(+/-)-1-(3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)ethylamine | 477312-23-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: (+/-)-1-(3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)ethylamine
• 英文别名: 1-(3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)ethylamine；1-(3,4-dihydro-2H-1,4-benzoxazin-6-yl)ethanamine
• CAS: 477312-23-5
• 化学式: C₁₀H₁₄N₂O
• 分子量: 178.234
• InChiKey: NUVWVCBXUZDRMG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  47.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (+/-)-1-(3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)ethylamine 在 4-二甲氨基吡啶 、 potassium carbonate 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 、 N,N-二异丙基乙胺 、 肼 作用下， 以 乙醇 、 二氯甲烷 、 丙酮 为溶剂， 生成
  参考文献：
  名称：

  (S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzooxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons

  摘要：

  (S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide ((S)-2) was identified as a potent and efficacious KCNQ2 opener. This compound demonstrated significant activity in reducing neuronal hyperexcitability in rat hippocampal slices, and the inhibition mediated by (S)-2 was reversed by the KCNQ blocker linopirdine. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.01.069
• 作为产物：
  描述：

  6-乙酰基-2H-1,4-苯并噁嗪-3(4H)-酮 在 镍 ammonium hydroxide 、 sodium hydroxide 、 lithium aluminium tetrahydride 、 盐酸羟胺 、 氢气 作用下， 以 四氢呋喃 、 甲醇 为溶剂， -78.0 ℃ 、344.74 kPa 条件下， 生成 (+/-)-1-(3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)ethylamine
  参考文献：
  名称：

  (S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzooxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons

  摘要：

  (S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide ((S)-2) was identified as a potent and efficacious KCNQ2 opener. This compound demonstrated significant activity in reducing neuronal hyperexcitability in rat hippocampal slices, and the inhibition mediated by (S)-2 was reversed by the KCNQ blocker linopirdine. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.01.069

文献信息

• [EN] PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USE AS JANUS KINASE MODULATORS<br/>[FR] COMPOSÉS DE PYRROLOPYRIMIDINE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DES JANUS KINASES
  申请人：TARGEGEN INC

  公开号：WO2009049028A1

  公开（公告）日：2009-04-16

  Provided herein are pyrrolopyrimidine compounds of Formula (I) wherein R1 is a heteroaryl containing at least one S atom, and optionally substituted on a ring carbon by one, two, or three substituents each independently selected from the group consisting of : halo, hydroxyl, nitro, formyl, formamido, cyano, sulfonyl, carboxy, amino, amido, acylamino, carbamoyl, sulphamoyl, alkyl, alkenyl, CF3, ureido, alkynyl, alkoxy, alkanoyl, alkoxycarbonyl, carbaldehyde oxime, N -alkylsulphamoyl, N-alkylcarbamoyl, -OR13R11 or -R13R11; R2 is phenyl or pyridinyl, wherein R2 optionally substituted on a ring carbon by one, two, or three substituents each indenpendently selected from the group consisting of : halo, hydroxyl, cyano, nitro, formyl, formamido, carboxy, sulfonyl, amino, amido, -N- alkyl -amino, carbamoyl, sulphamoyl, CF3, ureido, alkyl, alkenyl, alkynyl, alkoxy, alkanoyl, alkoxycarbonyl, N-alkylsulphamoyl, N-alkylcarbamoyl, -OR11, -OR12R11, or -R12R11; and methods of making and using the same. Such compounds may be used in inflammatory or myeloproliferative disorders. The disclosure also provides for treating cancer.

  本文提供了通式(I)的吡咯并嘧啶化合物，其中R1是含有至少一个硫原子的杂芳基，并且任选地在芳环碳上被一个、两个或三个取代基取代，这些取代基独立地从以下基团中选择：卤素、羟基、硝基、甲酰基、甲酰胺基、氰基、磺酰基、羧基、氨基、酰胺基、酰氨基、氨基甲酰基、磺酰胺基、烷基、烯基、CF3、脲基、炔基、烷氧基、烷酰基、烷氧羰基、羧醛肟、N-烷基磺酰胺基、N-烷基氨基甲酰基、-OR13R11或-R13R11；R2是苯基或吡啶基，其中R2任选地在环碳上被一个、两个或三个取代基取代，这些取代基独立地从以下基团中选择：卤素、羟基、氰基、硝基、甲酰基、甲酰胺基、羧基、磺酰基、氨基、酰胺基、-N-烷基-氨基、氨基甲酰基、磺酰胺基、CF3、脲基、烷基、烯基、炔基、烷氧基、烷酰基、烷氧羰基、N-烷基磺酰胺基、N-烷基氨基甲酰基、-OR11、-OR12R11或-R12R11；以及其制备和使用方法。这些化合物可用于炎症性或骨髓增生性疾病。该披露还提供了用于治疗癌症的方法。
• NOVEL TRICARBOCYANINE-CYCLODEXTRIN(S) CONJUGATES AND USE THEREOF
  申请人：CYANAGEN S.R.L.

  公开号：US20150328342A1

  公开（公告）日：2015-11-19

  The present invention relates to novel tricarbocyanine-cyclodextrin(s) conjugates useful as markers in the diagnosis of kidney diseases, a diagnostic composition comprising said conjugates, their use and their production.

  本发明涉及新型三芳基氰化物-环糊精共轭物，可用作肾脏疾病诊断中的标记物，包括所述共轭物的诊断组合物，它们的使用和生产。
• Process for the Preparation of Doxazosin and Salts Thereof
  申请人：Rao Dharmaraj Ramachandra

  公开号：US20120041199A1

  公开（公告）日：2012-02-16

  The present invention relates to a process for the preparation of doxazosin or salts thereof.

  本发明涉及一种制备多沙唑嗪或其盐的方法。
• [EN] OLIGONUCLEOTIDE COMPOSITIONS AND METHODS THEREOF<br/>[FR] COMPOSITIONS D'OLIGONUCLÉOTIDES ET PROCÉDÉS ASSOCIÉS
  申请人：WAVE LIFE SCIENCES LTD

  公开号：WO2021237223A1

  公开（公告）日：2021-11-25

  The present disclosure provides modified oligonucleotides and compositions and methods thereof. In some embodiments, provided technologies comprise modified sugars and/or modified internucleotidic linkages. In some embodiments, the present disclosure provides technologies for preparing modified oligonucleotides. In some embodiments, the present disclosure provides chirally controlled oligonucleotide compositions and methods for their preparation and uses.

  本公开提供了经修改的寡核苷酸及其组合物和方法。在某些实施方式中，提供的技术包括修改的糖或修改的核苷酸间连接。在某些实施方式中，本公开提供了用于制备修改的寡核苷酸的技术。在某些实施方式中，本公开提供了对手性控制的寡核苷酸组合物及其制备和用途的方法。
• Cinnamide derivatives as KCNQ potassium channel modulators
  申请人：——

  公开号：US20030166650A1

  公开（公告）日：2003-09-04

  There is provided novel cinnamide derivatives of Formula I 1 wherein R is C 1-4 alkyl or trifluoromethyl; R 1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R 2 and R 3 are each independently selected from the group consisting of hydrogen, C 1-4 alkyl, and halogen; R 4 is selected from the group consisting of di(C 1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C 1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R 5 is hydrogen, chloro or fluoro; or R 4 and R 5 taken together are —CH═CH—CH═CH— or —X(CH 2 ) m Y— in which X and Y are each independently selected from the group consisting of CH 2 , (CH 2 ) n N(R 9 )— and O, wherein m is 1 or 2; n is 0 or 1; and R 6 , R 7 , and R 8 are each independently selected from hydrogen, chloro and fluoro; and R 9 is selected from the group consisting of hydrogen, C 1-4 alkyl, hydroxyethyl, C 1-4 alkoxyethyl, cyclopropylmethyl, —CO 2 (C 1-4 alkyl), and —CH 2 CH 2 NR 10 R 11 in which R 10 and R 11 are each independently hydrogen or C 1-4 alkyl, which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.

  提供了一种新型的 Formula I1 中的肉桂酰胺衍生物，其中 R 为 C1-4 烷基或三氟甲基；R1 选自吡啶基、喹啉基、噻吩基、呋喃基、1,4-苯并二氧杂基、1,3-苯并二氧杂基、色基、茚基、联苯基、苯基和取代苯基，其中所述取代苯基取代有一个或两个取代基，每个取代基独立地选自卤素、C1-4 烷基、C1-4 烷氧基、三氟甲基、三氟甲氧基和硝基；R2 和 R3 各自独立地选自氢、C1-4 烷基和卤素；R4 选自二(C1-4 烷基)氨基、三氟甲氧基和可选取代的吗啉-4-基、吡啶基、嘧啶基、哌嗪基和吡嗪基，其中所述基带有一个或两个取代基，所述取代基独立地选自 C1-4 烷基、氨甲基、羟甲基、氯或氟；R5 为氢、氯或氟；或者 R4 和 R5 结合成 —CH═CH—CH═CH— 或 —X(CH2)mY—，其中 X 和 Y 各自独立地选自 CH2、(CH2)nN(R9)— 和 O，其中 m 为 1 或 2；n 为 0 或 1；R6、R7 和 R8 各自独立地选自氢、氯和氟；R9 选自氢、C1-4 烷基、羟乙基、C1-4 烷氧乙基、环丙基甲基、—CO2(C1-4 烷基) 和 —CH2CH2NR10R11，其中 R10 和 R11 各自独立地为氢或 C1-4 烷基，这些化合物是 KCNQ 钾通道的开放剂，可用于治疗对 KCNQ 钾通道的开放有反应的疾病。