Chemical compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

Reexamination Certificate

active

07858796

ABSTRACT:
The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I:where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof.The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

REFERENCES:
patent: 4775761 (1988-10-01), Strupczewski
patent: 5256673 (1993-10-01), Böttcher et al.
patent: 5330986 (1994-07-01), Shutske
patent: 6245799 (2001-06-01), Asselin et al.
patent: 2002/0147189 (2002-10-01), Cai et al.
patent: 2002/0161004 (2002-10-01), Browner et al.
patent: 2003/0022898 (2003-01-01), Burke et al.
patent: 3342632 (1985-06-01), None
patent: 19500689 (1996-07-01), None
patent: 19807993 (1999-09-01), None
patent: 19928424 (2000-12-01), None
patent: 10112151 (2002-09-01), None
patent: 10259244 (2004-07-01), None
patent: 279263 (1993-08-01), None
patent: 610134 (1994-08-01), None
patent: 416609 (1997-01-01), None
patent: 0812826 (1997-12-01), None
patent: 1077213 (2001-02-01), None
patent: 1134221 (2001-09-01), None
patent: 1209158 (2002-05-01), None
patent: WO9917773 (1999-04-01), None
patent: WO0130774 (2001-05-01), None
patent: WO0134598 (2001-05-01), None
patent: WO0158890 (2001-08-01), None
patent: WO0168648 (2001-09-01), None
patent: WO0183472 (2001-11-01), None
patent: WO0187298 (2001-11-01), None
patent: WO0198290 (2001-12-01), None
patent: WO0214317 (2002-02-01), None
patent: WO0216353 (2002-02-01), None
patent: WO0224679 (2002-03-01), None
patent: WO0228860 (2002-03-01), None
patent: WO0230353 (2002-04-01), None
patent: WO0230423 (2002-04-01), None
patent: WO0241843 (2002-05-01), None
patent: WO0244153 (2002-06-01), None
patent: WO0246171 (2002-06-01), None
patent: WO02051837 (2002-07-01), None
patent: WO02060386 (2002-08-01), None
patent: WO02094265 (2002-11-01), None
patent: WO02094322 (2002-11-01), None
patent: WO02094813 (2002-11-01), None
patent: WO03070706 (2003-01-01), None
patent: WO03010158 (2003-02-01), None
patent: WO03010163 (2003-02-01), None
patent: WO03022898 (2003-03-01), None
patent: WO03024935 (2003-03-01), None
patent: WO03024936 (2003-03-01), None
patent: WO03027075 (2003-04-01), None
patent: WO03035625 (2003-05-01), None
patent: WO03037886 (2003-05-01), None
patent: WO03084959 (2003-10-01), None
patent: WO03095430 (2003-11-01), None
patent: WO03103661 (2003-12-01), None
patent: WO2004019935 (2004-03-01), None
patent: WO2004022553 (2004-03-01), None
patent: WO2004024730 (2004-03-01), None
patent: WO2004024732 (2004-03-01), None
patent: WO2004024736 (2004-03-01), None
patent: WO2004075846 (2004-09-01), None
patent: WO2004089913 (2004-10-01), None
patent: WO2004106293 (2004-12-01), None
patent: WO2005012283 (2005-02-01), None
patent: WO2005035537 (2005-04-01), None
patent: WO 2005/067923 (2005-07-01), None
patent: WO2005067923 (2005-07-01), None
patent: WO2007/005534 (2007-01-01), None
C. G. Wermuth.The Practice of Medicinal Chemistry, Academic Press, pp. 203-214 (1996).
Abstract No. 98323-88-7 (Sep. 29, 1985).
Abstract No. 98323-88-7 (Sep. 29, 1985).
Aupperle et al., “NF-κB Regulation by IκB Kinase in Primary Fibroblast-Like Synoviocytes”J. Immunology(1999) 163:427-433.
Aupperle et al., “NF-κB Regulation by IκB Kinase-2 in Rheumatoid Arthritis Synoviocytes”J. Immunology(2001) 166:31496-31501.
Breton et al., “The Natural Product Hymenialdisine Inhibits Interleukin-8 Production in U937 Cells by Inhibition of Nuclear Factor-κB”JPET(1997) 282(1):459-466.
Burke et al., “BMS-345541 Is a Highly Selective Inhibitor of IκB Kinase That Binds at an Allosteric Site of the Enzyme and Blocks NF-κB-dependent Transcription in Mice”J. Biol Chem. (2003) 278:1450-1456.
Guttridge et al., “NF-κB-Induced Loss ofMyoDMessenger RNA: Possible Role in Muscle Decay and Cachexia”Science(2000) 289:2363-2365.
Murata et al., “Discovery of novel and selective IKK-β serine-threonine protein kinase inhibitors. Part 1.”Bioorg. Med. Chem. Letter(2003) 13:913-198.
Murata et al., “Synthesis and structure—activity relationships of novel IKK-β inhibitors. Part 2: Improvement of in vitro activity”Bioorg. Med. Chem. Letter(2004) 14(15):4013-4017 and “Synthesis and structure—activity relationships of novel IKK-β inhibitors. Part 3: Orally active anti-inflammatory agents,”Bioorg. Med. Chem. Letter(2004) 14(15):4019-4022.
Peet et al., “IκB Kinases α and β Show a Random Sequential Kinetic Mechanism and Are Inhibited by Staurosporine and Quercetin”J. Biol. Chem. (1999) 274:32655-32661.
Pierce, et al., “Novel Inhibitors of Cytokine-induced IκBα Phosphorylation and Endothelial Cell Adhesion Molecule Expression Show Anti-inflammatory Effects in Vivo”J. Biol. Chem. (1997) 272:21096-21103.
Roshak, et al., “Inhibition of NFκB-Mediated Interleukin-1β Stimulated Prostaglandin E2Formation by the Marine Natural Product Hymenialdisine”JPET(1997) 283(2):955-961.
Roshak, et al., “Manipulation of Distinct NFκB Proteins Alters Interleukin-1β-induced Human Rheumatoid Synovial Fibroblast Prostaglandin E2Formation”J. Biol. Chem. (1996) 271:31496-31501.
Sullivan et al., “2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3′,5′ -bis(trifluoromethyl)phenyl)-carboxamide: A Potent Inhibitor of NF-κB- and AP-1-Mediated Gene Expression Identified Using Solution-Phase Combinatorial Chemistry”J. Med. Chem. (1998) 41:413-419.
Tak et al., “Inhibitor of nuclear factor κB kinase β is a key regulator of synovial inflammation”Arthritis and Rheumatism(2001) 44(8):1897-1907.
Wahl et al., “Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B”J. Clin. Invest.(1998) 101(5):1163-1174.
Wisniewski et al., “Assay for IκB Kinases Using an in Vivo Biotinylated IκB Protein Substrate”Analytical Biochem. (1999) 274:220-228.

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

Chemical compounds does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Chemical compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Chemical compounds will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-4182544

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