Diastereoselective [3+2] Annulation of Aromatic/Vinylic Amides with Bicyclic Alkenes through Cobalt-Catalyzed C−H Activation and Intramolecular Nucleophilic Addition
dihydroepoxybenzofluorenone derivatives fromaromatic/vinylic amides and bicyclic alkenes is described. This new transformation proceeds through cobalt‐catalyzed C−H activation and intramolecular nucleophilic addition to the amide functional group. Transition‐metal‐catalyzed C−H activation reactions of secondary amides with alkenes usually lead to [4+2] or [4+1] annulation; to the best of our knowledge
[EN] SUBSTITUTED HETEROCYCLIC DERIVATIVES AS GPR AGONISTS AND USES THEREOF<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES SUBSTITUÉS EN TANT QU'AGONISTES DE GPR ET LEURS UTILISATIONS
申请人:PIRAMAL ENTPR LTD
公开号:WO2015028960A1
公开(公告)日:2015-03-05
The present invention generally relates to substituted heterocyclic derivatives (the compounds of Formula (I)), processes for their preparation, pharmaceutical compositions containing said compounds, their use as G-protein coupled receptor (GPR) agonists, particularly as GPR40 agonists and methods of using these compounds in the treatment of GPR40 mediated diseases or conditions such as Type 2 diabetes, obesity, dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
[EN] MULTIVALENT INHIBITORS OF SERUM AMYLOID P COMPONENT<br/>[FR] INHIBITEURS POLYVALENTS DE LA COMPOSANTE P DES AMYLOIDES SERIQUES
申请人:THERACARB INC
公开号:WO2004099173A1
公开(公告)日:2004-11-18
Novel glycerol cyclic pyruvate derivates were prepared and demonstrated to inhibit the binding of an immobilized D-proline derivative to serum amyloid P component (SAP) have been prepared. As such, the compounds of the invention are useful for treating amyloidosis and diseases associated with amyloidosis, for example Alzheimer's disease and maturity onset diabetes mellitus.
[EN] COMPOSITIONS AND METHODS FOR INHIBITING ACTIVITY OF HYPOXIA-INDUCIBLE TRANSCRIPTION FACTOR COMPLEX AND ITS USE FOR TREATMENT OF TUMORS<br/>[FR] COMPOSITIONS ET PROCÉDÉS D'INHIBITION DE L'ACTIVITÉ DU COMPLEXE DE FACTEUR DE TRANSCRIPTION INDUCTIBLE PAR L'HYPOXIE, ET UTILISATION DANS LE TRAITEMENT DE TUMEURS
申请人:UNIV SOUTHERN CALIFORNIA
公开号:WO2014035484A1
公开(公告)日:2014-03-06
Disclosed are epidithiodiketopiperazine compounds, pharmaceutical compositions based thereon and methods of treating, reducing or inhibiting transcription and translation of hypoxia-inducible genes. An embodiment of the present invention is directed to a method for interfering with hypoxia-induced transcriptional pathway. Generally, the method according to this embodiment comprises contacting a cell with at least one compound according to either Formula I, Formula II or Formula III, or a salt, solvent or hydrate thereof.
Regioselectivity in the Aryne Cross-Coupling of Aryllithiums with Functionalized 1,2-Dibromobenzenes
作者:Vincent Diemer、Manon Begaud、Frédéric R. Leroux、Françoise Colobert
DOI:10.1002/ejoc.201001283
日期:2011.1
Tri- and tetrasubstituted ortho-bromobiaryls have been synthesized in good-to-excellent yields by arynecross-coupling reactions starting from 1,3-dimethoxybenzene and functionalized1,2-dibromobenzenes. This study outlines the influence of the 1,2-dibromobenzene precursor as well as the reaction temperature on the outcome of the aryl-aryl bond formation and indicates, in the case of dissymmetrical