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US 12,760,032 B2Granted
Heterocyclic compounds
AssigneeHoffmann-La Roche Inc.
InventorsJoerg Benz, Uwe Grether, Benoit Hornsperger, Carsten Kroll, Bernd Kuhn, Rainer E. Martin, Fionn O'Hara, Hans Richter, Martin Ritter, Philipp Schmid
Life of this patent
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Abstract
The invention provides new heterocyclic compounds having the general formula (I) wherein X, Y, Z, A, L, B, and R1 to R3 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
Claims20
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- X is CH or N;
- Y and Z are independently CH2 or O, wherein at most one of Y and Z is O;
- L is selected from a covalent bond, —CHR4—, —OCH2—, and —CH2O;
- A is selected from C6-C10-aryl and 5- to 10-membered heteroaryl;
- B is a 4- to 7-membered heterocycle comprising 1-2 nitrogen atoms;
- R1 and R2 are independently selected from hydrogen, halogen, SF5, cyano, C1-6-alkyl, C1-6-alkoxy, halo-C1-6-alkyl, halo-C1-6-alkoxy, C6-C14-aryl, C3-C10-cycloalkyl, 5-14-membered heteroaryl, 3- to 14-membered heterocyclyl, C6-C14-aryloxy, C3-C10-cycloalkyloxy, 3- to 14-membered heterocyclyloxy, and 5-14-membered heteroaryloxy, wherein each of said 3- to 14-membered heterocyclyl, C6-C14-aryl, C3-C10-cycloalkyl, 5-14-membered heteroaryl, C6-C14-aryloxy, C3-C10-cycloalkyloxy, and 5-14-membered heteroaryloxy, are optionally substituted with 1-2 substituents selected from halogen, C1-6-alkyl, C1-6-alkoxy, halo-C1-6-alkyl and halo-C1-6-alkoxy;
- or
- R1 and R2, taken together with the atom(s) to which they are attached, form a 3- to 14-membered heterocycle that is optionally substituted with one or more C1-6-alkyl;
- R3 is selected from hydrogen and C1-6-alkyl;
- and
- R4 is selected from hydrogen, C6-C14-aryl and halo-C6-C14-aryl.
10 more elements
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- X is CH or N;
- Y is CH2 or O;
- Z is CH2;
- L is selected from a covalent bond and —CH2O—;
- A is phenyl;
- B is azetidinyl;
- R is selected from CF3 and (trifluoromethyl)cyclopropyl;
- R2 is selected from hydrogen and fluoro;
- and
- R3 is hydrogen.
8 more elements
A compound or a pharmaceutically acceptable salt thereof, selected from:
- [3-[[2-Fluoro-4-(trifluoromethyl)phenyl]methoxy]azetidin-1-yl]-[rac-(5aR,8aS)-4,5,5a,6,8,8a-hexahydro-1H-pyrrolo[3,4-g]indazol-7-yl]methanone;
- [3-[[2-Fluoro-4-(trifluoromethyl)phenyl]methoxy]azetidin-1-yl]-[rac-(1S,9R)-7-oxa-3,4,11-triazatricyclo[7.3.0.02,6]dodeca-2 (6),4-dien-11-yl]methanone;
- (−)- or (+)-[(1S,9R)-7-Oxa-3,4,11-triazatricyclo[7.3.0.02,6]dodeca-2 (6),4-dien-11-yl]-[3-[4-[1-(trifluoromethyl)cyclopropyl]phenyl]azetidin-1-yl]methanone;
- (+)- or (−)-[(1R,9S)-7-Oxa-3,4,11-triazatricyclo[7.3.0.02,6]dodeca-2 (6),4-dien-11-yl]-[3-[4-[1-(trifluoromethyl)cyclopropyl]phenyl]azetidin-1-yl]methanone;
- (−)- or (+)-[6-[(2,4-Difluorophenyl)methyl]-2-azaspiro[3.3]heptan-2-yl]-[(1S,9R)-7-oxa-3,4,11-triazatricyclo[7.3.0.02,6]dodeca-2 (6),4-dien-11-yl]methanone;
- (+)- or (−)-[6-[(2,4-Difluorophenyl)methyl]-2-azaspiro[3.3]heptan-2-yl]-[(1R,9S)-7-oxa-3,4,11-triazatricyclo[7.3.0.02,6]dodeca-2 (6),4-dien-11-yl]methanone;
- (−)- or (+)-[3-[[2-Fluoro-4-(trifluoromethyl)phenyl]methoxy]azetidin-1-yl]-[(5aR,8aS)-4,5,5a,6,8,8a-hexahydro-1H-pyrrolo[3,4-e]benzotriazol-7-yl]methanone;
- (+)- or (−)-[3-[[2-Fluoro-4-(trifluoromethyl)phenyl]methoxy]azetidin-1-yl]-[(5aS,8aR)-4,5,5a,6,8,8a-hexahydro-1H-pyrrolo[3,4-e]benzotriazol-7-yl]methanone;
- (−)- or (+)-[3-[[2-Fluoro-4-(trifluoromethyl)phenyl]methoxy]azetidin-1-yl]-[(1S,9R)-8-oxa-3,4,5,11-tetrazatricyclo[7.3.0.02,6]dodeca-2 (6),4-dien-11-yl]methanone;
- and
- (+)- or (−)-[3-[[2-Fluoro-4-(trifluoromethyl)phenyl]methoxy]azetidin-1-yl]-[(1R,9S)-8-oxa-3,4,5,11-tetrazatricyclo[7.3.0.02,6]dodeca-2 (6),4-dien-11-yl]methanone.
8 more elements
Dependencies are inferred from the claim text.