(1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethanamine trifluoroacetic acid salt | 1400190-86-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethanamine trifluoroacetic acid salt
• 英文别名: (1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethanamine trifluoroacetate；(1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethanamine;2,2,2-trifluoroacetic acid
• CAS: 1400190-86-4
• 化学式: C₂HF₃O₂*C₁₆H₁₅N₃O
• 分子量: 379.339
• InChiKey: WQVMMOHOCDYLGP-PFEQFJNWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.61
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  102
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  、 N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-2-carboxy-1-methoxypropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide 、 (1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethanamine trifluoroacetic acid salt 生成 N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide
  参考文献：
  名称：

  NOVEL BINDER-DRUG CONJUGATES (ADCs) AND USE OF SAME

  摘要：

  本专利申请涉及一种新型的N,N-二烷基月桂酰基脂肪酸类药物结合物（ADCs），针对表皮生长因子受体（EGFR，基因ID 1956）的靶向作用，这些ADCs的有效代谢物，制备这些ADCs的方法，使用这些ADCs治疗和/或预防疾病以及使用这些ADCs制备用于治疗和/或预防疾病的药物，特别是高增殖和/或血管生成性疾病，例如癌症。这种治疗可以作为单一疗法或与其他药物或治疗措施联合使用。

  公开号：

  US20150246136A1
• 作为产物：
  描述：

  tert-butyl (1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl carbamate 、 三氟乙酸 以 二氯甲烷 为溶剂， 反应 0.5h， 以86%的产率得到(1R)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethanamine trifluoroacetic acid salt
  参考文献：
  名称：

  NOVEL BINDER-DRUG CONJUGATES (ADCs) AND USE OF SAME

  摘要：

  本专利申请涉及针对靶向表皮生长因子受体（EGFR，基因ID 1956）的新型结合物-药物共轭物（ADCs）N，N-二烷基月桂酰基蛋白酶抑制剂，这些ADCs的有效代谢物，生产这些ADCs的方法，利用这些ADCs治疗和/或预防疾病，以及利用这些ADCs生产用于治疗和/或预防疾病的药物，特别是治疗高增殖和/或血管生成性疾病，如癌症。这种治疗可以作为单药疗法或与其他药物或其他治疗措施联合使用。

  公开号：

  US20150246136A1

文献信息

• NEW ANTIBODY DRUG CONJUGATES (ADCS) AND THE USE THEREOF
  申请人：SEATTLE GENETICS, INC.

  公开号：US20150023989A1

  公开（公告）日：2015-01-22

  The present application relates to new antibody drug conjugates (ADCs) of N,N dialkylauristatins directed against the target FGFR2, drug metabolites of said ADCs, a method for producing said ADCs, the use of said ADCs for the treatment and/or prevention of illnesses as well as the use of said ADCs for producing pharmaceuticals for the treatment and/or prevention of illnesses, particularly of hyperproliferative and/or angiogenic diseases such as carcinosis. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.

  本申请涉及针对FGFR2靶点的新抗体药物结合物（ADCs），所述ADCs的药物代谢产物，生产所述ADCs的方法，利用所述ADCs治疗和/或预防疾病以及利用所述ADCs生产用于治疗和/或预防疾病的药物，特别是治疗高增殖和/或血管生成性疾病如癌症。这种治疗可以作为单药疗法进行，也可以与其他药物或额外的治疗措施结合使用。
• Novel Binder-Drug Conjugates (ADCs) and Use of Same
  申请人：Lerchen Hans-Georg

  公开号：US20140127240A1

  公开（公告）日：2014-05-08

  The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.

  本专利申请涉及针对表皮生长因子受体（EGFR，基因ID 1956）的新型结合物-药物共轭物（ADCs）N，N-二烷基月桂酰基蛋白酶抑制剂，这些ADCs的有效代谢物，生产这些ADCs的方法，利用这些ADCs治疗和/或预防疾病以及利用这些ADCs生产用于治疗和/或预防疾病的药物，特别是治疗高增殖和/或血管生成性疾病，如癌症。这种治疗可以作为单药疗法或与其他药物或其他治疗措施联合使用。
• NEW BINDER-DRUG CONJUGATES (ADCS) AND USE THEREOF
  申请人：Lerchen Hans-Georg

  公开号：US20130066055A1

  公开（公告）日：2013-03-14

  The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.

  本申请涉及针对C4.4a靶点的新结合物-药物共轭物（ADCs），以及这些ADCs的活性代谢物，制备这些ADCs的方法，使用这些ADCs治疗和/或预防疾病，以及使用这些ADCs生产治疗和/或预防疾病的药物，更具体地说是治疗和/或预防高增殖和/或血管生成性疾病，例如癌症等。这种治疗可以作为单独治疗，也可以与其他药物或进一步的治疗措施结合使用。
• N-CARBOXYALKYLAURISTATINS AND USE THEREOF
  申请人：Lerchen Hans-Georg

  公开号：US20140080763A1

  公开（公告）日：2014-03-20

  The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.

  本申请涉及新的衍生物，通过羧基烷基基团取代N末端的单甲基金刚烷E和单甲基金刚烷F，以及制备这些衍生物的方法，将这些衍生物用于治疗和/或预防疾病，以及将这些衍生物用于生产治疗和/或预防疾病的药物，更具体地说是治疗和/或预防高增殖和/或血管生成异常疾病，如癌症疾病等。这种治疗可以作为单一疗法，也可以与其他药物或进一步的治疗措施结合使用。
• NOVEL BINDER-DRUG CONJUGATES (ADCS) AND USE THEREOF
  申请人：SEATTLE GENETICS, INC.

  公开号：US20150030618A1

  公开（公告）日：2015-01-29

  The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.

  本申请涉及针对C4.4a靶点的新型N，N-二烷基月桂酰基链霉素结合物（ADCs），这些ADCs的活性代谢物，制备这些ADCs的方法，使用这些ADCs治疗和/或预防疾病，以及使用这些ADCs制造治疗和/或预防疾病的药物，特别是治疗和/或预防过度增殖和/或血管生成性疾病，例如癌症。这样的治疗可以作为单一疗法或与其他药物或进一步治疗措施结合使用。