Ethynyl derivatives
AssigneeHoffmann-La Roche Inc.
InventorsBarbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
Life of this patent
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Abstract
The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
Claims16
A method for the treatment of anxiety, the method comprising administering to a mammal in need thereof an effective amount of a compound of formula I:
- wherein:
- R1 is lower alkyl;
- R2 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions;
- n is 0, 1 or 2;
- V/U are independently from each other O or CH2, wherein V and U cannot be simultaneously O;
- L is a five or six membered heteroaryl group, selected from:
- or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
A method for the treatment of anxiety, the method comprising administering to a mammal in need thereof an effective amount of a compound, wherein the compound is:
- (6S)-3-[2,6-Difluoro-4-[2-(3-pyridyl)ethynyl]phenyl]-1-methyl-spiro[hexahydropyrimidine-6,1′-tetralin]-2,4-dione;
- or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
A method for the treatment of anxiety, the method comprising administering to a mammal in need thereof an effective amount of a compound, wherein the compound is:
- (6S)-3-[2,6-Difluoro-4-[2-(3-pyridyl)ethynyl]phenyl]-1-methyl-spiro[hexahydropyrimidine-6,1′-indane]-2,4-dione;
- or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
A method for the treatment of anxiety, the method comprising administering to a mammal in need thereof an effective amount of a compound, wherein the compound is:
- ((5S)-3′-[2,6-Difluoro-4-(2-phenylethynyl)phenyl]-1′-methyl-spiro[7,8-dihydro-6H-quinoline-5,6′-hexahydropyrimidine]-2′,4′-dione;
- or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
A method for the treatment of anxiety, the method comprising administering to a mammal in need thereof an effective amount of a compound, wherein the compound is:
- (5S)-3′-[2,6-Difluoro-4-(2-phenylethynyl)phenyl]-1′-methyl-spiro[7,8-dihydro-6H-quinazoline-5,6′-hexahydropyrimidine]-2′,4′-dione;
- or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
A method for the treatment of anxiety, the method comprising administering to a mammal in need thereof an effective amount of a compound, wherein the compound is:
- (4S)-3′-[2,6-Difluoro-4-(2-phenylethynyl)phenyl]-1′-methyl-spiro[2,3-dihydropyrano[2,3-b]pyridine-4,6′-hexahydropyrimidine]-2′,4′-dione;
- or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
Dependencies are inferred from the claim text.