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US 7,803,816 B2Granted
MCH receptor antagonists
AssigneeHoffmann-La Roche Inc.
InventorsSteven Joseph Berthel, Shawn David Erickson, Nader Fotouhi, Robert Francis Kester, Kyungjin Kim, Steven Gregory Mischke, Yimin Qian, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Hong Wang
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Abstract
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of obesity, hyperphagia, anxiety, depression and related disorders and diseases.
Claims16
A compound of the formula (I):
- wherein:
- R1 is
- unsubstituted or mono-, di- or tri-substituted with a group selected from the group consisting of halogen, hydroxyl, —SCH3, phenyl, (C3-C6)cycloalkyl, oxygen, (C1-C6)alkoxy, branched or unbranched −(C1-C6)alkyl and branched or unbranched (C1-C6)alkyl substituted with hydroxyl;
- R2 is hydrogen, halogen, substituted or unsubstituted (C1-C6)alkyl, hydroxyl, —OCH2C(CH3)OH, —SCH3, —OSO2CH3, (C1-C6)alkoxy, —CH2OH or —CH2OCH3;
- R3 is H or halogen;
- R4 is hydrogen, halogen, (C1-C6)alkyl, —CN, —NH2, —NHCH3, —NHCO—R5, —OCH3 or azaindane;
- R5 is substituted or unsubstituted, branched or unbranched (C1-C6)alkyl, (C1-C6)alkoxy, (C3-C6)cycloalkyl, or a heterocycle which is a 5- or 6-membered heteroaromatic ring connected by a ring carbon which has from 1 to 3 hetero ring atoms selected from the group consisting of S, N and O;
- and pharmaceutically acceptable salts thereof.
5 more elements
Dependencies are inferred from the claim text.