吡咯啉-2,5-二羧酸 | 35634-41-4

• 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: 吡咯啉-2,5-二羧酸
• 中文别名: 吡咯烷-2,5-二羧酸
• 英文名称: acido pirrolidin-2,5-dicarbossilico
• 英文别名: pyrrolidine-2,5-dicarboxylic acid；2,5-pyrrolidinedicarboxylic acid；Pyrrolidin-2,5-dicarbonsaeure
• CAS: 35634-41-4；49653-02-3；72000-65-8；81702-31-0；93713-35-0；97275-65-5；97275-67-7
• 化学式: C₆H₉NO₄
• mdl: MFCD08753873
• 分子量: 159.142
• InChiKey: ZKXSPYPKBXRBNP-UHFFFAOYSA-N

物化性质

• 熔点：
  260-261 °C
• 沸点：
  420.3±45.0 °C(Predicted)
• 密度：
  1.456±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  86.6
• 氢给体数：
  3
• 氢受体数：
  5

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  吡咯啉-2,5-二羧酸 在 sodium carbonate 、 potassium carbonate 、 三乙胺 、 三氟乙酸 、 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 二氯甲烷 、 水 、 乙腈 为溶剂， 反应 80.5h， 生成 benzyl 5-acetyl-2-(benzyloxy)-1-oxo-2,5-diazaspiro[3.4]octane-6-carboxylate
  参考文献：
  名称：

  [EN] SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
  [FR] MODULATEURS SPIRO-LACTAMES ET BIS-SPIRO-LACTAMES DES RÉCEPTEURS NMDA ET LEURS UTILISATIONS

  摘要：

  揭示了具有调节NMDA受体活性潜力的化合物。这些化合物可用于治疗

  公开号：

  WO2018026792A1
• 作为产物：
  描述：

  dimethyl 1-benzylpyrrolidine-2,5-dicarboxylate 在 palladium 10% on activated carbon 、 氢气 、 sodium hydroxide 作用下， 以 甲醇 为溶剂， 20.0 ℃ 、2.03 MPa 条件下， 反应 26.0h， 生成 吡咯啉-2,5-二羧酸
  参考文献：
  名称：

  N-Heterocyclic dicarboxylic acids: Broad-spectrum inhibitors of metallo-β-lactamases with co-antibacterial effect against antibiotic-resistant bacteria

  摘要：

  In an effort to identify novel, broad-spectrum inhibitors against the metallo-beta-lactamases (M beta Ls), several N-heterocyclic derivatives were tested as inhibitors of M beta Ls CcrA, ImiS, and L1, which are representative enzymes from the distinct M beta L subclasses. Three N-heterocyclic dicarboxylic acid derivatives were competitive inhibitors of CcrA and L1, exhibiting K-i values <= 2 mu M, while only 2,4-thiazolidinedicarboxylic acid (1b) was a competitive inhibitor of ImiS. Two 2-mercapto-1,3,4-thiadiazole derivatives were noncompetitive inhibitors of CcrA and ImiS, exhibiting K-i values <7 mu M; however, these same compounds did not inhibit L1. Two 2-mercapto-1,3,4-triazole derivatives were shown not to inhibit any of the tested M beta Ls. The N-heterocyclic derivatives were tested for antibacterial activity by examining the MIC values for existing antibiotics in the presence/absence of these derivatives. Consistent with the steady-state inhibition data, the inclusion of three N-heterocyclic dicarboxylic acid derivatives resulted in lower MIC values when using Escherichia coli BL21(DE3) cells containing the CcrA or L1 plasmids or Klebsiella pneumoniae (ATCC 700603), while 1b was the only dicarboxylic acid derivative to lower the MIC value of E. coli cells containing the ImiS plasmid. Inclusion of the 2-mercapto-1,3,4-thiadiazole derivatives resulted in lower MIC values for E. coli cells containing ImiS or L1 plasmids; however, these derivatives did not alter the MIC values for K. pneumoniae or E. coli cells containing the L1 plasmid. None of the N-heterocyclic derivatives affected the MIC of two methicillin resistant Staphylococcus aureus (MRSA) strains. Taken together, these studies demonstrate that N-heterocyclic dicarboxylic acids 1a-c and pyridylmercaptothiadiazoles 2a,b are good scaffolds for future broad-spectrum inhibitors of the MbLs. (c) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.06.074

文献信息

• COSMETIC OR DERMATOLOGICAL COMPOSITION COMPRISING A POLYMER BEARING JUNCTION GROUPS, AND COSMETIC TREATMENT PROCESS
  申请人：Chodorowski-Kimmes Sandrine

  公开号：US20100239509A1

  公开（公告）日：2010-09-23

  The present patent application relates to a cosmetic or dermatological composition comprising, in a cosmetically or dermatologically acceptable medium, a polymer comprising: (a) a polymer backbone that may be obtained by reaction: of a polyol comprising 3 to 6 hydroxyl groups; of a monocarboxylic acid containing 6 to 32 carbon atoms; of a polycarboxylic acid comprising at least two carboxylic groups COOH, and/or of a cyclic anhydride such as a polycarboxylic acid and/or of a lactone comprising at least one carboxylic group COOH; and (b) at least one junction group linked to the said polymer backbone and capable of establishing H bonds with one or more partner junction groups, each pairing of a junction group involving at least three H (hydrogen) bonds. The patent application also concerns a cosmetic treatment process using the said composition.

  本专利申请涉及一种化妆品或皮肤科学组合物，包括在化妆品或皮肤科学上可接受的介质中，包含以下聚合物的组合物：(a) 由以下反应得到的聚合物骨架：含有3至6个羟基的多元醇；含有6至32个碳原子的一元羧酸；至少含有两个羧基COOH的多元羧酸，和/或类似多元羧酸的环酐和/或至少含有一个羧基COOH的内酯；以及(b) 至少一个连接到所述聚合物骨架的连接基团，并能够与一个或多个配对连接基团建立H键，每个连接基团的配对涉及至少三个H（氢）键。该专利申请还涉及使用所述组合物的化妆品处理过程。
• COMPOSITION COMPRISING A POLYCONDENSATE, METHOD OF TREATMENT, POLYCONDENSATE, AND METHOD OF PREPARATION
  申请人：GIUSTINIANI Pascal

  公开号：US20090028807A1

  公开（公告）日：2009-01-29

  The present application relates to a cosmetic or pharmaceutical, in particular lipstick, composition comprising a polycondensate The application also relates to a method of cosmetic treatment using the composition, the polycondensate thus defined and a method of preparing the polycondensate.

  本申请涉及一种化妆品或药用品，特别是口红，包括聚缩酸酯的组合物。该申请还涉及一种使用该组合物进行化妆处理的方法，所述聚缩酸酯的定义以及一种制备聚缩酸酯的方法。
• COSMETIC OR PHARMACEUTICAL COMPOSITION COMPRISING A POLYCONDENSATE, THE SAID POLYCONDENSATE AND METHOD OF COSMETIC TREATMENT
  申请人：Malle Gerard

  公开号：US20100272660A1

  公开（公告）日：2010-10-28

  The present application relates to a cosmetic or pharmaceutical composition comprising a polycondensate capable of being obtained by the reaction of the following monomers alone: of 10 to 30% by weight, relative to the total weight of the polycondensate, of one or more polyols comprising 3 to 6 hydroxyl groups; of 30 to 80% by weight, relative to the total weight of the polycondensate, of one or more linear, branched and/or cyclic, saturated or unsaturated, non-aromatic monocarboxylic acids comprising 6 to 32 carbon atoms; of 1 to 40% by weight, relative to the total weight of the polycondensate, of one or more polycarboxylic acids and/or cyclic anhydrides of such a polycarboxylic acid and/or lactones comprising at least one COOH group; and optionally of 0.1 to 15% by weight, relative to the total weight of the polycondensate, of one or more silicones having a hydroxyl and/or carboxyl functional group. The application also relates to a method of cosmetic treatment using the said composition, and the polycondensate thus defined.

  本申请涉及一种化妆品或药用组合物，包括由以下单体反应而得的聚缩酸酯：相对于聚缩酸酯的总重量，占10至30%的一种或多种含有3至6个羟基的多元醇；占30至80%的一种或多种线性、支链和/或环状、饱和或不饱和、非芳香族的单羧酸，含有6至32个碳原子；占聚缩酸酯总重量的1至40%的一种或多种多羧酸和/或多羧酸的环状酐和/或含有至少一个COOH基团的内酯；以及可选地占聚缩酸酯总重量的0.1至15%的一种或多种硅氧烷，具有羟基和/或羧基官能团。该申请还涉及使用所述组合物进行化妆处理的方法，以及如此定义的聚缩酸酯。
• [EN] DICYANOPYRROLIDINES AS DIPEPTIDYL PEPTIDASE IV INHIBITORS<br/>[FR] DICYANOPYRROLIDINES INHIBITEURS DE LA DIPEPTIDYL PEPTIDASE IV
  申请人：PFIZER PROD INC

  公开号：WO2005095339A1

  公开（公告）日：2005-10-13

  The invention provides compounds of formula (I), the prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein wherein R is as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof in the treatment of diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.

  该发明提供了如下式（I）的化合物，其前药和立体异构体，以及该化合物、前药和立体异构体的药用可接受盐，其中R如本文所定义；其药物组合物；其组合物；以及在治疗糖尿病并发症包括糖尿病神经病变、糖尿病肾病、糖尿病微血管病变等方面的用途。
• Diagnostic Agents Selective Against Metalloproteases
  申请人：Bracco Imaging S.p.A

  公开号：EP2147684A1

  公开（公告）日：2010-01-27

  The invention relates to aryl-sulphonamido compounds endowed with affinity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, G and n have the meanings reported in the specification, properly labelled with diagnostic imaging moieties or even radiotherapeutic moieties. The invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as diagnostic imaging agents or radiotherapeutic agents.

  本发明涉及具有亲和力对金属蛋白酶MMP的芳基磺酰胺化合物，其化学式如下（I），其中R，R1，R2，R3，G和n在规范中有所说明，适当地标记有诊断成像或放射治疗成分。本发明还涉及它们的制备过程、包含它们的药物组成物以及它们作为诊断成像剂或放射治疗剂的用途。