5-[(2RS)-2-cyclopropyl-7,8-dimethoxy-2H-chromen-5- ylmethyl]pyrimidine-2,4-diamine mesylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: 5-[(2RS)-2-cyclopropyl-7,8-dimethoxy-2H-chromen-5- ylmethyl]pyrimidine-2,4-diamine mesylate
• 英文别名: iclaprim mesylate；5-[(2-cyclopropyl-7,8-dimethoxy-2H-chromen-5-yl)methyl]pyrimidin-1-ium-2,4-diamine;methanesulfonate
• 化学式: (x)CH₄O₃S*C₁₉H₂₂N₄O₃
• 分子量: 450.5
• InChiKey: BQCQVDMEHSONNK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.94
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  168
• 氢给体数：
  3
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  甲烷磺酸 、 5-[(2-环丙基-7,8-二甲氧基-2H-色烯-5-基)甲基]嘧啶-2,4-二胺 以 乙醇 为溶剂， 以900 mg的产率得到5-[(2RS)-2-cyclopropyl-7,8-dimethoxy-2H-chromen-5- ylmethyl]pyrimidine-2,4-diamine mesylate
  参考文献：
  名称：

  [EN] CRYSTALLINE FORM OF ICLAPRIM MESYLATE
  [FR] FORME CRISTALLINE DE MÉSYLATE D'ICLAPRIM

  摘要：

  The present invention relates to a crystalline form of iclaprim mesylate and a process for its preparation. The invention also relates to a pharmaceutical composition comprising the crystalline form of iclaprim mesylate of the present invention, preferably in a predetermined and/or effective amount and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prophylaxis of bacterial infections caused by Gram positive bacteria.

  公开号：

  WO2020161284A1

文献信息

• Systems and methods for treating bacterial infection
  申请人：Motif BioSciences Inc.

  公开号：US10076522B2

  公开（公告）日：2018-09-18

  Therapeutic methods, kits, dosing regimens and uses as medicament are provided, for example, for the treatment of bacterial infection. The therapeutic methods can comprise intravenously administering to a subject who has a bacterial infection a pharmaceutical composition comprising a fixed amount of iclaprim. The administration of the fixed amount can achieve a Cmax(ss) below about 800 ng/mL, a T>MIC of between about 30% to about 95% and a ratio of AUC/MIC of about 20 to about 85, and the bacterial infection can be treated. The fixed amount can be about 70 mg to about 100 mg. The pharmaceutical composition can be infused into the subject about 1 to about 3 times a day daily over a time period of about 0.75 hours to about 4 hours.

  提供了治疗细菌感染的治疗方法、试剂盒、给药方案和药物用途等。治疗方法可包括向患有细菌感染的受试者静脉注射包含固定量iclaprim的药物组合物。固定量的给药可使Cmax(ss)低于约800纳克/毫升，T>MIC在约30%至约95%之间，AUC/MIC比值在约20至约85之间，细菌感染可得到治疗。定量可为约 70 毫克至约 100 毫克。该药物组合物可在约0.75小时至约4小时的时间段内每天向受试者输注约1至约3次。
• AQUEOUS PHARMACEUTICAL FORMULATION
  申请人：Acino Pharma AG

  公开号：EP2280688A1

  公开（公告）日：2011-02-09
• SYSTEMS AND METHODS FOR TREATING BACTERIAL INFECTION
  申请人：Motif Biosciences, Inc.

  公开号：EP3452042A1

  公开（公告）日：2019-03-13
• US7947293B2
  申请人：——

  公开号：US7947293B2

  公开（公告）日：2011-05-24
• [EN] MODIFIED FGF-23 POLYPEPTIDES AND THEIR USES<br/>[FR] POLYPEPTIDES FGF-23 MODIFIÉS ET LEURS UTILISATIONS
  申请人：AMBRX INC

  公开号：WO2009117622A2

  公开（公告）日：2009-09-24

  FGF-23 polypeptides comprising non-natural amino acids which may further be conjugated to a polymer or other moiety are disclosed.