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US 7,094,792 B2Granted
Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
AssigneeBiovitrum AB
InventorsTjeerd Barf, Rikard Emond, Guido Kurz, Marianne Nilsson, Jerk Vallgårda, Lian Zhang
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Abstract
The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
Claims4
A compound of Formula (I)
- wherein
- T is an aryl ring, optionally independently substituted by [R]n, wherein n is an integer 0–5, and R is hydrogen, aryl, optionally halogenated C1-6-alkyl, optionally halogenated C1-6-alkoxy, C1-6-alkylsulfonyl, carboxy, cyano, nitro, halogen, aryloxy, arylsulfonyl, arylamino, wherein aryl and aryloxy residues are further optionally substituted in one or more positions independently of each other by C1-6-acyl, C1-6-alkylthio, cyano, nitro, hydrogen, halogen, optionally halogenated C1-6-alkyl, optionally halogenated C1-6-alkoxy, amide which is optionally mono- or di-substituted, (benzoylamino)methyl, carboxy, or 2-thienylmethylamino;
- or T is selected from 5-(dimethylamino)-1-naphthyl and phenyl substituted with one or more of benzeneamino, benzylamino and 2-thienylmethylamino;
- R1 is hydrogen or C1-6-alkyl;
- X is CH2 or CO;
- Y is CO;
- B is hydrogen, C1-6-alkyl or dimethylaminomethyl;
- R2 is NR3R4, wherein R3 and R4 are each independently selected from hydrogen, ethyl, isopropyl, n-propyl, optionally halogenated C1-6-alkylsulfonyl, C1-6-alkoxy, 2-methoxyethyl, 2-hydroxyethyl, C1-6-acyl, cyclohexylmethyl, cyclopropanecarbonyl, aryl, optionally halogenated arylsulfonyl or C1-6-alkyl substituted with one or more aryl
- or a salt, hydrate or solvate thereof.
6 more elements
A compound selected from the group consisting of:
- 2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)-N-ethylacetamide
- 2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)-N,N-diethylacetamide
- 2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)acetamide
- N-[2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)ethyl]-N-ethylacetamide
- 2-{2-[(1,1′-biphenyl-4-ylsulfonyl)amino]-1,3-thiazol-5-yl}-N,N-diethylacetamide N,N-diethyl-2-(2-{[(4-propylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)acetamide
- 2-(2-{[(2,4-dichloro-6-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)-N,N-diethylacetamide
- 2-{2-[(1,1′-biphenyl-4-ylsulfonyl)amino]-1,3-thiazol-5-yl)-N,N-diisopropylacetamide
- N,N-diisopropyl-2-(2-{[(4-propylphenyl)sulfonyl]amino)-1,3-thiazol-5-yl)acetamide
- 2-(2-{[(2,4-dichloro-6-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)-N,N-diisopropylacetamide
- 2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)-N,N-dipropylacetamide
- 2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)-N,N diisopropylacetamide and
- N-[2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl )ethyl]acetamide.
9 more elements
Dependencies are inferred from the claim text.