Mammary Gland Development”, Cell, vol. 107, p. 763, 2001.
J. Bondeson, et al., “Defining therapeutic targets by using adenovirus: Blocking NF-kB inhibits both inflammatory and destructive mechanisms in rheumatoid synovium but spares anti-inflammatory mediators”, Proc. Natl. Acad. Sci. USA, vol. 96, p. 5668, 1999.
A.A. Beg, et al., “An Essential Role for NF-kB in Preventing TNF-alpha-Induced Cell Death”, Science, vol. 274, p. 782, 1996.
P.J. Barnes, “New Treatment for COPD”, Nature Reviews Drug Discovery, vol. 1, p. 437, 2002.
P.A. Baeuerle, et al., “NF-kB: Ten Years After”, Cell, vol. 87, p. 13, 1996.
F.A. Attaby, “Reactions of Styrylthienyl Ketone, Styryl Furyl Ketone with Thiocyanoacetamide . . . ”, Phosphorus, Sulfur, and Silicon, V139, n1, pp. 1-12 1998.
M.I. Abdel-Monem, et al., “Fluorine-containing heterocycles: synthesis and some reactions of new 3-amino-2-functionalized-6-(2′-thienyl)-4-trifluoromethylthieno[2,3-b]pyridines”, Pharmazie, vol. 56, No. 1, p. 41, 2001.
Karin, et al. “The IKK NF-kB System: A Treasure Trove for Drug Development” Nature Reviews Drug Discovery, 2004, vol. 3, No. 1, p. 17.
Nakanishi, et al., Nature Reviews Cancer Apr. 2005, v5, p. 297.
Sausville, et al., “Contributions of human tumor xenografts to anticancer drug development” Cancer Research, 2006, vol. 66, p. 3351.
Johnson, et al., “Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials.” British J. of Cancer, 2001, vol. 84, No. 10, p. 1424.
Vitali, T., et al., “Proprieta Biologiche di Composti 1,2-benzisotiazolici” Ateneo Parmense Acta Naturalia, vol. 7, No. 1, 1971, p. 71-109, xp009040652.
S.W. Schneller, et al., “Fused Thieno[3,2-d]-v-Triazine-4(3H)-Ones”, Heterocycles, vol. 3, No. 2, 1975, p. 135-138, xp009040651.
Beck, J.R., et al., “Synthesis of [1] Benzothieno [3,2-d]-v-triazine Derivatives. A unique Diazonium Ion Cyclization”, J. Org. Chem., vol. 41, No. 10, 1976, pp. 1733-1734, XP002244950.
J. Markert, et al., “Neue Synthesen Mit Elementarem Schwefei Darstellung Von 1,2-Benzisothiazolen

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

Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3921053

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