会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明授权
    • Pyrrolidine-indole compounds having 5-HT.sub.6 affinity
    • 具有5-HT 6亲和力的吡咯烷 - 吲哚化合物
    • US6100291A
    • 2000-08-08
    • US39269
    • 1998-03-16
    • Abdelmalik SlassiLouise EdwardsAnne O'BrienTao XinAshok Tehim
    • Abdelmalik SlassiLouise EdwardsAnne O'BrienTao XinAshok Tehim
    • C07D403/06C07D405/14C07D409/14A61K31/404
    • C07D403/06C07D405/14C07D409/14
    • Described herein are compounds with affinity for the 5-HT.sub.6 receptor, which have the general formula: ##STR1## wherein: R.sup.1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 is selected from the group consisting of H, C.sub.1-4 alkyl and benzyl;R.sup.3 is selected from the group consisting of COR.sup.5, SO.sub.2 R.sup.5, CONHC.sub.1-4 alkyl and C(S)SR.sup.6 ;R.sup.4a is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sup.4b is selected from the group consisting of H, hydroxy, halo, C.sub.3-7 cycloalkyloxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl;R.sup.4c is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sup.4d is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sup.5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C.sub.1-4 alkoxy, C.sub.1-4 alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylS--; andR.sup.6 is selected from C.sub.1-4 alkyl, allyl, propargyl and optionally substituted benzyl wherein the benzyl group is optionally substituted with 1-4 substituents selected from cyano, C.sub.1-4 alkyl and halo.Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT.sub.6 receptor is implicated, such as schizophrenia.
    • 本文描述的是对5-HT 6受体具有亲和性的化合物,其具有以下通式:其中:R 1选自H和C 1-4烷基; R 2选自H,C 1-4烷基和苄基; R3选自COR5,SO2R5,CONHC1-4烷基和C(S)SR6; R 4a选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; R4b选自H,羟基,卤素,C 3-7环烷氧基,C 1-4烷氧基,C 1-4烷基,苄氧基,苯氧基,三氟甲基,三氟甲氧基和乙烯基; R4c选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; R4d选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; R5选自苯基,吡啶基,噻吩基,喹啉基和萘基,其任选被1-4个选自C 1-4烷氧基,C 1-4烷基,卤素,硝基,三氟甲基,三氟甲氧基,1,2-亚甲二氧基, C 1-4烷基羰基,C 1-4烷氧羰基和C 1-4烷基S- 并且R 6选自C 1-4烷基,烯丙基,炔丙基和任选取代的苄基,其中苄基任选被1-4个选自氰基,C 1-4烷基和卤素的取代基取代。 还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症如精神分裂症的用途。
    • 4. 发明授权
    • Piperidine-indole compounds having 5-HT.sub.6 affinity
    • 具有5-HT 6亲和力的哌啶 - 吲哚化合物
    • US6133287A
    • 2000-10-17
    • US46669
    • 1998-03-24
    • Abdelmalik SlassiLouise EdwardsAnne O'BrienTao XinAshok Tehim
    • Abdelmalik SlassiLouise EdwardsAnne O'BrienTao XinAshok Tehim
    • A61K31/454C07D401/04A61K31/445
    • C07D401/04A61K31/454
    • Described herein are compounds with affinity for the 5-HT.sub.6 receptor, which have the general formula: wherein:R.sup.1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 is selected from the group consisting of H, C.sub.1-4 alkyl and benzyl;-- -- -- represents a single or double bond;R.sup.3 is selected from the group consisting of COR.sup.5 and SO.sub.2 R.sup.5 ;R.sup.4a is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sup.4b is selected from the group consisting of H, hydroxy, halo, C.sub.3-7 cycloalkyloxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl;R.sup.4c is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sub.4d is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sup.5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C.sub.1-4 alkoxy, C.sub.1-4 alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylS--. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT.sub.6 receptor is implicated, such as schizophrenia.
    • 本文描述的是对5-HT 6受体具有亲和性的化合物,其具有以下通式:其中:R 1选自H和C 1-4烷基; R 2选自H,C 1-4烷基和苄基; - - - 表示单键或双键; R3选自COR5和SO2R5; R 4a选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; R4b选自H,羟基,卤素,C 3-7环烷氧基,C 1-4烷氧基,C 1-4烷基,苄氧基,苯氧基,三氟甲基,三氟甲氧基和乙烯基; R4c选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; R4d选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; 并且R 5选自苯基,吡啶基,噻吩基,喹啉基和萘基,其任选被1-4个选自C 1-4烷氧基,C 1-4烷基,卤素,硝基,三氟甲基,三氟甲氧基,1,2-亚甲二氧基 ,C 1-4烷基羰基,C 1-4烷氧基羰基和C 1-4烷基。 还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症如精神分裂症的用途。