1,4-disubstituted piperazines
AssigneeRecordati S.A., Chemical and Pharmaceutical Company
InventorsAmedeo Leonardi, Gianni Motta, Carlo Riva, Luciano Guarneri, Elena Poggesi
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Abstract
Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are 1,4-disubstituted piperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.
Claims17
A compound of the formula:
- wherein
- n is 1 or 2,
- Het is a pyridine radical,
- R is a cycloalkyl or a monocyclic heteroaryl radical,
- wherein the monocyclic heteroaryl radical is an aromatic radical consisting from 5 to 6 ring atoms, and one or two of said ring atoms is a member selected from the group consisting of nitrogen, oxygen and sulfur,
- R3 is a hydrogen atom or a lower alkyl group,
- Z is a —CH2—,
- wherein B is selected from the group consisting of a heteroaryl radical and a substituted aryl radical, wherein said substituted aryl radical is represented the following formula:
- wherein R1 is a single substituent selected from the group consisting of alkoxy, halogen, nitro, amino, acylamino, alkylamino, and alkylsulfonylamino, and R2 is selected from the group consisting of an alkoxy, polyfluoroalkoxy, cyano, halogen and aminocarbonyl radical, and wherein said heteroaryl radical is selected from the group consisting of a monocyclic aromatic radical consisting from 5 to 6 ring atoms, wherein one or more of said ring atoms are selected from the group consisting of nitrogen, oxygen, and sulfur, and wherein said acylamino is selected from the group consisting of acetylamino, pivaloylamino, butanoylamino, phenylacetylamino, and formylamino,
- and enantiomers, diastereomers, N-oxides, crystalline forms, hydrates, and pharmaceutically acceptable salts thereof.
A method for treating neuromuscular dysfunction of the lower urinary tract in a mammal in need of such treatment, said method comprising administering to said mammal an effective amount for treating said dysfunction of a compound of the formula:
- wherein
- n is 1 or 2,
- Het is a pyridine radical,
- R is a cycloalkyl or a monocyclic heteroaryl radical,
- wherein the monocyclic heteroaryl radical is an aromatic radical consisting from 5 to 6 ring atoms, and one or two of said ring atoms is a member selected from the group consisting of nitrogen, oxygen and sulfur,
- R3 is a hydrogen atom or a lower alkyl group,
- Z is a —CH2—,
- wherein B is selected from the group consisting of a heteroaryl radical, an unsubstituted aryl radical, and a substituted aryl radical, wherein said substituted aryl radical is represented by the following formula:
- wherein R1 is a single substituent selected from the group consisting of alkoxy, halogen, nitro, amino, acylamino, alkylamino, dialyklamino and alkylsulfonylamino, and R2 is selected from the group consisting of an alkoxy, polyfluoroalkoxy, cyano, halogen and aminocarbonyl radical, and
- wherein said heteroaryl radical is selected from the group consisting of a mono or a bicyclic aromatic radical consisting from 5 to 12 ring atoms, wherein one or more of said ring atoms are selected from the group consisting of nitrogen, oxygen, and sulfur;
- and wherein said acylamino is selected from the group consisting of acetylamino, pivaloylamino, butanoylamino, phenylacetylamino, and formylamino;
- and enantiomers, diastereomers, N-oxides, crystalline forms, hydrates, and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.