L-精氨酰胺二盐酸盐 | 14975-30-5

• 物质功能分类: 生物化工 - 氨基酸及其衍生物 - 其他氨基酸衍生物
• 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: L-精氨酰胺二盐酸盐
• 英文名称: (S)-2-Amino-5-guanidinopentanamide dihydrochloride
• 英文别名: (2S)-2-amino-5-(diaminomethylideneamino)pentanamide;dihydrochloride
• CAS: 14975-30-5
• 化学式: C6H17Cl2N5O
• 分子量: 246.14
• InChiKey: LYMQLFYWIDCFLC-FHNDMYTFSA-N

物化性质

• 溶解度：
  溶于氯仿、二氯甲烷、乙酸乙酯、DMSO、丙酮等。

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  134
• 氢给体数：
  6
• 氢受体数：
  3

安全信息

• 危险品标志：
  T
• 安全说明：
  S36/37
• 危险类别码：
  R20/21/22
• WGK Germany：
  1,2
• 海关编码：
  2925290090
• 危险性防范说明：
  P280,P305+P351+P338,P310
• 危险性描述：
  H302,H315,H319,H332,H335

制备方法与用途

应用范围广泛，L-精氨酰胺二盐酸盐，即H-Arg-NH₂·2HCl，是一种氨基酸衍生物。据文献记载，它不仅可用于制备蜂胶提纯材料，还能用于合成含有六个氨基酸的活性多肽——六胜肽。

反应信息

• 作为反应物：
  描述：

  L-精氨酰胺二盐酸盐 生成 2-[1-[(4S)-4-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-(4-ethoxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-3-methylbutanoyl]amino]-4-oxobutanoyl]amino]-5-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-oxopentyl]cyclohexyl]acetic acid
  参考文献：
  名称：

  CALLAHAN, JAMES F.;HUFFMAN, WILLIAM F.;NEWLANDER, KENNETH A.

  摘要：

  DOI：

文献信息

• Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1022268A1

  公开（公告）日：2000-07-26

  The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to arylalkanoyl derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), R(6a) and R(6b) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula I, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, to and the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

  本发明涉及用于抑制血液凝固蛋白的新化合物，更具体地，是指式I的芳烷酰衍生物， 其中R(1)、R(2)、R(3)、R(4)、R(5)、R(6a)和R(6b)的含义如权利要求中所示。式I的化合物是血液凝固酶因子Xa的抑制剂。本发明还涉及制备式I化合物的方法，抑制因子Xa活性和血液凝固的方法，使用式I化合物治疗和预防可以通过抑制因子Xa活性来治疗或预防的疾病，如血栓栓塞性疾病，以及使用式I化合物制备用于治疗上述疾病的药物。本发明还涉及包含式I化合物的组合物，与惰性载体混合或以其他方式相关联，尤其是包含式I化合物的药物组合物，以及药用可接受的载体物质和辅助物质。
• Self-precipitating pharmaceutical formulations for the moified release of an active principle
  申请人：Checot Frederic

  公开号：US20090011028A1

  公开（公告）日：2009-01-08

  The present invention relates to novel pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time of several days, or even several weeks. The invention relates, in a first aspect, to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloïdal particles of a polymer (PO), wherein said formulation satisfies the following four conditions: (a) the polymer (PO) is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said cationic groups being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said hydrophobic groups (GH) being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.5; (c) at the pHf value, the polymer (PO) forms a colloïdal solution which associates spontaneously and noncovalently with the active principle (AP); (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp. The invention also relates to a process for the preparation of such formulations and to a process for the preparation of medicaments including such formulations.

  本发明涉及用于在数天甚至数周内持续释放活性成分（AP）的新型药物配方。该发明涉及第一方面的液体配方，包括至少一种活性成分（AP）和基于聚合物（PO）的胶体颗粒的水悬浮液，其中该配方满足以下四个条件： (a) 聚合物（PO）是一种包含谷氨酸残基的多氨基酸，其中 一些谷氨酸残基各自携带一个阳离子基团（CG），这些阳离子基团相互相同或不同，以及 其他谷氨酸残基各自携带一个亲水性基团（GH），这些亲水性基团（GH）相互相同或不同， (b) 该配方的pHf值在3.0和6.5之间； (c) 在pHf值下，聚合物（PO）形成与活性成分（AP）自发且非共价地结合的胶体溶液； (d) 1毫升该配方在与1毫升测试缓冲溶液Tp混合时沉淀。 该发明还涉及制备此类配方的方法以及包括此类配方的药物的制备方法。
• [EN] GUANIDINE DERIVATIVES FOR THE TREATMENT OF HEPATITIS C<br/>[FR] DÉRIVÉS DE GUANIDINE POUR LE TRAITEMENT DE L'HÉPATITE C
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2014116768A1

  公开（公告）日：2014-07-31

  Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

  公式I的化合物，包括其药用盐，以及使用这些化合物的组合物和方法，已经列出。这些化合物对丙型肝炎病毒（HCV）具有活性，可能对感染HCV的患者有治疗作用。
• [EN] MOLECULAR DESIGN OF NEW ANTIBIOTICS AND ANTIBIOTIC ADJUVANTS AGAINST MCR STRAINS<br/>[FR] CONCEPTION MOLÉCULAIRE DE NOUVEAUX ANTIBIOTIQUES ET ADJUVANTS D'ANTIBIOTIQUES CONTRE LES SOUCHES MCR
  申请人：SINGAPORE HEALTH SERV PTE LTD

  公开号：WO2020236084A1

  公开（公告）日：2020-11-26

  The present invention relates to a compound comprising a hydrophobic moiety, a linker and N-containing moiety. The present invention also relates to the method of synthesizing the compound and the use of the compound as an antibiotic or an adjuvant for an antibiotic.

  本发明涉及一种包含疏水基团、连接剂和含氮基团的化合物。本发明还涉及合成该化合物的方法以及将该化合物用作抗生素或抗生素辅助剂的用途。
• Insulinotropic peptide synthesis using solid and solution phase combination techniques
  申请人：Chen Lin

  公开号：US20090292108A1

  公开（公告）日：2009-11-26

  The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.

  本发明涉及使用固相和溶液相（“混合”）方法合成胰岛素促分泌肽的制备。通常，该方法包括使用固相化学合成三种不同的肽中间片段。然后，使用溶液相化学将额外的氨基酸材料添加到第三个片段中，然后在溶液中将第三个片段耦合到第二个片段，然后再将第一片段耦合到溶液中。或者，在固相中将不同的第二个片段耦合到第一片段。然后，使用溶液相化学将额外的氨基酸材料添加到不同的第三个片段中。随后，将这个不同的第三个片段耦合到耦合的第一个和不同的第二个片段中的溶液相中。在其中一个片段中使用假丝氨酸可以减轻该片段的固相合成，并且还可以减轻该片段与其他片段的随后溶液相耦合。本发明非常有用，可用于形成胰岛素促分泌肽，例如GLP-1（7-36）及其天然和非天然对应物。