- INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
-
The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as T
- -
-
Page/Page column 69; 75; 130
(2013/04/25)
-
- The dutch resolution variant of the classical resolution of racemates by formation of diastereomeric salts: Family behaviour in nucleation inhibition
-
The resolution of racemates through their diastereomeric salts can be positively affected by the addition of small amounts of suitable nucleation inhibitors. This discovery is a logical extension of "Dutch Resolution", in which equimolar amounts of resolving agents that are members of the same family (i.e., structurally related) are used. We conducted a systematic search for nucleation inhibitors of the resolving agent 1-phenylethylamine. A wide range of amines that bear possible family resemblances to 1-phenylethylamine was investigated. It was found that (R)-1-phenylbutylamine is a good inhibitor of (R)-1-phenylethylamine. Results of turbidity measurements showed that, for the model case of mandelic acid resolution, the chief effect of this inhibitor was to widen the metastable zone for the more soluble diastereomer. This observation is in accordance with previous experience. Further scouting for possible family members revealed a wide variation in the effectiveness of inhibitors, dependent on their structure. By far the most effective inhibitors are bifunctional 1-phenylethylamine and/or 1-phenylbutylamine analogues. The effect of racemic inhibitors was found to approach that of enantiomerically pure inhibitors of the same absolute configuration of the 1-phenylethylamine used for resolution. The most effective inhibitors were tested for the resolution of a structural variety of racemates, and were shown to be broadly applicable.
- Dalmolen, Jan,Tiemersma-Wegman, Theodora D.,Nieuwenhuijzen, Jose W.,Van Der Sluis, Marcel,Van Echten, Erik,Vries, Ton R.,Kaptein, Bernard,Broxterman, Quirinius B.,Kellogg, Richard M.
-
p. 5619 - 5624
(2007/10/03)
-
- Hypoglycemic α cycloalkylphenylmethyl, furanalkyl, and thiophenealkyl lactamimides
-
A series of α cycloalkylphenylmethyl lactamimides and a series of furan and thiophenealkyl lactamimides were prepared for biological evaluation as an extension of earlier findings of hypoglycemic activity in lactamimides. Several compounds produced pronouced hypoglycemia after oral administration to fasted, glucose primed rats.
- Grisar,Claxton,Wiech
-
p. 365 - 369
(2007/10/04)
-