与非选择性临床使用的药物相比,γ-氨基丁酸A型受体(GABA A R)的亚基选择性调节被认为产生的副作用更少。在这里,β2/ 3亚基选择性GABA A R调节剂戊烯酸(VA)和洛雷唑(LOR)指导了结构简化的新型亚基选择性配体的合成。我们使用两个微电极电压钳技术研究了它们对非洲爪蟾卵母细胞中表达的GABA A Rs的影响。与VA和LOR相比,五种化合物显示出对GABA诱发的电流的调制显着更有效,并且保留了效力和选择性。化合物18 [(E)-2–氰基-3-(2,4-二氯苯基)丁-2-烯酰胺]诱导了最大的GABA诱导的氯离子电流调制(E max:3114±242%),而12 [(Z)-3 -(2,4-二氯苯基)丁-2-乙腈]显示出最高的效价(EC 50:13±2μM)。此外,在海马神经元中12促进了阶段性和强直性GABA的抑制作用,并且体内研究显示,与戊二醛和LOR相比,抗戊烯四唑(PTZ)诱
The present invention relates to a process for the manufacture of an angiotensin receptor blocker (ARB: also called angiotension II receptor antagonist or AT1 receptor antagonist) and salts, thereof, to novel intermediates and process steps.
The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.
[EN] PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES<br/>[FR] PROCESSUS DE PREPARATION DE DERIVES DE TETRAZOLE ISSUS DE BORE ORGANO ET D'AZIDES D'ALUMINIUM ORGANO
申请人:NOVARTIS AG
公开号:WO2005014602A1
公开(公告)日:2005-02-17
The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.
本发明涉及一种制备取代四唑的方法,根据该方法获得的化合物,新的反应物和新的四唑衍生物。
Process for the preparation of tetrazole derivatives from organo boron and organo aluminium azides
申请人:Sedelmeier Gottfried
公开号:US20070043098A1
公开(公告)日:2007-02-22
The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.
本发明涉及一种制备取代四氮唑的方法,根据该方法获得的化合物、新的反应物和新的四氮唑衍生物。
PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES
申请人:Sedelmeier Gottfried
公开号:US20110184187A1
公开(公告)日:2011-07-28
The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.