PPAR active compounds

Details PPAR active compounds PPAR active compounds

2007-02-27

2009-02-17

Saeed, Kamal A (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C548S400000, C548S416000, C548S452000, C514S359000, C514S408000, C514S410000, C514S412000, C514S415000

Reexamination Certificate

active

07491831

ABSTRACT:
Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.

REFERENCES:
patent: 3489767 (1970-01-01), Yamamoto et al.
patent: 3511841 (1970-05-01), Archer et al.
patent: 4150949 (1979-04-01), Smith
patent: 4568649 (1986-02-01), Bertoglio-Matte
patent: 4626513 (1986-12-01), Burton et al.
patent: 5075313 (1991-12-01), Yu et al.
patent: 5283251 (1994-02-01), Okada et al.
patent: 5466689 (1995-11-01), Yamamoto et al.
patent: 5747276 (1998-05-01), Hoch et al.
patent: 5763198 (1998-06-01), Hirth et al.
patent: 5840485 (1998-11-01), Lebl et al.
patent: 5877007 (1999-03-01), Housey
patent: 6090912 (2000-07-01), Lebl et al.
patent: 6178384 (2001-01-01), Kolossvary
patent: 6243980 (2001-06-01), Bronstein et al.
patent: 6288234 (2001-09-01), Griffin
patent: 6294330 (2001-09-01), Michnick et al.
patent: 6329389 (2001-12-01), Suzuki et al.
patent: 6337344 (2002-01-01), Defossa et al.
patent: 6395768 (2002-05-01), Pappolla et al.
patent: 6635655 (2003-10-01), Jayyosi et al.
patent: 7348338 (2008-03-01), Arnold et al.
patent: 2004/0006071 (2004-01-01), Simoneau et al.
patent: 2005/0004115 (2005-01-01), Sharma et al.
patent: 2006/0111426 (2006-05-01), Bonnert et al.
patent: 2007/0149603 (2007-06-01), Arnold et al.
patent: 2008/0045581 (2008-02-01), Artis et al.
patent: 0 154 734 (1990-08-01), None
patent: 0620214 (1994-10-01), None
patent: 1219595 (2002-07-01), None
patent: 1285908 (2003-02-01), None
patent: 1661879 (2006-05-01), None
patent: 1128607 (1968-09-01), None
patent: 2407318 (2005-04-01), None
patent: WO 91/13060 (1991-09-01), None
patent: WO 9113060 (1991-09-01), None
patent: WO 9604906 (1996-02-01), None
patent: WO 00/64876 (2000-11-01), None
patent: WO 01/38305 (2001-05-01), None
patent: WO 02/30863 (2002-04-01), None
patent: WO 2004/056740 (2004-07-01), None
patent: WO 2005/009958 (2005-02-01), None
patent: WO 2005/037763 (2005-04-01), None
patent: WO 2005/040112 (2005-05-01), None
patent: WO 2005/044787 (2005-05-01), None
patent: WO 2005/054176 (2005-06-01), None
FDA Clinical Trials [online], [retrieved on Mar. 13, 2008]. Retrieved from the Internet, □□URL: http://www.fda.gov/oashi/clinicaltrials/default.htm.
Diabetes [online], [retrieved on Mar. 13, 2008]. Retrieved from the Internet, □□URL: http://www.merck.com/mmpe/print/sec12/ch158/ch158b.html.
Eczema [online], [retrieved on Mar. 13, 2008]. Retrieved from the Internet, □□URL: http://www.nlm.nih.gov/medlineplus/eczema.html.
Ulcerative Colitis [online], [retrieved on Mar. 3, 2008]. Retrieved from the Internet,□□URL: http://www.nlm.nih.gov/medlineplus/ulcerativecolitis.html.
Colitis [online], [retrieved on Mar. 13, 2008]. Retrieved from the Internet,□□ URL: http://www.nlm.nih.gov/medlineplus/ency/article/000259.htm.
Collagenous Colitis [online], [retrieved on Mar. 13, 2008]. Retrieved from the Internet,□□ URL: http://digestive.niddk.nih.gov/ddiseases/pubs/collagenouscolitis/index.htm.
Cancer [online], [retrieved Mar. 13, 2008]. Retrieved from the Internet, □□URL: http://www.nlm.nih.gov/medlineplus/cancer.html.
Lala et al. Cancer and Metastasis Reviews (1998), 17(1), 91.
Golub et al. Science (1999). 286, 531.
Buchan and Hassall, PPAR agonists as direct modulators of the vessel wall in cardiovascular disease. Med. Res. Rev. 20(5): 350-366, 2000.
VanZandt et al., Discovery of 3-[(4,5,7-Trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (Lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. J.Med.Chem., 48:3141-3152, 2005.
Mahindroo et al., Novel indole-based peroxisome proliferator-activated receptor agonists: Design, SAR, structural biology, and biological activities. J.Med.Chem. 48:8194-8208, 2005.
International Search Report from PCT Application PCT/US2006/034747, Feb. 7, 2007.
Aldred, et al., “Peroxisome proliferator-activated receptor gamma is frequently downregulated in a diversity of sporadic nonmedullary thyroid carcinomas,”Oncogene22:3412-3416 (2003).
Alfthan, “Surface Plasmon Resonance Biosensors as a Tool in Antibody Engineering,”Biosensors&Bioelectronics13:653-63 (1998).
Al-Obeidi, “Peptide and Peptidomimetic Libraries—Molecular Diversity and Drug Design,”Mol Biotechnol9(3):205-223 (1998).
Amersdorfer and Marks, “Phage Libraries for Generation of Anti-Botulinum scFv Antibodies,”Methods in Molecular Biology145:219-40 (2001).
Azimov, et al., “Nucleophilic Substitution Reactions in 6-Chlor-5-Azaindolines,”Chem. Heterocycl. Compd.17(12):1208-1216 (1981).
Bartlett et al., “CAVEAT: A Program to facilitate the structure-derived design of biologically active molecules.” In Molecular Recognition: Chemical and Biological Problems. The Proceedings of an International Symposium, University of Exeter, Apr. 1989,Royal Society of Chemistry, Cambridge I82-I96 (1989).
Bagshaw and Harris, “Measurement of Ligand Binding to Proteins,”Spectrophotometry and Spectrofluorometry: A Practical Approach4:91-114 (1987).
Bell, “Spectroscopy In Biochemistry,”CRC PressI:155-194 (1981).
Belletire, J.L., “Acylcyanamides: Versatile Synthetic Intermediates,”Synthetic Communications18:2063-2071 (1988).
Berger and Wagner, “Physiological and Therapeutic Roles of Peroxisome Proliferator-Activated Receptors,”Diabetes Technology&Therapeutics4:163-174 (2002).
Boehm, et al., “Novel Inhibitors and DNA Gyrase: 3D Structure Based Biased Needle Screening, Hit Validation by Biophysical Methods, and 3D Guided Optimization. A Promising Alternative to Random Screening,”J. Med. Chem.43:2664-2674 (2000).
Bohacek, et al., “Multiple Highly Diverse Structures Complementary to Enzyme Binding Sites: Results of Extensive Application of ade NovoDesign Incorporating Combinatorial Growth,”J. Am. Chem. Soc.116:5560-5571 (1994).
Böhm,“On the Use of LUDI to Search the Fine Chemicals Directory for Ligands of Proteins of Known Three-Dimensional Structure,”J. Comp. Aided Molec. Design 8:623 (1994).
Bolger and Sherman, “Computer Modeling of Combing Site Structure of Anti-Hapten Monocional Antibodies,”Methods Enz.203:21-45 (1991).
Brenner et al., “Encoded Combinatorial Chemistry,”Proc. Natl. Acad. Sci.USA 89:5381-5383 (1992).
Buchheit, et al., “The Serotonin 5-HT4Receptor. 2. Structure—Activity Studies of the Indole Carbazimidamide Class of Agonists,”J. Med. Chem.38:2331-2338 (1995).
Burstein, et al. “Use of the Peroxisome Proliferator-Activated Receptor (PPAR) γ Ligand Troglitazone as Treatment for Refractory Breast Cancer: a Phase II Study,”Breast Cancer Research and Treatment79:391-397 (2003).
Bychikhina, et al., “Electrophilic Substitution Reactions in 1-Benzyle-6-Methoxy-7-Cyano-5-Azaindole and 6-Oxo-5-Azaindoline,”Chemistry of Heterocyclic Compounds18:268-271 (1982).
Cantello, et al., “[[a-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as Potent Antihyperglycemic Agents,”J. Med. Chem.37:3977-3985 (1994).
Cao, et al., “Dual Probes for the Dopamine Transporter ando1Receptors: Novel Piperazinyl Alkyl-bis(4′-fluorophenyl)amine Analogues as Potential Cocaine-Abuse Therapeutic Agents,”J. Med. Chem.46:2589-2598 (2003).
Carell et al., “New Promise in Combinatorial Chemistry: Synthesis, Characterization, and Screening of Small-Molecule Libraries Solution,”Chem. Biol.3:171-183 (1995).
Chabala, “Solid-Phase Combinatorial Chemistry and Novel Tagging Methods for Identifying Leads,”Curr Opin Biotechnol6(6):633-9 (1995).
Checovich et al., “Fluorescence Polarization—a New Tool for Cell and Molecular Biology,”Nature375:254-256 (1995).
Cheung, et al., “Synthesis of 2-chloro-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin

Affiliated with

Also associated with

Rating

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

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-4068035