- NOVEL 9-AZA-BICYCLO[3.3.1]NON-3-YLOXY CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
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This invention relates to novel 9-aza-bicyclo[3.3.1]non-3-yloxy chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
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- 9-AZABICYCLO [3 . 3 . 1] NONANE DERIVATIVES AS MONOAMINE REUPTAKE INHIBITORS
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The present invention relates to a 9-azabicyclo[3.3.1]nonane derivative of formula (I), wherein R1 is H or C1-5alkyl; X is O or NR2, wherein R2 is H, C1-5alkyl or C2-5acyl and Ar is C6-10aryl or a 5-10 membered heteroaryl ring system, both being optionally substituted with one to three of R3-R5 independently selected from halogen, C1-5alkyl, C1-5alkoxy, C3-6cycloalkyl, C2-5alkenyl, C2-5alkynyl, CN, NO2, hydroxy, phenyl, phenoxy and phenylC1-2alkoxy, wherein said C1-5alkyl and C1-5alkoxy are optionally substituted with one to three halogens and wherein said phenyl, phenoxy and phenylC1-2alkoxy are optionally substituted with one to three substituents independently selected from halogen and methyl or two of R3-R5 at adjacent positions together form a methylenedioxy or propylene unit, with the proviso that the compounds exo-9-methyl-3-phenoxy-9-azabicyclo[3.3.1]nonane and N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1H indazole-5-amine are excluded, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 9-azabicyclo[3.3.1]nonane derivatives and to their use in therapy.
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Page/Page column 62-63
(2010/11/26)
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- COMBINATION OF A STEROID SULFATASE INHIBITOR AND AN ASCOMYCIN
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A combination of a steroid sulfatase inhibitor and an ascomycin, which combination is useful as a pharmaceutical.
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Page/Page column 40-41
(2010/11/23)
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- ANTI-INFLAMMATORY COMPOUNDS
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The use of a steroid sulfatase inhibitor in the preparation of a medicament for the treatment of inflammatory diseases.
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Page/Page column 36-37
(2008/06/13)
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- BICYCLIC FIVE-MEMBERED HETEROARYL DERIVATIVES AND THEIR USE AS RENIN INHIBITORS
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The invention relates to novel five-membered heteroaryl derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions comprising one or more of those compounds and especially their use as inhibitors of renin.
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Page/Page column 28
(2010/11/23)
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