这封信详细介绍了咪唑并[4,5- b ]吡啶类作为B-Raf激酶抑制剂的合成和评价。这些化合物以B-Raf的DFG-in,αC-螺旋构象结合,这是与显着的激酶选择性相关的结合模式。结构与活性之间的关系研究涉及优化这些分子的ATP裂隙结合区,并产生化合物23,这是一种具有出色的酶/细胞效能和激酶选择性的抑制剂。
[EN] SUBSTITUTED PYRIDINE AND PYRAZINE BMI-1 INHIBITORS<br/>[FR] INHIBITEURS DE BMI-1 À BASE DE PYRIDINE ET DE PYRAZINE SUBSTITUÉES
申请人:PTC THERAPEUTICS INC
公开号:WO2015076800A1
公开(公告)日:2015-05-28
Amine substituted pyridine and pyrazine compounds and forms thereof that inhibit the function and reduce the level of B -cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
[EN] NOVEL INHIBITORS OF BACTERIAL GLUTAMINYL CYCLASES FOR USE IN THE TREATMENT OF PERIODONTAL AND RELATED DISEASES<br/>[FR] NOUVEAUX INHIBITEURS DE GLUTAMINYL-CYCLASES BACTÉRIENNES DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DE PARODONTOPATHIES ET DE MALADIES ASSOCIÉES
申请人:FRAUNHOFER GES FORSCHUNG
公开号:WO2019162458A1
公开(公告)日:2019-08-29
The present invention relates to novel compounds which are particularly useful as inhibitors of bacterial glutaminyl cyclases (bacQC); pharmaceutical compositions comprising such compounds; compounds and/or pharmaceutical compositions for use in methods for treatment, in particular for use in the treatment of periodontitis and related conditions; as well as to crystals comprising bacterial glutaminyl cyclases, methods for identifying candidate compounds which may associate with the binding pocket of a bacQC and/or are bacQC inhibitors.
The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
[EN] BENZOPHENONES AS INHIBITORS OF REVERSE TRANSCRIPTASE<br/>[FR] BENZOPHENONES AGISSANT COMME INHIBITEURS DE LA TRANSCRIPTASE INVERSE
申请人:GLAXO GROUP LTD
公开号:WO2001017982A1
公开(公告)日:2001-03-15
The present invention includes benzophenone compounds (I) which are useful in the treatment of HIV infections.
本发明包括苯甲酮化合物(I),其在治疗HIV感染方面具有用处。
HETEROARYL DERIVATIVES AS PROTEIN KINASE INHIBITORS
申请人:Honold Konrad
公开号:US20090318428A1
公开(公告)日:2009-12-24
Objects of the present invention are the compounds of formula I
their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.