- SULFUR CHELATED RUTHENIUM COMPOUNDS USEFUL AS OLEFIN METATHESIS CATALYSTS
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Sulfur chelated ruthenium compounds represented by the following formula: wherein M indicates the ruthenium metal bound to a benzylidene carbon; R represents C1-C7 alkyl group or optionally substituted aryl; X1 and X2 each independently represent halogen; Y1 and Y2 each independently denote unsubstituted or alkyl-substituted phenyl; and Z independently represents hydrogen, electron withdrawing or electron donating substituent, with m being an integer from 1 to 4, and processes and compositions related thereto.
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Paragraph 0074
(2014/06/23)
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- Design and synthesis of phenylpyrrolidine phenylglycinamides as highly potent and selective TF-FVIIa inhibitors
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Inhibitors of the Tissue Factor/Factor VIIa (TF-FVIIa) complex are promising novel anticoagulants that show excellent efficacy and minimal bleeding in preclinical models. On the basis of a zwitterionic phenylglycine acylsulfonamide 1, a phenylglycine benz
- Zhang, Xiaojun,Jiang, Wen,Jacutin-Porte, Swanee,Glunz, Peter W.,Zou, Yan,Cheng, Xuhong,Nirschl, Alexandra H.,Wurtz, Nicholas R.,Luettgen, Joseph M.,Rendina, Alan R.,Luo, Gang,Harper, Timothy M.,Wei, Anzhi,Anumula, Rushith,Cheney, Daniel L.,Knabb, Robert M.,Wong, Pancras C.,Wexler, Ruth R.,Priestley, E. Scott
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supporting information
p. 188 - 192
(2014/03/21)
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- Studies on electronic effects in O-, N- and S-chelated ruthenium olefin-metathesis catalysts
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A short overview on the structural design of the Hoveyda-Grubbs-type ruthenium initiators chelated through oxygen, nitrogen or sulfur atoms is presented. Our aim was to compare and contrast O-, N- and S-chelated ruthenium complexes to better understand the impact of electron-withdrawing and -donating substituents on the geometry and activity of the ruthenium complexes and to gain further insight into the trans-cis isomerisation process of the S-chelated complexes. To evaluate the different effects of chelating heteroatoms and to probe electronic effects on sulfur- and nitrogen-chelated latent catalysts, we synthesised a series of novel complexes. These catalysts were compared against two well-known oxygen-chelated initiators and a sulfoxide-chelated complex. The structures of the new complexes have been determined by single-crystal X-ray diffraction and analysed to search for correlations between the structural features and activity. The replacement of the oxygen-chelating atom by a sulfur or nitrogen atom resulted in catalysts that were inert at room temperature for typical ring-closing metathesis (RCM) and cross-metathesis reactions and showed catalytic activity only at higher temperatures. Furthermore, one nitrogen-chelated initiator demonstrated thermo-switchable behaviour in RCM reactions, similar to its sulfur-chelated counterparts.
- Tzur, Eyal,Szadkowska, Anna,Ben-Asuly, Amos,Makal, Anna,Goldberg, Israel,Wozniak, Krzysztof,Grela, Karol,Lemcoff, N. Gabriel
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experimental part
p. 8726 - 8737
(2010/10/19)
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- BENZAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 48
(2010/09/17)
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- Sulfur chelated ruthenium compounds useful as olefin metathesis catalysts
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Sulfur chelated ruthenium compounds and methods and compositions involving the same. A method may relate to subjecting an olefin to a metathesis reaction in the presence of a sulfur chelated ruthenium compound. A composition may relate to an olefin starting material dissolved in an organic solvent together with a sulfur chelated ruthenium compound.
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- MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention relates generally to novel macrocycles of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 112
(2008/12/07)
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- BICYCLIC LACTAM FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 79-80
(2008/12/07)
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- PHENYLGLYCINAMIDE DERIVATIVES USEFUL AS ANTICOAGULANTS
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The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
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Page/Page column 78-79
(2008/06/13)
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