Studies towards the total synthesis of mumbaistatin: synthesis of highly substituted benzophenone and anthraquinone building blocks
摘要:
Model compounds and building blocks for a planned total synthesis of the highly potent glucose-6-phosphate (G6P) translocase inhibitor mumbaistatin (1) and structural analogs were elaborated: compound 1 represents a lead structure in the development of potential new antidiabetic drugs. With the model substrate 20 it was demonstrated that highly functionalized, tetra-ortho-substituted benzophenones can be prepared by nucleophilic addition of an aryllithium-building block to a benzaldehyde followed by oxidation. For compound 37, a potential precursor of the anthraquinone part of mumbaistatin, various approaches via aryne/phthalide annulations were developed and evaluated. The required functionalized arenes were prepared exploiting, among others, regioselective bromination and ortho-lithiation reactions. Coupling reactions of the anthracene-carbaldehyde 44 derived from 37 with various metalated arenes proved to be unexpectedly difficult and failed so far. (C) 2003 Elsevier Science Ltd. All rights reserved.
[EN] HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS<br/>[FR] DÉRIVÉS D'HYDANTOÏNE UTILES EN TANT QU'INHIBITEURS DE KV3
申请人:AUTIFONY THERAPEUTICS LTD
公开号:WO2012076877A1
公开(公告)日:2012-06-14
The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
该发明提供了化合物的公式(I):所述化合物是Kv3通道的抑制剂,可用于预防或治疗相关疾病。
Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
申请人:Chao J. Hannguang
公开号:US20050267119A1
公开(公告)日:2005-12-01
The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y
1
receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y
1
receptor activity.
UREA ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS
申请人:Chao Hannguang J.
公开号:US20080280905A1
公开(公告)日:2008-11-13
The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y
1
receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y
1
receptor activity.
The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
本发明提供了式(I)的化合物:所述化合物是Kv3通道的抑制剂,用于预防或治疗相关疾病。
Arene-metal complex in organic synthesis: directed regioselective lithiation of (.pi.-substituted benzene)chromium tricarbonyl complexes