[EN] FUSED TRICYCLIC THIOPHENE DERIVATIVES AS MEK INHIBITORS<br/>[FR] DÉRIVÉS DE THIOPHÈNE TRICYCLIQUE CONDENSÉS SERVANT D'INHIBITEURS DE MEK
申请人:UCB PHARMA SA
公开号:WO2009093009A1
公开(公告)日:2009-07-30
A series of fused tricyclic thiophene derivatives, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
Chromogenic conjugates for color-based detection of targets are described. The conjugates comprise a chromogenic moiety such as rhodamine, rhodol or fluorescein. The chromogenic moiety is linked to a peroxidase substrate. The chromogenic conjugates can be used in immunohistochemical analysis and in situ hybridization. The conjugates can be used to detect 1, 2, 3 or more targets in a sample by color.
[EN] FUSED THIOPHENE DERIVATIVES AS MEK INHIBITORS<br/>[FR] DÉRIVÉS DE THIOPHÈNE CONDENSÉS SERVANT D'INHIBITEURS DE MEK
申请人:UCB PHARMA SA
公开号:WO2009093013A1
公开(公告)日:2009-07-30
A series of 7-oxo-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives, and analogues thereof, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
The present invention is concerned with isoxazole-pyridine derivatives of formula I
wherein X, R
1
to R
6
are as described herein. The compounds are active on the GABA A α5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
本发明涉及式I的异恶唑-吡啶衍生物
其中X,R1至R6如本文所述。这些化合物对GABA A α5受体结合位点具有活性,并可用于治疗认知障碍,如阿尔茨海默病。
A formal method for the de-N,N-dialkylation of Sommelet–Hauser rearrangement products
Selective amine de-alkylation enables the conversion of Sommelet–Hauserrearrangement products into 2-aryl-2-bromoacetic acid derivatives. These compounds are valuable synthetic intermediates in the synthesis of α-aryl-α-amino or α-aryl-β-amino acid derivatives. The method presented herein is a formal de-N,N-dialkylation of Sommelet–Hauserrearrangement products.