5-(tert-butoxycarbonyl)aminopentyl isocyanate | 76197-74-5

• 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: 5-(tert-butoxycarbonyl)aminopentyl isocyanate
• 英文别名: 5-(t-BOC amino)-pentylisocyanate；5-t-Butoxycarbonylaminopentyl isocyanate；tert-butyl N-(5-isocyanatopentyl)carbamate
• CAS: 76197-74-5
• 化学式: C₁₁H₂₀N₂O₃
• 分子量: 228.291
• InChiKey: DZGYKHZDKXIPQL-UHFFFAOYSA-N

物化性质

• 沸点：
  336.2±25.0 °C(Predicted)
• 密度：
  1.02±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  16
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  67.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  methyl 3-(2-aminophenyl)acrylate 、 5-(tert-butoxycarbonyl)aminopentyl isocyanate 以 苯 为溶剂， 生成
  参考文献：
  名称：

  T-type Ca2+ channel blockers suppress the growth of human cancer cells

  摘要：

  In order to further clarify the role of T-type Ca2+ channels in cell proliferation, we have measured the growth inhibition of human cancer cells by using our potent T-type Ca2+ channel blockers. As a result, KYS05090, a most potent T-type Ca2+ channel blocker, was found to be as potent as doxorubicin against some human cancer cells without acute toxicity. Therefore, this letter provides the biological results that T-type calcium channel is important in regulating the important cellular phenotype transition leading to cell proliferation, and thus novel T-type Ca2+ channel blocker presents new prospects for cancer treatment. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.06.034

文献信息

• Compositions and methods for treating mast-cell mediated conditions
  申请人：AXYS Pharmaceuticals, Inc.

  公开号：US06022969A1

  公开（公告）日：2000-02-08

  Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.

  描述了用于预防和治疗由肥大细胞介导的炎症性疾病的新化合物、组合物和方法。这些化合物、组合物和方法对与呼吸道相关的炎症性疾病，如哮喘和过敏性鼻炎，以及其他类型的免疫介导性炎症性疾病，如类风湿性关节炎、结膜炎和炎症性肠病、各种皮肤病症，以及某些病毒性疾病具有预防和治疗作用。这些化合物包括对肥大细胞蛋白酶组胺酶的强效和选择性抑制剂。用于治疗这些疾病的组合物包括口服、吸入、局部和静脉制剂，以及包含这些制剂的装置。
• [EN] COMPOSITIONS AND METHODS FOR TREATING MAST-CELL INFLAMMATORY CONDITION<br/>[FR] COMPOSITIONS ET PROCEDES DE TRAITEMENT DE MALADIES INFLAMMATOIRES PROVOQUEES PAR LES MASTOCYTES
  申请人：ARRIS PHARMACEUTICAL CORPORATION

  公开号：WO1996009297A1

  公开（公告）日：1996-03-28

  (EN) Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.(FR) L'invention concerne de nouveaux composés, compositions et procédés efficaces pour la prévention et le traitement de maladies inflammatoires provoquées par les mastocytes. Ces composés, compositions et procédés sont efficaces pour la prévention et le traitement de maladies inflammatoires associées aux voies respiratoires, telles que l'asthme et la rhinite allergique, ainsi que d'autres types de maladies inflammatoires d'origine immune, telles que la polyarthrite rhumatoïde, la conjonctivite et les inflammations intestinales, différentes maladies dermatologiques, ainsi que certaines maladies virales. Les composés comprennent des inhibiteurs puissants et sélectifs de la protéase tryptase des mastocytes. Les compositions de traitement de ces maladies comprennent des préparations s'administrant par voie orale, nasale, locale ou parentérale, ainsi que des systèmes contenant lesdites préparations.

  新型化合物、组合物和方法被描述为有效预防和治疗由肥大细胞介导的炎症性疾病。这些化合物、组合物和方法对于预防和治疗与呼吸道相关的炎症性疾病，如哮喘和过敏性鼻炎，以及其他类型的免疫介导的炎症性疾病，如类风湿性关节炎、结膜炎和炎症性肠病、各种皮肤状况以及某些病毒性疾病都有效。这些化合物包括肥大细胞蛋白酶酶抑制剂，具有强效和选择性。治疗这些疾病的组合物包括口服、吸入、局部和静脉制剂以及包含这些制剂的设备。
• 5-Fluorouracil derivatives, and their pharmaceutical compositions
  申请人：Fujisawa Pharmaceutical Company, Ltd.

  公开号：US04349552A1

  公开（公告）日：1982-09-14

  A compound of the formula: ##STR1## wherein R is a bridged alicyclic group selected from the group consisting of norbornyl, norbornenyl, bicyclo[2,2,2]-heptyl and adamantyl optionally substituted by at least one substituent selected from the group consisting of lower alkyl, carboxy, lower alkoxycarbonyl, alkylidenedioxy, N,N-di(lower)alkylcarbamoyl, amino, loweralkoxycarbonylamino and halogen. The present compound is useful in the therapeutic treatment of cancer in human beings and animals.

  分子式为：##STR1## 其中R是从诺博烯基，诺博烯基，双环[2,2,2]-庚烷基和金刚烷基中选择的桥式脂环基，可以选择性地被至少一种取代基所取代，所述取代基选择自下列群体：低碳基，羧基，低碳基氧羰基，烷基二氧基，N，N-二（低）烷基氨基甲酰基，氨基，低碳基氧羰基氨基和卤素。该化合物在治疗人类和动物的癌症中有用。
• Amatoxin-Armed Therapeutic Cell Surface Binding Components Designed for Tumour Therapy
  申请人：Faulstich Heinz

  公开号：US20120100161A1

  公开（公告）日：2012-04-26

  The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of a toxin and a target-binding moiety, e.g. an antibody, which are useful in the treatment of cancer. In particular, the toxin is an amatoxin, and the target-binding moiety is preferably directed against tumour-associated antigens. In particular, the amatoxin is conjugated to the antibody by linker moieties. In particular the linker moieties are covalently bound to functional groups located in positions of the amatoxin proved as preferred positions for the attachment of linkers with respect to optimum antitumor activity. In a further aspect the invention relates to pharmaceutical compositions comprising such target-binding moiety toxin conjugates and to the use of such target-binding moiety toxin conjugates for the preparation of such pharmaceutical compositions. The target-binding moiety toxin conjugates and pharmaceutical compositions of the invention are useful for the treatment of cancer.

  本发明涉及肿瘤治疗。在一个方面，本发明涉及毒素和靶向结合基团（例如抗体）的共轭物，其在癌症治疗中有用。特别地，毒素是一种阿马毒素，靶向结合基团首选针对肿瘤相关抗原。特别地，阿马毒素通过连接基团与抗体结合。特别地，连接基团是共价结合到阿马毒素中被证明是最佳抗肿瘤活性的位置上的功能基团。在另一个方面，本发明涉及包括这样的靶向结合基团毒素共轭物的制药组合物，并且涉及使用这样的靶向结合基团毒素共轭物制备这样的制药组合物。本发明的靶向结合基团毒素共轭物和制药组合物对于肿瘤治疗有用。
• AMATOXIN-ARMED THERAPEUTIC CELL SURFACE BINDING COMPONENTS DESIGNED FOR TUMOUR THERAPY
  申请人：Deutsches Krebsforschungszentrum

  公开号：US20160089450A1

  公开（公告）日：2016-03-31

  The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of a toxin and a target-binding moiety, e.g. an antibody, which are useful in the treatment of cancer. In particular, the toxin is an amatoxin, and the target-binding moiety is preferably directed against tumour-associated antigens. In particular, the amatoxin is conjugated to the antibody by linker moieties. In particular the linker moieties are covalently bound to functional groups located in positions of the amatoxin proved as preferred positions for the attachment of linkers with respect to optimum antitumor activity. In a further aspect the invention relates to pharmaceutical compositions comprising such target-binding moiety toxin conjugates and to the use of such target-binding moiety toxin conjugates for the preparation of such pharmaceutical compositions. The target-binding moiety toxin conjugates and pharmaceutical compositions of the invention are useful for the treatment of cancer.

  本发明涉及肿瘤治疗。在一个方面，本发明涉及毒素和靶向结合基团（例如抗体）的共轭物，其在癌症治疗中有用。特别是，毒素是一种阿马毒素，而靶向结合基团最好是针对肿瘤相关抗原的。特别是，阿马毒素通过连接基团与抗体结合。特别是，连接基团是共价结合到阿马毒素中的位置的功能基团上的，这些位置被证明是连接剂与最佳抗肿瘤活性相关的首选位置。在另一个方面，本发明涉及包含这种靶向结合基团毒素共轭物的制药组合物，并且涉及使用这种靶向结合基团毒素共轭物制备这种制药组合物。本发明的靶向结合基团毒素共轭物和制药组合物可用于癌症治疗。