(4R,5S)-4-Methyl-5-phenyl-3-propanoyl-oxazolidin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: (4R,5S)-4-Methyl-5-phenyl-3-propanoyl-oxazolidin-2-one
• 英文别名: 4-methyl-5-phenyl-3-propanoyl-1,3-oxazolidin-2-one
• 化学式: C₁₃H₁₅NO₃
• 分子量: 233.26
• InChiKey: ZMRFZBKROHCLIL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  三氟甲磺酸二丁硼 、 (4R,5S)-4-Methyl-5-phenyl-3-propanoyl-oxazolidin-2-one 生成 3-[(E)-1-dibutylboranyloxyprop-1-enyl]-4-methyl-5-phenyl-1,3-oxazolidin-2-one
  参考文献：
  名称：

  KINOSHITA, TAKUMI;MIYATA, MASAAKI;ISMAIL, SHAHNAZ M.;FUJIMOTO, YOSHINORI;+, CHEM. AND PHARM. BULL., 36,(1988) N 1, 134-141

  摘要：

  DOI：

文献信息

• [EN] COMPOSITION FOR THE TREATMENT OF IGF-1R EXPRESSING CANCER<br/>[FR] COMPOSITION POUR LE TRAITEMENT D'UN CANCER EXPRIMANT IGF-1R
  申请人：PF MEDICAMENT

  公开号：WO2017072196A1

  公开（公告）日：2017-05-04

  The present invention relates to a method for the treatment of IGF-IR expressing cancers as well as to a compositions and a kit for said traitment. From one aspect, the invention reates to the combined use of a first antibody for the determination of the IGF-IR status of a cancer and a second antibody used as an ADC for the treatment of said cancer.

  本发明涉及一种用于治疗表达IGF-IR的癌症的方法，以及用于所述治疗的组合物和试剂盒。从一方面来说，发明涉及第一抗体用于确定癌症的IGF-IR状态和第二抗体作为ADC用于治疗所述癌症的联合使用。
• [EN] CONJUGATION LINKERS, CELL BINDING MOLECULE-DRUG CONJUGATES CONTAINING THE LIKERS, METHODS OF MAKING AND USES SUCH CONJUGATES WITH THE LINKERS<br/>[FR] LIEURS DE CONJUGAISON, CONJUGUÉS MÉDICAMENT-MOLÉCULE DE LIAISON À UNE CELLULE CONTENANT LESDITS LIEURS, PROCÉDÉS DE PRÉPARATION ET D'UTILISATION DE TELS CONJUGUÉS AVEC LES LIEURS
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2018086139A1

  公开（公告）日：2018-05-17

  The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.

  本发明涉及具有丙炔基、取代丙烯酰（丙烯酰）或二取代丙酰基的连接剂，并使用这些连接剂将化合物，特别是细胞毒性药剂，与细胞结合分子结合。
• NEW EPOTHIOLONE DERIVATIVES, PROCESS FOR THEIR PRODUCTION, AND THEIR PHARMACEUTICAL USE
  申请人：KLAR Ulrich

  公开号：US20090018342A1

  公开（公告）日：2009-01-15

  This invention relates to the new epothilone derivatives of general formula I, in which substituents Y, Z, R 2a , R 2b , R 3 , R 4a , R 4b , D-E, R 5 , R 6 , R 7 , R 8 and X have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanomas, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (psoriasis, arthritis). To avoid uncontrolled proliferation of cells and for better compatibility of medical implants, they can be applied or introduced into polymer materials. The compounds according to the invention can be used alone or to achieve additive or synergistic actions in combination with other principles and classes of substances that can be used in tumor therapy.

  本发明涉及一般式I的新的环丙沙星衍生物，其中取代基Y、Z、R2a、R2b、R3、R4a、R4b、D-E、R5、R6、R7、R8和X的含义如说明中所示。这些新化合物通过稳定形成的微管来与微管蛋白相互作用。它们能够以特定的阶段影响细胞分裂，并适用于治疗恶性肿瘤，例如卵巢、胃、结肠、腺癌、乳腺、肺、头颈部癌症、恶性黑色素瘤、急性淋巴细胞性和髓细胞性白血病。此外，它们还适用于抗血管生成治疗以及治疗慢性炎症性疾病（如牛皮癣、关节炎）。为了避免细胞的无控制增殖和更好地兼容医学植入物，它们可以应用或引入到聚合物材料中。本发明的化合物可以单独使用或与其他用于肿瘤治疗的原则和类别的物质相结合以实现加成或协同作用。
• KIT COMPRISING IGF-1R ANTIBODY-DRUG-CONJUGATE AND ITS USE FOR THE TREATMENT OF CANCER
  申请人：PIERRE FABRE MEDICAMENT

  公开号：EP3498301A1

  公开（公告）日：2019-06-19

  The present invention relates to an antibody-drug-conjugate capable of binding IGF-1R. From one aspect, the invention relates to an antibody-drug-conjugate comprising an antibody capable of binding to IGF-1R, said antibody being conjugated to at least one drug selected from derivatives of dolastatin 10 and auristatins. The invention also comprises method of treatment and the use of said antibody-drug-conjugate for the treatment of cancer.

  本发明涉及一种能够结合 IGF-1R 的抗体-药物-轭合物。从一个方面来说，本发明涉及一种抗体-药物-轭合物，它包括一种能够与 IGF-1R 结合的抗体，所述抗体与至少一种选自多拉他汀 10 和曙红的衍生物的药物结合。本发明还包括治疗癌症的方法和使用所述抗体-药物共轭物的方法。
• ANTIBODY-DRUG-CONJUGATE AND ITS USE FOR THE TREATMENT OF CANCER
  申请人：PIERRE FABRE MEDICAMENT

  公开号：EP3607996A1

  公开（公告）日：2020-02-12

  The present invention relates to an antibody-drug-conjugate. From one aspect, the invention relates to an antibody-drug-conjugate comprising an antibody capable of binding to a Target, said antibody being conjugated to at least one drug selected from derivatives of dolastatin 10 and auristatins. The invention also comprises method of treatment and the use of said antibody-drug-conjugate for the treatment of cancer.

  本发明涉及一种抗体-药物共轭物。从一个方面来看，本发明涉及一种抗体-药物-共轭物，该抗体-药物-共轭物包含一种能够与靶标结合的抗体，所述抗体与至少一种选自多拉他汀 10 和曙红的衍生物的药物共轭。本发明还包括治疗癌症的方法和使用所述抗体-药物-共轭物的方法。