[EN] BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE [FR] INHIBITEURS DE BENZYLETHER ET BENZYLAMINO DE BETA-SECRETASE POUR TRAITER LA MALADIE D'ALZHEIMER
[EN] MACROCYCLES AS PIM INHIBITORS<br/>[FR] MACROCYCLES EN TANT QU'INHIBITEURS DE PIM
申请人:AMGEN INC
公开号:WO2014022752A1
公开(公告)日:2014-02-06
The invention relates to compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
[EN] 1,3,5-SUBSTITUTED PHENYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE<br/>[FR] DERIVES DE PHENYLE 1,3,5-SUBSTITUES UTILES COMME INHIBITEURS DE LA BETA-SECRETASE POUR LE TRAITEMENT DE LA MALADIE D'ALZHEIMER
申请人:MERCK & CO INC
公开号:WO2005103020A1
公开(公告)日:2005-11-03
The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Lanthanide‐catalyzed alkynyl exchange through C−C single‐bondcleavage assisted by a secondary amino group is reported. A lanthanide amido complex is proposed as a key intermediate, which undergoes unprecedented reversible β‐alkynyl elimination followed by alkynyl exchange and imine reinsertion. The in situ homo‐ and cross‐dimerization of the liberated alkyne can serve as an additional driving force
[EN] BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE<br/>[FR] INHIBITEURS DE BENZYLETHER ET BENZYLAMINO DE BETA-SECRETASE POUR TRAITER LA MALADIE D'ALZHEIMER
申请人:MERCK & CO INC
公开号:WO2005051914A1
公开(公告)日:2005-06-09
The present invention is directed to benzylether and benzylamino derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.