2-氨基壬二酸 | 3721-87-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 2-氨基壬二酸
• 中文别名: DL-2-氨基壬二酸
• 英文名称: 2-aminononane-1,9-dioic acid
• 英文别名: DL-2-amino-1,9-nonanedioic acid；α-aminoazelaic acid；DL-α-Amino-azelainsaeure；2-Aminononanedioic acid
• CAS: 3721-87-7
• 化学式: C₉H₁₇NO₄
• 分子量: 203.238
• InChiKey: PEATYEGLPLYRIN-UHFFFAOYSA-N

物化性质

• 熔点：
  235-236 °C(Solv: ethanol (64-17-5); water (7732-18-5))
• 沸点：
  394.2±37.0 °C(Predicted)
• 密度：
  1.192±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  14
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  101
• 氢给体数：
  3
• 氢受体数：
  5

安全信息

• 海关编码：
  2922499990

反应信息

• 作为反应物：
  描述：

  2-氨基壬二酸 生成 DL-2-Amino-azelainsaeure-dimethylester
  参考文献：
  名称：

  Andruskiewicz,R. et al., Polish Journal of Chemistry, 1978, vol. 52, p. 2147 - 2156

  摘要：

  DOI：

文献信息

• [EN] FORMULATION AND METHOD OF PREPARATION<br/>[FR] FORMULATION ET PROCÉDÉ DE PRÉPARATION
  申请人：GE HEALTHCARE AS

  公开号：WO2019185607A1

  公开（公告）日：2019-10-03

  There is described formulations for human or animal administration and to a method of preparation thereof. In particular, there is described more stable pharmaceutical formulations, such as those for intravenous administration, and to a method of preparation thereof. There are also described lyophilised formulations having an active pharmaceutical ingredient (API), a buffering agent and a lyoprotectant, wherein the API is an imaging agent comprising at least one cMet binding peptide, suitable for optically imaging the mammalian body in vivo. Also described are a method of preparing a lyophilised formulation, a pharmaceutical composition, and a kit for the preparation of the pharmaceutical composition. Further described are methods of imaging using the formulation or pharmaceutical composition, such as in detection, diagnosis, surgery, staging, treatment, monitoring of treatment, monitoring of disease progression or monitoring therapy of conditions such as cancer.

  描述了用于人类或动物给药的配方以及其制备方法。特别是，描述了更稳定的药物配方，例如用于静脉给药的配方，以及其制备方法。还描述了冻干配方，其中包含一种活性药物成分（API）、缓冲剂和冻干保护剂，其中API是包含至少一种cMet结合肽的成像剂，适用于体内光学成像哺乳动物体。还描述了制备冻干配方的方法、药物组合物和用于制备药物组合物的工具包。此外，还描述了使用该配方或药物组合物进行成像的方法，例如在癌症的检测、诊断、手术、分期、治疗、治疗监测、疾病进展监测或治疗监测等方面。
• Constrained helical peptides and methods of making same
  申请人：——

  公开号：US20020151473A1

  公开（公告）日：2002-10-17

  Provided are cyclized peptides with a constrained region(s) having an &agr;-helical conformation. Constrained helical peptides having amino acid sequences from HIV gp41 are provided, as is their use in preparing antibodies that prevent viral membrane fusion. Also provided are methods for making such cyclized peptides.

  提供了具有约束区域的环状肽，其具有α-螺旋构象。提供了具有来自HIV gp41的氨基酸序列的约束螺旋肽，以及它们在制备能够预防病毒膜融合的抗体中的应用。还提供了制备这种环状肽的方法。
• Inhibitors of Kynurenine Aminotransferase and Uses Therefor
  申请人：Schwarcz Robert

  公开号：US20110144064A1

  公开（公告）日：2011-06-16

  Provided herein are methods of decreasing a level of kynurenic acid in a cell and of treating a pathophysiological condition in a subject associated with an increase in kynurenic acid in a subject. In these methods the inhibitory action of dicarboxylic acids or derivatives or analogs thereof are effective to inhibit activity of kynurenine aminotransferase II. Also provided is a method of screening for potential inhibitory compounds for kynurenine aminotransferase II. The dicarboxylic acids or derivatives or analogs thereof may have the structural formula, where R 1 is H, NH 2 or NHCH 3 , R 2 is H or CH 3 , n is 0 to 14, and X is —COOH, CH 2 OH, —PO 3 H 2 , —SO 3 H, or —SO 3 H; or a pharmacologically acceptable salt.

  本文提供了一种降低细胞中犬尿酸水平和治疗与犬尿酸增加相关的主体病理状况的方法。在这些方法中，二羧酸或其衍生物或类似物的抑制作用可以有效地抑制犬尿酸氨基转移酶II的活性。还提供了一种筛选潜在犬尿酸氨基转移酶II抑制剂的方法。二羧酸或其衍生物或类似物可以具有结构式，其中R1为H，NH2或NH ，R2为H或CH3，n为0到14，X为—COOH，CH2OH，—PO3H2，—SO3H或—SO3H；或药理学上可接受的盐。
• Prostaglandin analogue imidazole derivatives, processes for their preparation and a pharmaceutical composition containing them
  申请人：BEECHAM GROUP PLC

  公开号：EP0006719A1

  公开（公告）日：1980-01-09

  A compound of the formula (I): wherein: X is O of S; Y is -CH2-CH2-, -CH=CH- or -C≡C-; n is 1 to 5; R, is hydrogen or CO2R1 represents an ester group in which the R, moiety contains from 1 to 12 carbon atoms; R2 is hydrogen or C1-4 alkyl; R3 is hydroxy or protected hydroxy; R4 is C1-9 alkyl, C3-8 cycloalkyl or C3-8 cycloalkyl - C1-6 alkyl; or R2 and R4 taken with the carbon atom to which they are joined represent a C5-8 cycloalkyl group; and R5 is (CH2)aNR6R7, wherein a is 0 to 3 and R6 and R7 are hydrogen, C1-4 alkyl or phenyl C1-4 alkyl, or Re and R7 taken with the nitrogen atom to which they are joined represent a 4 to 7 membered heterocyclic ring which may contain as sole further hetero atom one oxygen atom or one optionally C1-4 alkyl substituted nitrogen atom; allyl or propargyl; (CH2)b-CO -(CH2)c-CH3 wherein b+c is 1 to 5 and b is not zero; or S-R8 wherein R8 is C1-6 alkyl, phenyl, or phenyl substituted by a halogen, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy or nitro group, and salts thereof have useful pharmaceutical activity including bronchodilator activity. They can be prepared according to four methods.

  式 (I) 的化合物： 其中 X 是 S 的 O Y是-CH2- -、-CH=CH-或-C≡C-； n 是 1 至 5； R，是氢或 CO2R1 代表酯基，其中 R，分子含有 1 至 12 个碳原子； R2 是氢或 C1-4 烷基； R3 是羟基或受保护的羟基； R4 是 C1-9 烷基、C3-8 环烷基或 C3-8 环烷基-C1-6 烷基；或 R2 和 R4 与它们连接的碳原子一起代表 C5-8 环烷基；以及 R5为( )aNR6R7，其中a为0至3，R6和R7为氢、C1-4烷基或苯基C1-4烷基，或Re和R7与连接它们的氮原子一起代表一个4至7个成员的杂环，该杂环可包含一个氧原子或一个任选被C1-4烷基取代的氮原子作为唯一的杂原子；烯丙基或丙炔基；( )b-CO-( )c-CH3，其中 b+c 为 1 至 5，b 不为零；或 S-R8，其中 R8 为 C1-6 烷基、苯基或被卤素、三氟甲基、C1-6 烷基、C1-6 烷氧基或硝基取代的苯基。它们可以通过四种方法制备。
• Optically active hydantoin derivatives, their synthesis, pharmaceutical formulations containing them, and intermediates
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0019223A1

  公开（公告）日：1980-11-26

  Compounds of formula (I) having only two optically active centres, may exist as four isomers, each of which may be prepared by resolving a racemic amino-diester intermediate in the preparation thereof. The racemic amino-diester is selectively hydrolysed to the corresponding mono-ester which is acylated and subsequently selectively deacylated to produce the resolved mono-ester. Isomers of compounds of formula (I) having a particular configuration are biologically more active than the corresponding isomers having other configurations and are useful in medicine, either as the raw compound or in a pharmaceutical formulation, for example in inhibiting platelet aggregation.

  式 (I) 化合物 只有两个光学活性中心，可以存在四种异构体，每种异构体都可以通过分解制备过程中的外消旋氨基二酯中间体来制备。外消旋氨基二酯被选择性水解为相应的单酯，单酯被酰化，随后选择性脱酰化，生成已解析的单酯。 具有特定构型的式 (I) 化合物异构体比具有其他构型的相应异构体具有更高的生物活性，可作为原料化合物或药物制剂用于医药领域，例如抑制血小板聚集。