59621-76-0Relevant academic research and scientific papers
Phenoxyphenyl sulfone N-formylhydroxylamines (Retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors
Wada,Holms,Curtin,Dai,Florjancic,Garland,Guo,Heyman,Stacey,Steinman,Albert,Bouska,Elmore,Goodfellow,Marcotte,Tapang,Morgan,Michaelides,Davidsen
, p. 219 - 232 (2007/10/03)
A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated as matrix metalloproteinases (MMP) inhibitors. The substitution of the ether linkage of ABT-770 (5) with a sulfone group 13a led to a substantial increase in activity against MMP-9 but was accompanied by a loss of selectivity for inhibition of MMP-2 and -9 over MMP-1 and diminished oral exposure. Replacement of the biphenyl P1′ substituent with a phenoxyphenyl group provided compounds that are highly selective for inhibition of MMP-2 and -9 over MMP-1. Optimization of the substituent adjacent to the retrohydroxamate center in this series led to the clinical candidate ABT-518 (6), a.highly potent, selective, orally bioavailable MMP inhibitor that has been shown to significantly inhibit tumor growth in animal cancer models.
Matrix metalloprotease inhibitors
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, (2012/01/30)
The present invention relates to compounds of Formula I: STR1 that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.
Sulphur- and oxygen-containing diaryl compounds
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, (2008/06/13)
The sulphur- and oxygen-containing diaryl compounds of the formula: STR1 in which A and B, which may be the same or different, represent O, S, SO or SO2, Alk is a C1 -C4 hydrocarbon radical with a straight or branched chain, R represents COOH, an esterified COOH group, a carboxylic amide group, OH, O-SO2 CH3, NH2, NHR1, NR1 R2, NHZOH, NHZNR1 R2, C(=NH)NH2, C(=NH)NHOH or 2-Δ2 -imidazolinyl, Z is a C2 -C4 hydrocarbon radical with a straight or branched chain, and R1 and R2 each represent a C1 -C3 lower alkyl group, or together form, with the nitrogen atom to which they are linked, a N-heterocyclic group of 5 to 7 ring atoms which can be substituted and can comprise a second hetero-atom, and their addition salts with bases when R is COOH, and their addition salts with acids when R is a basic radical, are useful pharmacological agents in the treatment of circulatory complaints such as cardio-vascular illnesses.
