The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.
Tetrahydronicotinamide derivatives, a process for producing the same and a pharmaceutical composition comprising the same
申请人:Chugai Seiyaku
Kabushiki Kaisha
公开号:EP0083378A1
公开(公告)日:1983-07-13
1,4,5,6-Tetrahydronicotinamide derivatives represented by the formula:
wherein R is a phenyl or pyridyl group which may have one or more substituents, or a salt thereof.
A process of preparing the same and a pharmaceutical composition containing the same.
The compounds suppress the aggregation of platelets, and have antiinflammatory, antipyretic and analgesic activity.
1,4,5,6-四氢烟酰胺衍生物,其代表式为
其中 R 为苯基或吡啶基,可带有一个或多个取代基,或其盐。
一种制备上述化合物的工艺和一种含有上述化合物的药物组合物。
这些化合物可抑制血小板的聚集,并具有抗炎、解热和镇痛活性。
Direct synthesis of primary arylamines via C–N cross-coupling of aryl bromides and triflates with amides
Aryl halides and triflates are coupled with primary amides to give the corresponding arylamines in the presence of a palladium catalyst, a suitable ligand, and a base. The catalyst system performs well for a large number of different substrates at 100-150 degrees C without solvent, and with low catalyst levels (0.12 mol% Pd). Nicotinamide might be useful as a nitrogen source in the Pd-catalyzed amination reaction. (C) 2009 Elsevier Ltd. All rights reserved.
Harrington, Philip M., Heterocycles, 1993, vol. 35, # 2, p. 683 - 687