tBoc-AlaAlaOH | 51513-85-0

• 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
• 英文名称: tBoc-AlaAlaOH
• 英文别名: 2-({2-[(Tert-butoxycarbonyl)ammonio]propanoyl}amino)propanoate；2-[2-[(2-methylpropan-2-yl)oxycarbonylazaniumyl]propanoylamino]propanoate
• CAS: 51513-85-0
• 化学式: C₁₁H₂₀N₂O₅
• mdl: MFCD13187990
• 分子量: 260.29
• InChiKey: BZNDDHWTEVCBAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.727
• 拓扑面积：
  105
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tBoc-AlaAlaOH 在 N-甲基吗啉 作用下， 以 四氢呋喃 为溶剂， 反应 1.05h， 生成 {1-[1-(Biphenyl-4-ylcarbamoyl)-ethylcarbamoyl]-ethyl}-carbamic acid tert-butyl ester
  参考文献：
  名称：

  Peptide conformational distributions as studied by electron-transfer kinetics

  摘要：

  The preparation and electron-transfer (ET) behavior of a homologous series of alanine oligomers bearing naphthoyl groups at the N-termini and biphenylylamide groups at the C-termini is described. Electron pulse radiolysis was used to generate the corresponding radical anions, and the rates of ET were monitored at 700 nm (decay of donor) and at 500 nm (growth of acceptor). Several systems displayed ET decays too fast to measure (k(et) > 10(10)), and in the others multiexponential decay kinetics were observed. The ET decay of dipeptide 3 could be fit to two exponential described by rate constants of 5.2 x 10(8) (22%) and 5.6 x 10(9) s-1 (78%). In the longer peptides, the fit of the rate constants (and their relative contributions to total intensity) becomes less well-defined, suggesting additional conformational diversity.

  DOI：

  10.1021/jo00018a034

文献信息

• PRODRUGS OF FUSED-BICYCLIC C5aR ANTAGONISTS
  申请人：CHEMOCENTRYX, INC.

  公开号：US20190300526A1

  公开（公告）日：2019-10-03

  The present disclosure provides, inter alia, Compounds of Formulae IA, IB, IC, IIA, IIB and IIC or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.

  本公开提供了化合物IA、IB、IC、IIA、IIB和IIC的结构，或其在药学上可接受的盐，这些化合物是C5a受体的调节剂。还提供了包括治疗涉及C5a病理性激活的疾病或疾病的药物组合物和使用方法，以及非药物应用。
• [EN] ANTI-HUMAN VISTA ANTIBODIES AND USE THEREOF<br/>[FR] ANTICORPS ANTI-VISTA HUMAINS ET UTILISATION ASSOCIÉE
  申请人：IMMUNEXT INC

  公开号：WO2021216913A1

  公开（公告）日：2021-10-28

  The invention provides anti-VISTA antibody drug conjugates which may be used for targeted delivery of anti-inflammatory agents such as steroids to immune cells, e.g., myeloid cells. The invention also provides methods of using anti-VISTA antibody drug conjugates in the treatment of inflammatory and/or autoimmune conditions and/or for alleviating the toxicity of anti-inflammatory agents such as steroids.

  本发明提供了抗VISTA抗体药物偶联物，可用于针对免疫细胞（例如，髓系细胞）的靶向递送抗炎剂，例如类固醇。本发明还提供了在治疗炎症和/或自身免疫状况以及/或减轻抗炎剂（如类固醇）的毒性中使用抗VISTA抗体药物偶联物的方法。
• Tumour targeting prodrugs activated by metallo matrixproteinases
  申请人：——

  公开号：US20040248765A1

  公开（公告）日：2004-12-09

  A-(B) n —X   (I) A-(B) n -Q   (II) Structural Relationship of Example ( 8 ) to its Potential Metabolites 1 Numbers in Parentheses denote examples in the specification A compound is of general formula (I) wherein (A) is a moiety comprising one of more of a heterocylcic ring, a carbocyclic ring and a fused ring system, the ring or ring system being essential for a biological activity of the compound by action at a nucleic acid or protein target (B) is a bivalent spacer molecule attached directly to the ring system n is an integer 0 or 1 and (X) is a monovalent moiety containing a amide bond that is cleavable by the action of a matrix metalloproteinase enzyme such as to produce a compound of formula (II) wherein the efficacy of the biological activity of the compound of formula (II) is increased over that of the compound of formula (I).

  化合物的结构关系示例（8）与其潜在代谢产物的关系 1. 括号中的数字表示规范中的示例 化合物具有通式（I），其中（A）是包含杂环环、碳环环和融合环系统中的一个或多个的基团，该环或环系统通过作用于核酸或蛋白靶标而对化合物的生物活性至关重要；（B）是直接连接到环系统的二价间隔分子；n是整数0或1；（X）是含有可被基质金属蛋白酶酶作用而可裂解的酰胺键的一价基团，从而产生通式（II）的化合物，其中通式（II）的化合物的生物活性效力比通式（I）的化合物增加。
• PRODRUGS OF CYTOTOXIC ACTIVE AGENTS HAVING ENZYMATICALLY CLEAVABLE GROUPS
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20190077752A1

  公开（公告）日：2019-03-14

  The invention relates to novel prodrugs or conjugates of the general formula (Ia) in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are masked with legumain-cleavable groups and hence release the drug, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers.

  该发明涉及通式(Ia)的新型前药或结合物，其中细胞毒性药物，例如动力蛋白抑制剂，被腿蛋白酶可切割基团掩蔽，从而释放药物，并且涉及使用这些前药或结合物用于治疗和/或预防疾病，以及使用这些前药或结合物用于生产用于治疗和/或预防疾病的药物，特别是治疗和/或预防高增殖和/或血管生成异常的疾病，例如癌症。
• PREPARATION AND USE OF IMMUNOSTIMULATORY COUPLING COMPLEX WHICH IS DELIVERED AND ACTIVATED IN TARGETED MANNER
  申请人：Yafei Shanghai Biolog Medicine Science & Technology Co., Ltd.

  公开号：EP4108675A1

  公开（公告）日：2022-12-28

  The present disclosure provides for the preparation and use of immunostimulatory conjugate complexes for targeted delivery and activation. In particular, the present disclosure provides compounds represented by the formula MI-S-C-A for use as linker, and drug-linked pharmaceutical compounds represented by the formula MI-S-C-A-D. The pharmaceutical compounds of the present disclosure have improved water solubility, reduced cytotoxicity, and enhanced pharmaceutical activity.

  本公开提供了免疫刺激偶联物复合物的制备和使用，以进行靶向传递和激活。特别地，本公开提供了由公式MI-S-C-A表示的化合物作为连接剂，以及由公式MI-S-C-A-D表示的药物偶联制剂。本公开的药物化合物具有改善的水溶性，降低的细胞毒性和增强的药物活性。