[EN] ISOQUINOLINE-5-SULFONIC ACID AMIDES AS INHIBITORS OF AKT (PROTEIN KINASE B)<br/>[FR] UTILISATION D'AMIDES D'ACIDE ISOQUINOLINE-5-SULFONIQUE COMME INHIBITEURS DE L'AKT (PROTEINE KINASE B)
申请人:LILLY CO ELI
公开号:WO2004094386A1
公开(公告)日:2004-11-04
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
本发明涉及化合物式(I):作为AKT活性抑制剂,对易感肿瘤和病毒感染的治疗有用。
Inhibitors of akt (protein kinase b)
申请人:Al-Awar Salim Rima
公开号:US20070043040A1
公开(公告)日:2007-02-22
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
本发明涉及化合物式(I):作为AKT活性抑制剂,可用于治疗易感性肿瘤和病毒感染。
Inhibitors of Akt (protein kinase B)
申请人:Eli Lilly and Company
公开号:US07414063B2
公开(公告)日:2008-08-19
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
本发明涉及化合物式(I): 作为AKT活性的抑制剂,适用于治疗易感肿瘤和病毒感染。
Synthesis and antidepressant activity of substituted (.omega.-aminoalkoxy)benzene derivatives
作者:Ryoji Kikumoto、Akihiro Tobe、Shinji Tonomura
DOI:10.1021/jm00134a004
日期:1981.2
A series of substituted (omega-aminoalkoxy)benzene derivatives has been synthesized and screened for potential antidepressant activities. The effect of structural variation of these molecules has been systematically examined. Antidepressant activity was clearly displayed by 2-benzyl-1-[4-(methylamino)butoxy]benzene (7), 2-(2-hydroxybenzyl)-1-[4-(methylamino)butoxy]benzene (19), 1-[4-(methylamino)butoxy]-2-phenoxybenzene (29), and 1-[4-(methylamino)butoxy]-2-(phenylthio)benzene (31) in further pharmacological studies. These compounds did not possess the anticholinergic, antihistaminic, and muscle-relaxant side effects common to tricyclic antidepressants.
Dopamine/Serotonin Receptor Ligands. 9. Oxygen-Containing Midsized Heterocyclic Ring Systems and Nonrigidized Analogues. A Step toward Dopamine D<sub>5</sub> Receptor Selectivity
作者:Thomas W. Wittig、Michael Decker、Jochen Lehmann
DOI:10.1021/jm049720x
日期:2004.8.1
Eleven-membered heterocycles (dibenz[g,j]-1-oxa-4-azacycloundecenes) and open-chain analogues were synthesized and investigated for affinities to human dopamine receptor subtypes. The moderately rigidized rings displayed nanomolar and sulmanomolar K-i values at D-1-like receptors with a significant D-1 to D-2 and a slight D-5 to D-6 selectivity. The open-chain analogues showed lower affinities but significant D-1 to D-2 selectivities. Compound 3 (K-i(D-5) = 0.57 nmol) showed antagonistic or inverse agonistic binding characteristics in a functional Ca assay.