264624-26-2Relevant articles and documents
Inverse 1,2,3-triazole-1-yl-ethyl substituted hydroxamates as highly potent matrix metalloproteinase inhibitors: (Radio)synthesis, in vitro and first in vivo evaluation
Hugenberg, Verena,Riemann, Burkhard,Hermann, Sven,Schober, Otmar,Sch?fers, Michael,Szardenings, Katrin,Lebedev, Artem,Gangadharmath, Umesh,Kolb, Hartmuth,Walsh, Joseph,Zhang, Wei,Kopka, Klaus,Wagner, Stefan
supporting information, p. 6858 - 6870 (2013/10/01)
Noninvasive imaging and quantification of matrix metalloproteinase (MMP) activity in vivo are of great (pre)clinical interest. This can potentially be realized by using radiolabeled MMP inhibitors (MMPIs) as positron emission tomography (PET) imaging agen
Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3- methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET
Wagner, Stefan,Breyholz, Hans-J?rg,Law, Marilyn P.,Faust, Andreas,H?ltke, Carsten,Schr?er, Sandra,Haufe, Günter,Levkau, Bodo,Schober, Otmar,Sch?fers, Michael,Kopka, Klaus
, p. 5752 - 5764 (2008/03/27)
An approach to the in vivo imaging of locally upregulated and activated matrix metalloproteinases (MMPs) found in many pathological processes is offered by positron emission tomography (PET). Hence, appropriate PET radioligands for MMP imaging are required. Here, we describe the syntheses of novel fluorinated MMP inhibitors (MMPIs) based on lead structures of the broad-spectrum inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)-amino]-3-methyl-butanamide (CGS 25966) and N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](3-picolyl)-amino]-3- methyl-butanamide (CGS 27023A). Additionally, tailor-made precursor compounds for radiolabeling with the positron-emitter 18F were synthesized. All prepared hydroxamate target compounds showed high in vitro MMP inhibition potencies for MMP-2, MMP-8, MMP-9, and MMP-13. As a consequence, the promising fluorinated hydroxamic acid derivative 1f was resynthesized in its 18F-labeled version via two different procedures yielding the potential PET radioligand [18F]If. As expected, the biodistribution behavior of this novel compound and that of the more hydrophilic variant [ 18F]1j, also developed by our group, indicates that there was no tissue specific accumulation in wild-type (WT) mice.
ARYLOXYETHYLAMINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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Page/Page column 131, (2008/06/13)
The present invention relates to aryloxyethylamine compounds of the formula (I) and the physiologically tolerated acid addition salts thereof. The variables have the meanings given in the claims and the description. The invention also relates to the use o
Keratinocyte growth inhibitors and hydroxamic acid derivatives
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Page 25, (2010/02/06)
This invention relates to a keratinocyte-proliferation inhibitor comprising as active ingredient a compound having an activity of inhibiting the solubilization of heparin-binding EGF-like growth factor bound to cell membranes and a compound of the formula (I); or pharmaceutically acceptable salt thereof, wherein R1, R2, R3 are hydrogen atom or alkyl and X is substituted benzene or the like.