N,N-bis(2-chloroethyl)-1-methylbenzimidazol-5-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: N,N-bis(2-chloroethyl)-1-methylbenzimidazol-5-amine
• 化学式: C₁₂H₁₅Cl₂N₃
• 分子量: 272.17
• InChiKey: DKLLQFHQWRIREA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  21.1
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] PLATINUM PRODRUGS AND METHODS OF MAKING AND USING THEREOF<br/>[FR] PROMÉDICAMENTS AU PLATINE ET PROCÉDÉS POUR LES PRÉPARER ET LES UTILISER
  申请人：UNIV GEORGIA

  公开号：WO2016144889A1

  公开（公告）日：2016-09-15

  Disclosed herein are prodrugs of platinum containing anticancer agents such as cisplatin that contain an alkylating moiety. Upon administration, the prodrugs release the platinum containing anticancer agent and the alkylating agent, which can form an adduct with DNA or can protect the platinum containing agent from removal. The disclosed prodrugs can be used to treat various cancers, including cisplatin resistant cancers.

  本文揭示了铂类抗癌药物（如顺铂）的前药，其中包含一种烷基化基团。在给药时，前药会释放出铂类抗癌药物和烷基化剂，这些剂可以与DNA形成加合物，或者可以保护铂类药物免受去除。揭示的前药可用于治疗各种癌症，包括顺铂耐药癌症。
• Platinum prodrugs and methods of making and using thereof
  申请人：UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.

  公开号：US10457700B2

  公开（公告）日：2019-10-29

  Disclosed herein are prodrugs of platinum containing anticancer agents such as cisplatin that contain an alkylating moiety. Upon administration, the prodrugs release the platinum containing anticancer agent and the alkylating agent, which can form an adduct with DNA or can protect the platinum containing agent from removal. The disclosed prodrugs can be used to treat various cancers, including cisplatin resistant cancers.

  本文公开了含有烷基化分子的含铂抗癌剂（如顺铂）的原药。给药时，原药释放出含铂抗癌剂和烷化剂，后者可与 DNA 形成加合物，或保护含铂抗癌剂不被移除。所公开的原药可用于治疗各种癌症，包括顺铂抗药性癌症。
• Bendamustine Formulations
  申请人：InnoPharma, Inc.

  公开号：US20140080880A1

  公开（公告）日：2014-03-20

  A lyophilized bendamustine composition consisting of bendamustine hydrochloride, an aqueous solvent, and optionally an excipient, and a method of preparation thereof for treating a condition in a subject are provided. The aqueous solvent includes, for example, water, an acid, a base, or a salt, etc. The excipient includes at least one cryoprotectant, for example, sucrose, trehalose, mannitol, etc. A pre-lyophilization bendamustine composition is lyophilized, for example, by freezing, primary drying, annealing, secondary drying, condensed cooling and evacuation at preset temperatures to obtain the lyophilized bendamustine composition as a cake, a powder, or a solid concentrate. The lyophilized bendamustine composition is free of a non-aqueous solvent. Reconstitution is performed by mixing the lyophilized bendamustine composition with an aqueous solvent for about 30 seconds to 300 seconds. The reconstituted bendamustine product containing about 0.2 wt % to about 2.5 wt % by weight of impurities is administered to the subject in need thereof.
• PARENTERAL COMPOSITIONS OF BENDAMUSTINE
  申请人：HETERO RESEARCH FOUNDATION

  公开号：US20160310598A1

  公开（公告）日：2016-10-27

  Described herein are parenteral compositions of bendamustine. More particularly, parenteral compositions of bendamustine are in the form of solution.
• PLATINUM PRODRUGS AND METHODS OF MAKING AND USING THEREOF
  申请人：UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.

  公开号：US20180044362A1

  公开（公告）日：2018-02-15

  Disclosed herein are prodrugs of platinum containing anticancer agents such as cisplatin that contain an alkylating moiety. Upon administration, the prodrugs release the platinum containing anticancer agent and the alkylating agent, which can form an adduct with DNA or can protect the platinum containing agent from removal. The disclosed prodrugs can be used to treat various cancers, including cisplatin resistant cancers.