- PYRIDAZINE DERIVATIVES AS RORc MODULATORS
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Compounds of formula I: or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R1, R2, R3, R4 and R5are as defined herein. Also disclosed are methods of making the compounds and using the compounds f
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Page/Page column 38; 39
(2016/11/21)
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- The synthesis of novel disorazoles
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Big little brother: The simplified disorazole analogue 1 exhibits its cytotoxic activity at low nanomolar concentrations and provides selectivities not observed for the parent natural product.
- Schaeckel, Romy,Hinkelmann, Bettina,Sasse, Florenz,Kaiesse, Markus
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supporting information; experimental part
p. 1619 - 1622
(2010/06/16)
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- Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151)
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Described herein is a modern approach to the rapid preparation and evaluation of compounds as potential back-up drug candidates. GW311616A, 1, a derivative of pyrrolidine trans-lactams, has previously been described as a potent, orally active inhibitor of
- Macdonald, Simon J. F.,Dowle, Michael D.,Harrison, Lee A.,Clarke, Geoffrey D. E.,Inglis, Graham G. A.,Johnson, Martin R.,Shah, Pritom,Smith, Robin A.,Amour, Augustin,Fleetwood, Gill,Humphreys, Davina C.,Molloy, Christopher R.,Dixon, Mary,Godward, Rosalind E.,Wonacott, Alan J.,Singh, Onkar M. P.,Hodgson, Simon T.,Hardy, George W.
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p. 3878 - 3890
(2007/10/03)
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- Total synthesis of (-)-virginiamycin M2 using second-generation vinylogous urethane chemistry
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Antibiotics known as the virginiamycins consist of two groups-polyunsaturated macrolactones (type A) and peptidic macrolactones (type B). Mixtures of type A and type B virginiamycins exhibit very high potency against a variety of bacteria. Total syntheses
- Schlessinger,Li
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p. 3301 - 3302
(2007/10/03)
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