5-Hydroxy-N-tert-butyl-Δ³-pyrrolin-2-on | 55991-50-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯啉
• 英文名称: 5-Hydroxy-N-tert-butyl-Δ³-pyrrolin-2-on
• 英文别名: 1-tert-butyl-5-hydroxy-1,5-dihydro-pyrrol-2-one；1-tert-butyl-2-hydroxy-2H-pyrrol-5-one
• CAS: 55991-50-9
• 化学式: C₈H₁₃NO₂
• 分子量: 155.197
• InChiKey: IKJPTLXOXVRGDL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Substituted pyrimidine compounds, compositions and medicinal applications thereof
  申请人：JUBILANT BIOSYS LIMITED

  公开号：US10273224B2

  公开（公告）日：2019-04-30

  The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.

  本公开涉及式（I）的嘧啶化合物、其立体异构体、同系物、药学上可接受的盐、多晶型物、溶液和水合物。本公开还涉及这些嘧啶化合物的制备工艺以及含有这些化合物的药物组合物。本公开的化合物可用于治疗、预防或抑制由表皮生长因子受体（EGFR）家族激酶介导的疾病和紊乱。
• Cytotoxic peptides and conjugates thereof
  申请人：NOVARTIS AG

  公开号：US10787480B2

  公开（公告）日：2020-09-29

  Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.

  本文公开了如本文所述的式 (I) 的新型细胞毒性肽： 以及使用这种肽制造免疫结合剂（即抗体药物结合剂）的方法 本发明还描述了免疫结合剂（即抗体药物结合剂），其包含与抗原结合分子（如抗体）连接的这种新型细胞毒性肽；其中这种免疫结合剂可用于治疗细胞增殖性疾病。本发明进一步提供了包含这些免疫共轭物的药物组合物、包含这些免疫共轭物与治疗共用试剂的组合物，以及使用这些免疫共轭物和组合物治疗细胞增殖障碍的方法。
• Near-IR light-cleavable conjugates and conjugate precursors
  申请人：The United States of America, as represented by the Secretary, Department of Health and Human Services

  公开号：US10874739B2

  公开（公告）日：2020-12-29

  Embodiments of near-infrared light-cleavable heptamethine cyanine-based conjugates, particularly targeting agent-drug conjugates, according to Formula I and conjugate precursors are disclosed. The disclosed targeting agent-drug conjugates are useful for targeted delivery and release of a drug. Methods of making and using the conjugates and precursors also are disclosed.

  本发明公开了根据式 I 和共轭物前体的近红外光可裂解七亚甲基青基共轭物，特别是靶向制剂-药物共轭物的实施例。所公开的靶向药剂-药物共轭物可用于药物的靶向递送和释放。还公开了制造和使用这些共轭物和前体的方法。
• Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors
  申请人：NUVATION BIO INC.

  公开号：US11192900B2

  公开（公告）日：2021-12-07

  Novel bromodomain and extraterminal domain (BET) inhibitors contanining substituted 2-pyridones and therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.

  本研究提供了含有取代的 2-吡啶酮的新型溴结构域和外结构域（BET）抑制剂，以及使用这些新型 BET 抑制剂治疗病症和疾病的方法。
• Indoleamine 2,3-dioxygenase inhibitor, method for preparation and use thereof
  申请人：NANJING HUAWE MEDICINE TECHNOLOGY GROUP CO., LTD.

  公开号：US11214554B2

  公开（公告）日：2022-01-04

  A novel indoleamine 2,3-dioxygenase inhibitor and/or its pharmaceutically acceptable salts can used, in the preparation of a drug for indoleamine 2,3-dioxygenase (IDO) related diseases, such as cancer, Alzheimer's, depression, cataract, etc.

  一种新型吲哚胺-2,3-二氧化酶抑制剂和/或其药学上可接受的盐类可用于制备治疗吲哚胺-2,3-二氧化酶（IDO）相关疾病（如癌症、老年痴呆症、抑郁症、白内障等）的药物。