Purinones and 1H-imidazopyridinones as PKC-theta inhibitors

Details Purinones and 1H-imidazopyridinones as PKC-theta inhibitors Purinones and 1H-imidazopyridinones as PKC-theta inhibitors

2011-08-02

2011-08-02

Berch, Mark (Department: 1622)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S263220, C514S263230, C514S263370, C544S230000, C544S276000, C544S323000, C544S326000, C546S119000, C546S279100, C546S276400

Reexamination Certificate

active

07989459

ABSTRACT:
A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKCθ. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I:whereinR1is chosen from nitrogen-attached heterocyclyl, nitrogen-attached substituted heterocyclyl wherein the point of attachment is a nitrogen heteroatom, andR2is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl.A representative example is:

REFERENCES:
patent: 4247556 (1981-01-01), von Bebenburg et al.
patent: 4813998 (1989-03-01), Van Lommen et al.
patent: 5493011 (1996-02-01), Jung et al.
patent: 5705625 (1998-01-01), Civin et al.
patent: 5916792 (1999-06-01), Civin et al.
patent: 6313129 (2001-11-01), Uckun et al.
patent: 6372740 (2002-04-01), Murata et al.
patent: 6432947 (2002-08-01), Arnaiz et al.
patent: 6452005 (2002-09-01), Uckun et al.
patent: 6506738 (2003-01-01), Yu et al.
patent: 6582357 (2003-06-01), Ouchi et al.
patent: 2004/0116435 (2004-06-01), Eriksson et al.
patent: 2004/0116449 (2004-06-01), Changelian
patent: 2004/0157739 (2004-08-01), Ahrens et al.
patent: 2005/0032725 (2005-02-01), Rao et al.
patent: 2007/0021443 (2007-01-01), Ohlmeyer et al.
patent: 2007/0253896 (2007-11-01), Le Brazidec et al.
patent: 2008/0085898 (2008-04-01), Lu et al.
patent: 2008/0119496 (2008-05-01), Ohlmeyer et al.
patent: 2008/0207613 (2008-08-01), Styles et al.
patent: 2008/0214580 (2008-09-01), Neagu et al.
patent: 2008/0220256 (2008-09-01), Bhattacharya et al.
patent: 2008/0254029 (2008-10-01), Yanni et al.
patent: 2008/0287468 (2008-11-01), Ohlmeyer et al.
patent: 2009/0023723 (2009-01-01), Cole et al.
patent: 2009/0069289 (2009-03-01), Neagu et al.
patent: 2009/0281075 (2009-11-01), Roughton et al.
patent: 2010/0093998 (2010-04-01), Isobe et al.
patent: 2010/0099870 (2010-04-01), Isobe et al.
patent: 2010/0120799 (2010-05-01), Lazarides et al.
patent: 2010/0130491 (2010-05-01), Bonnert et al.
patent: 2011/0046131 (2011-02-01), Neagu et al.
patent: 2238689 (1997-05-01), None
patent: 2841209 (1979-04-01), None
patent: 10 2005 042742 (2007-03-01), None
patent: 0 277 384 (1988-08-01), None
patent: 0 807 629 (1997-11-01), None
patent: 1043324 (2000-10-01), None
patent: 1221444 (2002-07-01), None
patent: 07075798 (1995-03-01), None
patent: 2004 217582 (2004-08-01), None
patent: 99/41248 (1999-08-01), None
patent: 00/12089 (2000-03-01), None
patent: 01/19828 (2001-03-01), None
patent: WO 02/055521 (2002-07-01), None
patent: 03/051277 (2003-06-01), None
patent: 2004/043386 (2004-05-01), None
patent: 2004/099204 (2004-11-01), None
patent: WO 2005/023761 (2005-03-01), None
patent: 2005/066156 (2005-07-01), None
patent: 2006/069080 (2006-06-01), None
patent: WO 2006/074985 (2006-07-01), None
patent: WO 2006/087538 (2006-08-01), None
patent: WO 2006/091737 (2006-08-01), None
patent: 2006/096270 (2006-09-01), None
patent: 2006/108103 (2006-10-01), None
patent: 2007/035873 (2007-03-01), None
patent: WO 2007/058990 (2007-05-01), None
patent: WO 2007/140222 (2007-12-01), None
patent: WO 2007/146712 (2007-12-01), None
patent: WO 2008/043019 (2008-04-01), None
patent: WO 2008/043031 (2008-04-01), None
patent: WO 2008/051493 (2008-05-01), None
patent: WO 2008/051494 (2008-05-01), None
patent: WO 2008060301 (2008-05-01), None
patent: WO 2008/075196 (2008-06-01), None
patent: WO 2008143674 (2008-11-01), None
patent: WO 2008/152099 (2008-12-01), None
patent: WO 2009/062059 (2009-05-01), None
Bakavoli, M., Journal of Sciences, Islamic Republic of Iran (1995), 6(3), 158-162.
Cetkovic-Cvrlje et al., “Targeting Janus kinase 3 in the treatment of leukemia and inflammatory diseases,”Arch. Immunol. Ther. Exp., vol. 52, pp. 69-82 (2004.).
Ortmann et al., “Janus kinases and signal transducers and activators of transcription: their roles in cytokine signaling, development and immunoregulation,”Arthritis Res., vol. 2, pp. 16-32 (2000).
Yamaoka et al., “The Janus kinases (Jaks),”Genome Biology, vol. 5:253, pp. 253.1-253.6 (2004).
Uckun et al., “Structure-based Design of Novel Anticancer Agents,”Current Cancer Drug Targets, vol. 1(1), pp. 59-71 (2001).
Kawahara et al., “Critical role of the interleukin 2 (IL-2) receptor γ-chain associated Jak3 in the IL-2-induced c-fosand c-myc, but notbcl-2, gene induction,”Proc. Natl. Acad. Sci., vol. 92, pp. 8724-8728 (1995).
O'Shea et al., “A New Modality for Immunosuppression: Targeting the Jak/Stat Pathway,”Nature Reviews, vol. 3, pp. 555-564 (2004).
Papageorgiou et al., “Is Jak3 a new drug target for immunomodulation-based therapies?”TRENDS in Pharmacological Sciences, vol. 25(11), pp. 558-562 (2004).
Lin et al., “Constitutive Activation of Jak3/Stat3 in Colon Carcinoma Tumors and Cell Lines”,American Journal of Pathology, vol. 167(4), pp. 969-980 (2005).
Dana et al, “Role of Immunity and Inflammation in Corneal and Ocular Surface Disease Associated with Dry Eye,”Lacrimal Gland, Tear Film and Dry Eye Syndromes 3, pp. 729-738 (2002).
Nagelhout et al., “Preservation of Tear Film Integrity and Inhibition of Corneal Injury by Dexamethasone in a Rabbit Model of Lacrimal Gland Inflammation-Induced Dry Eye,”Journal of Ocular Pharmacology and Therapeutics, vol. 21(2), pp. 139-148 (2005).
Pflugfelder, S., “Perspective Anti-inflammatory Therapy for Dry Eye,”American Journal of Ophthalmology, vol. 137(2), pp. 337-342 (2004).
Amin et al., “Inhibition of Jak3 induces apoptosis and decreases anaplastic lymphoma kinase activity in anaplastic large cell lymphoma,”Oncogene, vol. 22, pp. 5399-5407 (2003).
Frantz, S., “Playing Dirty”,Nature, vol. 437, pp. 942-943 (2005).
Lai et al., “Jak3 activation is significantly associated with ALK expression in anaplastic large cell lymphoma,”Human Pathology, vol. 36, pp. 939-944 (2005).
Beijersbergen van Henegouwen GM et al., Hydrolysis of RRR0alpha-tocopheryl acetate (vitamin # acetate) in the skin and its UV protecting activity (an in vivo study with the rat)J Photochem Photobiol, Jul. 29, 2005, vol. 1, pp. 45-51.
Cadena-Amaro et al., Bioorganic & Medicinal Chemistry Letters, 2005, vol. 15, Issue 4, pp. 1069-1073.
Chem Abstracts Search #1 1996:496070 CAPLUS: Bakavoli et al., Synthesis of 4,5′-bis-pyrimidines and some related bis-fused pyrimidines, Journal of Sciences, Islamic Republic of Iran (1995), 6(3), 158-162.
Chem Abstracts Search #2 1980:604652 CAPLUS: Brazilian patent No. BR 7806210, Apr. 1, 1980.
Frankowski, Synthesis of imidazo [4,5-c][1,2]diazepine systems and their ribonucleosides, Tetrahedron, 1986, vol. 42, Issue 5, pp. 1511-1528.
Gaulon et al., A General and Facile Route to New Trisubstituted Purin-8-ones, Synthesis, Jul. 2005, p. 2227.
International Search Report dated Mar. 20, 2009 in International Application No. PCT/US2008/082832, filed Nov. 7, 2008.
Lum et al., 2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as hinhibitors of glycogen synthase kinase-3 (GSK-3), Bioorganic & Medicinal Chemistry Letters, 2008, vol. 18, Issue 12, pp. 3578-3581.
Pochet et al., Construction of a self-complementary nucleoside from deoxyguanosine, Comptes Rendus de l'Academie des Sciences, Serie III: Sciences de la Vie, 1996, vol. 319, Issue 1, pp. 1-7.
Rokos et al., 8.2-Anhydro-8-Hydroxypurine αD-Ribosides, J. Carbohydrates, Nucleosides, Nucleotides, 1976, vol. Issue 77-91.
International Search Report dated Jan. 9, 2007 in International Application No. PCT/US2006/036833, filed Sep. 21, 2006.
International Search Report dated Jan. 7, 2010 in International Application No. PCT/US2009/048062, filed Jun. 19, 2009.
International Search Report from International Application No. PCT/US2007/080447, 2008.
International Search Report from International Application No. PCT/US2007/080464, 2008.
Cetkovic-Cvrlje et al., “Dual Targeting of Burton's Tyrosine Kinase and Janus Kinase 3 with Rationally Designed Inhibitors Prevents Graft-Versus-Hos

Affiliated with

Also associated with

Rating

Purinones and 1H-imidazopyridinones as PKC-theta inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Purinones and 1H-imidazopyridinones as PKC-theta inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Purinones and 1H-imidazopyridinones as PKC-theta inhibitors will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2756024