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US 2011/0257402 A1Published application
Pyrrazolopyridine compounds as dual nk1/nk3 receptor antagonists
AssigneeHoffmann-La Roche Inc.
InventorsPhilippe Jablonski, Matthias Nettekoven, Angëlique Patiny-Adam, Hasane Ratni, Heinz Stadler
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Abstract
The present invention relates to a compound of formula I wherein R1, R2, R3, Ar, and n are as defined herein or to a pharmaceutically active acid addition salt. Compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
Claims9
A compound of formula I
- wherein
- R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, —C(O)-lower alkyl, —C(O)—CH2-lower alkoxy, —C(O)—C3-6-cycloalkyl, —(CH2)o—C(O)—NRR′, —(CH2)oS(O)2-lower alkyl or —S(O)2—NR,R′;
- o is 0 or 1;
- R and R′ are each independently hydrogen or lower alkyl, or together with the N atom to which they are attached form a 5 or 6 membered heterocycloalkyl ring;
- R2 is hydrogen or lower alkyl;
- R3 is halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen;
- and when n is 2, each R3 is the same or different;
- n is 1 or 2;
- Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted by hydroxy or cyano, or is a five or six membered heteroaryl group, selected from thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen;
- or a pharmaceutically active acid-addition salt thereof.
7 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, —C(O)-lower alkyl, —C(O)—CH2-lower alkoxy, —C(O)—C3-6-cycloalkyl, —(CH2)o—C(O)—NRR′, —(CH2)oS(O)2-lower alkyl or —S(O)2—NR,R′;
- o is 0 or 1;
- R and R′ are each independently hydrogen or lower alkyl, or together with the N atom to which they are attached form a 5 or 6 membered heterocycloalkyl ring;
- R2 is hydrogen or lower alkyl;
- R3 is halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen;
- and when n is 2, each R3 is the same or different;
- n is 1 or 2;
- Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted by hydroxy or cyano, or is a five or six membered heteroaryl group, selected from thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen;
- or a pharmaceutically active acid-addition salt thereof
- and a pharmaceutically acceptable salt thereof
8 more elements
Dependencies are inferred from the claim text.