- SUBSTITUTED HETEROCYCLIC AMIDE COMPOUND AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
-
Provided are a substituted heterocyclic amide compound having a selective inhibitory effect on RIPK1, and a pharmaceutically acceptable salt, a stereoisomer, a solvate or a prodrug thereof, and a pharmaceutical composition containing the compound, and the
- -
-
-
- O-GLYCOPROTEIN-2-ACETAMIDO-2-DEOXY-3-D-GLYCOPYRANOSIDASE INHIBITORS
-
Described herein are compounds represented by formula (I") or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, Ra, Rb, m, n, Y
- -
-
-
- Bicyclic Benzimidazole Compounds and Their Use as Metabotropic Glutamate Receptor Potentiators
-
Compounds of Formula I: wherein A, B, D, L, R1, R2, R3, R4, m, and n are as defined for Formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
- -
-
Page/Page column 65
(2009/08/14)
-
- Stereoselective process for a CCR3 antagonist
-
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
-
p. 262 - 271
(2012/12/22)
-
- Efficient preparation of (3S)-3-(4-fluorobenzyl)piperidinium mandelate
-
Methods for the preparation of (3S)-3-(4-fluorobenzyl)piperidine (2) and its mandelate salt (9) are described. The first generation synthesis started from 3-benzylpiperidone, and required Boc protection of the nitrogen for efficient separation of the enantiomers using chromatography on a chiral stationary phase. Subsequently, a resolution method using (R)-mandelic acid, produced high %ee salt 9 after recrystallization and eliminated the need for Boc protection. The third generation route, starting from pyridine-3- carboxaldehyde, led to a streamlined synthesis of racemate 2 and was optimized for producing multi-hundred gram quantities of the chiral salt.
- Emmett, George C.,Cain, Gary A.,Estrella, Melissa J.,Holler, Edd R.,Piecara, James S.,Blum, Andrew M.,Mical, Alfred J.,Teleha, Christopher A.,Wacker, Dean A.
-
-
- Substituted fused bicyclic amines as modulators of chemokine receptor activity
-
The present application describes modulators of CCR3 of formula (Ia) and (Ib): or pharmaceutically acceptable salt forms thereof, wherein Z, R1, R2, R3, R4, R5, R5′, R6, a, b, c, d, and u are as defined herein. 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 said modulators are disclosed.
- -
-
Page/Page column 23
(2010/02/13)
-
- A facile synthesis of 3-(substituted benzyl)piperidines
-
A convenient new method has been developed for preparation a series of 3-(substituted benzyl)piperidines by addition of substituted phenylmagnesium bromide to pyridine-3-carboxaldehyde followed by one pot deoxygenation and heteroaromatic ring saturation in the presence of palladium catalyst.
- ágai, Béla,Nádor, Adrienn,Proszenyák, ágnes,Tárkányi, Gábor,Faigl, Ferenc
-
p. 7897 - 7900
(2007/10/03)
-
- Piperidine amides as modulators of chemo kine receptor activity
-
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
- -
-
-