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US 8,618,296 B2Granted
Arylethynyl derivatives
AssigneeHoffmann-La Roche Inc.
InventorsLuke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
Life of this patent
Estimating the term…
Abstract
The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2′, R3, R3′, R4, R4′, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
Claims6
The compound of formula I-B 1
- wherein
- U is ═N— or ═C(R5)—;
- V is —CH═ or —N═;
- W is ═CH— or ═N—;
- with the proviso that only one of U, V or W is nitrogen;
- R5 is hydrogen, methyl or halogen;
- R1 is phenyl or heteroaryl, each of which is optionally substituted by one or two substituents, selected from halogen, lower alkyl and lower alkoxy;
- R2 and R2′ are each independently hydrogen, lower alkyl, hydroxy, lower alkoxy, C3-C6-cycloalkyl, or CH2-lower alkoxy, or together with the carbon atom to which they are attached form a C3-C6-cycloalkyl group or a ring containing —CH2OCH2—;
- R3 and R3′ are each independently hydrogen, lower alkyl, or CH2-lower alkoxy or together with the carbon atom to which they are attached form a C3-C6-cycloalkyl group;
- or R3 and R2 together with the carbon atom to which they are attached form a C3-6-cycloalkyl group or a ring containing —(CH2)2OCH2—;
- and
- R7 and R7′ are each independently hydrogen, hydroxy, lower alkyl or lower alkoxy;
- or a pharmaceutically acceptable acid addition salt, a racemic mixture, an enantiomer, an optical isomer and/or stereoisomer thereof.
10 more elements
Dependencies are inferred from the claim text.