(S)-Camazepam | 102818-70-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: (S)-Camazepam
• 英文别名: [(3S)-7-chloro-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl] N,N-dimethylcarbamate
• CAS: 102818-70-2
• 化学式: C₁₉H₁₈ClN₃O₃
• 分子量: 371.8
• InChiKey: PXBVEXGRHZFEOF-KRWDZBQOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  62.2
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] TRIAZOLOBENZAZEPINES AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] TRIAZOLOBENZAZÉPINES UTILISÉES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
  申请人：RICHTER GEDEON NYRT

  公开号：WO2019116324A1

  公开（公告）日：2019-06-20

  The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

  本发明涉及一般式(I)的5,6-二氢-4H-[1,2,4]三唑并[4,3-a][1]苯并蒽啉衍生物和/或其盐和/或其几何异构体和/或其立体异构体和/或其对映异构体和/或其消旋体和/或其非对映异构体和/或其生物活性代谢物和/或其前药和/或其溶剂化合物和/或其水合物和/或其多晶形式，这些化合物是中枢和/或外周作用的V1a受体调节剂，特别是V1a受体拮抗剂。本发明的另一个主题是制备这些化合物的过程以及制备过程的中间体。该发明还涉及含有这些化合物或与一个或多个其他活性物质一起的药物组合物，以及在治疗和/或预防与V1a受体功能相关的疾病或症状中的用途。
• Oral pharmaceutical compositions containing cyclodextrins as taste masking agent
  申请人：——

  公开号：US20040115258A1

  公开（公告）日：2004-06-17

  The application discloses oral pharmaceutical compositions which are tasted in the mouth during administration. Fast-dissolving tablets, chewable tablets and effervescent dispersions are exemplified. To mask the taste of unpleasant-tasting active ingredients, it has been found that blending with cyclodextrin without the conventional complex formation is effective. Consequently more economical modes of manufacture such as simple granulation and dry blending can be used.

  该申请揭示了口服制剂，其在给药过程中在口腔中被品尝。快速溶解片剂、可咀嚼片剂和泡腾分散剂是示例。为了掩盖令人不愉快的活性成分的味道，发现与β-环糊精混合而无需传统的复合形成是有效的。因此，可以使用更经济的制造方式，如简单的制粒和干混合。
• [EN] TRICYCLIC COMPOUNDS AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS TRICYCLIQUES UTILISÉS EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
  申请人：RICHTER GEDEON NYRT

  公开号：WO2019116325A1

  公开（公告）日：2019-06-20

  The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

  本发明涉及通式（I）的5,6-二氢-4H-[1,2,4]三唑[4,3-a][1]苯并蒽啉衍生物和/或其盐和/或其几何异构体和/或其立体异构体和/或其对映异构体和/或其消旋体和/或其二对映异构体和/或其生物活性代谢物和/或其前药和/或其溶剂化合物和/或其水合物和/或其多晶型，这些化合物是中枢和/或外周作用V1a受体调节剂，特别是V1a受体拮抗剂。本发明的另一个主题是化合物的制备方法以及制备过程的中间体。该发明还涉及含有这些化合物或与一个或多个其他活性物质一起的药物组合物，以及在治疗和/或预防与V1a受体功能相关的疾病或症状中的使用。
• [EN] METHODS OF TREATING ABNORMAL MUSCULAR ACTIVITY<br/>[FR] MÉTHODES DE TRAITEMENT D'UNE ACTIVITÉ MUSCULAIRE ANORMALE
  申请人：AUSPEX PHARMACEUTICALS INC

  公开号：WO2015077520A1

  公开（公告）日：2015-05-28

  Methods for treating abnormal muscular activity are disclosed. The methods may be performed remotely and permit monitoring of a subject outside a healthcare provider's office.

  披露了治疗异常肌肉活动的方法。这些方法可以远程执行，并允许在医疗提供者办公室之外监测受试者。
• [EN] BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2<br/>[FR] INHIBITEURS BENZOQUINOLINE DU TRANSPORTEUR DE MONOAMINE VÉSICULAIRE 2
  申请人：AUSPEX PHARMACEUTICALS INC

  公开号：WO2015077521A1

  公开（公告）日：2015-05-28

  The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof. (I)

  本发明涉及新的囊泡单胺转运体2（VMAT2）的苯并喹啉抑制剂，其药物组合物以及使用方法。