Antagonists of melanin concentrating hormone receptor

Details Antagonists of melanin concentrating hormone receptor Antagonists of melanin concentrating hormone receptor

2005-07-26

2005-07-26

Seaman, D. Margaret (Department: 1625)

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

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

C540S601000, C544S284000, C544S324000, C546S157000, C514S312000

Reexamination Certificate

active

06921821

ABSTRACT:
This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I:where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9and Ring A are defined in the specification. Coumarin and quinolone compounds where R1and R2together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.

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Marsh, D. J., et al., “Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism”,PNAS, 99(5):3240-3245 (2002).
Qu, D., et al., “A role for melanin-concentrating hormone in the central regulation of feeding behaviour”,Nature, 380:243-247 (1996).
Rossi, M., et al., “Melanin-Concentrating Hormone Acutely Stimulates Feeding, But Chronic Administration Has No Effect on Body Weight”,Endocrinology, 138(1):351-355 (1997).
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