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US 2012/0071459 A1Published application
Bis-pyridylpyridones as melanin-concentrating hormone receptor 1 antagonists
AssigneeGlaxoSmithKline LLC
InventorsSiegfried Benjamin Christensen, IV, Donghui Qin, Shuhul Chen, Shi Lu
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Abstract
The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
Claims21
A compound of Formula (I),
- or a pharmaceutically acceptable salt thereof wherein:
- R1 is a saturated 6-12 membered heterocyclic ring system containing 1 or 2 ring nitrogen atoms and an optional ring oxygen atom, which ring system incorporates spiro rings and which is attached to the pyridine ring via a nitrogen atom;
- R2 is selected from the group consisting of:
- hydrogen, C1-6alkyl, —C(O)NRaRb, —C(O)Ra, —SO2Ra, —C(O)ORa, oxo, —C(O)NRaRb, —NRaRb, —NRaC(O)Rb, —NRaC(O)ORb, and —NRaSO2Rb;
- Ra is selected from the group consisting of:
- hydrogen, C1-6alkyl, and C3-6cycloalkyl;
- Rb is selected from the group consisting of:
- hydrogen, C1-6alkyl, C3-6cycloalkyl, aryl, and heteroaryl;
- or Ra and Rb together with the nitrogen to which they are attached form a heterocycloalkyl, and said heterocycloalkyl is optionally substituted with one, two, or three Rc groups;
- R3 is H, F, Cl, C1-3alkyl, cyclopropyl, C1-3alkoxy, amino, C1-3alkylamino, oxo, or CN;
- Rc is H, F, Cl, C1-6alkyl, C3-6cycloalkyl, C1-3alkoxy, amino, C1-3alkylamino, oxo, or CN;
- X is (CH2)m;
- m is 0-2;
- n is 0-3;
- p is 0-3;
- with the proviso that R2 is not —NRaCOOH or —NRaSO2H.
13 more elements
The compound of Formula (I)(A), (I)(B) or (I)(C), wherein said R1 is selected from:
- 1-oxo-2,7-diazaspiro[4.5]decan-7-yl, 2,7-diazaspiro[4.4]nonan-2-yl, 1,7-diazaspiro[4.5]decan-7-yl, 1,7-diazaspiro[4.4]nonan-7-yl, 1,8-diazaspiro[5.5]undecan-8-yl, 2,7-diazaspiro[3.5]nonan-2-yl, 2,6-diazaspiro[3.5]nonan-2-yl, 1-oxo-2,7-diazaspiro[3.5]nonan-7-yl, 7-methylamino-5-azaspiro[2.4]heptan-5-yl, 2,8-diazaspiro[4.5]decan-8-yl, and 1-oxa-4,9-diazaspiro[5.5]undecan-4-yl.
21-24. (canceled)
Dependencies are inferred from the claim text.