(2S)-2-[(2S)-4-[(2E,4E,6R)-6-[(1S,3S,4S,5S,8S)-1,4-dimethylspiro[2,9-dioxabicyclo[3.3.1]non-6-ene-8,2'-oxirane]-3-yl]-4-methylhepta-2,4-dienoyl]-5-hydroxy-1-[(2S,5S,6S)-5-hydroxy-6-methyloxan-2-yl]-3-oxo-2H-pyrrol-2-yl]-N-methylpropanamide

• 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: (2S)-2-[(2S)-4-[(2E,4E,6R)-6-[(1S,3S,4S,5S,8S)-1,4-dimethylspiro[2,9-dioxabicyclo[3.3.1]non-6-ene-8,2'-oxirane]-3-yl]-4-methylhepta-2,4-dienoyl]-5-hydroxy-1-[(2S,5S,6S)-5-hydroxy-6-methyloxan-2-yl]-3-oxo-2H-pyrrol-2-yl]-N-methylpropanamide
• 化学式: C₃₂H₄₄N₂O₉
• 分子量: 600.7
• InChiKey: UEFVDAXLJNYMAZ-ONVRBHABSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  43
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.66
• 拓扑面积：
  147
• 氢给体数：
  3
• 氢受体数：
  10

文献信息

• [EN] PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS<br/>[FR] COMPOSÉS PHARMACEUTIQUES POUR LE TRAITEMENT DE TROUBLES MÉDIÉS PAR LE COMPLÉMENT
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2020198062A1

  公开（公告）日：2020-10-01

  This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl -mediated disorders.

  这份披露提供了用于治疗医学疾病的药物化合物，例如包括补体介导的疾病在内的补体Cl-介导的疾病。
• [EN] METHODS OF FOLDING A GRAFT COPOLYMER WITH DUAL ANTICANCER DRUGS AND RELATED APPLICATIONS<br/>[FR] PROCÉDÉS DE REPLIEMENT D'UN COPOLYMÈRE GREFFÉ PORTEUR D'UN DUO DE MÉDICAMENTS ANTICANCÉREUX, ET APPLICATIONS ASSOCIÉES
  申请人：UNIV NORTH CAROLINA STATE

  公开号：WO2015179402A1

  公开（公告）日：2015-11-26

  A graft copolymer having drug-containing side chains is described. The graft copolymer can be prepared, for example, by directly polymerizing a drug- containing monomer on multiple sites of a linear copolymer. When exposed to water, the graft copolymer can form uniform nanocarriers, e.g., nanomicelles, optionally encapsulating additional drugs, e.g., non-covalently in the interior of the nanocarriers, for coordinated drug delivery of a plurality of drugs. Also described herein is the use of the nanocarriers for delivery of therapeutic agents, particularly the dual delivery of chemotherapeutic agents to treat tumors.

  一种具有含药侧链的嫁接共聚物被描述。该嫁接共聚物可以通过在线性共聚物的多个位点上直接聚合含药单体来制备。当暴露在水中时，该嫁接共聚物可以形成均匀的纳米载体，例如纳米胶束，可选择地在纳米载体的内部非共价地封装额外的药物，以协调输送多种药物的药物传递。本文还描述了利用这些纳米载体输送治疗剂，特别是双重输送化疗剂以治疗肿瘤。
• [EN] CYCLIN-DEPENDENT KINASE INHIBITORS<br/>[FR] INHIBITEURS DE KINASES CYCLINE-DÉPENDANTES
  申请人：SPV THERAPEUTICS INC

  公开号：WO2020140055A1

  公开（公告）日：2020-07-02

  Described herein are compounds and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, methods of treatment, and medical uses. The compounds described herein are modulators of cyclin-dependent kinases, and are useful in the treatment or alleviation of protein kinase associated disorders, including cancer, infectious diseases, autoimmune diseases, or cardiovascular diseases.

  本文描述了化合物及其药用盐，以及它们的药物组合物，治疗方法和医疗用途。本文描述的化合物是细胞周期依赖性激酶的调节剂，并且在治疗或缓解蛋白激酶相关疾病方面具有用途，包括癌症，传染病，自身免疫疾病或心血管疾病。
• [EN] HYDROGEN PEROXIDE-ACTIVATED COMPOUNDS AS SELECTIVE ANTI-CANCER THERAPEUTICS<br/>[FR] COMPOSÉS ACTIVÉS PAR DU PEROXYDE D'HYDROGÈNE SERVANT D'AGENTS THÉRAPEUTIQUES ANTI-CANCÉREUX SÉLECTIFS
  申请人：UNIV CINCINNATI

  公开号：WO2016054486A1

  公开（公告）日：2016-04-07

  Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of hydrogen peroxide and are therefore selective anti-cancer therapeutics for cancers associated with elevated reactive oxygen species (ROS). Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.

  提供的是以下式I的化合物：式I的化合物在过氧化氢的存在下被激活，因此是针对与升高活性氧种（ROS）相关的癌症的选择性抗癌治疗剂。还提供了用于治疗与ROS增加相关的癌症的方法和药物组合物。
• Prodrugs containing novel bio-cleavable linkers
  申请人：Satyam Apparao

  公开号：US20060046967A1

  公开（公告）日：2006-03-02

  The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

  本发明提供了公式(I)的化合物或其药用可接受的盐。本发明还提供了包含一个或多个公式I的化合物或其中间体以及一个或多个药用可接受的载体、车辆或稀释剂的药物组合物。本发明进一步提供了包括制备方法和使用方法在内的前药，包括释放一氧化氮的前药、双前药和相互前药，由公式I的化合物组成。