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US 2008/0176839 A1Published application
Spiropiperidine derivatives as nk3 antagonists
AssigneeHoffmann-La Roche Inc.
InventorsJoanie Marie Caroon, Michael Patrick Dillon, Bo Han, Matthias Nettekoven, Hasane Ratni, Walter Vifian
Life of this patent
Estimating the term…
Abstract
The present invention relates to a compound of formula I wherein R1, R2, R3, R4, R7, m and n are as defined herein. These compounds are high potential NK-3 receptor antagonists useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
Claims31
A compound of formula
- wherein
- R1 is hydrogen or lower alkyl;
- R2 is lower alkyl, lower hydroxyalkyl or —(CHR5)x-A;
- R5 is hydrogen, lower alkyl, lower hydroxyalkyl, or heteroaryl optionally substituted by lower alkyl;
- A is a cycloalkyl, aryl, heterocyclyl or heteroaryl ring, which rings are optionally substituted by one or more R6, wherein R6 is lower alkyl, lower alkoxy, lower alkylsulfonyl, cyano, halogen, lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or is aryl, heterocyclyl or heteroaryl optionally substituted by lower alkyl or is cycloalkyl optionally substituted by lower alkyl;
- x is 0, 1, 2 or 3;
- or R1 and R2 together with the N-atom to which they are attached form a heterocyclyl or heteroaryl ring, which rings are optionally substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, lower alkylsulfonyl, halogen, cycloalkyl, benzyl and aryl;
- R3 is hydrogen or halogen;
- R4 is hydrogen or lower alkyl;
- R7 is hydrogen, halogen or lower alkyl;
- m is 1 or 2;
- when m is 2, each R3 can be the same or different;
- n is 1 or 2;
- o is 1 or 2;
- when o is 2, each R7 can be the same or different;
- or a pharmaceutically suitable acid addition salt thereof.
13 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- R1 is hydrogen or lower alkyl;
- R2 is lower alkyl, lower hydroxyalkyl or —(CHR5)x-A;
- R5 is hydrogen, lower alkyl, lower hydroxyalkyl, or heteroaryl optionally substituted by lower alkyl;
- A is a cycloalkyl, aryl, heterocyclyl or heteroaryl ring, which rings are optionally substituted by one or more R6, wherein R6 is lower alkyl, lower alkoxy, lower alkylsulfonyl, cyano, halogen, lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or is aryl, heterocyclyl or heteroaryl optionally substituted by lower alkyl or is cycloalkyl optionally substituted by lower alkyl;
- x is 0, 1, 2 or 3;
- or R1 and R2 together with the N-atom to which they are attached form a heterocyclyl or heteroaryl ring, which rings are optionally substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, lower alkylsulfonyl, halogen, cycloalkyl, benzyl and aryl;
- R3 is hydrogen or halogen;
- R4 is hydrogen or lower alkyl;
- R7 is hydrogen, halogen or lower alkyl;
- m is 1 or 2;
- when m is 2, each R3 can be the same or different;
- n is 1 or 2;
- o is 1 or 2;
- when o is 2, each R7 can be the same or different;
- or a pharmaceutically suitable acid addition salt thereof and a pharmaceutically acceptable carrier.
13 more elements
Dependencies are inferred from the claim text.