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US 2003/0114517 A1Published application
Substituted urea neuropeptide Y Y5 receptor antagonists
AssigneeSchering Corporation
InventorsWilliam J. Greenlee, Ying Huang, Joseph M. Kelly, Stuart W. McCombie, Andrew W. Stamford, Yusheng Wu
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Abstract
A novel class of compounds such as antagonists of the neuropeptide Y Y5 receptor, methods of making such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more diseases associated with the neuropeptide Y Y5 receptor are disclosed.
Claims29
A compound having the structural formula I:
- 462
- R1 is hydrogen or (C1-C6)alkyl;
- R2 is hydrogen, (C1-C6)alkyl, (C3-C9)cycloalkyl or (C3-C7)cycloalkyl(C1-C6)alkyl;
- 463
- where Z is OR10 or —N(R9)(R10);
- j is 0, 1 or 2;
- k is 1 or 2;
- l is 0, 1 or 2;
- m is 0, 1 or 2;
- p is 1, 2 or 3;
- r is 1, 2 or 3;
- and s is 0, 1,2,3,4, 5 or 6;
- R4 is a subsituent independently selected from hydrogen, —OH, halogen, haloalkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, —CN, (C1-C6)alkylO-, (C3-C7)cycloalkylO-, (C1-C6)alkyl(C3-C7)cycloalkylO-, (C1-C6)alkylS-, (C3-C7)cycloalkylS-, (C1-C6)alkyl(C3-C7)cycloalkylS-, —NR9R10, —NO2, —CONR9R10 and —NR2COR10;
- R5 is a substituent independently selected from hydrogen, halogen, —OH, haloalkyl, haloalkoxy, —CN, —NO2, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, (C1-C6)alkylO-, (C3-C7)cycloalkylO-, (C1-C6)alkyl(C3-C7)cycloalkylO-, —CONH2 and —CONR9R10;
- R6 is (C1-C6)alkylSO2—, (C3-C7)cycloalkylSO2—, (C1-C6)alkyl(C3-C7)cycloalkylSO2—, (C1-C6)haloalkylSO2—, hydroxy(C2-C6)alkyl)SO2,-, (amino(C2-C6)alkyl)SO2—, alkoxy(C2-C6)alkyl)SO2—, alkylamino(C2-C6)alkyl)SO2—, dialkylamino(C2-C6)alkyl)SO2—, arylSO2—, heteroarylSO2—, aryl(C2-C6-alkylSO2—, R9R10NSO2—, (C1-C6)alkylC(O)—, (C3-C7)cycloalkylC(O)—, (C3-C7)cycloalkyl(C1-C6)alkylC(O)—, arylC(O)—, heteroarylC(O)—, R9R10NC(O)—, —(S)CNR9R10, aryl, heteroaryl, —(CH2)nC(O)NR9R10, alkylS(NCN═)C—, R9R1ON(NCN═)C—, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl(C1-C6)alkyl, heteroaryl(C1-C6)alkyl, or R9OC(O)—;
- R7=hydrogen or alkyl;
- R8 is hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl, heteroaryl, (C1-C6)alkylSO2—, (C3-C7)cycloalkylSO2—, (C1-C6)alkyl(C3-C7)cycloalkylSO2—, (C1-C6)haloalkylSO2— or arylSO2—;
- R9 is hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl(C1-C6)alkyl, aryl, acyl or heteroaryl;
- and,
- R10 is hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl(C1-C6)alkyl, aryl or heteroaryl;
- or R9 and R10 taken together with the nitrogen atom form a 4-7 membered ring containing 1 or 2 heteroatoms selected from N, O or S with proviso that two O or S atoms are not adjacent to one another;
- n=1to 6;
- or a pharmaceutically acceptable salt and/or hydrate thereof.
20 more elements
A compound of the formula
- 470
- or a pharmaceutically acceptable salt and/or hydrate thereof.
Dependencies are inferred from the claim text.