Organic compounds -- part of the class 532-570 series – Organic compounds – Chalcogen in the nitrogen containing substituent
Reexamination Certificate
2000-08-08
2001-11-13
Bernhardt, Emily (Department: 1624)
Organic compounds -- part of the class 532-570 series
Organic compounds
Chalcogen in the nitrogen containing substituent
C544S121000, C544S235000, C544S238000, C544S353000, C544S354000, C544S357000, C544S360000, C544S365000, C544S367000, C544S368000, C544S371000, C544S372000, C544S379000, C544S393000
Reexamination Certificate
active
06316617
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to certain amide substituted benzylamine derivatives which selectively bind to mammalian Neuropeptide Y1 (NPY1) receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds and compositions in treating physiological disorders associated with an excess of Neuropeptide Y, especially feeding disorders and certain cardiovascular diseases.
2. Description of the Related Art
Neuropeptide Y, a peptide first isolated in 1982, is widely distributed in the central and peripheral neurons and is responsible for a multitude of biological effects in the brain and the periphery. Various animal studies have shown that activation of Neuropeptide Y
1
receptors is related to vasoconstriction, Wahlestedt et al., Regul. Peptides, 13: 307-318 (1986), McCauley and Westfall, J. Pharmacol. Exp. Ther. 261: 863-868 (1992), and Grundemar et al., Br. J. Pharmacol. 105: 45-50 (1992); and to stimulation of consummatory behavior, Flood and Morley, Peptides, 10: 963-966 (1989), Leibowitz and Alexander, Peptides, 12: 1251-1260 (1991), and Stanley et al., Peptides, 13: 581-587 (1992).
Grundemar and Hakanson, TiPS, May 1994 [Vol. 15], 153-159, state that, in animals, Neuropeptide Y is a powerful stimuli of food intake, and an inducer of vasoconstriction leading to hypertension. They further point out that low levels of Neuropeptide Y is associated with loss of appetite. These reports clearly indicate that compounds that inhibit the activity of this protein will reduce hypertension and appetite in animals.
REFERENCES:
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patent: 5962455 (1999-10-01), Blum et al.
patent: 5985873 (1999-11-01), Blum et al.
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Gehlert et al, Exp. Opin. Invest. Drugs 6 P 1827-1838 (1997).
Grundemar et al., TIPS, 15, P 153-159 (1994).
Blum Charles A.
DeSimone Robert
Hutchison Alan
Peterson John M.
Bernhardt Emily
Neurogen Corporation
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