柠檬酸氢二铵 | 3012-65-5

• 物质功能分类: 有机原料 - 有机金属盐
• 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: 柠檬酸氢二铵
• 中文别名: 柠檬酸氢铵；柠檬酸氢二；二碱式柠檬酸铵；柠檬酸二铵
• 英文名称: 1,2,3-Propanetricarboxylic acid, 2-hydroxy-, diammonium salt
• 英文别名: diazanium;hydron;2-hydroxypropane-1,2,3-tricarboxylate
• CAS: 3012-65-5
• 化学式: C6H14N2O7
• 分子量: 226.18
• InChiKey: YXVFQADLFFNVDS-UHFFFAOYSA-N

物化性质

• 熔点：
  185 °C (dec.)(lit.)
• 沸点：
  100 °C(lit.)
• 密度：
  1.22 g/mL at 20 °C
• 蒸气密度：
  1.8 (vs air)
• 溶解度：
  H2O:1 Mat 20 °C,透明，无色
• 最大波长(λmax)：
  λ: 260 nm Amax: ≤0.05λ: 280 nm Amax: ≤0.03
• LogP：
  -2.840
• 物理描述：
  Ammonium citrate is a white granular solid. It is soluble in water. The primary hazard is the threat to the environment. Immediate steps should be taken to limit its spread to the environment. It is used in pharmaceuticals, and in chemical analysis.
• 颜色/状态：
  Granules or crystals
• 气味：
  Slight ammoniacal

计算性质

• 辛醇/水分配系数(LogP)：
  -3.17
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  140
• 氢给体数：
  4
• 氢受体数：
  7

ADMET

代谢

研究膳食柠檬酸铵和静脉注射乳酸钠在大鼠中的代谢命运的结果显示，尿素合成在很大浓度范围内代表了几乎恒定的管理氨分数。除了谷氨酰胺和尿素，标记的氮也出现在肌酸、甘氨酸、丙氨酸、脯氨酸、组氨酸、精氨酸、谷氨酸和天冬氨酸中。...检查了未经处理和生长激素处理的垂体切除大鼠的肝脏、心脏、肾脏、脾脏和肌肉部分中来自柠檬酸铵的(15)N的掺入蛋白质，并发现根据管理途径的不同，代谢命运存在差异。皮下注射促进了酰胺氮的标记，表明通过谷氨酰胺合成有大量的分布。相比之下，口服或腹腔注射导致标记精氨酸、谷氨酸和其他肝脏的α-氨基酸。酰胺氮的标记程度远低于皮下注射。标记的组织分布也根据进入途径不同而有所不同。/柠檬酸铵/

Results of studies on the metabolic fate of dietary ammonium citrate and intravenously-administered ammonium lactate in rats showed that urea synthesis represented a nearly constant fraction of the administered ammonia over a large concentration range. Besides glutamine and urea, labelled nitrogen also appeared in creatine, glycine, alanine, proline, histidine, arginine, glutamic acid, and aspartic acid. ...The incorporation of (15)N from ammonium citrate into proteins of liver, heart, kidney, spleen, and muscle fractions of untreated and growth hormone-treated, hypophysectomized rats /was examined/, and found differences in the metabolic fate, depending on the route of administration. Subcutaneous injection facilitated the labelling of amide nitrogen, indicating extensive disposition via glutamine synthesis. In contrast, intragastric or intraperitoneal administration resulted in the labelling of arginine, glutamic acid, and other alpha-amino acids of the liver. Amide-nitrogen was labelled to a much lesser extent than by the subcutaneous route. The tissue distribution of the label also differed according to the route of entry. /Ammonium citrate/

来源:Hazardous Substances Data Bank (HSDB)

代谢

研究探讨了饮食中柠檬酸铵和静脉注射乳酸钠在大鼠体内的代谢命运。结果显示，在大范围的浓度下，尿素合成占所施用氨的几乎恒定比例。除了谷氨酰胺和尿素外，标记的氮也出现在肌酸、甘氨酸、丙氨酸、脯氨酸、组氨酸、精氨酸、谷氨酸和天冬氨酸中。... 对未经处理和生长激素处理的垂体切除大鼠的肝脏、心脏、肾脏、脾脏和肌肉部分中的蛋白质进行了柠檬酸铵中(15)N的掺入研究，并发现根据给药途径的不同，代谢命运也存在差异。皮下注射促进了酰胺氮的标记，表明通过谷氨酰胺合成的广泛分布。相比之下，灌胃或腹膜内给药导致肝脏中的精氨酸、谷氨酸和其他α-氨基酸的标记。酰胺氮的标记程度远低于皮下注射。标记物的组织分布也根据进入途径的不同而有所差异。/柠檬酸铵/

Results of studies on the metabolic fate of dietary ammonium citrate and intravenously-administered ammonium lactate in rats showed that urea synthesis represented a nearly constant fraction of the administered ammonia over a large concentration range. Besides glutamine and urea, labelled nitrogen also appeared in creatine, glycine, alanine, proline, histidine, arginine, glutamic acid, and aspartic acid. ...The incorporation of (15)N from ammonium citrate into proteins of liver, heart, kidney, spleen, and muscle fractions of untreated and growth hormone-treated, hypophysectomized rats /was examined/, and found differences in the metabolic fate, depending on the route of administration. Subcutaneous injection facilitated the labelling of amide nitrogen, indicating extensive disposition via glutamine synthesis. In contrast, intragastric or intraperitoneal administration resulted in the labelling of arginine, glutamic acid, and other alpha-amino acids of the liver. Amide-nitrogen was labelled to a much lesser extent than by the subcutaneous route. The tissue distribution of the label also differed according to the route of entry. /Ammonium citrate/

来源:Hazardous Substances Data Bank (HSDB)

代谢

研究探讨了饮食中柠檬酸铵和静脉注射乳酸钠在大鼠体内的代谢命运。结果显示，在大范围的浓度下，尿素合成占所施用氨的几乎恒定比例。除了谷氨酰胺和尿素外，标记的氮也出现在肌酸、甘氨酸、丙氨酸、脯氨酸、组氨酸、精氨酸、谷氨酸和天冬氨酸中。... 对未经处理和生长激素处理的垂体切除大鼠的肝脏、心脏、肾脏、脾脏和肌肉部分中的蛋白质进行了柠檬酸铵中(15)N的掺入研究，并发现根据给药途径的不同，代谢命运也存在差异。皮下注射促进了酰胺氮的标记，表明通过谷氨酰胺合成的广泛分布。相比之下，灌胃或腹膜内给药导致肝脏中的精氨酸、谷氨酸和其他α-氨基酸的标记。酰胺氮的标记程度远低于皮下注射。标记物的组织分布也根据进入途径的不同而有所差异。/柠檬酸铵/

Results of studies on the metabolic fate of dietary ammonium citrate and intravenously-administered ammonium lactate in rats showed that urea synthesis represented a nearly constant fraction of the administered ammonia over a large concentration range. Besides glutamine and urea, labelled nitrogen also appeared in creatine, glycine, alanine, proline, histidine, arginine, glutamic acid, and aspartic acid. ...The incorporation of (15)N from ammonium citrate into proteins of liver, heart, kidney, spleen, and muscle fractions of untreated and growth hormone-treated, hypophysectomized rats /was examined/, and found differences in the metabolic fate, depending on the route of administration. Subcutaneous injection facilitated the labelling of amide nitrogen, indicating extensive disposition via glutamine synthesis. In contrast, intragastric or intraperitoneal administration resulted in the labelling of arginine, glutamic acid, and other alpha-amino acids of the liver. Amide-nitrogen was labelled to a much lesser extent than by the subcutaneous route. The tissue distribution of the label also differed according to the route of entry. /Ammonium citrate/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

L-蛋氨酸和甜菜碱HCl被发现可以缓解由过量L-谷氨酸引起的雏鸡生长抑制。过量的L-蛋氨酸对L-谷氨酸和 diammonium citrate引起的生长抑制具有保护作用，反之，补充L-丝氨酸和甲酸钠并不能防止谷氨酸或精氨酸引起的生长抑制。结果与假设一致，即高水平的膳食蛋白质和单一氨基酸的过量氮会增加对预成甲基组的需求。

L-methionine and betaine HCl were found to alleviate the growth depression /in chicks/ caused by excessive levels of L-glutamic acid. Excessive levels of L-methionine had a protective effect against growth depression caused by L-glutamate and diammonium citrate, and conversely, supplementary L-serine and sodium formate were not protective against glutamic acid- or arginine-induced growth depression. The results are consistent with the hypothesis that the preformed methyl group requirement is increased by high levels of dietary protein and excessive nitrogen from a single amino acid.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

基本治疗：建立专利气道（如有需要，使用口咽或鼻咽气道）。必要时进行吸痰。观察呼吸不足的迹象，并在必要时协助通气。通过非循环呼吸面罩以10至15升/分钟的速度给予氧气。监测肺水肿的迹象，并在必要时进行治疗……。监测休克的迹象，并在必要时进行治疗……。对于眼睛污染，立即用水冲洗眼睛。在运输过程中，用0.9%的生理盐水（NS）连续冲洗每只眼睛……。不要使用催吐剂。对于摄入，如果患者能够吞咽、有强烈的呕吐反射且不流口水，则用水冲洗口腔，并给予5毫克/千克，最多200毫升的水进行稀释……。不要尝试中和。/氨和相关化合物/

Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for signs of pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mg/kg up to 200 ml of water for dilution if the patent can swallow, has a strong gag reflex, and does not drool ... . Do not attempt to neutralize. /Ammonia and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

高级治疗：对于失去意识、严重肺水肿或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。使用带有气囊-阀-面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿……。对于严重的支气管痉挛，考虑给予β激动剂，如沙丁胺醇……。监测心率和必要时治疗心律失常……。开始静脉输注D5W/SRP：“保持开放”，最低流量/。如果出现低血容量的迹象，使用0.9%的生理盐水（NS）或乳酸林格氏液（LR）。对于伴有低血容量迹象的低血压，谨慎给予液体。如果病人在正常血容量下出现低血压，考虑使用血管加压药。注意液体过载的迹象……。使用丙美卡因氢氯化物协助眼部冲洗……。/氨及其相关化合物/

Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag-valve-mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias if necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Consider vasopressors if patient is hypotensive with a normal fluid volume. Watch for signs of fluid overload ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Ammonium and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

征兆与症状：尘埃：刺激眼睛、鼻子和喉咙；如果吸入，会引起咳嗽或呼吸困难。固态：刺激皮肤和眼睛。

/SIGNS AND SYMPTOMS/ Dust: irritating to eyes, nose and throat; if inhaled will cause coughing or difficult breathing. Solid: irritating to skin and eyes.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

实验室动物：急性暴露/ 使用大量氯化铵、硝酸盐、醋酸盐、碳酸氢盐、柠檬酸盐、乳酸盐、扁桃酸盐、磷酸盐、硫酸盐等，可能会出现足够的吸收，产生利尿和系统性氨中毒，尤其是如果该物质通过 parenterally（非口服途径，例如注射）给药。/柠檬酸铵/

/LABORATORY ANIMALS: Acute Exposure/ With large doses of ammonium chloride, nitrate, acetate, bicarbonate, citrate, lactate, mandelate, phosphate, sulfate, etc, there arises the possibility of sufficient absorption to produce a diuresis and systemic ammonia poisoning, particularly if the material is administered parenterally. /Ammonium citrate/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

柠檬酸铵（15）N的分布，通过不同途径给药，进入垂体切除大鼠各种组织的蛋白质中/进行了检查/。在胃内、腹腔内和皮下给药15N-柠檬酸铵后的72小时内，肝脏、肾脏和脾脏中蛋白质结合的（15）N浓度高于心脏或肌肉部分。在最初的6小时内，胃内给药途径给出了更高的值，此后，进入肝脏蛋白质的（15）N量并未受到给药途径的显著影响。然而，在大多数其他研究中，通过胃内给药途径的（15）N结合倾向最小，其次是腹腔内和皮下给药途径，后者使更多的标记氨明显地提供给广泛分布的谷氨酰胺合成酶（EC 6.3.1.2）系统。/柠檬酸铵/

...The distribution of (15)N from ammonium citrate, administered by different routes, into the proteins of various tissues of hypophysectomized rats /was examined/. The liver, kidney, and spleen contained greater concentrations of (15)N incorporated into proteins than heart or muscle fractions during 72 hr following intragastric, intraperitoneal, and subcutaneous administration of 15N-ammonium citrate. After the first 6 hr, during which the intragastric route gave higher values, the quantity of (15)N incorporated into liver-protein was not substantially affected by the route of administration. In most of the other tissues studied, however, (15)N incorporation tended to be least by the intragastric route, followed, in increasing order, by the intraperitoneal and subcutaneous routes. By the last route, more labelled ammonia was apparently made available to the widely distributed glutamine-synthetase (EC 6.3.1.2) system. /Ammonium citrate/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

...研究了通过不同途径给予柠檬酸铵(15)N在切除垂体的大鼠各种组织蛋白质中的分布。在给予15N-柠檬酸铵后72小时内，肝脏、肾脏和脾脏中蛋白质结合的(15)N浓度高于心脏或肌肉部分。在最初的6小时内，通过胃内途径给予的值更高，此后，进入肝脏蛋白质中的(15)N量基本上不受给药途径的影响。然而，在大多数其他研究中，通过胃内途径的(15)N结合倾向最小，其次是腹膜内和皮下途径，这两种途径的(15)N结合量逐渐增加。通过最后一种途径，更多的标记氨显然被广泛分布的谷氨酰胺合成酶(EC 6.3.1.2)系统利用。/柠檬酸铵/

...The distribution of (15)N from ammonium citrate, administered by different routes, into the proteins of various tissues of hypophysectomized rats /was examined/. The liver, kidney, and spleen contained greater concentrations of (15)N incorporated into proteins than heart or muscle fractions during 72 hr following intragastric, intraperitoneal, and subcutaneous administration of 15N-ammonium citrate. After the first 6 hr, during which the intragastric route gave higher values, the quantity of (15)N incorporated into liver-protein was not substantially affected by the route of administration. In most of the other tissues studied, however, (15)N incorporation tended to be least by the intragastric route, followed, in increasing order, by the intraperitoneal and subcutaneous routes. By the last route, more labelled ammonia was apparently made available to the widely distributed glutamine-synthetase (EC 6.3.1.2) system. /Ammonium citrate/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

柠檬酸铵（15）N的分布，通过不同途径给药，进入垂体切除大鼠各种组织的蛋白质中/进行了检查/。在胃内、腹腔内和皮下给药15N-柠檬酸铵后的72小时内，肝脏、肾脏和脾脏中蛋白质结合的（15）N浓度高于心脏或肌肉部分。在最初的6小时内，胃内给药途径给出了更高的值，此后，进入肝蛋白质的（15）N量并没有受到给药途径的显著影响。然而，在大多数其他研究中，通过胃内给药途径的（15）N结合倾向最小，其次是腹腔内和皮下给药途径，后者使更多的标记氨明显地提供给广泛分布的谷氨酰胺合成酶（EC 6.3.1.2）系统。/柠檬酸铵/

...The distribution of (15)N from ammonium citrate, administered by different routes, into the proteins of various tissues of hypophysectomized rats /was examined/. The liver, kidney, and spleen contained greater concentrations of (15)N incorporated into proteins than heart or muscle fractions during 72 hr following intragastric, intraperitoneal, and subcutaneous administration of 15N-ammonium citrate. After the first 6 hr, during which the intragastric route gave higher values, the quantity of (15)N incorporated into liver-protein was not substantially affected by the route of administration. In most of the other tissues studied, however, (15)N incorporation tended to be least by the intragastric route, followed, in increasing order, by the intraperitoneal and subcutaneous routes. By the last route, more labelled ammonia was apparently made available to the widely distributed glutamine-synthetase (EC 6.3.1.2) system. /Ammonium citrate/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• TSCA：
  Yes
• 危险品标志：
  Xi
• 安全说明：
  S26,S36
• 危险类别码：
  R36/37
• WGK Germany：
  3
• 海关编码：
  2923900090
• 危险品运输编号：
  UN 9087
• RTECS号：
  GE7545000
• 危险标志：
  GHS07
• 危险性描述：
  H319,H335
• 危险性防范说明：
  P261,P305 + P351 + P338

制备方法与用途

用途
用作分析试剂和缓冲剂，还可测定肥料中的磷酸盐、防锈以及作为增塑剂。

反应信息

• 作为反应物：
  描述：

  柠檬酸氢二铵 、 环氧氯丙烷 生成 1-O-(3-chloro-2-hydroxypropyl) 2-O,3-O-dimethyl 2-hydroxypropane-1,2,3-tricarboxylate
  参考文献：
  名称：

  KLOPOTEK, ALOJZY;IWANCZUK, EDWARD

  摘要：

  DOI：
• 作为产物：
  描述：

  柠檬酸 生成 柠檬酸氢二铵
  参考文献：
  名称：

  ROSCA, DUMITRU;AMBRONO, DANIELA;INDREI, LIVIUS

  摘要：

  DOI：

文献信息

• NOVEL INHIBITORS OF GLUTAMINYL CYCLASE
  申请人：Buchholz Mirko

  公开号：US20080267911A1

  公开（公告）日：2008-10-30

  Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: R 1 represents and R 2 , R 3 , R 4 , R 5 , R 6 , X 1 , X 2 , X 3 , X 4 , Y and Z are as defined throughout the description and the claims.

  式(I)的化合物，其组合物及用途用于疾病治疗，或其药学上可接受的盐、溶剂化合物或多晶形式，包括其所有互变异构体和立体异构体，其中： R1代表，而R2、R3、R4、R5、R6、X1、X2、X3、X4、Y和Z如描述和权利要求中所定义。
• [EN] NOVEL INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS
  申请人：PROBIODRUG AG

  公开号：WO2018178384A1

  公开（公告）日：2018-10-04

  The invention relates to a compound of formula (I): A-B-D-E (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is selected from monocyclic and bicyclic heteroaryl, which may independently substituted by alkyl or amino; B is selected from alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups may independently be substituted by alkyl; D is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted; and E is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted. The compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N- terminal glutamate residues into pyroglutamic acid under liberation of water.

  该发明涉及以下式(I)的化合物：A-B-D-E (I)或其药学上可接受的盐、溶剂或多型体，包括其所有互变异构体和立体异构体，其中：A选自可以独立由烷基或氨基取代的单环和双环杂环基；B选自烷基、杂环烷基、烷基氨基、芳基、杂芳基、环烷基、杂环烷基和烷基烯，其中这些基团可以独立地被烷基取代；D选自芳基氨基、杂芳基氨基、环烷基氨基、杂环烷基、杂环烷基氨基、脲、硫代酰胺、硫脲、磺酰胺、亚砜和磺酰胺，其中这些芳基、杂芳基、环烷基和杂环烷基基团可以独立地被取代；E选自芳基、杂芳基、环烷基、杂环烷基，其中这些芳基、杂芳基、环烷基和杂环烷基基团可以独立地被取代。式(I)的化合物是谷氨酰环化酶（QC，EC 2.3.2.5）的抑制剂。QC催化N-末端谷氨酸残基的分子内环化成吡咯谷氨酸（5-氧代脯氨酰，pGlu*），释放氨气，并催化N-末端谷氨酸残基的分子内环化成吡咯谷氨酸，释放水。
• NOVEL INHIBITORS
  申请人：Heiser Ulrich

  公开号：US20110092501A1

  公开（公告）日：2011-04-21

  The invention relates to novel pyrrolidine derivatives of formula (I): wherein R 1 , R 2 and R 3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

  本发明涉及新颖的吡咯烷衍生物，其具有如下公式(I)：其中R1、R2和R3如本文所述定义，作为谷氨酰胺环化酶（QC，EC 2.3.2.5）的抑制剂。谷氨酰胺环化酶催化N末端谷氨酰胺残基形成焦谷氨酸（5-氧代脯氨酸，pGlu*）的分子内环化，并释放氨，以及催化N末端谷氨酸残基形成焦谷氨酸的分子内环化，并释放水。
• METHODS FOR THE CONVERSION OF A SUBSTITUTED FURAN TO A SUBSTITUTED PYRROLE
  申请人：Kreischer Bruce E.

  公开号：US20120083609A1

  公开（公告）日：2012-04-05

  The present invention discloses processes for producing substituted pyrrole compounds, such as 2,5-disubstituted pyrroles. Synthetic processes which directly convert substituted furan compounds to substituted pyrrole compounds, via a reaction of the substituted furan compound with ammonia and/or an ammonium salt in the presence of a catalyst, also are described.

  本发明揭示了生产取代吡咯化合物的过程，例如2,5-二取代吡咯化合物。还描述了一种合成过程，该过程通过将取代呋喃化合物与氨和/或铵盐在催化剂存在下反应，直接转化为取代吡咯化合物。
• Novel Inhibitors
  申请人：Heiser Ulrich

  公开号：US20120237475A1

  公开（公告）日：2012-09-20

  Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R a , n, R 1 and R 2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).

  式(I)的新颖杂环衍生物：或其药用可接受的盐、溶剂合物或多晶形式，包括其所有互变异构体和立体异构体，其中Ra、n、R1和R2如本文所定义，作为谷氨酰环化酶（QC，EC 2.3.2.5）的抑制剂。

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