6-azauracil derivatives as thyroid receptor ligands

Details 6-azauracil derivatives as thyroid receptor ligands 6-azauracil derivatives as thyroid receptor ligands

2005-08-16

2005-08-16

Balasubramanian, Venkataraman (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C544S182000

Reexamination Certificate

active

06930107

ABSTRACT:
The present invention provides novel compounds of the Formula Iand prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1to R8and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, overweight condition, hyperlipidemia, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression, osteoporosis, cardiac arrhythmias, glaucoma and congestive heart failure are also provided.

REFERENCES:
patent: 3852289 (1974-12-01), Mylari et al.
patent: 3882115 (1975-05-01), Mylari
patent: 3883525 (1975-05-01), Mylari
patent: 3883527 (1975-05-01), Brennan
patent: 3883528 (1975-05-01), Mylari
patent: 3896172 (1975-07-01), Mylari et al.
patent: 3905971 (1975-09-01), Miller
patent: 3912723 (1975-10-01), Miller
patent: 4198407 (1980-04-01), Rosner et al.
patent: 4239888 (1980-12-01), Miller
patent: 4640917 (1987-02-01), Rosner et al.
patent: 5256631 (1993-10-01), Lindner et al.
patent: 979457 (1975-12-01), None
patent: 992538 (1976-07-01), None
patent: 2358851 (1974-06-01), None
patent: 2532363 (1977-02-01), None
patent: 0737672 (1996-10-01), None
patent: WO9418229 (1994-08-01), None
patent: 917390 (1991-09-01), None
Wolft Manfred E. “Burger's Medicinal Chemistry, 5ed, Part 1”, John Wiley & Sons, 1995, pp. 975-977.
Banker, G.S. et al, “Modern Pharmaceutics, 3ed.”, Marcel Dekker, New York. 1996, p. 596.
A. H. Underwood, et al.,Nature, vol. 324: pp. 425-429 (1986).
B. L. Mylari, et al., J. Med. Chem., 1977, vol. 20, No. 4, 475-483, “Anticoccidial Derivatives of 6-Azauracil. 1. Enhancement of Activity by Benzylation of Nitrogen-1. Observations on the Design of Nucleotide Analogues in Chemotherapy.”
M. W. Miller, et al., J. Med. Chem., 1979, vol. 22, No. 12, 1483-1487, “Anticoccidial Derivatives of 6-Azauracil. 2. High Potency and Long Plasma Life of N1-Phenyl Structures12”.
M. W. Miller, t al., J. M d. Chem., 1980, vol. 23, No. 10, 1083-1087. “Anticoccidial Derivatives of 6-Azauracil. 3. Synthesis, High Activity, and Short Plasma Half-life of 1-Phenyl-6-azauracils Containing Sulfonamide Substituents1.”
M. W. Miller, et al., J. Med. Chem., 1981, vol. 24, No. 11, 1337-1342, “Anticoccidial Derivatives of 6-Azauracil. 4. A 1000-fold Enhancement of Potency by Phenyl Sulfide and Phenyl Sulfone Side Chains1. ”
R. D. Carroll, et al., J. Med. Chem., 1983, vol. 26, No. 1, 96-100, “Anticoccidial Derivatives of 6-Azauracil. 5. Potentiation by Benzophenone Side Chains”.
K.-B. Rhyu, et al., J. Chem. Inf. Comput. Sci., 1996, vol. 36, No. 3, “A 3D-QSAR Study of Anticoccidial Triazines Using Molecular Shape Analysis.”
K.-B. Rhyu, et al. J. Chem. Inf. Comput. Sci., 1995, vol. 35, No. 4, 771-778, “a 3D-QSAR Study of Anticoccidial Triazines Using Molecular Shape Analysis.”
A. C. Good, et al., J. Med. Chem., 1993, vol. 36, No. 20, 2929-2937, “QSAR's from Similarity Matrices. Technique Validation and Application in the Comparison of Different Similarity Evaluation Methods.”
J. W. McFarland, J. Med. Chem., 1992, vol. 35, No. 14, 2543-2550, “Comparative Molecular Field Analysis of Anticoccidial Triazines”.
J. W. McFarland, et al., J. Med. Chem., 1991, vol. 34, No. 6, 1908-1911, “Linear Discriminant and Multiple Regression Analyses of Anticoccidial Triazines”.
A. N. Chekhlov, et al., Dokl. Akad. Nauk (1993), 329 (5), 603-7.
N. S. Zefirov, et al., Dokl. Akad. Nauk (1992), 327 (4-6), 504-8.
A. P. Ricketts, et al., Antimicrobial Agents and Chemotherapy, Oct. 1992, vol. 36, pp. 2338-2341, “In Vivo Expression of in Vitro Anticoccidial Activity”.
M. J. Lynch, et al., J. Agric. Food. Chem., vol. 25, No. 6, pp. 1344-1353, 1977, “Tissue Residue and Comparative Metabolism Studies on Triazuril in the Chicken, Rat, Dog, and Monkey.”
J. F. Ryley, et al., Parasitology (1974), 68, 69-79, “Anticoccidial activity of an azauracil derivative.”

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