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US 7,402,604 B2Granted
Positive modulators of nicotinic receptor agonists
AssigneeAstraZeneca AB
InventorsDavid Gurley, James Rosamond
Life of this patent
Estimating the term…
Abstract
Compounds according to formula I: wherein R1, W, R2, R3, X, R4 and R5 are as described in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission.
Claims8
A compound of Formula I:
- wherein:
- R1 represents hydrogen or C1-C4alkyl;
- W represents C(O)NR6;
- R2 represents (CH2)pCH[(CH2)qR7](CH2)tR8;
- R3 and R5 independently represent hydrogen or C1-C4alkyl;
- R4 represents hydrogen or C1-C4alkyl;
- R6 represents hydrogen or C1-C4alkyl;
- R7 is Ar;
- R8 is selected from CN, N3, or OR10, where R10 is H;
- Ar represents phenyl or naphthyl;
- Ar is optionally substituted with one or more substituents independently selected from:
- hydrogen, halogen, C1-C4alkyl, CN, NO2, CF3, OR12, NR12R13 and COOR12;
- R12 and R13 independently represent hydrogen, C1-C4alkyl, aryl, or heteroaryl, and
- p, q, and t are independently 0, 1 or 2;
- or an enantiomer thereof, or a pharmaceutically-acceptable salt thereof.
12 more elements
A compound selected from:
- (R)-N-(2-hydroxy-1-phenylethyl) 4-hydroxy-1-methyl-1H-indole-2-carboxamide;
- (S)-N-(2-azido-1-benzylethyl)-4-hydroxy-1-methyl-1H-indole-2-carboxamide;
- (R)-N-(2-azido-1-benzylethyl)-4-hydroxy-1-methyl-1H-indole-2-carboxamide;
- N-(1-phenyl-3-butynyl)-4-hydroxy-1-methyl-1H-indole-2-carboxamide;
- (S)-N-[2-azido-1-(4-methoxybenzyl)ethyl]-4-hydroxy-1-methyl-1H-indole-2-carbox-amide, and
- (S)-N-[1-benzyl-2-hydroxyethyl]-4-hydroxy-1-methyl-1H-indole-2-carboxamide,
- or an enantiomer thereof, or a pharmaceutically-acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.