5- [4-(azetidin-3-yloxy)-phenyl]-2-phenyl-5H-thiazolo[5,4-C]...

Details 5- [4-(azetidin-3-yloxy)-phenyl]-2-phenyl-5H-thiazolo[5,4-C]... 5- [4-(azetidin-3-yloxy)-phenyl]-2-phenyl-5H-thiazolo[5,4-C]...

2007-11-15

2011-11-01

Chandrakumar, Nizal S (Department: 1625)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

08049013

ABSTRACT:
The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “-----” is absent or is optionally a bond; q is 1 or 2; R1is independently selected from hydrogen, —C1-C2alkyl, halo, hydroxy, —C1-C2haloalkyl, —C1-C3alkoxy, cyano, —O—C3-C4cycloalkyl, and —OC1-C2haloalkyl; R2is selected from the group consisting of hydrogen, —C1-C3alkyl, hydroxy, —C1-C3alkoxy, cyano, —C1-C2haloalkyl, —OC1-C2haloalkyl, and halo; R3is selected from the group consisting of hydrogen, —C1-C4alkyl, —C2-C4haloalkyl, —C2-C4alkylOH, —C3-C6cycloalkyl, —CH2C3-C6cycloalkyl, —C2-C4alkyl-O—C1-C4alkyl, —C(O)C1-C4alkyl, —C(O)C1-C4haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2alkyl, and —C1-C2haloalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture thereof, useful in the treating, preventing or ameliorating of symptoms associated with obesity and related diseases.

REFERENCES:
patent: WO 03/033476 (2003-04-01), None
patent: WO 2006/066174 (2006-06-01), None
Witty, et al., “Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849,”Bioorganic and Medicinal Chemistry Letters, vol. 16, No. 18, pp. 4872-4878 (2006).
Dyck, et al., “A Thienopyridazinone-Based Melanin-Concentrating Hormone Receptor 1 Antagonist with Potent in Vivo Anorectic Properties,” Journal of Medicinal Chemistry, American Chemical Society, vol. 49, No. 13, pp. 3753-3756 (2006); XP003003117.

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