专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

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

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。

3. 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。

4. 发明授权

US5856510A 5-alkenyl and 5-alkynyl indole compounds 失效
标题翻译： 5-链烯基和5-炔基吲哚化合物
公开(公告)号：US5856510A
公开(公告)日：1999-01-05
申请号：US767322
申请日：1996-12-16
申请人： Oingchang Meng , Abdelmalik Slassi , Louise Edwards , Sumanas Rakhit
发明人： Oingchang Meng , Abdelmalik Slassi , Louise Edwards , Sumanas Rakhit
IPC分类号： C07D209/16 , C07D403/04 , C07D403/14 , C07D409/14 , C07D403/02 , A61K31/405 , A61K31/415 , C07D209/02 , C07D209/04
CPC分类号： C07D403/04 , C07D209/16 , C07D403/14 , C07D409/14
摘要： Described herein are compounds selective for 5-HT.sub.1D -like receptors, which have the general formula: ##STR1## wherein: R.sup.1 is selected from H, aryl and aryl substituted with 1, 2 or 3 substituents independently selected from loweralkyl, loweralkoxy, loweralkylcarbonyl, loweralkyl-S--, loweralkyl-S(O)--, loweralkyl-SO.sub.2 -, S.dbd.C.dbd.N--, O.dbd.C.dbd.N--, halo, loweralkoxycarbonyl, nitro, amino, loweralkyl-NH--, (loweralkyl).sub.2 --N--, loweralkyl-SO.sub.2 -loweralkyl-;A is a double or triple bond;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; andR.sup.7 and R.sup.8 are independently selected from H and loweralkyl or R.sup.7 and R.sup.8, together with the nitrogen atom to which they are attached, form an optionally substituted 3- to 6-membered ring;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：本文描述了对具有以下通式的5-HT1D样受体选择性的化合物：1和被1,2或3个独立地选自低级烷基，低级烷氧基，低级烷基羰基，低级烷基-S-，低级烷基-S（O） - ， - 低级烷基-SO 2 - ，S = C = N-，O = C = N-，卤素，低级烷氧基羰基，硝基，氨基，低级烷基-NH-，（低级烷基）2-N-，低级烷基-SO 2 - 低级烷基 - A是双重或三重键; R 2选自式II，III，IV和V的组：V 3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; 并且R 7和R 8独立地选自H和低级烷基，或者R 7和R 8与它们所连接的氮原子一起形成任选取代的3至6元环; 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。

5. 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。

6. 发明授权

US5627194A Anti-viral guanidino-substituted compounds 失效
标题翻译：抗病毒胍基取代的化合物
公开(公告)号：US5627194A
公开(公告)日：1997-05-06
申请号：US322492
申请日：1994-10-14
申请人： Sumanas Rakhit , Abdelmalik Slassi
发明人： Sumanas Rakhit , Abdelmalik Slassi
IPC分类号： C07C279/16 , C07D211/06 , C07H15/04 , C07H15/08 , A61K31/35 , A61K31/17 , A61K31/38 , A61K31/445
CPC分类号： C07H15/04 , C07C279/16 , C07D211/06 , C07H15/08
摘要： Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.
摘要翻译：描述了新的胍基取代的化合物，其具有以下通式（I）：其中X可以是碳，氧，氮或硫; R 1可以是H，OH，直链或支链的低级烷基，低级烷氧基，低级（烷基取代的烷氧基），低级烷基 - 胺，低级烷基 - 硫代，羟基取代的低级烷氧基，低级烷氧基 - 烷氧基取代的低级烷氧基，烷基胺，烷氧基取代的低级烷基胺和末端胍基取代的直链的支链低级烷基，低级烷氧基，低级（烷基取代的烷氧基），低级烷基 - 胺或低级烷基 - 硫代; R2和R3独立地为直链或支链的低级烷基，烷氧基，烷基取代的烷氧基和烷基胺之一。已经发现这些化合物有效地抑制疱疹病毒复制。特别优选的根据式（I）的化合物是胍基取代的糖衍生物。

7. 发明授权

US07868008B2 Substituted isoindolones and their use as metabotropic glutamate receptor potentiators 失效
标题翻译：取代的异吲哚酮及其作为代谢型谷氨酸受体增强剂的用途
公开(公告)号：US07868008B2
公开(公告)日：2011-01-11
申请号：US12063018
申请日：2006-02-15
申请人： Bradford Van Wagenen , Radhakrishnan Ukkiramapandian , Joshua Clayton , Ian Egle , James Empfield , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi , Gary Steelman , Rebecca Urbanek , Sally Walsh
发明人： Bradford Van Wagenen , Radhakrishnan Ukkiramapandian , Joshua Clayton , Ian Egle , James Empfield , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi , Gary Steelman , Rebecca Urbanek , Sally Walsh
IPC分类号： C07D209/46 , C07D401/06 , C07D401/14 , A61K31/4035 , A61K31/454
CPC分类号： C07D209/46 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/14
摘要： The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
摘要翻译：本发明涉及式I化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和n如说明书中对式I所定义。本发明还涉及制备化合物的方法和用于制备中的新中间体，含有该化合物的药物组合物，以及该化合物在治疗中的用途。

8. 发明授权

US07585881B2 Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists 失效
标题翻译：额外的杂多环化合物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：US07585881B2
公开(公告)日：2009-09-08
申请号：US11053752
申请日：2005-02-09
申请人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald McLeod , Alexander Mindis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tau Xin , Jalaj Arora
发明人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald McLeod , Alexander Mindis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tau Xin , Jalaj Arora
IPC分类号： A61K31/4439 , C07D401/14 , C07D413/04
CPC分类号： C07D487/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention relates to new compounds of formula I, to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
摘要翻译：本发明涉及新的式I化合物，含有该化合物的药物制剂，以及该化合物在预防和/或治疗mGluR5受体介导的病症中的用途。

9. 发明申请

US20090131454A1 New compounds 067 失效
标题翻译：新化合物067
公开(公告)号：US20090131454A1
公开(公告)日：2009-05-21
申请号：US12285988
申请日：2008-10-17
申请人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
发明人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
IPC分类号： A61K31/497 , C07D401/14 , C07D403/14 , A61K31/506 , A61K31/4439
CPC分类号： C07D401/14 , C07D403/14
摘要： The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.
摘要翻译：本发明涉及新化合物，它们在治疗中的用途和包含所述新化合物的药物组合物。

10. 发明申请

US20080125436A1 MgluR5 modulators 失效
标题翻译： MgluR5调节剂
公开(公告)号：US20080125436A1
公开(公告)日：2008-05-29
申请号：US11902784
申请日：2007-09-25
申请人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Peter Dove , Tao Xin , Tomislav Stefanac
发明人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Peter Dove , Tao Xin , Tomislav Stefanac
IPC分类号： A61K31/513 , A61K31/501 , A61K31/497 , A61K31/4439 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D413/14 , C07D401/14
摘要： The present invention is directed to compounds of formula I: Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
摘要翻译：本发明涉及式I化合物：其中R 1至R 5，X和Z在说明书中进一步定义。本发明还涉及制备化合物和制备中使用的方法，含有该化合物的药物组合物以及该化合物在治疗中的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式