- PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present application describes modulators of MIP-1 of formula (I) : or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
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Page/Page column 68-69
(2009/03/07)
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- Stereoselective process for a CCR3 antagonist
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A convergent, multikilogram, stereoselective synthesis of 1 is described. A key fragment, (S)-3-(4-fluorobenzyl)piperidine (2) was synthesized from valerolactam in three steps using our recently discovered Ir-BDPP-catalyzed asymmetric hydrogenation. Anoth
- Yue, Tai-Yuen,McLeod, Douglas D.,Albertson, Kevin B.,Beck, Steven R.,Deerberg, Joerg,Fortunak, Joseph M.,Nugent, William A.,Radesca, Lilian A.,Tang, Liya,Xiang, Cathie Dong
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p. 262 - 271
(2012/12/22)
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- Asymmetric catalytic hydrogenation process for preparation of chiral cyclic beta-aminoesters
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A novel process for the asymmetric synthesis of substituted cyclic β-amino-carboxylates of the type shown in the specification from appropriate β-enamino-ester starting materials is described. These compounds are useful as intermediates for MMP and TACE i
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- Asymmetric synthesis of a new helix-forming β-amino acid: trans-4-aminopiperidine-3-carboxylic acid
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We report a synthesis of a protected derivative of trans-4aminopiperidine-3-carboxylic acid (APiC). The route provides either enantiomer. All intermediates are purified by crystallization, and large-scale preparation is therefore possible. An analogous ro
- Schinnerl, Marina,Murray, Justin K.,Langenhan, Joseph M.,Gellman, Samuel H.
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p. 721 - 726
(2007/10/03)
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- Stereoselective reduction of enantiopure β-enamino esters by hydride: A convenient synthesis of both enantiopure β-amino esters
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The reduction of enantiopure β-enamino esters 1 with sodium triacetoxyborohydride in acetic acid is described. This occurs with good diastereo- and enantioselectivity to yield β-amino esters 2 and 3 (after hydrogenolysis of the N-chiral group). A model is
- Cimarelli, Cristina,Palmieri, Gianni
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p. 5557 - 5563
(2007/10/03)
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- Diastereo and Enantioselective Entry to β-Amino Esters by Hydride Reduction of Homochiral β-Enamino Esters.
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The reduction of homochiral β-enamino esters 1 with sodium triacetoxyborohydride, which occurs with good diastereo- and enantioselectivity in the β-amino esters 2, is described.The procedure allows a straightforward preparation of compounds with known bio
- Cimarelli, Cristina,Palmieri, Gianni,Bartoli, Giuseppe
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p. 1455 - 1458
(2007/10/02)
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