Indolinone derivatives substituted in the 6 position, the preparation thereof and their use as pharmaceutical compositions
申请人:Heckel Armin
公开号:US20060194813A1
公开(公告)日:2006-08-31
The present invention relates to indolinone derivatives substituted in the 6 position of general formula
wherein
R
1
to R
6
and X are defined as in claim
1
, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
BETA-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
申请人:Takeda Chemical Industries, Ltd.
公开号:EP1132376A1
公开(公告)日:2001-09-12
A compound of the formula:
wherein Ar is an aromatic group; X and Y are a bivalent group selected from -O-, -S-, -CO-, -SO-, -SO2-, -NR8-,-CONR8-, SO2NR8 and -COO- (wherein R8 is H, a hydrocarbon group or acyl), or a bivalent C1-6 aliphatic hydrocarbon group which may contain one or two above bivalent groups; R1 and R2 are H or C1-6 alkyl, or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring; and ring A is a monocyclic aromatic ring, or a salt thereof or a prodrug thereof exhibits an excellent inhibitory activity of the production and/or the secretion of amyloid-β protein.
式中的化合物: 其中 Ar 是芳香基;X 和 Y 是选自-O-、-S-、-CO-、-SO-、-SO2-、-NR8-、-CONR8-、SO2NR8 和-COO-(其中 R8 是 H、烃基或酰基)的二价基团,或可包含一个或两个上述二价基团的二价 C1-6 脂肪族烃基; R1和R2为H或C1-6烷基,或R1和R2可与相邻的氮原子一起形成含氮杂环;以及环A为单环芳香环,或其盐或其原药对淀粉样β蛋白的产生和/或分泌具有极佳的抑制活性。
IN 6-STELLUNG SUBSTITUIERTE INDOLINONDERIVATE, IHRE HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL