Substituted thieno[3,2-D]pyrimidines as melanin...

Details Substituted thieno[3,2-D]pyrimidines as melanin... Substituted thieno[3,2-D]pyrimidines as melanin...

2011-08-02

2011-08-02

Moore, Susanna (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Silicon containing doai

C514S260100, C514S081000, C544S278000, C544S229000

Reexamination Certificate

active

07989433

ABSTRACT:
The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof:

REFERENCES:
patent: 3674836 (1972-07-01), Creger
patent: 3983140 (1976-09-01), Endo et al.
patent: 4027009 (1977-05-01), Grier et al.
patent: 4231938 (1980-11-01), Monaghan et al.
patent: 4346227 (1982-08-01), Terahara et al.
patent: 4379785 (1983-04-01), Weyer et al.
patent: 4448784 (1984-05-01), Glamkowski et al.
patent: 4450171 (1984-05-01), Hoffman et al.
patent: 4499289 (1985-02-01), Baran et al.
patent: 4613610 (1986-09-01), Wareing
patent: 4639436 (1987-01-01), Junge et al.
patent: 4647576 (1987-03-01), Hoefle et al.
patent: 4681893 (1987-07-01), Roth
patent: 4686237 (1987-08-01), Anderson
patent: 4759923 (1988-07-01), Buntin et al.
patent: 4871721 (1989-10-01), Biller
patent: 4904769 (1990-02-01), Rauenbusch
patent: 4924024 (1990-05-01), Biller
patent: 5006530 (1991-04-01), Angerbauer et al.
patent: 5011930 (1991-04-01), Fujikawa et al.
patent: 5177080 (1993-01-01), Angerbauer et al.
patent: 5260440 (1993-11-01), Hirai et al.
patent: 5273995 (1993-12-01), Roth
patent: 5354772 (1994-10-01), Kathawala
patent: 5385929 (1995-01-01), Bjorge et al.
patent: 5434150 (1995-07-01), Austel et al.
patent: 5447954 (1995-09-01), Gribble et al.
patent: 5488064 (1996-01-01), Sher
patent: 5491134 (1996-02-01), Sher et al.
patent: 5506219 (1996-04-01), Robl
patent: 5541204 (1996-07-01), Sher et al.
patent: 5594016 (1997-01-01), Ueno et al.
patent: 5612359 (1997-03-01), Murugesan
patent: 5686104 (1997-11-01), Mills et al.
patent: 5691322 (1997-11-01), Robl
patent: 5698527 (1997-12-01), Kim
patent: 5712396 (1998-01-01), Magnin et al.
patent: 5753675 (1998-05-01), Wattanasin
patent: 5770615 (1998-06-01), Cheng et al.
patent: 5776983 (1998-07-01), Washburn et al.
patent: 5990145 (1999-11-01), Wehner et al.
patent: 6011045 (2000-01-01), Wehner et al.
patent: 6043265 (2000-03-01), Murugesan et al.
patent: 6414002 (2002-07-01), Cheng et al.
patent: 6482821 (2002-11-01), Wehner et al.
patent: 7553836 (2009-06-01), Zhao
patent: 7745447 (2010-06-01), Washburn et al.
patent: 2007/0093509 (2007-04-01), Washburn et al.
patent: 196 22 222 (1997-04-01), None
patent: 0 142 146 (1985-05-01), None
patent: 0 221 025 (1987-05-01), None
patent: 0 531 883 (1993-03-01), None
patent: 0 675 714 (1995-10-01), None
patent: 0 818 448 (1998-01-01), None
patent: 0 992 496 (2000-04-01), None
patent: 1 022 272 (2000-07-01), None
patent: 2 596 393 (1987-10-01), None
patent: 2 205 837 (1988-12-01), None
patent: 2 304 106 (1997-03-01), None
patent: 54-32794 (1979-10-01), None
patent: WO 86/03488 (1986-06-01), None
patent: WO 94/15592 (1994-07-01), None
patent: WO 95/15954 (1995-06-01), None
patent: WO 97/21993 (1997-06-01), None
patent: WO 97/35576 (1997-10-01), None
patent: WO 97/48701 (1997-12-01), None
patent: WO 98/49899 (1998-11-01), None
patent: WO 99/00353 (1999-01-01), None
patent: WO 00/01389 (2000-01-01), None
patent: WO 00/15201 (2000-03-01), None
patent: WO 00/30665 (2000-06-01), None
patent: WO 00/38722 (2000-07-01), None
patent: WO 00/39077 (2000-07-01), None
patent: WO 00/50574 (2000-08-01), None
patent: WO 00/73288 (2000-12-01), None
patent: WO 02/10146 (2002-02-01), None
patent: WO 02/101146 (2002-12-01), None
patent: WO 03/033476 (2003-04-01), None
patent: WO 03/035624 (2003-05-01), None
patent: WO 2004/058762 (2004-07-01), None
patent: WO 2004/092181 (2004-10-01), None
patent: WO 2005/023782 (2005-03-01), None
patent: WO 2005/042541 (2005-05-01), None
patent: WO 2005/047293 (2005-05-01), None
patent: WO 2005/103039 (2005-11-01), None
patent: WO 2005/105805 (2005-11-01), None
patent: WO 2007/050723 (2007-05-01), None
patent: WO 2007/050726 (2007-05-01), None
Arnold, Z. et al., “Synthetic Reactions of Dimethylformamide. XXVII. A Simple Synthesis of Aminomalonaldehyde Derivatives”, Collection Czechoslov. Chem. Commun., vol. 38, pp. 2633-2640 (1973).
Beccalli, E.M. et al., “Pd-catalyzed intramolecular cyclization of pyrrolo-2-carboxamides: regiodivergent routes to pyrrolo-pyrazines and pyrrolo-pyridines”, Tetrahedron, vol. 61, pp. 1077-1082 (2005).
Bergman, J. et al., “Synthesis of Indoles via Ring Closure of 2-Alkylnitroaniline Derivatives”, Tetrahedron, vol. 46, No. 17, pp. 6085-6112 (1990).
Berlin, A. et al., “3-Alkylthiopyrroles: Synthesis and Oxidative Polymerization to Conductive Materials”, J. Chem. Soc. Perkin Trans. 2, pp. 699-704 (1990).
Biller, S.A. et al., “Isoprenoid (Phosphinylmethyl)phosphonates as Inhibitors of Squalene Synthetase”, Journal of Medicinal Chemistry, vol. 31, No. 10, pp. 1869-1871 (1988).
Biller, S.A. et al., “Squalene Synthase Inhibitors”, Current Pharmaceutical Design, vol. 2, No. 1, pp. 1-40 (1996).
Boatman, R.J. et al., “Some Novel Reactions of Pyrrolecarboxylic Acid Chlorides”, J. Org. Chem., vol. 41, No. 18, pp. 3050-3051 (1976).
Borowsky, B. et al., “Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist”, Nature Medicine, vol. 8, No. 8, pp. 825-830 (2002).
Brimble, M.A. et al., “Synthesis of 2-Methylpyrrolo[1,2-a]pyrazin-1(2H)-one”, Aust. J. Chem., vol. 41, pp. 1583-1590 (1988).
Budhram, R.S. et al., “13C NMR Spectra of 2,3-Dihydro-1H-pyrrolo[1,2-c]imidazol-1,3-dione and its Thione Analogues”, Organic Magnetic Resonance, vol. 13, No. 2, pp. 89-91 (1980).
Capson, T.L., “Synthesis and Evaluation of Ammonium Analogs of Carbocationic Intermediates in Squalene Biosynthesis”, dissertation, Department of Medicinal Chemistry, University of Utah, pp. iv-v, Table of Contents, 16-17, 40-43, 48-51, Summary (Jun. 1987).
Carpenter, A.J. et al., “Novel benzimidazole-based MCH R1 antagonists”, Bioorganic & Medicinal Chemistry Letters, vol. 16, pp. 4994-5000 (2006).
Corey, E.J. et al., “Application of Unreactive Analogs of Terpenoid Pyrophosphates to Studies of Multistep Biosynthesis. Demonstration That ‘Presqualene Pyrophosphate’ Is an Essential Intermediate on the Path to Squalene”, Journal of the American Chemical Society, vol. 98, No. 5, pp. 1291-1293 (1976).
Focella, A. et al., “The Synthesis of Two Phenacetin Metabolites”, Canadian Journal of Chemistry, vol. 50, pp. 2025-2030 (1972).
Ghiselli, G., “The Pharmacological Profile of FCE 27677: A Novel ACAT Inhibitor with Potent Hypolipidemic Activity Mediated by Selective Suppression of the Hepatic Secretion of ApoB-100-Containing Lipoprotein”, Cardiovascular Drug Reviews, vol. 16, No. 1, pp. 16-30 (1998).
Gupton, J.T. et al., “Application of 2-Substituted Vinamidinium Salts to the Synthesis of 2,4-Disubstituted Pyrroles”, J. Org. Chem. vol. 55, No. 15, pp. 4735-4740 (1990).
Handy, S.T. et al., “An unusual dehalogenation in the Suzuki coupling of 4-bromopyrrole-2-carboxylates”, Tetrahedron Letters, vol. 44, pp. 427-430 (2003).
Hara, S., “Ileal Na+/bile acid cotransporter inhibitors”, Drugs of the Future, vol. 24, No. 4, pp. 425-430 (1999).
Hertzog, D.L. et al., “The discovery and optimization of pyrimidinone-containing MCH R1 antagonists”, Bioorganic & Medicinal Chemistry Letters, vol. 16, pp. 4723-4727 (2006).
Iwanowicz, E.J. et al., “Inhibitors of Inosine Monophosphate Dehydrogenase: SARs about theN-[3-Methoxy-4-(5-oxazolyl)phenyl Moiety”, Bioorganic & Medicinal Chemistry Letters, vol. 13, pp. 2059-2063 (2003).
Jabin, I. et al., “Reaction of Cyclohexanone Benzylimines with Ethylidenemalonate Diesters. Diphenyl 2-Ehtylidenemalonate: A Highly Electrophilic Synthetic Equivalent of Crotonic Esters”, J. Org. Chem., vol. 66, No. 1, pp. 256-261 (2001).
Katritzky, A.R. et al., “Novel Synthesis of Bicycles with Fused Pyrrole, Indole, Oxazole, and Imidazole Rings”, J. Org. Chem., vol. 69, No. 26, pp. 9313-9315 (2004).
Kowalski, T.J. et al., “Melanin-concentrating horm

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