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US 6,911,477 B2Granted
Muscarinic receptor agonists
AssigneePfizer Inc.
InventorsAnabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
Life of this patent
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Abstract
This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.
Claims2
A compound of the formula
- wherein X is (C1-C10)alkyl or (C3-C10)cycloalkyl, wherein said (C3-C10)cycloalkyl may optionally be substituted with from one to three substituents independently selected from the group consisting of —OR6, (C1-C4)alkyl, oxo and a ketal of the formula —O—(CH2)n—O—;
- n is an integer from one to three;
- m is an integer from one to three;
- p is an integer from one to three;
- Y is N or CH;
- Z is NR7R8, (C3-C10)cycloalkyl, (C1-C10)alkyl, pyridyl or phenyl;
- wherein said phenyl or (C3-C10)cycloalkyl may optionally be substituted with from one to three substituents independently selected from the group consisting of (C1-C6)alkyl, halo, hydroxy, (C1-C6)alkoxy, amino, (C1-C6)-alkylamino, di(C1-C6)alkylamino and trifluoromethoxy;
- R2 is phenyl optionally substituted with from one to three substituents independently selected from the group consisting of (C1-C6)alkyl, halo, hydroxy, (C1-C6)alkoxy, amino, (C1-C6)alkylamino, di(C1-C6)-alkylamino, —CF3, —CN, —COR6, NHCOR6 and trifluoromethoxy;
- R3 is phenyl optionally substituted with from one to three substituents independently selected from the group consisting of (C1-C6)alkyl, halo, hydroxy, (C1-C6)alkoxy, amino, (C1-C6)alkylamino, di(C1-C6)-alkylamino and trifluoromethoxy;
- R6 is hydrogen or (C1-C6)alkyl;
- and
- R7 and R8 are independently (C1-C10)alkyl or R7 and R8 taken together with the nitrogen atom to which they are attached form a (five to seven)-membered saturated heterocyclic ring in which one of the ring atoms may optionally be replaced with a heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, wherein said (five to seven)-membered saturated heterocyclic ring may optionally be substituted with from one to three substituents independently selected from the group consisting of —OR6, (C1-C4)alkyl, oxo and a ketal of the formula —O—(CH2)p—O—;
- with the proviso that said substituted heterocycles may not be substituted in the two position by hydroxy or a ketal;
- and the pharmaceutically acceptable salts thereof.
11 more elements
Dependencies are inferred from the claim text.