7-Benzofuranbutanamide, 2,3-dihydro-alpha-hydroxy-gamma,gamma-dimethyl-N-(4-methyl-1-oxo-1H-2,3-benzoxazin-6-yl)-alpha-(trifluoromethyl)-, (+)- | 669073-68-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: 7-Benzofuranbutanamide, 2,3-dihydro-alpha-hydroxy-gamma,gamma-dimethyl-N-(4-methyl-1-oxo-1H-2,3-benzoxazin-6-yl)-alpha-(trifluoromethyl)-, (+)-
• 英文别名: 4-(2,3-dihydro-1-benzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamide
• CAS: 669073-68-1
• 化学式: C₂₄H₂₃F₃N₂O₅
• 分子量: 476.4
• InChiKey: VRZVKIJRJRBQJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  97.2
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• IMMUNOABLATIVE THERAPIES
  申请人：AVM Biotechnology, LLC

  公开号：EP3488851A1

  公开（公告）日：2019-05-29

  This invention pertains to pharmaceutical compositions comprising a glucocorticoid for use in the treatment of diseases by immunoablation. The compositions of the invention may be for use in the treatment of diseases that are mediated by immune cells such as lymphocytes.

  本发明涉及包含糖皮质激素的药物组合物，用于通过免疫消融治疗疾病。本发明的组合物可用于治疗由淋巴细胞等免疫细胞介导的疾病。
• A GROUP OF CHIMERIC ANTIGEN RECEPTORS (CARS)
  申请人：St. Anna Kinderkrebsforschung

  公开号：EP3632461A1

  公开（公告）日：2020-04-08

  Disclosed is a group of chimeric antigen receptors (CARs) consisting of two, three or four CAR molecules, wherein the members of the group of CARs can be different or identical in their amino acid sequences to one another, and wherein each of the CAR molecules of the group comprise at least a transmembrane domain and an ectodomain comprising either an antigen binding moiety or a binding site to which another polypeptide is able to bind, wherein the another polypeptide comprises an antigen binding moiety; wherein each CAR molecule of the group comprises at least one dimerization domain, wherein this dimerization of a pair of dimerization domains is either induced by a regulating molecule and optionally reduced by another regulating molecule, or occurs in the absence of a regulating molecule and is reduced by a regulating molecule, and wherein the ectodomain of each CAR molecule of the group in its prevalent conformation is free of cysteine amino acid moieties which are able to form intermolecular disulphide bonds with other CAR molecules of the group, respectively, and wherein the antigen binding moieties of the CAR molecules of the group and of the other polypeptides being able to bind to the CAR molecules of the group are either specific for one target antigen or for a non-covalent or a covalent complex of different target antigens.

  公开了一组嵌合抗原受体（CAR），由两个、三个或四个 CAR 分子组成、 其中，该组 CAR 成员的氨基酸序列可以彼此不同或相同，以及 其中该组的每个 CAR 分子至少包括一个跨膜结构域和一个外结构域，该结构域包括抗原结合分子或另一种多肽可与之结合的结合位点，其中另一种多肽包括抗原结合分子； 其中该组的每个 CAR 分子包括至少一个二聚化结构域，一对二聚化结构域的这种二聚化或者由调节分子诱导并可选地被另一个调节分子降低，或者在没有调节分子的情况下发生并被调节分子降低，以及 其中，该组每个 CAR 分子的外结构域在其盛行构象中不含半胱氨酸氨基酸分子，而半胱氨酸氨基酸分子可分别与该组其他 CAR 分子形成分子间二硫键，以及 其中，该组 CAR 分子和能与该组 CAR 分子结合的其他多肽的抗原结合分子对一种靶抗原或不同靶抗原的非共价或共价复合物具有特异性。
• COMPOUNDS HAVING CASPASE INHIBITORY ACTIVITY, PHARMACEUTICAL AGENT CONTAINING SAID COMPOUNDS AND FOR TREATING OR PREVENTING CORNEAL ENDOTHELIAL SYMPTOMS, DISORDERS, OR DISEASES, AND APPLICATION OF SAID PHARMACEUTICAL AGENT
  申请人：The Doshisha

  公开号：EP3639855A1

  公开（公告）日：2020-04-22

  The present invention provides a composition for treating or preventing corneal endothelial symptoms, disorders, or diseases that are attributed to TGF-β signaling in corneal endothelial cells. Provided by the present invention is a composition that includes a compound and that is for treating or preventing endothelial symptoms, disorders, or diseases, wherein, when the compound comes into contact with immortalized cells of Fuchs' corneal endothelial dystrophy, (i) said immortalized cells exhibit a cell survival rate (%) of approximately 90% or more after being cultured for 24-28 hours in Dulbecco's modified Eagle medium (DMEM) + 2% fetal bovine serum (FBS) + 1% penicillin/streptomycin (P/S), and (ii) the ratio of caspase 3/7 activity (%) in the presence of TGF-β with respect to said cellular survival rate (%) is at most 0.8 after being cultured for 24-28 hours in Dulbecco's modified Eagle medium (DMEM) + 2% fetal bovine serum (FBS) + 1% penicillin/streptomycin (P/S).

  本发明提供了一种用于治疗或预防角膜内皮症状、失调或疾病的组合物，这些症状、失调或疾病归因于角膜内皮细胞中的TGF-β信号传导。本发明提供了一种包含化合物的组合物，该组合物用于治疗或预防内皮症状、紊乱或疾病，其中，当该化合物与福氏角膜内皮营养不良症的永生化细胞接触时、(i) 在杜氏改良鹰培养基（DMEM）+2% 胎牛血清（FBS）+1% 青霉素/链霉素（P/S）中培养 24-28 小时后，所述永生化细胞表现出约 90% 或以上的细胞存活率（%），以及 (ii) 在 TGF-β 存在下，caspase 3/7 活性（%）与所述细胞存活率（%）之比至多为 0.在杜氏改良老鹰培养基（DMEM）+2% 胎牛血清（FBS）+1% 青霉素/链霉素（P/S）中培养 24-28 小时后，细胞存活率（%）最多为 0.8。
• Replacement of cytotoxic preconditioning before cellular immunotherapy
  申请人：AVM BIOTECHNOLOGY, LLC

  公开号：US11219628B2

  公开（公告）日：2022-01-11

  Provided herein are novel therapeutic compositions and methods that keep cellular immunotherapies in the circulation or at the site of injection for extended periods of time without resorting to the use of cytotoxic preconditioning. For example, the compositions and methods herein lymphodeplete and reduce or ablate sites in the secondary lymphatics where the cellular immunotherapy is bound and sequestered, without the use of cytotoxic preconditioning.

  本文提供的新型治疗组合物和方法可在不使用细胞毒性预处理的情况下，使细胞免疫疗法在循环中或注射部位保持较长时间。例如，本发明的组合物和方法可在不使用细胞毒性预处理的情况下，使细胞免疫疗法在次级淋巴管中的结合和螯合部位发生淋巴清除、减少或消融。
• REPLACEMENT OF CYTOTOXIC PRECONDITIONING BEFORE CELLULAR IMMUNOTHERAPY
  申请人：AVM Biotechnology, LLC

  公开号：EP3490605A1

  公开（公告）日：2019-06-05