An optimized procedure is given for the synthesis of novel 3-(arylamino)-1,2,4-triazin-5-one building blocks from commercially available material. By employing these building blocks, a practical protocol is described for the functionalization of the 5-position of the triazine core with anilines orphenols.
Treatment of neuropathic pain with 6h-pyrrolo[3,4-d]pyridazine compounds
申请人:Anker Burke Naomi
公开号:US20060154929A1
公开(公告)日:2006-07-13
6H-pyrrolo[3,4-d]pyridazine compounds and methods of their use of as ligands of voltage gated calcium channels (VGCC), useful in the treatment of neuropathic pain, and psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other.
Treatment of neuropathic pain with 6H-pyrrolo[3,4-d]pyridazine compounds
申请人:Merck & Co. Inc.
公开号:US07465730B2
公开(公告)日:2008-12-16
6H-pyrrolo[3,4-d]pyridazine compounds and methods of their use of as ligands of voltage gated calcium channels (VGCC), useful in the treatment of neuropathic pain, and psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other.
Sterically hindered electron-deficient anilines are coupled to the 6-position of the purine core only when activated as their corresponding TFA-amide. The free anilines did not react under all conditions tested. After aqueous work-up, the TFA-group is lost.This procedure provides a new tool in the construction of purines functionalized with a sterically hindered electron-deficient aniline in the 6-position.