1-(3-oxobutyl)-2,5-dihydro-1H-pyrrole-2,5-dione | 1546506-43-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1-(3-oxobutyl)-2,5-dihydro-1H-pyrrole-2,5-dione
• 英文别名: 1-(3-oxobutyl)pyrrole-2,5-dione
• CAS: 1546506-43-7
• 化学式: C₈H₉NO₃
• 分子量: 167.16
• InChiKey: KJSBCHYZICJDPV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  54.4
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] SELECTIVE DRUG RELEASE FROM INTERNALIZED CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS<br/>[FR] LIBÉRATION SÉLECTIVE DE MÉDICAMENT À PARTIR DE CONJUGUÉS INTERNALISÉS DE COMPOSÉS BIOLOGIQUEMENT ACTIFS
  申请人：SEAGEN INC

  公开号：WO2021055865A1

  公开（公告）日：2021-03-25

  The invention relates to conjugates of biologically active compounds, wherein such a conjugate is comprised of a sequence of amino acids containing a tripeptide that confers selective cleavage by tumor tissue homogenate for release of free drug and/or improves biodistribution into the tumor tissue in comparison to normal tissue homogenate from the same species, wherein the normal tissue is the site of an adverse event associated with administration to a human subject in need thereof of a therapeutically effective amount of a comparator conjugate whose amino acid sequence is a dipeptide known to be selectively cleavable by Cathepsin B.

  该发明涉及生物活性化合物的缀合物，其中所述缀合物包含一个氨基酸序列，该序列包含一个三肽，该三肽能够通过肿瘤组织匀浆选择性裂解以释放自由药物和/或与同一物种的正常组织匀浆相比，改善了药物在肿瘤组织中的生物分布，其中所述正常组织是与向需要治疗的人体受试者施用治疗有效量的比较缀合物相关的不良事件的发生部位，该比较缀合物的氨基酸序列是已知可被组织蛋白酶B选择性裂解的二肽。
• [EN] COMPOSITIONS AND METHODS FOR INHIBITING PROTEIN EMBRYONIC ECTODERM DEVELOPMENT ACTIVITY AND TREATING DISEASE<br/>[FR] COMPOSITIONS ET PROCÉDÉS POUR L'INHIBITION DE L'ACTIVITÉ DE DÉVELOPPEMENT D'ECTODERME EMBRYONNAIRE DE PROTÉINE ET DE TRAITEMENT D'UNE MALADIE
  申请人：EXO THERAPEUTICS INC

  公开号：WO2021195183A1

  公开（公告）日：2021-09-30

  The invention provides compounds that are inhibitors of the protein embryonic ectoderm development (EED), pharmaceutical compositions, their use in modulating the activity of EED, and their use in the treatment of medical disorders, such as cancer. The invention further provides methods of treating medical disorders, such as cancer, and covalently modifying and/or modulating the activity of EED, using an agent that reacts with, and forms a covalent bond to, cysteine324 of EED.

  这项发明提供了抑制蛋白胚胎外胚层发育（EED）的化合物，药物组合物，它们在调节EED活性中的应用，以及它们在治疗癌症等医学疾病中的应用。该发明还提供了治疗医学疾病（如癌症）的方法，并利用一种与EED的半胱氨酸324发生反应并形成共价键的试剂，对EED进行共价修饰和/或调节活性。
• [EN] NEW TECHNOLOGY TO CONJUGATE THE TACCALONOLIDE MICROTUBULE STABILIZERS WITH LINKERS/PAYLOADS<br/>[FR] NOUVELLE TECHNOLOGIE POUR CONJUGUER LES STABILISATEURS TACCALONOLIDES DE MICROTUBULES AVEC DES LIEURS/CHARGES UTILES
  申请人：DU LIN

  公开号：WO2020185610A1

  公开（公告）日：2020-09-17

  The present disclosure is concerned with taccalonolide analogs and conjugated taccalonolide analogs useful as cellular probes and in the treatment of, for example, hyperproliferative disorders such as cardiovascular diseases and cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

  本公开涉及可用作细胞探针和用于治疗高增殖性疾病，如心血管疾病和癌症的塔卡龙内酯类似物和共轭塔卡龙内酯类似物。本摘要旨在作为在特定领域搜索的扫描工具，并不意味着对本发明的限制。
• ANTIBODY DRUG CONJUGATES (ADCS) AND ANTIBODY PRODRUG CONJUGATES (APDCS) WITH ENZYMATICALLY CLEAVABLE GROUPS
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：US20180169256A1

  公开（公告）日：2018-06-21

  The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.

  这项发明涉及新型结合物-前药偶联物（APDCs），其中结合物与动力蛋白纺锤体抑制剂的非活性前体化合物偶联，以及抗体药物偶联物ADCs以及制备这些APDCs和ADCs的方法。
• POTENT AND SELECTIVE INHIBITORS OF NAV1.7
  申请人：AMGEN INC

  公开号：US20160024159A1

  公开（公告）日：2016-01-28

  Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Na V 1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Na V 1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

  本文揭示了一种物质组合物，包括一种孤立的多肽，该多肽是一种外周限制的NaV1.7抑制剂。在一些公开的实施方式中，这种孤立的多肽是NaV1.7的抑制剂。其他实施方式是该物质组合物的共轭实施方式和含有该物质组合物的药物组合物。还揭示了编码一些创新多肽的孤立核酸和表达载体以及含有它们的重组宿主细胞。还揭示了一种治疗或预防疼痛的方法。