N-(4,5-Dihydro-1H-imidazol-2-yl)quinoxalin-2-amine | 391241-54-6

• 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: N-(4,5-Dihydro-1H-imidazol-2-yl)quinoxalin-2-amine
• CAS: 391241-54-6
• 化学式: C₁₁H₁₁N₅
• 分子量: 213.24
• InChiKey: ACYGVAVUNGWGBY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  62.2
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Complexes Comprising alpha2-Adrenergic Receptor Agonists and Compositions
  申请人：McIntire Gregory L.

  公开号：US20080293728A1

  公开（公告）日：2008-11-27

  A complex comprises at least an α 2 -adrenergic receptor agonist and a compound that provides an opposite charge to a charge on the α 2 -adrenergic receptor agonist, wherein the complex is charge neutral as a whole and has a solubility in a range from about 0.3 μg/ml to about 2.5 mg/ml in water at pH of about 7 and temperature of about 25° C. The complex is included in a composition, device, or implant for use in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.

  一个复合物至少包含一个α2肾上腺素受体激动剂和一个提供与α2肾上腺素受体激动剂相反电荷的化合物，其中整体上复合物是电中性的，在pH约为7和温度约为25°C的水中的溶解度在约0.3μg/ml至约2.5mg/ml的范围内。该复合物包含在一种组合物、设备或植入物中，用于在神经组织的组分中进行神经保护，以防止这些组分的逐渐退化。特别是，这样的组合物、设备或植入物可用于为视神经系统的细胞和组分提供神经保护。
• [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。
• [EN] METHOD OF USING (2-IMIDAZOLIN-2-YLAMINO) QUINOXALINES IN TREATING OCULAR NEURAL INJURY<br/>[FR] PROCEDE D'UTILISATION DE (2-IMIDAZOLIN-2-YLAMINO) QUINOXALINES POUR TRAITER DES LESIONS NERVEUSES OCULAIRES
  申请人：ALLERGAN

  公开号：WO1997001339A1

  公开（公告）日：1997-01-16

  (EN) A method according to which neuroprotection is conferred upon ocular nerve cells by administration of a drug of formula (I) to the optic nerve and/or retina of a mammal within a period prior to or following an insult to ocular nerve cells but prior to cell death, wherein the 2-imidazolin-2-ylamino group may be in either the 5- or 6-position of the quinoxaline nucleus; x, y and z may be in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy is disclosed.(FR) Ce procédé permet de conférer une neuroprotection aux cellules du nerf oculaire, par l'administration, sur le nerf optique et/ou la rétine d'un mammifère, dans une période précédant ou suivant une agression contre les cellules du nerf optique, mais avant la mort cellulaire, d'un médicament de formule (I), où le groupe 2-imidazolin-2-ylamino peut se trouver en position 5- ou 6- du noyau de quinoxaline; x, y et z peuvent se trouver en l'une ou l'autre des positions 5-, 6-, 7- ou 8- restantes et sont choisis parmi hydrogène, halogène, alkyle inférieur, alcoxy inférieur ou trifluorométhyle; et R représente un substituant facultatif, placé en position 2- ou 3- du noyau quinoxaline, qui peut être hydrogène, alkyle inférieur ou alcoxy inférieur.

  一种通过在哺乳动物的视神经和/或视网膜内在视神经细胞受损但细胞死亡之前的时期内施用公式（I）的药物来赋予视神经细胞神经保护的方法揭示了。其中2-咪唑啉-2-基氨基团可以位于喹噁啉核的5位或6位中的任一位置；x、y和z可以位于其余5位、6位、7位或8位中的任意位置，并且被选自氢、卤素、低烷基、低烷氧基或三氟甲基；而R是在喹噁啉核的2位或3位中的可选取代基，可以是氢、低烷基或低烷氧基。
• Compounds, formulations, and methods for treating or preventing rosacea
  申请人：DeJovin Jack

  公开号：US20060171974A1

  公开（公告）日：2006-08-03

  In methods, compounds, and topical formulations for treatment of rosacea incorporating compounds represented by the formulas below: wherein each of R 1 , R 2 , and R 3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R 4 and R 5 is independently hydrogen, alkyl, or alkoxy; and each of R 6 and R 7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A 1 , A 3 , and A 4 is independently hydrogen or alkyl; and A 2 is independently hydrogen or hydroxy; and wherein each of B 1 , B 2 , and B 3 is independently hydrogen, hydroxy, or alkoxy; and each of B 4 and B 5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat rosacea and its symptoms.

  在治疗酒渣鼻的方法、化合物和局部制剂中，包含以下式子所代表的化合物：其中R1、R2和R3各自独立地为氢、卤素、烷基或烷氧基；R4和R5各自独立地为氢、烷基或烷氧基；R6和R7各自独立地为氢、硝基、烷基或烷氧基；其中A1、A3和A4各自独立地为氢或烷基；A2独立地为氢或羟基；B1、B2和B3各自独立地为氢、羟基或烷氧基；B4和B5各自独立地为氢或烷基。将这些化合物作为喷雾、雾化剂、气雾剂、溶液、乳液、凝胶、霜、软膏、糊剂、乳膏和悬浮液进行局部涂抹，以治疗酒渣鼻及其症状。