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US 9,067,911 B2Granted
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.
Claims17
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 substituted by one or two CF3 groups and optionally substituted by one or two substituents selected from halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy halogen, cycloalkyl, lower alkoxy, S-lower alkyl, heteroaryl, heterocycloalkyl, and phenyl optionally substituted by R′, to give no more than three substituents total on Ar;
- 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 substituted by one or two CF3 groups and optionally substituted by one or two substituents selected from halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy halogen, cycloalkyl, lower alkoxy, S-lower alkyl, heteroaryl, heterocycloalkyl, and phenyl optionally substituted by R′, to give no more than three substituents total on Ar;
- 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.