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US 2002/0058671 A1Published application
Neuropeptide Y antagonists
AssigneePfizer Inc.
InventorRichard L. Elliott
Life of this patent
Estimating the term…
Abstract
Compounds of the formula 1 are neuropeptide antagonists and are effective in treating feeding disorders, cardiovascular diseases and other physiological disorders related to an excess of neuropeptide Y.
Claims9
A compound of the formula
- 15
- Wherein X is NR4R5 where R4 and R5 are selected independently from C1-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, C2-C8 alkynyl, C2-C8 alkylalkoxy, alkylaryl, alkylheteroaryl, SO2R7, or SO2NR7R8;
- each optionally substituted with 1-2 substituents independently selected from R6;
- or R4 and R5 are taken together to form a nitrogen containing ring of 3 to 8 atoms, optionally substituted with 1-2 substituents independently selected from R6;
- C5-C8 cycloalkenyl, optionally substituted with 1-2 substituents independently selected from R6;
- or a heterocyclic ring containing up to two heteroatoms selected from the group consisting of —O—, —NR7—, and —S(O)m— optionally substituted with 1-3 substituents independently selected from R6. Furthermore, when R4 and R5 are taken together to be C3-C8 cycloalkyl, C5-C8 cycloalkenyl, or a heterocyclic ring as described above then said ring system may be further substituted to form an additional 3-8 membered ring optionally containing up to two heteroatoms selected from the group consisting of —O—, —NR7—, and —S(O)m—. Furthermore, R5 may be selected from NR7R8;
- and
- R6 is selected from hydrogen;
- halogen, nitro, cyano, hydroxy, alkylalkoxy, COOH, C1-C6 alkyl;
- C1-C6 hydroxyalkyl, C1-C6 aminoalkyl, aryl, heteroaryl, aryloxy, heteroaryloxy, alkoxy;
- acyloxy, NR7NR8, C1-C4 alkylthio, mono-, di-, or trihaloalkyl;
- and
- R7and R8 are independently selected from H, C1-C6 alkyl;
- C2-C6 alkenyl, alkylalkoxy, C2-C6 alkynyl, aryl, or heteroaryl;
- and may be joined to form a carbocyclic or heterocyclic ring;
- and
- Y is selected from C1-C6alkyl;
- alkoxyalkyl, C2-C6 alkenyl;
- C2-C6alkynyl, alkoxy, aryl, or heteroaryl, or NR4R5 as defined for X;
- and
- R3 is selected from aryl or heteroaryl, optionally substituted with 1-3 substituents chosen from R6;
- m is 0, 1, or 2;
- And with the proviso that Y is not CF3;
- And with the further proviso that when Y is alkyl or alkoxy, X is not NR6(CH2)nNR7R8.
21 more elements
A compound selected from the group consisting of:
- 2-Chloro-8-phenyl-6-pyrrolidin-1-yl-7H-purine;
- 8-Phenyl-2,6-di-pyrrolidin-1-yl-7H-purine;
- 8-Phenyl-2,6-di-piperidin-1-yl-7H-purine;
- 8-Phenyl-2-piperidin-1-yl-6-pyrrolidin-1-yl-7H-purine;
- N2,N2,N6,N6-Tetramethyl-8-phenyl-7H-purine-2,6-diamine;
- Benzyl-(8-phenyl-6-pyrrolidin-1-yl-7H-purin-2-yl)-amine;
- and
- Dimethyl-(8-phenyl-6-pyrrolidin-1-yl-7H-purin-2-yl)-amine.
5 more elements
A pharmaceutical composition for inhibiting a pathological condition in a mammal characterized by or associated with an excess of neuropeptide Y, which comprises a compound of formula I or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.