Back to results
US 2013/0158050 A1Published application
Piperidine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsSabine Kolczewski, Emmanuel Pinard, Henri Stalder
Life of this patent
Estimating the term…
Abstract
The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.
Claims18
A compound of formula I
- wherein
- R1 is hydrogen, lower alkyl, CD3, —(CH2)n—CHO, —(CH2)n—O-lower alkyl, —(CH2)n—OH, —(CH2)n-cycloalkyl or heterocycloalkyl;
- R2 is hydrogen, halogen, hydroxy, lower alkyl, di-lower alkyl, —OCH2—O-lower alkyl, or lower alkoxy;
- or the piperidin ring together with R2 forms 4-aza-spiro[2.5]oct-6-yl;
- Ar is phenyl optionally substituted by one, two or three substituents selected from halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl, lower alkoxy, S-lower alkyl, heteroaryl, heterocycloalkyl, and phenyl optionally substituted by R′,
- R′ is lower alkyl, lower alkoxy, lower alkoxy substituted by halogen, or heteroaryl;
- R is phenyl optionally substituted by one or two R′;
- and
- n is 0, 1 2 or 3;
- or a pharmaceutically acceptable acid addition salt, racemic mixture, enantiomer, or optical isomer thereof.
7 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- R1 is hydrogen, lower alkyl, CD3, —(CH2)n—CHO, —(CH2)n—O-lower alkyl, —(CH2)n—OH, —(CH2)n-cycloalkyl or heterocycloalkyl;
- R2 is hydrogen, halogen, hydroxy, lower alkyl, di-lower alkyl, —OCH2—O-lower alkyl, or lower alkoxy;
- or the piperidin ring together with R2 forms 4-aza-spiro[2.5]oct-6-yl;
- Ar is phenyl optionally substituted by one, two or three substituents selected from halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl, lower alkoxy, S-lower alkyl, heteroaryl, heterocycloalkyl, and phenyl optionally substituted by R′,
- R′ is lower alkyl, lower alkoxy, lower alkoxy substituted by halogen, or heteroaryl;
- R is phenyl optionally substituted by one or two R′;
- and
- n is 0, 1 2 or 3;
- or a pharmaceutically acceptable acid addition salt, racemic mixture, enantiomer, or optical isomer thereof and a pharmaceutically acceptable carrier.
7 more elements
Dependencies are inferred from the claim text.