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    • 8. 发明授权
      US6166072A Amino acid derivatives 失效
    • Amino acid derivatives
    • 氨基酸衍生物
    • US6166072A
    • 2000-12-26
    • US342492
    • 1999-06-29
    • Stanley Charles Bell , Michael De Vivo , Allen Hopper , Methvin Isaac , Anne O'Brien , Vassil Ilya Ognyanov , Richard Schumacher
    • Stanley Charles Bell , Michael De Vivo , Allen Hopper , Methvin Isaac , Anne O'Brien , Vassil Ilya Ognyanov , Richard Schumacher
    • C07C323/60 , A61K31/21
    • C07C323/60
    • Described herein are compounds having the general formula: ##STR1## wherein: Ar.sup.1 and Ar.sup.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sup.1 or Ar.sup.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sup.1 and Ar.sup.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;wherein Ar.sup.1 and Ar.sup.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;R.sup.3 is selected from the group consisting of H and aryl, which may be substituted as for Ar.sup.1 ;R.sup.4 and R.sup.5 are independently selected from the group consisting of H, alkyl, alkanoyl, benzoyl and benzyl.
    • 本文描述的是具有以下通式的化合物：其中：Ar 1和Ar 2是独立选择的芳基，任选地被选自烷基，环烷基，烷氧基，烷酰基，芳烷基，芳烷氧基，卤素，NO 2，Ph，CF 3， CN，OH，亚甲二氧基，亚乙二氧基，SO 2 NRR'，NRR'，CO 2 R（其中R和R'独立地选自H和烷基）和可如上所述被取代的第二芳基; 其中任何环烷基或芳基取代基通过可以是单键的桥连元件连接到Ar 1或Ar 2上，亚乙烯基，亚乙炔基，Z基，-Z-（CH 2）n - 基， - （CH 2） ）nZ-基或-Z-（CH2）nZ-基，其中Z表示O原子，S原子，NH基或N-烷基，n是1至4的整数; 其中Ar1和Ar2可以通过单键连接到它们连接的中心原子上，亚烷基，亚烯基或亚炔基; 其中Ar1和Ar2可以通过单键连接到它们连接的中心原子上，亚烷基，亚烯基或亚炔基; R 3选自H和芳基，其可以被取代为Ar 1; R 4和R 5独立地选自H，烷基，烷酰基，苯甲酰基和苄基。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US6162824A Tricylic amino-acid derivatives 失效
    • Tricylic amino-acid derivatives
    • US6162824A
    • 2000-12-19
    • US365070
    • 1999-07-30
    • Vassil I. Ognyanov , Allen Hopper , Stanley Charles Bell , Eric A. Meade , Michael De Vivo
    • Vassil I. Ognyanov , Allen Hopper , Stanley Charles Bell , Eric A. Meade , Michael De Vivo
    • C07C229/22 , C07C229/28 , C07C229/30 , C07C229/36 , C07D233/76 , C07D335/14 , A61K31/38 , A61K31/195 , C07C211/00 , C07D333/22
    • C07C229/30 , C07C229/22 , C07C229/28 , C07C229/36 , C07C2601/02 , C07C2603/18 , C07D233/76 , C07D335/14
    • Described herein are compounds which have the general formula: ##STR1## or a prodrug or pharmaceutically acceptable salt, solvate or hydrate thereof wherein:R.sup.1 is selected from the group consisting of H, alkyl and the counter ion for a basic addition salt;X is selected from the group consisting of CR.sup.9 R.sup.10, S, O, SO, SO.sub.2, NH and N-alkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.9 and R.sup.10 are independently selected from the group consisting of H and alkyl;R.sup.5 and R.sup.6 are independently selected from the group consisting of H, alkyl and phenyl, or, alternatively, R.sup.5 and R.sup.6 together may form a methylene group or a 3- to 6-membered a spirocyclic group;wherein, when X is CR.sup.9 R.sup.10, one or both pairs of R.sup.5 and R.sup.9 or R.sup.6 and R.sup.10 may join to form a double or triple bondR.sup.7 is selected from the group consisting of Formula II-V: ##STR2## which are all optionally substituted, at nodes other than R.sup.8, with 1-4 substituents independently selected from the group consisting of alkyl, halo, aryl (which may be substituted as for R.sup.8), trifluoromethyl, trifluoromethoxy, nitro, cyano, amino, mono-alkylamino, di-alkylamino, alkoxycarbonyl, alkylcarbonyl, alkoxythiocarbonyl, alkylthiocarbonyl, alkoxy, alkylS-, phenoxy, --SO.sub.2 NH.sub.2, --SO.sub.2 NHalkyl, --SO.sub.2 N(alkyl).sub.2 and 1,2-methylenedioxy; and wherein any of the benzo-fused rings in structures II to V may be replaced by a 5- or 6-membered heterocyclic ring selected from the group consisting of pyridine, thiophene, furan and pyrrole;wherein R.sup.8 is selected from the group consisting of H, alkyl, benzyl, cycloalkyl, indanyl and an optionally substituted aryl group, wherein the optional substituents are independently selected from 1-4 members of the group consisting of alkyl, halo, aryl, trifluoromethyl, trifluoromethoxy, nitro, cyano, amino, mono-alkylamino, di-alkylamino, alkoxycarbonyl, alkylcarbonyl, alkoxythiocarbonyl, alkylthiocarbonyl, alkoxy, alkylS-, phenoxy, --SO.sub.2 NH.sub.2, --SO.sub.2 NHalkyl, --SO.sub.2 N(alkyl).sub.2 and 1,2-methylenedioxy;--represents a single or double bond;Y is selected from the group consisting of O, S, SO, NH, N-alkyl, CH.sub.2, CH-alkyl, C(alkyl).sub.2, and C.dbd.O;Z is selected from the group consisting of CH.sub.2, O, S, NH and N-alkyl when--is a single bond;Z is selected from the group consisting of CH and N when--is a double bond.Also described is the use of these compounds as pharmaceuticals.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US07358057B2 QM-7 and QT-6 cells transfected with mutant cell surface expressed channel receptors and assays using the transfected cells 失效
    • QM-7 and QT-6 cells transfected with mutant cell surface expressed channel receptors and assays using the transfected cells
    • 用突变体细胞表面表达的通道受体转染的QM-7和QT-6细胞，并使用转染的细胞进行测定
    • US07358057B2
    • 2008-04-15
    • US10434364
    • 2003-05-09
    • Daguang Wang , Michael De Vivo
    • Daguang Wang , Michael De Vivo
    • C12N15/09 , G01N33/567
    • C07K14/70571 , C12N2503/02 , C12N2510/00 , G01N33/5041 , G01N33/944
    • The present invention relates e.g., to QM-7 or QT-6 cells comprising a heterologous mutant nicotinic α7 acetylcholine receptor and/or a nucleic acid encoding it, or a fragment or variant thereof. In a preferred embodiment, the mutant nicotinic α7 acetylcholine receptor subunit has a mutation in the M2 domain. QM-7 and QT-6 cells of the invention are useful for, e.g., assays such as high throughput assays that measure the influx of cations, such as Ca++ ions, into a cell. Such assays can be used, e.g., to identify agents that modulate the expression and/or activity of a mutant cell-surface-expressed channel receptor (e.g., the nicotinic α7 receptor), and which thus modulate, e.g., among other functions, processes involved in the central nervous system, such as learning and memory.
    • 本发明涉及例如包含异源突变体烟碱型α7乙酰胆碱受体的QM-7或QT-6细胞和/或编码它的核酸或其片段或变体。 在优选的实施方案中，突变体烟碱型α7乙酰胆碱受体亚基在M2结构域中具有突变。 本发明的QM-7和QT-6细胞可用于例如测定例如测量阳离子如Ca ++离子进入细胞的高通量测定的测定。 可以使用这种测定法，例如，鉴定调节突变细胞表面表达的通道受体（例如，烟碱型α7受体）的表达和/或活性的试剂，并因此调节，例如其它功能，过程 参与中枢神经系统，如学习和记忆。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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