64409-12-7Relevant academic research and scientific papers
Direct probing molecular twist and tilt in aromatic self-assembled monolayers
Ballav, Nirmalya,Schuepbach, Bjoern,Dethloff, Ole,Feulner, Peter,Terfort, Andreas,Zharnikov, Michael
, p. 15416 - 15417 (2008/09/19)
Using a nitrile tailgroup as a spectroscopic marker, both twist and tilt of the aromatic backbones in several typical aromatic SAMs on Au(111) have been directly determined in a single experiment. Whereas the exact value of the twist angle depends on the molecular architecture, it was found to be quite noticeable in all SAMs (40-50°) and close to the respective value for aromatic bulk systems (32°). Copyright
3-Arylsulfonyl-2 (substituted methyl) propanoic acid derivatives as matrix metalloproteinase inhibitors
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Page column 30, (2010/02/07)
Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO—NH— or HO—, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., —NH—CO-Ph) and benzamido substituted on the terminal phenyl ring by C1-C4alkyl, fluoro, chloro, cyano or C1-4alkoxy; R2is selected from (a) —S—Ar or —S—CH2—Ar wherein Ar is an aromatic moiety; (b) —O—Ar wherein Ar is as defined above; (c) —S-Het or —S—CH2-Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.
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.
Cyclic imino derivatives and pharmaceutical compositions containing them
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, (2008/06/13)
The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
β-D-phenylthioxylosides, their method of preparation and their use as therapeutic agents
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, (2008/06/13)
The present invention relates, by way of novel industrial products, to the β-D-phenylthioxyloside compounds of the formula STR1 in which: X represents a sulfur atom or an oxygen atom; R1, R2 and R3, which are identical or different, each represent a hydrogen atom, a nitro group, a cyano group, a group --CO--R (in which R represents a C1 -C4 alkyl group or a trifluoromethyl group), an amino group, an acetamido group (NHCOCH3), a C1 -C4 alkoxy group, a trifluoromethyl group or a phenyl group substituted by one or more cyano, nitro or trifluoromethyl groups, it being possible for R1 and R2, taken together, to form, with the phenyl group to which they are bonded, a β-naphthalenyl group which is unsubstituted or substituted by one or more cyano, nitro or trifluoromethyl groups; and Y represents the hydrogen atom or an aliphatic acyl group. These compounds are useful as therapeutic agents, especially as venous antithrombotics.
