6-(2-imidazolinylamino)-5-methylquinoxaline | 91147-45-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-(2-imidazolinylamino)-5-methylquinoxaline
• 英文别名: UK14304；N-(4,5-dihydro-1H-imidazol-2-yl)-5-methylquinoxalin-6-amine
• CAS: 91147-45-4
• 化学式: C₁₂H₁₃N₅
• 分子量: 227.269
• InChiKey: QZUXRMOPAGPTIY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  62.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  溴莫尼定 以53的产率得到6-(2-imidazolinylamino)-5-methylquinoxaline
  参考文献：
  名称：

  Method for using (2-imidazolin-2-ylamino) quinoxalines to reduce or

  摘要：

  披露了某些（2-咪唑啉-2-基氨基）喹喔啉。当直接给哺乳动物眼睛施用时，这种喹喔啉可以降低或维持眼内压力。

  公开号：

  US05021416A1

文献信息

• 6-(2-imidazolinylamino)quinoxaline compounds useful as alpha-2
  申请人：The Procter & Gamble Company

  公开号：US06117871A1

  公开（公告）日：2000-09-12

  The subject invention relates to methods of treating alpha-2 adenoreceptor modulated disorders, comprising administration, to a mammal in need of such treatment, of a safe and effective amount of a compound having the following structure: ##STR1## wherein: (a) R is unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; and (b) R' is selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thiol; and halo. The subject invention also relates compounds and compositions for preventing or treating of disorders modulated by alpha-2 adrenoreceptors.

  该发明涉及治疗α-2腺苷受体调节性疾病的方法，包括向需要此类治疗的哺乳动物施用具有以下结构的化合物的安全有效量：##STR1##其中：(a) R为未取代的C.sub.1 -C.sub.3烷基或烯基；和(b) R'选自氢；未取代的C.sub.1 -C.sub.3烷基或烯基；未取代的C.sub.1 -C.sub.3烷基硫醚或烷氧基；羟基；硫醇；和卤素。该发明还涉及预防或治疗由α-2肾上腺素受体调节的疾病的化合物和组合物。
• [EN] (2-IMIDAZOLIN-2-YLAMINO) QUINOXALINE DERIVATIVES FOR THE TREATMENT OF PAIN<br/>[FR] DERIVES DE (2-IMIDAZOLIN-2-YLAMINO) QUINOXALINE POUR LE TRAITEMENT DE LA DOULEUR
  申请人：ALLERGAN SALES INC

  公开号：WO2000038684A1

  公开（公告）日：2000-07-06

  A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having formula (I), and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R3, R4 and R5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain.

  一种治疗哺乳动物的方法，包括向哺乳动物施用一种有效量的化合物，以在哺乳动物中提供所需的治疗效果，所述化合物选自具有公式（I）的化合物组和其药学上可接受的酸加盐和混合物，其中R1和R2分别选自包含1至4个碳原子的烷基基团和含1至4个碳原子的烷氧基基团的基团组，2-咪唑啉-2-基氨基团可以位于喹喔啉核的5-、6-、7-或8-位置中的任何一个，而R3、R4和R5分别位于剩余喹喔啉核的5-、6-、7-或8-位置中的一个，并且是独立选自Cl、Br、H和含1至3个碳原子的烷基基团的基团组。这些化合物在施用于哺乳动物时，提供所需的治疗效果，如减轻外周疼痛。
• [EN] METHODS FOR USING (2-IMIDAZOLIN-2-YLAMINO) QUINOXALINE DERIVATIVES<br/>[FR] MODES D'UTILISATION DE DERIVES DE LA QUINOXALINE (2 - IMIDAZOLIN - 2 - YLAMINO)
  申请人：ALLERGAN

  公开号：WO1995010280A1

  公开（公告）日：1995-04-20

  (EN) A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having formula (I), and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R3, R4 and R5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, reduction of at least one effect of an inflammatory disorder, increase in renal fluid flow, and alteration in the rate of fluid transport in the gastrointestinal tract.(FR) Méthode de traitement de mammifères consistant à leur administrer une dose à effet thérapeutique d'un produit sélectionné parmi ceux d'un groupe de formule (I) et leurs sels d'addition d'acide pharmacocompatibles ou leurs mélanges, où R1 et R2 sont choisis parmi un groupe de radicaux alkyle à 1 à 4 atomes de carbone et parmi un groupe de radicaux alcoxy à 1 à 4 atomes de carbone. Le groupe (2 - imidazolin - 2 - ylamino) peut occuper indifféremment la position 5, 6, 7, 8 dans le noyau de quinoxaline, et R3, R4 et R5 sont chacun situés dans l'une des positions 5, 6, 7 ou 8 restantes du noyau de quinoxaline et sont choisis indépendamment dans le groupe consistant en radicaux Cl, Br, H et alkyle contenant 1 à 3 atomes de carbone. L'administration de ces produits a les effets thérapeutiques escomptés, à savoir: réduction des douleurs périphériques, anesthésie du SNC, constriction d'un ou plusieurs vaisseaux sanguins, atténuation ou prévention d'au moins un des effets de l'ischémie, décongestion des voies nasales, atténuation d'au moins un des effets de troubles d'ordre inflammatoire, accroissement du débit rénal et modification du transit des fluides dans les voies gastro-intestinales.

  一种治疗哺乳动物的方法包括向哺乳动物施用一种有效量的化合物，以提供所需的治疗效果，所述化合物选自具有式（I）的化合物组和其药学上可接受的酸加成盐和混合物，其中R1和R2各自选自含有1至4个碳原子的烷基基团和含有1至4个碳原子的烷氧基团的基团组，2-咪唑啉-2-基氨基团可以在喹喔啉核的5-、6-、7-或8-位置中的任何一个位置上，而R3、R4和R5分别位于喹喔啉核的其余5-、6-、7-或8-位置中的一个位置上，并且独立地选自包括Cl、Br、H和含有1至3个碳原子的烷基基团的基团组。当向哺乳动物施用这些化合物时，可提供所需的治疗效果，如减轻外周疼痛、中枢神经系统的麻醉、收缩一个或多个血管、减少或预防缺血的至少一种效应、减轻一个或多个鼻腔通道的充血、减少至少一种炎症性疾病的效应、增加肾脏液体流量和改变胃肠道中液体的运输速率。
• Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
  申请人：Allergan

  公开号：US05552403A1

  公开（公告）日：1996-09-03

  A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.2 each is independently selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide treatment for ischemia.

  一种治疗哺乳动物的方法包括向哺乳动物施用一种有效量的化合物，该化合物被选自以下化合物组合：##STR1##以及其药学上可接受的酸盐和混合物，其中R.sub.1和R.sub.2各自独立地选自含1至4个碳原子的烷基基团和含1至4个碳原子的烷氧基基团，2-咪唑啉-2-基氨基团可以位于喹喔啉环的5-, 6-, 7-或8-位置中的任何一个位置，而R.sub.3、R.sub.4和R.sub.5分别位于剩余的喹喔啉环的5-, 6-, 7-或8-位置之一，并且独立地选自Cl、Br、H和含1至3个碳原子的烷基基团的组合。当这些化合物被施用于哺乳动物时，可以治疗缺血。
• Methods for using (2-imidazolin-2-ylamino) Quinoxaline derivatives
  申请人：Allergan

  公开号：US05756503A1

  公开（公告）日：1998-05-26

  A method of treating a mammal is disclosed comprising administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain.

  本发明揭示了一种治疗哺乳动物的方法，包括向哺乳动物施用有效量的化合物，以在哺乳动物中提供所需的治疗效果，所述化合物从以下组中选择：##STR1##和其药学上可接受的酸盐和混合物，其中R.sub.1和R.sub.2各自选择自含1到4个碳原子的烷基基团和含1到4个碳原子的烷氧基团的组中，2-咪唑啉-2-基氨基团可以位于喹喔啉环的5-、6-、7-或8-位置中的任何一个位置，而R.sub.3、R.sub.4和R.sub.5分别位于剩余喹喔啉环的5-、6-、7-或8-位置中的一个位置，并且独立地选择自Cl、Br、H和含1到3个碳原子的烷基基团的组中。当这些化合物被施用于哺乳动物时，它们提供所需的治疗效果，例如减轻周围疼痛。