9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one;dihydrochloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one;dihydrochloride
• 化学式: C18H21Cl2N3O
• 分子量: 366.3
• InChiKey: JJIHADPISHURTP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.97
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  39.8
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• ONDANSETRON EXTENDED RELEASE SOLID DOSAGE FORMS FOR TREATING EITHER NAUSEA, VOMITING OR DIARRHEA SYMPTOMS
  申请人：RedHill Biopharma Ltd.

  公开号：US20150258029A1

  公开（公告）日：2015-09-17

  A method of treating a patient comprises orally administering a solid oral dosage form comprising a core comprising a non-ionic polymer matrix, a first amount of ondansetron dispersed within the matrix, and a salt dispersed within the matrix, wherein the first amount of ondansetron ranges from about 9 mg to about 28 mg; a first seal coat surrounding the core, wherein the first seal coat is comprised of a non-ionic polymer matrix; and an immediate release drug layer surrounding the first seal coat and comprising a non-ionic polymer and a second amount of ondansetron dispersed therein, wherein the second amount of ondansetron ranges from about 3 mg to about 8 mg, wherein release of ondansetron from the solid oral dosage form provides exposure to ondansetron for a minimum period of 16 hours so as to result in a reduction in frequency of vomiting, nausea, diarrhea, or a combination thereof.

  一种治疗患者的方法包括口服固体口服剂型，该剂型包括核心，其中包括非离子聚合物基质、分散在基质中的第一量奥替酸片剂，以及分散在基质中的盐，其中第一量奥替酸片剂的范围为约9毫克至约28毫克；第一密封层包围核心，其中第一密封层由非离子聚合物基质组成；以及立即释放药物层包围第一密封层，其中包括非离子聚合物和分散在其中的第二量奥替酸片剂，第二量奥替酸片剂的范围为约3毫克至约8毫克，其中奥替酸片剂从固体口服剂型中释放，提供至少16小时的奥替酸曝露时间，以减少呕吐、恶心、腹泻或其组合的发生频率。
• Compositions, methods and kits for treating diarrhea-predominant irritable bowel syndrome
  申请人：RedHill Biopharma Ltd.

  公开号：US10668050B2

  公开（公告）日：2020-06-02

  A method of treating a patient comprises orally administering a solid oral dosage form comprising a core comprising a non-ionic polymer matrix, a first amount of ondansetron dispersed within the matrix, and a salt dispersed within the matrix, wherein the first amount of ondansetron ranges from about 9 mg to about 28 mg; a first seal coat surrounding the core, wherein the first seal coat is comprised of a non-ionic polymer matrix; and an immediate release drug layer surrounding the first seal coat and comprising a non-ionic polymer and a second amount of ondansetron dispersed therein, wherein the second amount of ondansetron ranges from about 3 mg to about 8 mg, wherein release of ondansetron from the solid oral dosage form provides exposure to ondansetron for a minimum period of 16 hours so as to result in a reduction in frequency of vomiting, nausea, diarrhea, or a combination thereof.

  一种治疗患者的方法包括口服固体口服剂型，该剂型包括由非离子聚合物基质组成的核心、分散在基质中的第一量昂丹司琼和分散在基质中的盐，其中第一量昂丹司琼的范围为约9毫克至约28毫克；围绕核心的第一密封涂层，其中第一密封涂层由非离子聚合物基质组成；其中第二量的昂丹司琼约为 3 毫克至约 8 毫克，其中昂丹司琼从固体口服剂型中的释放使昂丹司琼的暴露时间至少为 16 小时，从而降低呕吐、恶心、腹泻或其组合的频率。
• METHODS FOR TREATING DIARRHEA PREDOMINANT IRRITABLE BOWEL SYNDROME
  申请人：RedHill Biopharma Ltd.

  公开号：US20200253933A1

  公开（公告）日：2020-08-13

  A method of treating a patient comprises orally administering a solid oral dosage form comprising a core comprising a non-ionic polymer matrix, a first amount of ondansetron dispersed within the matrix, and a salt dispersed within the matrix, wherein the first amount of ondansetron ranges from about 9 mg to about 28 mg; a first seal coat surrounding the core, wherein the first seal coat is comprised of a non-ionic polymer matrix; and an immediate release drug layer surrounding the first seal coat and comprising a non-ionic polymer and a second amount of ondansetron dispersed therein, wherein the second amount of ondansetron ranges from about 3 mg to about 8 mg, wherein release of ondansetron from the solid oral dosage form provides exposure to ondansetron for a minimum period of 16 hours so as to result in a reduction in frequency of vomiting, nausea, diarrhea, or a combination thereof.
• US9675588B2
  申请人：——

  公开号：US9675588B2

  公开（公告）日：2017-06-13
• [EN] ONDANSETRON EXTENDED RELEASE SOLID DOSAGE FORMS FOR TREATING EITHER NAUSEA, VOMITING OR DIARRHEA SYMPTOMS<br/>[FR] FORMES GALÉNIQUES SOLIDES À LIBÉRATION PROLONGÉE DE L'ONDANSÉTRON UTILISABLES EN VUE DU TRAITEMENT DES NAUSÉES, DES VOMISSEMENTS OU DE LA DIARRHÉE
  申请人：REDHILL BIOPHARMA LTD

  公开号：WO2015136377A2

  公开（公告）日：2015-09-17

  A method of treating a patient comprises orally administering a solid oral dosage form comprising a core comprising a non-ionic polymer matrix, a first amount of ondansetron dispersed within the matrix, and a salt dispersed within the matrix, wherein the first amount of ondansetron ranges from about 9 mg to about 28 mg; a first seal coat surrounding the core, wherein the first seal coat is comprised of a non-ionic polymer matrix; and an immediate release drug layer surrounding the first seal coat and comprising a non-ionic polymer and a second amount of ondansetron dispersed therein, wherein the second amount of ondansetron ranges from about 3 mg to about 8 mg, wherein release of ondansetron from the solid oral dosage form provides exposure to ondansetron for a minimum period of 16 hours so as to result in a reduction in frequency of vomiting, nausea, diarrhea, or a combination thereof.