- Antithrombotic agents
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This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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- Antithrombotic agents
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This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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- N2-aroylanthranilamide inhibitors of human factor Xa
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Reversal of the A-ring amide link in 1,2-dibenzamidobenzene 1 (fXa K(ass) = 0.81 x 106 L/mol) led to a series of human factor Xa (hfXa) inhibitors based on N2-aroylanthranilamide 4. Expansion of the SAR around 4 showed that only smal
- Yee, Ying K.,Tebbe, Anne Louise,Linebarger, Jared H.,Beight, Douglas W.,Craft, Trelia J.,Gifford-Moore, Donetta,Goodson Jr., Theodore,Herron, David K.,Klimkowski, Valentine J.,Kyle, Jeffrey A.,Sawyer, J. Scott,Smith, Gerald F.,Tinsley, Jennifer M.,Towner, Richard D.,Weir, Leonard,Wiley, Michael R.
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p. 873 - 882
(2007/10/03)
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- Hypolipidemic 2-[4-(1,1-dimethylethyl)phenyl]-4H-3,1-benzoxazin-4-ones. Structure-activity relationships of a novel series of high-density lipoprotein elevators
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The preparation and plasma lipid altering characteristics of a series of 4H-3,1-benzoxazin-4-ones are described. Hypocholesterolemic, hypotriglyceridemic, and high-density-lipoprotein elevating properties are found for derivatives bearing a 4-(1,1-dimethylethyl)phenyl group at the 2-position, and this activity is displayed in both hypercholesterolemic and in normolipidemic rats when the ring system is substituted at position 6 with hydrogen, methyl, chloro, or iodo groups, and is optimal when the 6-position is substituted by a bromine atom. Evidence is presented suggesting that a metabolite or degradation product is responsible for the changes in lipoprotein concentration observed with active molecules of this type. Synthesis of anticipated degradation products of the active molecules gave products displaying the expected in vivo activity, but no improvement in the narrow therapeutic margin of the best compound, 6-bromo-2-[4-(1,1-dimethylethyl)phenyl]-4H-3,1-benzoxazin-4-one, was obtained.
- Fenton,Newton,Wyman,Bagge,Dron,Riddell,Jones
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p. 265 - 272
(2007/10/02)
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