4-[(1R)-2-amino-1-hydroxyethyl]benzene-1,2-diol;4-[(1R)-1-hydroxy-2-(methylamino)ethyl]benzene-1,2-diol

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: 4-[(1R)-2-amino-1-hydroxyethyl]benzene-1,2-diol;4-[(1R)-1-hydroxy-2-(methylamino)ethyl]benzene-1,2-diol
• 化学式: C17H24N2O6
• 分子量: 352.4
• InChiKey: RSKGRRKIHWKEFC-PVSSEACSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.44
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  159
• 氢给体数：
  8
• 氢受体数：
  8

文献信息

• Mammalian ICYP (Iodocyanopindolol) receptor and its applications
  申请人：Vetigen

  公开号：EP0848059A1

  公开（公告）日：1998-06-17

  An isolated and substantially pure mammal polypeptide different from known adrenergic, serotonine and dopamine receptors, existing at least on mammalian muscle and eosinophils membranes, for instance in rat, guinea pig and humans. The invention also relates to plasmids containing the genes coding for said polypeptide, to host cells transformed by genes coding for the above mentioned polypeptide, to nucleotide probes capable of hybridizing with the genes coding for the above mentioned polypeptide, and to polyclonal and monoclonal antibodies directed against the above mentioned polypeptide. Said polypeptide is characterized in that it contains sites such that when said sites are exposed at the surface of a cell, they are able of binding iodocyanopindolol (ICYP) under blockade of α, β1, β2, β3-AR, serotonine 5-HT1A and serotonine 5-HT1B receptors, said binding being saturable, reversible and able to be displaced by a β-adrenergic receptor agonist SM-11044 with stereoselectivity but not by isoproterenol, norepinephrine, epinephrine, serotonine, dopamine or BRL-37344, said polypeptide (1) having an apparent molecular weight of about 30-40 kDa when labeled with 125I-iodocyanopindolol after photoaffinity labeling and separation by electrophoresis and an apparent molecular weight of about 60-80 kDa in Western blot, and (2) generating a fragment having the following formula DPX1FFQHRIHX2FSIFNX3 by acidic cleavage, wherein, X1 represents S (SEQ ID N°5) or X (SEQ ID N°6), X2 represents V (SEQ ID N°6) or W (SEQ ID N°5) and X3 represents S (SEQ ID N°5) or H (SEQ ID N°6), said polypeptide being present at least on muscles and eosinophils membranes and being a non-adrenergic receptor.

  一种分离的、纯度很高的哺乳动物多肽，它不同于已知的肾上腺素能受体、血清素受体和多巴胺受体，至少存在于哺乳动物的肌肉和嗜酸性粒细胞膜上，例如存在于大鼠、豚鼠和人体内。 本发明还涉及含有上述多肽编码基因的质粒、由上述多肽编码基因转化的宿主细胞、能与上述多肽编码基因杂交的核苷酸探针以及针对上述多肽的多克隆抗体和单克隆抗体。 上述多肽的特征在于它含有这样的位点：当上述位点暴露在细胞表面时，它们能够在 α、β1、β2、β3-AR、5-羟色胺 5-HT1A 和 5-HT1B 受体的阻断下结合碘氰基吲哚洛尔（ICYP）、所述结合具有饱和性、可逆性，能被β-肾上腺素能受体激动剂 SM-11044 以立体选择性取代，但不能被异丙肾上腺素、去甲肾上腺素、肾上腺素、血清素、多巴胺或 BRL-37344 取代、所述多肽(1)在光亲和标记后用 125I-碘氰基吲哚标记并通过电泳分离时表观分子量约为 30-40 kDa，在 Western 印迹中表观分子量约为 60-80 kDa，(2)通过酸性裂解生成具有下式 DPX1FFQHRIHX2FSIFNX3 的片段、其中，X1 代表 S（SEQ ID N°5）或 X（SEQ ID N°6），X2 代表 V（SEQ ID N°6）或 W（SEQ ID N°5），X3 代表 S（SEQ ID N°5）或 H（SEQ ID N°6），所述多肽至少存在于肌肉和嗜酸性粒细胞膜上，是一种非肾上腺素能受体。
• NOVEL CYCLOHEXANE DERIVATIVE, PRODRUG THEREOF AND SALT THEREOF, AND THERAPEUTIC AGENT CONTAINING THE SAME FOR DIABETES
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：EP1783110A1

  公开（公告）日：2007-05-09

  A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): (wherein A is -O-, -CH2-, or -NH-; n is an integer selected between 0 and 1; R6 and R7 each independently is hydrogen or C1-6 alkyl; m is an integer selected among 1-3; Q is selected among the following formulae Q1 to Q5; Ar1 is optionally substituted arylene or optionally substituted heteroarylene, provided that the heteroarylene may be bonded to an aromatic carbocycle or aromatic heterocycle to form a fused ring; and Ar2 is optionally substituted aryl or optionally substituted heteroaryl), a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, or the like each containing the compound.

  一种环己烷衍生物，具有降低血糖水平的功能，并具有药物所需的优越性能，如持久的药物活性、代谢稳定性和安全性；以及一种药物组合物，用于预防或治疗由高血糖引起的疾病，如糖尿病，如胰岛素依赖型糖尿病（1型糖尿病）或非胰岛素依赖型糖尿病（2型糖尿病）、糖尿病并发症和肥胖症。衍生物是由式（I）代表的化合物： (其中 A 是-O-、-CH2-或-NH-；n 是选自 0 和 1 之间的整数；R6 和 R7 各自独立地是氢或 C1-6 烷基；m 是选自 1-3 之间的整数；Q 是选自下式 Q1 至 Q5 之间的整数； Ar1是任选取代的芳基或任选取代的杂芳基，条件是杂芳基可以键合到芳香族碳环或芳香族杂环上以形成融合环；以及Ar2是任选取代的芳基或任选取代的杂芳基）、该化合物的原药或二者的药学上可接受的盐。还提供了含有该化合物的药物、药物组合物或类似物。
• NOVEL GLUCITOL DERIVATIVE, PRODRUG THEREOF AND SALT THEREOF, AND THERAPEUTIC AGENT CONTAINING THE SAME FOR DIABETES
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：EP1803721A1

  公开（公告）日：2007-07-04

  The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.

  本发明提供了一种葡萄糖醇衍生物，该衍生物具有降低血糖水平的功能，并具有药物所需的优越性能，如持久的药物活性；还提供了一种药物组合物，用于预防或治疗由高血糖引起的疾病，如糖尿病、糖尿病并发症和肥胖症。衍生物是由式 (I) 所代表的化合物： 其中 m 是选自 1-3 的整数；R1 至 R4 各自独立地是任选取代的烷基等；Ar1 是任选取代的萘基；A 是任选取代的杂芳基、该化合物的原药或二者的药学上可接受的盐。此外，还提供了各自含有该化合物的药物、药物组合物等。
• HUMAN beta3 ADRENERGIC RECEPTOR LIGAND, AND FOOD OR PHARMACEUTICAL PRODUCT CONTAINING THE SAME
  申请人：Ricom Corporation

  公开号：EP2316445A1

  公开（公告）日：2011-05-04

  A human adrenergic ß3 receptor ligand containing the following 3 components: (A) an unsaturated fatty acid having not less than three double bonds or a pharmaceutically acceptable salt thereof; (B) an unsaturated fatty acid having one or two double bond(s) or a pharmaceutically acceptable salt thereof; and (C) a saturated fatty acid or a pharmaceutically acceptable salt thereof; and a food product and a pharmaceutical containing it, especially, an agent for prophylaxis and/or amelioration of lifestyle-related diseases such as obesity, adipositas, diabetes, hyperlipemia, hypertension and/or gout.

  一种人肾上腺素能ß3 受体配体，含有以下 3 种成分：(A) 具有不少于三个双键的不饱和脂肪酸或其药学上可接受的盐；(B) 具有一个或两个双键的不饱和脂肪酸或其药学上可接受的盐；(C) 饱和脂肪酸或其药学上可接受的盐；以及含有该配体的食品和药品，特别是用于预防和/或改善与生活方式有关的疾病，如肥胖、脂肪肝、糖尿病、高脂血症、高血压和/或痛风。
• ACYLATED BRADYKININ ANTAGONISTS AND USES THEREFOR
  申请人：BOSTON UNIVERSITY

  公开号：EP0502987A1

  公开（公告）日：1992-09-16