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US 9,802,944 B2Granted
Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors
AssigneeHoffmann-La Roche Inc.
InventorsPatrick Di Giorgio, Jerome Hert, Daniel Hunziker, Holger Kuehne, Patrizio Mattei, Markus Rudolph
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
Claims23
A compound of formula (I)
- wherein
- R1 is pyridinyl substituted with R3, R4, and R5;
- A is —N—;
- W is —C(O)—;
- R2 is:
- R3 is tetrahydropyranylmethoxy;
- R4 is cycloalkyl;
- R5 is H;
- m, n, p and q are independently selected from 1 and 2;
- and
- R9 is H, alkyl, halogen, haloalkyl or alkoxy;
- or a pharmaceutically acceptable salt thereof.
9 more elements
The compound
- ((3aR,8aS)-2-(1H-benzo[d][1,2,3]triazole- 5-carbonyl)octahydropyrrolo[3,4-d]azepin- 6(7H)-yl)(2-cyclopropyl-6-((tetrahydro- 2H-pyran-4-yl)methoxy)pyridin-4- yl)methanone;
- or a pharmaceutically acceptable salt thereof.
The compound
- ((3aR,8aS)-6-(2-cyclopropyl-6- ((tetrahydro-2H-pyran-4- yl)methoxy)isonicotinoyl)- octahydropyrrolo[3,4-d]azepin-2(1H)- yl)(4,5,6,7-tetrahydro-1H- benzo[d][1,2,3]triazol-5-yl)methanone;
- or a pharmaceutically acceptable salt thereof.
The compound
- ((3aR,8aS)-2-(1H-benzo[d][1,2,3]triazole- 5-carbonyl)octahydropyrrolo[3,4-d]azepin- 6(2H)-yl)(3-cyclopropyl-5-((tetrahydro- 2H-pyran-4- yl)methoxy)phenyl)methanone;
- or a pharmaceutically acceptable salt thereof.
The compound
- ((3aR,8aS)-6-(2-cyclopropyl-6- ((tetrahydro-2H-pyran-4- yl)methoxy)isonicotinoyl)- octahydropyrrolo[3,4-d]azepin-2(1H)- yl)((R)-4,5,6,7-tetrahydro-1H- benzo[d][1,2,3]triazol-5-yl)methanone;
- or a pharmaceutically acceptable salt thereof.
The compound
- ((3aR,8aS)-6-(3-cyclopropyl-5- ((tetrahydro-2H-pyran-4- yl)methoxy)benzoyl)octahydropyrrolo[3,4- d]azepin-2(1H)-yl)((R)-4,5,6,7-tetrahydro- 1H-benzo[d][1,2,3]triazol-5-yl)methanone;
- or a pharmaceutically acceptable salt thereof.
The compound
- ((3aR,8aS)-6-(2-Cyclopropyl-6- ((tetrahydro-2H-pyran-4- yl)methoxy)isonicotinoyl)octa- hydropyrrolo[3,4-d]azepin-2(1H)-yl)((S)- 4,5,6,7-tetrahydro-1H- benzo[d][1,2,3]triazol-5-yl)methanone;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.