A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an ...alpha-methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
We report the discovery of novel histamine H(3) receptor antagonists based on 4-(1H-imidazol-4-yl)methylpiperidine. The most potent compounds in the series (e.g., 7) result from the attachment of a ...substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
We report the discovery of novel histamine H
3 receptor antagonists based on 4-(1
H-imidazol-4-yl)methylpiperidine. The most potent compounds in the series (e.g.,
7) result from the attachment of a ...substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker
We report the discovery of novel histamine H
3 receptor antagonists based on 4-(1
H-imidazol-4-yl)methylpiperidine. The most potent compounds in the series (e.g.,
7) result from the attachment of a substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
A series of novel five-membered urea derivatives as potent NK sub(1) receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an ...alpha -methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
A series of novel five-membered urea derivatives as potent NK
1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an ...α-methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified.
Full text
Available for:
GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
7.
Enantiomerization of an atropisomeric drug Friary, Richard J.; Spangler, Michael; Osterman, Rebecca ...
Chirality (New York, N.Y.),
1996, 1996-00-00, Volume:
8, Issue:
5
Journal Article
A series of novel five- and six-membered ring urea derivatives have been described as potent and selective NK
1 receptor antagonists. Several compounds in this series exhibited good oral activity and ...brain penetration. Syntheses of these compounds are also described herein.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
The TanDEM-X mission based on two satellites provides a radar interferometer in space with the goal to derive a global Digital Elevation Model (DEM) with never achieved quality for a global coverage: ...a global DEM with a relative height accuracy of 2m and 10m absolute. In order to achieve this mission goal, the distance between both satellites, the so called baseline has to be known extreme precisely. Only then, systematic baseline errors can be detected and compensated for, i.e. an accurate calibration of the global DEM can be ensured. The paper describes the procedure and the results of calibrating the baseline, verifying the outstanding accuracy of this calibration procedure.
