- BICYCLIC TRIAZOLE A4 INTEGRIN INHIBITORS
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The compounds of the present invention are novel bicyclic triazole amino acid-derivatives useful as a4 integrin receptor antagonists. The invention is further directed to methods for treating integrin mediated disorders including, but not limited to, infl
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Page/Page column 38-39
(2008/06/13)
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- The Baylis-Hillman reaction with chiral α-amino aldehydes under racemization-free conditions
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The Baylis-Hillman reaction with chiral α-amino aldehydes has been revisited. The reaction carried out under the influence of ultrasound avoids the aldehyde racemization almost completely, providing useful chiral substrates which can be used as starting materials for the synthesis of natural products. To demonstrate the synthetic applicability of these adducts, the easy preparation of a bicyclic lactam with an indolizidinic skeleton was accomplished. Georg Thieme Verlag Stuttgart.
- Coelho, Fernando,Diaz, Gaspar,Abella, Carlos A. M.,Almeida, Wanda P.
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p. 435 - 439
(2007/10/03)
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- Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha
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The present application describes novel β-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3
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Page/Page column 48
(2010/11/30)
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- 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor
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5-(4-Chlorophenyl)-3-(1-(4-chlorobenzyl)piperidin-4-yl)pyrazole (3) was identified from screening of the Merck sample collection as a human dopamine D4 (hD4) receptor ligand with moderate affinity (61 nM) and 4-fold selectivity over human D2 (hD2) recepto
- Rowley, Michael,Collins, Ian,Broughton, Howard B.,Davey, William B.,Baker, Raymond,Emms, Frances,Marwood, Rosemarie,Patel, Shil,Patel, Smita,Ragan, C. Ian,Freedman, Stephen B.,Ball, Richard,Leeson, Paul D.
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p. 2374 - 2385
(2007/10/03)
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