Substituted indole compounds, their preparation and use in medicaments
申请人:LABORATORIOS DEL DR. ESTEVE, S.A.
公开号:EP1717227A1
公开(公告)日:2006-11-02
The present invention relates to substituted indole compounds of general formula I,
a process for their preparation, medicaments comprising substituted indole compounds as well as the use of substituted indole compounds for the preparation of medicaments, which are suitable e.g. for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
本发明涉及通式 I 的取代吲哚化合物、
本发明涉及取代的吲哚化合物、其制备工艺、包含取代的吲哚化合物的药物以及使用取代的吲哚化合物制备药物,这些药物适用于预防和/或治疗至少部分通过5-HT6受体介导的紊乱或疾病。
5HT6-Ligands such as sulfonamide derivatives in drug-induced weight-gain
申请人:Laboratorios del Dr. Esteve S.A.
公开号:EP2018861A1
公开(公告)日:2009-01-28
The present invention relates to the use of Compounds binding to the 5HT6 receptor such as sulfonamide compounds of formula I in the manufacture of a medicament for the treatment of weight gain, obesity or associated cardio-metabolic risk factors induced by a therapeutic drug.
wherein
--Z either represents =C(R10) or -CH2 or =N;
and wherein
either
Y represents -S(O2)-R13, while X represents R1;
or
X represents R1, while Y represents (CH2)n-R11 or
Y represents R1, while X represents (CH2)n-R12;
while
one of R9a, R9b, R9c, or R9d represents N(R3)-S(O2)-A, or N-(S(O2)-A)2.
本发明涉及与 5HT6 受体结合的化合物如式 I 的磺酰胺化合物在制造治疗药物中的用途,该药物用于治疗由治疗药物诱发的体重增加、肥胖或相关的心血管代谢危险因素。
其中
--Z代表=C(R10)或-CH2或=N;
其中
或者
Y 代表 -S(O2)-R13,而 X 代表 R1;
或
X 代表 R1,而 Y 代表 (CH2)n-R11 或
Y 代表 R1,而 X 代表 (CH2)n-R12;
同时
R9a、R9b、R9c 或 R9d 中的一个代表 N(R3)-S(O2)-A,或 N-(S(O2)-A)2。
Development of an organo- and enzyme-catalysed one-pot, sequential three-component reaction
作者:Angela Kinnell、Thomas Harman、Matilda Bingham、Alan Berry、Adam Nelson
DOI:10.1016/j.tet.2012.02.010
日期:2012.9
A one-pot, three-component process is described which involves both organo- and enzyme-catalysed carbon-carbon bond-forming steps. In the first step, an organocatalyst catalyses the aldol reaction between acetaldehyde and a glyoxylamide. After dilution with additional aqueous buffer, and addition of pyruvate and an aldolase enzyme variant, a second aldol reaction occurs to yield a final product. Crucially, it was possible to develop a reaction in which both the organo- and enzyme-catalysed reactions could be performed in the same aqueous buffer system. The reaction described is the first example of a one-pot, three-component reaction in which the two carbon-carbon bond-forming processes are catalysed using the combination of an organocatalyst and an enzyme. (C) 2012 Elsevier Ltd. All rights reserved.
NEW CENTRALLY ACTING 6,7,8,9-TETRAHYDRO-3H-BENZ(e)INDOLE HETEROCYCLICS
申请人:THE UPJOHN COMPANY
公开号:EP0510068A1
公开(公告)日:1992-10-28
COMBINATION OF NMDA- RECEPTOR LIGAND AND A COMPOUND WITH 5-HT6 RECEPTOR AFFINITY