The present invention relates to compounds that are inhibitors of c-jun N-terminal kinase 1, 2, or 3 (JNK1, JNK2, or JNK3), compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the activation of JNK1, JNK2 and JNK3.
[EN] INHIBITORS OF Akt ACTIVITY<br/>[FR] INHIBITEURS DE L'ACTIVITE DE AKT
申请人:SMITHKLINE BEECHAM CORP
公开号:WO2005011700A1
公开(公告)日:2005-02-10
Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yI compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
[EN] C-28 AMINES OF C-3 MODIFIED BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS<br/>[FR] AMINES EN C28 DE DÉRIVÉS D'ACIDE BÉTULINIQUE MODIFIÉ EN C-3 EN TANT QU'INHIBITEURS DE MATURATION DU VIH
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2012106188A1
公开(公告)日:2012-08-09
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. In particular, the following compounds are provided herein, including pharmaceutically acceptable salts thereof: a compound of formula (I), a compound of formula (II), and a compound of formula (III).
Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide c-Jun NH<sub>2</sub>-Terminal Kinase Inhibitors
作者:Hongyu Zhao、Michael D. Serby、Zhili Xin、Bruce G. Szczepankiewicz、Mei Liu、Christi Kosogof、Bo Liu、Lissa T. J. Nelson、Eric F. Johnson、Sanyi Wang、Terry Pederson、Rebecca J. Gum、Jill E. Clampit、Deanna L. Haasch、Cele Abad-Zapatero、Elizabeth H. Fry、Cristina Rondinone、James M. Trevillyan、Hing L. Sham、Gang Liu
DOI:10.1021/jm060465l
日期:2006.7.1
C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK inhibitors could be valuable tools to study the therapeutic benefits of inhibiting these enzymes and as leads for potential drugs targeting JNKs. In this
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.