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1. 发明授权

US5998462A 5-alkyl indole compounds 失效
标题翻译： 5-烷基吲哚化合物
公开(公告)号：US5998462A
公开(公告)日：1999-12-07
申请号：US767323
申请日：1996-12-16
申请人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
发明人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
IPC分类号： C07D209/16 , C07D403/06 , A61K31/40
CPC分类号： C07D403/06 , C07D209/16
摘要： Described herein are compounds selective for the 5-HT.sub.1D -like receptor, which have the general formula: ##STR1## wherein: R.sup.1 is linear or branched loweralkyl;R.sup.2 is selected from a group of Formula II, III, IV and V: ##STR2## R.sup.3 is selected from H and loweralkyl; R.sup.4 is selected from H and loweralkyl;One of R.sup.5 and R.sup.6 is H and the other is independently selected from H, loweralkoxy, loweralkyl and hydroxy; andn is 1-3;or a salt, solvate or hydrate thereof.Also described is the use of these compounds as pharmaceuticals to treat indications where stimulation of the 5-HT.sub.1D -like receptor is implicated, such as migraine.
摘要翻译：本文描述的是对具有以下通式的5-HT1D样受体有选择性的化合物：其中：R1是直链或支链的低级烷基; R2选自式II，III，IV和V的基团：R3选自H和低级烷基; R4选自H和低级烷基; R5和R6之一是H，另一个独立地选自H，低级烷氧基，低级烷基和羟基; n为1-3; 或其盐，溶剂合物或水合物。还描述了这些化合物作为药物用于治疗涉及5-HT1D样受体的刺激的指征，例如偏头痛。

2. 发明授权

US5654431A 5-alkoxy tryptamine derivatives 失效
标题翻译： 5-烷氧基色胺衍生物
公开(公告)号：US5654431A
公开(公告)日：1997-08-05
申请号：US655588
申请日：1996-05-30
申请人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
发明人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
IPC分类号： C07D209/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14 , C07D209/08 , C07D221/06
CPC分类号： C07D403/06 , C07D209/14 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14
摘要： Novel 5-alkoxy tryptamine derivatives are provided, corresponding to the general formula: ##STR1## in which R may be alkaline, X may be amino, and Y is various N-heterocyclic or N-branched chain moieties. The compounds show selective binding to 5-HT.sub.1D receptor subtypes, and have potential pharmaceutical utility in manufacture of migraine-treating drugs.
摘要翻译：提供了新的5-烷氧基色胺衍生物，其对应于通式：其中R可以是碱性的，X可以是氨基，Y是各种N-杂环或N-支链部分。这些化合物显示出与5-HT1D受体亚型的选择性结合，并且在制造偏头痛药物方面具有潜在的药用效用。

3. 发明授权

US5998438A 5-cyclo indole compounds 失效
标题翻译： 5-环吲哚化合物
公开(公告)号：US5998438A
公开(公告)日：1999-12-07
申请号：US976103
申请日：1997-11-21
申请人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
发明人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
IPC分类号： C07D209/14 , C07D209/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14 , A61K31/40
CPC分类号： C07D401/04 , C07D209/14 , C07D209/18 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14
摘要： 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; andR.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.
摘要翻译：本文描述了对具有以下通式的5-HT1D样受体选择性的化合物：其中A选自六元非芳族任选取代的碳环和六元非芳族任选取代的杂环具有一个或两个选自O，S，SO，SO 2和N 4的杂原子; R1选自H和OH; n为化学结构允许的0或1; R2选自CR5CR6CH2NR7R8或式II，III或IV的基团：R3选自H和苯甲酰基; R4选自H，低级烷基，苄基，低级烷基羰基，低级烷基氨基羰基，低级烷基氨基硫代羰基，低级烷酰基，低级烷基氨基酰亚胺和低级烷氧基取代的低级亚烷基; R5和R6独立地选自H，低级烷氧基和羟基; R 7和R 8独立地选自H和低级烷基或R 7和R 8形成亚烷基桥，其与它们所连接的氮原子一起产生任选取代的3至6元环; 表示单键或双键; 并且R 9，R 10和R 11独立地选自H和低级烷基。还描述了这些化合物作为药物用于治疗涉及5-HT1D样受体的刺激的指征，例如偏头痛。

4. 发明授权

US5770742A Thiophene-tryptamine derivatives 失效
标题翻译：噻吩 - 色胺衍生物
公开(公告)号：US5770742A
公开(公告)日：1998-06-23
申请号：US648842
申请日：1996-05-16
申请人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
发明人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
IPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D403/06
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： 5-Thiophene-substituted tryptamine analogs are provided, which exhibit selectivity towards 5-HT.sub.D1 receptors and consequently show potential in alleviation of the symptoms of migraine. The analogs are represented by the following general chemical formula: ##STR1## in which X represents H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or halogen, at the 4- or 5-position of the thiophene nucleus; Y represents a direct bond or a C.sub.1 -C.sub.3 alkylene group optionally substituted with hydroxyl: and Z represents amino, mono- or di-N-lower alkyl-substituted amino, or optionally N-lower alkyl-substituted pyrrolidine.
摘要翻译：提供了5-噻吩取代的色胺类似物，其显示出对5-HTD1受体的选择性，因此显示缓解偏头痛症状的潜力。类似物由以下通用化学式表示：其中X表示噻吩核的4-或5-位上的X表示H，C 1 -C 4烷基，C 1 -C 4羟基烷基或卤素的 Y表示直接键或任选被羟基取代的C 1 -C 3亚烷基：Z表示氨基，单或二-N-低级烷基取代的氨基或任选的N-低级烷基取代的吡咯烷。

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