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US 6,472,398 B1Granted
Spiropiperidine derivatives as melanocortin receptor agonists
AssigneeMerck & Co., Inc.
InventorsBrenda L. Palucki, Ravi P. Nargund
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Abstract
Certain novel spiropiperidine derivatives of structural formula Ia wherein the substituents are as defined herein are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Claims11
A compound having structural formula Ia:
- wherein
- n is 0, 1, or 2;
- X is N-SO2R8;
- R6 is hydrogen, halo, or methoxy;
- R2 is hydrogen or methyl;
- R9 is hydrogen or halo;
- R4a and R4b are each independently selected from the group consisting of
- hydrogen,
- amidino,
- C1-4 alkyl,
- (CH2)0-1 aryl,
- (CH2)0-1C3-6 cycloalkyl,
- CO2R7,
- CO(CH2)0-1C(Me)2NH2,
- COC(Me)2NHCO2R7,
- (CH2)2OR7,
- COR7,
- CONR7R7,
- SO2R7, and
- SO2NR7R7;
- in which aryl is unsubstituted or substituted with one to three groups independently selected from R6;
- and alkyl and cycloalkyl are unsubstituted or substituted with one to three groups independently selected from R6 and oxo;
- each R7 is independently selected from the group consisting of
- hydrogen,
- C1-8 alkyl,
- (CH2)n-aryl, and
- (CH2)nC3-7 cycloalkyl;
- and
- R8 is selected from the group consisting of
- hydrogen,
- C1-8 alkyl,
- (CH2)n-aryl, and
- (CH2)nC3-7 cycloalkyl;
- wherein aryl is unsubstituted or substituted with one to three groups independently selected from R6;
- and alkyl, cycloalkyl, and (CH2)n are unsubstituted or substituted with one to three groups independently selected from R6 and oxo;
- or a pharmaceutically acceptable salt thereof.
33 more elements
Dependencies are inferred from the claim text.