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US 7,071,195 B2Granted
Amine and amide derivatives as ligands for the neuropeptide Y Y5 receptor useful in the treatment of obesity and other disorders
AssigneeOrtho-McNeil Pharmaceutical, Inc.
InventorsScott L. Dax, James McNally, Mark Youngman
Life of this patent
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Abstract
Amine and amide derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing amines and amides of formula A as the active ingredient are described. The amines and amides of formula A are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
Claims8
A compound of the formula
- wherein R1 is independently selected from the group consisting of H;
- alkyl;
- substituted alkyl;
- alkoxy;
- halo;
- substituted alkoxy;
- hydroxy;
- trifluoralkyl;
- nitro;
- amino;
- alkylamino;
- cycloalkylamino;
- cyano;
- carboxy;
- cycloalkyl;
- phenyl;
- and substituted phenyl;
- R2 is pyridyl;
- B1 is hydrogen;
- B2 is hydrogen;
- or B1 and/or B2 are methylene and joined together to form a five or six membered ring;
- Y is methylene or carbonyl;
- L is selected from the group consisting of
- R3 is independently selected from the group consisting of C1-6 alkyl;
- substituted C1-8alkyl;
- cycloalkyl;
- substituted cycloalkyl;
- naphthyl;
- substituted naphthyl;
- heteroaryl;
- and substituted heteroaryl;
- R4 is independently selected from the group consisting of hydrogen;
- C1-8alkyl;
- C1-8alkoxy;
- substitued C1-8alkoxy;
- hydroxy;
- halogen;
- cyano;
- nitro;
- amino;
- C1-8alkylamino;
- and C1-8dialkylamino;
- R5 is independently selected from the group consisting of hydrogen;
- C1-8alkyl;
- C1-8alkylcarbonyl;
- aroyl;
- carbamoyl;
- amidino;
- C1-8alkyl;
- C1-8alkylaminocarbonyl;
- (arylamino)carbonyl;
- and arylC1-8alkylcarbonyl;
- R6 is independently selected from hydrogen and C1-8alkyl;
- n is 1–2;
- m is 0–3;
- p is 1–3;
- and
- q is 1–3;
- provided that when L is (N-methylene)piperazin-4-yl, then Z is phenyl or naphthyl;
- when L is (N-methylene)piperidin-4-yl, then Z is N-sulfonamido, N(aryl)sulfonamido, 2,3-dihydro-2-oxo-1H-benzimidazol-1-yl, benzamido, phenylureido, phenylacetamido or (phenoxy)carbonylamino;
- when L is (N-methylene)-4-acetyl-piperidin-4-yl, then Z is phenyl or naphthyl and Y is carbonyl;
- and when L is (N-methylene)piperidin-4,4-diyl, then Z is 1-aryl-2,3-dihydro-4-oxo-imidazol-5,5-diyl and Y is carbonyl;
- and enantiomers, diastereomers and pharamaceutically acceptable salts thereof.
60 more elements
Dependencies are inferred from the claim text.