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US 6,294,534 B1Granted
Spiropiperidine derivatives as melanocortin receptor agonists
AssigneeMerck & Co., Inc.
InventorsRavi P. Nargund, Brenda L. Palucki, Zhixiong Ye, Raman K. Bakshi, Arthur A. Patchett, Leonardus H. T. Van Der Ploeg
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Abstract
Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.
Claims15
A compound having the formula I:
- wherein
- Cy2 is a six-membered aromatic ring containing 0 or 1N atom or cyclohexane;
- Q is
- X is CH2, CHCO2Rb, CHSO2Ra, CHC(O)N(Rb)2, NRb, NSO2Ra, NSO2N(Rb)2, NCORa, NCON(Rb)2, CHN(Rb)CORa, CHN(Rb)SO2Ra, CHCH2ORb, or CH(CH2)-heteroaryl;
- Y is (CH2)r, CH—C1-8alkyl, or C═O;
- R1 is H, C1-8alkyl, CH(Rb)-aryl, CH(Rb)-heteroaryl, (CH2)n—C5-6cycloalkyl in which aryl and heteroaryl are optionally substituted by one or two Rcgroups;
- R2 is H or halo;
- Ra is Rb, (CH2)nN(Rb)2, (CH2)nN(Rb)C(═NRd)NRb, (CH2)nNH-2-pyridyl, (CH2)nNH-2-imidazolyl, (CH2)nNH-2-thiazolyl, (CH2)nNH-2-pyrimidinyl,
- Rb is H, C1-8alkyl, (CH2)naryl, (CH2)nheteroaryl, C3-6cycloalkyl;
- or 2 Rb together with the nitrogen atom to which they are attached form a 5- or 6-membered ring optionally containing an additional heteroatom selected from O, S, and NR1;
- Rc is Rb, halo, ORb, NHSO2Rb, N(Rb)2, CN, NO2, SO2N(Rb)2, SO2Rb, CF3, OCF3;
- or two Rc groups attached to adjacent carbon atoms together form methylenedioxy;
- Rd is H, NO2, or CN;
- Cy is aryl or 5- or 6-membered carbocyclyl;
- n is 0 to 3;
- m, p and q are independently 0, 1 or 2;
- r is 1, 2 or 3;
- or a pharmaceutically acceptable salt thereof.
15 more elements
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.