N6-[[(4-硝基苯基)甲氧基]羰基]-L-赖氨酸 | 3557-90-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N6-[[(4-硝基苯基)甲氧基]羰基]-L-赖氨酸
• 英文名称: N^ε-(4-Nitro-benzyloxycarbonyl)-L-lysin
• 英文别名: N^ε-(p-Nitro-benzyloxycarbonyl)-L-lysin；(2S)-2-azaniumyl-6-[(4-nitrophenyl)methoxycarbonylamino]hexanoate
• CAS: 3557-90-2
• 化学式: C₁₄H₁₉N₃O₆
• 分子量: 325.321
• InChiKey: XMTCOKGMBIHVBJ-LBPRGKRZSA-N

物化性质

• 熔点：
  239-240 °C
• 沸点：
  582.9±50.0 °C(Predicted)
• 密度：
  1.332±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  23
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  148
• 氢给体数：
  3
• 氢受体数：
  7

安全信息

• 海关编码：
  2924299090
• 储存条件：
  -20°C

反应信息

• 作为反应物：
  描述：

  对硝基苯甲醇 、 N6-[[(4-硝基苯基)甲氧基]羰基]-L-赖氨酸 在 苯磺酸 作用下， 生成 N^ε-(p-Nitro-benzyloxycarbony)-L-lysin-p-nitro-benzylester
  参考文献：
  名称：

  Preparation of Benzyl and p-Nitrobenzyl Esters of Amino Acids¹

  摘要：

  DOI：

  10.1021/jo01064a043
• 作为产物：
  描述：

  L-赖氨酸盐酸盐 、 氯甲酸对硝基苄酯 生成 N6-[[(4-硝基苯基)甲氧基]羰基]-L-赖氨酸
  参考文献：
  名称：

  Modified Benzyloxycarbonyl Groups for Protection of ε-Amino Group of Lysine

  摘要：

  DOI：

  10.1246/bcsj.43.1883

文献信息

• Traceless Ubiquitination
  申请人：Chin Jason

  公开号：US20140148576A1

  公开（公告）日：2014-05-29

  The invention related to a tRNA synthetase capable of binding delta-substituted lysine, wherein said tRNA synthetase comprises amino acid sequence corresponding to the amino acid sequence of at least L271 to Y349 of MbPyIRS, wherein said sequence comprises 5 or fewer substitutions within the amino acid sequence corresponding to the amino acid sequence of at least L271 to Y349 of MbPyIRS; and wherein said synthetase comprises W at amino acid position 349 relative to MbPyIRS.

  该发明涉及一种能够结合δ-取代赖氨酸的tRNA合成酶，其中该tRNA合成酶包括与MbPyIRS的至少L271到Y349的氨基酸序列相对应的氨基酸序列，其中该序列在与MbPyIRS的至少L271到Y349的氨基酸序列相对应的氨基酸序列内仅包含5个或更少的替换；并且该合成酶在相对于MbPyIRS的氨基酸位置349处包含W。
• Use of enzyme inhibitors of the dipeptidypeptidase iv (ec3.3.14.5) in addition to the aminopeptidase n (ec 3.4.11.2), individually or in a combination thereof, and pharmaceutical preparations thereof for the prevention and/or therapy of ischaemia-caused acute and chronic neurodegenerative process and illnesses, for example
  申请人：——

  公开号：US20040147434A1

  公开（公告）日：2004-07-29

  The present invention relates to a process wherein, by a separate or simultaneous administration and effect of inhibitors of the enzymes alanyl aminopeptidase (APN) and dipeptidyl peptidase IV (DP IV) or of enzymes having the same or a similar substrate specifity, the damage of cerebral tissue as a consequence of an ischemia or a cranial/cerebral trauma can be reduced or prevented. The invention shows that the separate or combined application of inhibitory substances of the above-mentioned enzymes or of corresponding preparations or administration forms is definitely suitable for a prevention and therapy of the above indications.

  本发明涉及一种工艺，通过单独或同时施用丙氨酰氨基肽酶（APN）和二肽基肽酶 IV（DP IV）的抑制剂或具有相同或相似底物特异性的酶的抑制剂并发挥其作用，可减少或预防因缺血或颅脑外伤造成的脑组织损伤。 本发明表明，单独或联合应用上述酶的抑制物质或相应的制剂或给药形式，绝对适用于上述适应症的预防和治疗。
• Combinations of enzyme inhibitor-containing preparations and the use thereof
  申请人：Ansorge Siegfried

  公开号：US20050014699A1

  公开（公告）日：2005-01-20

  The invention comprises a process wherein the DNA synthesis and, thus, the proliferation of mononuclear cells (MNZ) and of T cells as well is inhibited by the simultaneous and combined inhibition of the enzyme activity (I) of alanyl aminopeptidase and of dipeptidyl peptidase IV; (II) of dipeptidyl peptidase IV and of the angiotensin-converting enzyme; (III) of dipeptidyl peptidase IV and of prolyl oligopeptidase; and (IV) of dipeptidyl peptidase IV and of X-Pro-aminopeptidase to an extent which cannot be achieved by an application of a single one of said enzyme inhibitors, even at a higher dosage. Although the said inhibitors exercise an influence on the very same process finally, i.e. the DNA synthesis and, thus, the proliferation of immune cells, this effect is not complete and is not long lasting when a single inhibitor is applied. From the functional overlap of enzymatic activities results an additive/superadditive inhibitory effect on the DNA synthesis and proliferation by the simultaneous inhibition of more than one of the above enzymes, as our data show. Our invention shows that the simultaneous application of substances inhibiting the above enzymes or of corresponding preparations and administration forms, respectively, is well suitable for a therapy of autoimmune diseases and chronic diseases with an inflammatory genesis as well as for a treatment of rejection episodes after a transplantation.

  本发明包括一种工艺，在该工艺中，通过同时和联合抑制(I) 丙氨酰氨基肽酶和二肽基肽酶 IV 的酶活性，抑制 DNA 合成，从而抑制单核细胞（MNZ）和 T 细胞的增殖；(II) 二肽基肽酶 IV 和血管紧张素转换酶； (III) 二肽基肽酶 IV 和脯氨酰寡肽酶；以及 (IV) 二肽基肽酶 IV 和 X-脯氨酰肽酶，其抑制程度是单用一种上述酶抑制剂所无法达到的，即使使用较大剂量也是如此。虽然上述抑制剂最终会对相同的过程，即 DNA 合成产生影响，从而影响免疫细胞的增殖，但在使用单一抑制剂时，这种影响并不完全，也不持久。正如我们的数据所显示的那样，由于酶活性的功能重叠，通过同时抑制上述一种以上的酶，会对 DNA 合成和增殖产生叠加/超叠加抑制作用。我们的发明表明，同时应用抑制上述酶的物质或相应的制剂和给药形式，非常适合用于治疗自身免疫性疾病和炎症性慢性疾病，以及治疗移植后的排斥反应。
• Use of inhibitors of enzymes having activities of amino peptidase N and/or dipeptidyl peptidase IV and of pharmaceutical preparations thereof for a therapy and prevention of chronical neurodegenerative diseases
  申请人：Striggow Frank

  公开号：US20050113310A1

  公开（公告）日：2005-05-26

  The invention relates to a process for the treatment of neurodegenerative diseases wherein mis-folded proteins accumulate in characteristic lesions and contribute substantially to a pathogenesis and to an inflammatory reaction magnifying the damage, by the isolated or joint effect of inhibitors of the alanyl amino peptidase (APN) and of the dipeptidyl peptidase N (DP IV). Our results show that the application of inhibitors of the above-referenced enzymes or of preparations and dosage forms containing such inhibitors is definitely suitable for a therapy and prevention of dementia diseases and conditions.

  本发明涉及一种通过丙氨酰氨基肽酶（APN）和二肽基肽酶 N（DP IV）抑制剂的单独或联合作用来治疗神经退行性疾病的方法，在这种疾病中，错误折叠的蛋白质聚集在特征性病变中，并在很大程度上导致了发病机制和扩大损害的炎症反应。我们的研究结果表明，应用上述酶的抑制剂或含有此类抑制剂的制剂和剂型，绝对适用于治疗和预防痴呆症疾病和病症。
• Use of enzyme inhibitors with aminopeptidase n and/or dipeptidylpeptidase IV activities and pharmaceutical preparations produced therefrom for the therapy and prevention of dermatological diseases with seborrhoeic hyperproliferation and altered differentiation states
  申请人：Ansorge Siegfried

  公开号：US20060040850A1

  公开（公告）日：2006-02-23

  The invention relates to a process for the-inhibition of the DNA synthesis necessary for the proliferation of human sebaceous cells (sebocytes) by the isolated or joint effect of inhibitors of alanyl aminopeptidase (APN) and dipetidyl peptidase IV (DP IV) expressed by these cells. The DNA synthesis (proliferation) of human sebaceous cells is inhibited by the administration of the inhibitors of APN and/or of DP IV depending on the dose. Our invention shows that, for a therapy and for a prevention of dermatological diseases with sebaceous hyperproliferation and modified conditions of differentiation, the application of inhibitors of the above-mentioned enzymes and of corresponding pharmaceutical preparations and dosage forms thereof is suitable.

  本发明涉及一种通过单独使用或联合使用丙氨酰氨基肽酶（APN）和二乙酰肽酶 IV（DP IV）抑制剂来抑制人类皮脂腺细胞（皮脂细胞）增殖所需的 DNA 合成的工艺。人皮脂腺细胞的 DNA 合成（增殖）会受到 APN 抑制剂和/或 DP IV 抑制剂（视剂量而定）的抑制。我们的发明表明，在治疗和预防皮脂腺过度增生和分化条件改变的皮肤病时，应用上述酶的抑制剂和相应的药物制剂及其剂型是合适的。