Provided are compounds and compositions which modulate the level or activity of PIP4K2C. Also provided are methods for treating diseases or conditions by modulating (e.g., reducing) the level or activity of a PIP4K2C, comprising administering the compounds and compositions.
INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
申请人:LES LABORATOIRES SERVIER
公开号:US20160176848A1
公开(公告)日:2016-06-23
Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description.
Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
Compounds of Formula la, lb, or Ic, are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.
[EN] 2,6,7,8 SUBSTITUTED PURINES AS HDM2 INHIBITORS<br/>[FR] PURINES 2,6,7,8-SUBSTITUÉES UTILISÉES EN TANT QU'INHIBITEURS DE HDM2
申请人:MERCK SHARP & DOHME
公开号:WO2014120748A1
公开(公告)日:2014-08-07
The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
hydroboration with catecholborane), alkyl iodides (via iodineatom transfer) and xanthates is reported. The reaction proceeds under neutral conditions since no acid is needed to activate the heterocycle and no external oxidant is required. A rateconstant for the addition of a primary radical to N-methoxylepidinium >107 M−1 s−1 was experimentally determined. This rateconstant is more than one order of magnitude
报道了N-甲氧基吡啶鎓盐与由烯烃(通过与儿茶酚硼烷的硼氢化反应)、烷基碘化物(通过碘原子转移)和黄原酸盐产生的烷基自由基的单烷基化反应。反应在中性条件下进行,因为不需要酸来活化杂环,也不需要外部氧化剂。将伯自由基添加到N-甲氧基吡啶鎓的速率常数>10 7 M -1 s -1是通过实验确定的。该速率常数比将伯烷基自由基添加到质子化来比啶所测得的速率常数大一个数量级以上,这表明甲氧基吡啶鎓盐对自由基具有显着的反应性。该反应已用于制备独特的吡啶化萜类化合物,并扩展到富电子烯烃(包括烯醇酯、烯醇醚和烯酰胺)的三组分碳吡啶基化反应。