申请人:Allelix Biopharmaceuticals, Inc.
公开号:US05998438A1
公开(公告)日:1999-12-07
Described herein are compounds selective for a 5-HT.sub.1D -like receptor, which have the general formula: ##STR1## wherein A is selected from a six-membered, non-aromatic, optionally substituted carbocycle and a six-membered, non-aromatic, optionally substituted heterocycle having one or two heteroatoms selected from O, S, SO, SO.sub.2 and N.sup.4 ; R.sup.1 is selected from H and OH; n is 0 or 1 as permited by chemical structure; R.sup.2 is selected from CR.sup.5 CR.sup.6 CH.sub.2 NR.sup.7 R.sup.8 or a group of formula II, III or IV: ##STR2## R.sup.3 is selected from H and benzoyl; R.sup.4 is selected from H, loweralkyl, benzyl, loweralkylcarbonyl, loweralkylaminocarbonyl, loweralkylaminothiocarbonyl, loweralkanoyl, loweralkylaminoimide and loweralkoxy-substituted loweralkylene; R.sup.5 and R.sup.6 are independently selected from H, loweralkoxy and hydroxy; R.sup.7 and R.sup.8 are independently selected from H and loweralkyl or R.sup.7 and R.sup.8 form an alkylene bridge which, together with the nitrogen atom to which they are attached, creates an optionally substituted 3- to 6-membered ring; denotes a single or double bond; and R.sup.9, R.sup.10 and R.sup.11 are independently selected from H and loweralkyl. Also described is the use of these compounds as pharmaceuticals to treat indications where stimulation of a 5-HT.sub.1D -like receptor is implicated, such as migraine.
本文描述的是对5-HT.sub.1D-类受体具有选择性的化合物,其具有以下通式:##STR1##其中A选自一个六元非芳香族、可选择性取代的碳环和一个六元非芳香族、可选择性取代的杂环,其中含有一个或两个来自O、S、SO、SO.sub.2和N.sup.4的杂原子;R.sup.1选自H和OH;n根据化学结构允许为0或1;R.sup.2选自CR.sup.5 CR.sup.6 CH.sub.2 NR.sup.7 R.sup.8或具有以下式II、III或IV的基团:##STR2##R.sup.3选自H和苯甲酰基;R.sup.4选自H、较低烷基、苄基、较低烷基羰基、较低烷基氨基羰基、较低烷基氨基硫氨基羰基、较低烷酰基、较低烷基氨基亚胺和较低烷氧基取代的较低烷基烯;R.sup.5和R.sup.6独立选自H、较低烷氧基和羟基;R.sup.7和R.sup.8独立选自H和较低烷基,或者R.sup.7和R.sup.8形成一个与它们附着的氮原子一起构成一个可选择性取代的3-至6-成员环的烷基桥;表示单键或双键;R.sup.9、R.sup.10和R.sup.11独立选自H和较低烷基。还描述了将这些化合物用作药物来治疗刺激5-HT.sub.1D-类受体所涉及的症状,如偏头痛。