hydrochloride salt of 7-chloro-3-methyl-2-H-1,2,4-benzothiadiazine | 1098065-89-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻二嗪
• 英文名称: hydrochloride salt of 7-chloro-3-methyl-2-H-1,2,4-benzothiadiazine
• 英文别名: 7-chloro-3-methyl-4H-1lambda6,2,4-benzothiadiazine 1,1-dioxide;hydrochloride；7-chloro-3-methyl-4H-1λ6,2,4-benzothiadiazine 1,1-dioxide;hydrochloride
• CAS: 1098065-89-4
• 化学式: C₈H₇ClN₂O₂S*ClH
• 分子量: 267.136
• InChiKey: XOMXSKMQTHTAKJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.29
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  66.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  氯甲苯噻嗪 在 盐酸 作用下， 以 乙醚 为溶剂， 生成 hydrochloride salt of 7-chloro-3-methyl-2-H-1,2,4-benzothiadiazine
  参考文献：
  名称：

  Pharmaceutical formulations of potassium ATP channel openers and uses thereof

  摘要：

  本发明提供了立即或长期给予某些钾ATP（KATP）通道开放剂给受试者，以实现治疗涉及KATP通道的疾病或病症的新型药效学、药代动力学、治疗、生理、代谢和组成成果。还提供了制药配方、给药方法和剂量，以实现这些成果并减少治疗个体中不良反应的发生率。此外，还提供了联合给予KATP通道开放剂与其他药物治疗人类和动物疾病的方法。

  公开号：

  US20060051418A1

文献信息

• SALTS OF POTASSIUM ATP CHANNEL OPENERS AND USES THEREOF
  申请人：Cowen Neil M.

  公开号：US20120238554A1

  公开（公告）日：2012-09-20

  Provided are immediate or prolonged administration of certain salts of K ATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving K ATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

  提供了对KATP通道开放剂的某些盐，如重组胰岛素受体激动剂二甲基硫環氧化物的即时或长期给药，以实现治疗涉及KATP通道的疾病或病状的新型药效学、药代动力学、治疗、生理、代谢和组成结果。还提供了制药配方、给药方法和剂量，以实现这些结果并减少治疗个体的不良反应发生率。此外，还提供了共同给药这些盐与其他药物治疗人类和动物疾病的方法。
• Salts of potassium ATP channel openers and uses thereof
  申请人：Essentialis, Inc.

  公开号：EP2404604A1

  公开（公告）日：2012-01-11

  Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

  本发明提供了对受试者立即或长期施用 KATP 通道开放剂（如二氮氧）的某些盐类，以在治疗涉及 KATP 通道的疾病或病症时实现新的药效学、药代动力学、治疗学、生理学、新陈代谢和成分结果。此外，还提供了盐类的药物制剂、给药方法和剂量，这些制剂、给药方法和剂量可实现这些结果，并降低受治疗者不良反应的发生率。此外，还提供了将盐类与其他药物联合给药以治疗人类和动物疾病的方法。
• Methods for treating subjects with prader-willi syndrome or smith-magenis syndrome
  申请人：Essentialis, Inc.

  公开号：US10058557B2

  公开（公告）日：2018-08-28

  Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers, optionally in combination with growth hormone, to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are methods of co-administering KATP channel openers with other drugs (e.g., in combination with growth hormone) to treat diseases of humans and animals (e.g., Prader-Willi Syndrome (PWS), Smith-Magenis syndrome (SMS), and the like.

  本发明提供了对受试者立即或长期施用某些钾 ATP（KATP）通道开放剂（可选择与生长激素联合施用）的方法，以在治疗涉及 KATP 通道的疾病或病症时实现新的药效学、药代动力学、治疗学、生理学、代谢和成分结果。此外，还提供了 KATP 通道开放剂的药物制剂、给药方法和剂量，这些药物制剂、给药方法和剂量可实现这些结果，并降低受治疗者不良反应的发生率。此外，还提供了将 KATP 通道开放剂与其他药物（如与生长激素联合使用）共同施用以治疗人类和动物疾病（如普拉德-威利综合征（PWS）、史密斯-马吉尼斯综合征（SMS）等）的方法。
• Methods for treating subjects with Prader-Willi syndrome or Smith-Magenis syndrome
  申请人：Essentialis, Inc.

  公开号：US10456408B2

  公开（公告）日：2019-10-29

  Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers, optionally in combination with growth hormone, to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are methods of co-administering KATP channel openers with other drugs (e.g., in combination with growth hormone) to treat diseases of humans and animals (e.g., Prader-Willi Syndrome (PWS), Smith-Magenis syndrome (SMS), and the like.

  本发明提供了对受试者立即或长期施用某些钾 ATP（KATP）通道开放剂（可选择与生长激素联合施用）的方法，以在治疗涉及 KATP 通道的疾病或病症时实现新的药效学、药代动力学、治疗学、生理学、代谢和成分结果。此外，还提供了 KATP 通道开放剂的药物制剂、给药方法和剂量，这些药物制剂、给药方法和剂量可实现这些结果，并降低受治疗者不良反应的发生率。此外，还提供了将 KATP 通道开放剂与其他药物（如与生长激素联合使用）共同施用以治疗人类和动物疾病（如普拉德-威利综合征（PWS）、史密斯-马吉尼斯综合征（SMS）等）的方法。
• Compositions and methods for ophthalmic and/or other applications
  申请人：The Johns Hopkins University

  公开号：US10945948B2

  公开（公告）日：2021-03-16

  Particles, compositions, and methods that aid particle transport in mucus are provided. The particles, compositions, and methods may be used, in some instances, for ophthalmic and/or other applications. In some embodiments, the compositions and methods may involve modifying the surface coatings of particles, such as particles of pharmaceutical agents that have a low aqueous solubility. Such compositions and methods can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for ophthalmic applications, and may be used for delivering pharmaceutical agents to the front of the eye and/or the back of the eye.

  本文提供了有助于颗粒在粘液中传输的颗粒、组合物和方法。这些微粒、组合物和方法在某些情况下可用于眼科和/或其他应用。在某些实施方案中，这些组合物和方法可能涉及颗粒表面涂层的改性，例如水溶性较低的药剂颗粒。此类组合物和方法可用于实现药剂颗粒通过体内粘液屏障的高效运输，应用范围广泛，包括药物输送、成像和诊断应用。在某些实施方案中，包括此类微粒的药物组合物非常适合眼科应用，可用于将药剂输送到眼球前部和/或眼球后部。