(3Z)-6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (3Z)-6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid
• 化学式: C₁₈H₁₄N₄O₅S
• 分子量: 398.4
• InChiKey: OQANPHBRHBJGNZ-BKUYFWCQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  146
• 氢给体数：
  3
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  (R)-3-环己烯甲酸 、 三甲基溴硅烷 、 N,N-二异丙基乙胺 、 (3Z)-6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid 、 以 二甲基亚砜 为溶剂， 以, 31, 987 (1990)] to give a white solid, (2.13 g, 57%)的产率得到依度沙班杂质80
  参考文献：
  名称：

  Compounds

  摘要：

  环己烷和环己烯衍生物及其药学上可接受的衍生物在哺乳动物中，特别是人类中用于治疗细菌感染的方法中具有用途。

  公开号：

  US20060189604A1
• 作为产物：
  描述：

  柳氮磺吡啶 、 6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid 生成 (3Z)-6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid
  参考文献：
  名称：

  DRUG DEPOTS FOR TREATMENT OF PAIN AND INFLAMMATION IN SINUS AND NASAL CAVITIES OR CARDIAC TISSUE

  摘要：

  提供有效的疼痛和/或炎症治疗。通过在心脏组织附近或鼻腔或鼻窦内植入可生物降解的药物沉积膜、贴片、条或海绵，可以减轻、预防或治疗疼痛和/或炎症。

  公开号：

  US20100239632A1

文献信息

• HIGH PENETRATION PRODRUG COMPOSITIONS OF ANTIMICROBIALS AND ANTIMICROBIAL-RELATED COMPOUNDS
  申请人：Yu Chongxi

  公开号：US20100040548A1

  公开（公告）日：2010-02-18

  The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

  该发明提供了一种新型高渗透性复合物（HPC）或高渗透性前药（HPP）的组合物，包括抗微生物和抗微生物相关化合物，这些化合物能够以高渗透效率穿越生物屏障。HPP能够在穿越生物屏障后转化为母药活性药物或药物代谢物，从而可以治疗母药或代谢物所能治疗的疾病。此外，HPP能够到达母药可能无法进入或在目标区域获得足够浓度的区域，从而提供新的治疗方法。HPP可以通过各种给药途径向受试者施用，例如，局部给药到病情作用部位以高浓度，或者系统给药到生物体内并以更快速度进入全身循环。
• [EN] PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION CONTAINING SULFASALAZINE AND / OR A SULFASALAZINE ORGANIC SALT, PRODUCTION PROCESS AND USE<br/>[FR] COMPOSITION PHARMACEUTIQUE POUR ADMINISTRATION ORALE CONTENANT DE LA SULFASALAZINE ET/OU UN SEL ORGANIQUE DE SULFASALAZINE, PROCÉDÉ DE PRODUCTION ET UTILISATION
  申请人：MEDAC GES FUER KLINISCHE SPEZIALPRAEPARATE MBH

  公开号：WO2019101904A1

  公开（公告）日：2019-05-31

  The present invention relates to a new pharmaceutical composition for oral administration containing sulfasalazine and/or a sulfasalazine organic salt, production processes and uses,in particular in the treatment of a disease or condition in which modulation of inflammatory cells is beneficial, a disease or condition concerning bones or joints and/or the gastro-intestinal tract.

  本发明涉及一种新的口服药物组合物，含有磺胺嘧啶和/或磺胺嘧啶有机盐，生产工艺和用途，特别是在调节炎症细胞对益处的疾病或病况中，涉及骨骼或关节和/或胃肠道的疾病或病况的治疗。
• [EN] SULFASALAZINE SALTS, PRODUCTION PROCESSES AND USES<br/>[FR] SELS DE SULFASALAZINE, PROCÉDÉS DE PRODUCTION ET UTILISATIONS
  申请人：MEDAC GES FUER KLINISCHE SPEZIALPRAEPARATE MBH

  公开号：WO2019101903A1

  公开（公告）日：2019-05-31

  The present invention relates to new crystal salt forms of sulfasalazine, in particular crystal Form A of the D(-)-N-methylglucamine (meglumine) salt of sulfasalazine (see Figure 1), crystal form A of the piperazine salt of sulfasalazine (see Figure 2) and crystal Form B of the diethylamine salt of sulfasalazine (see Figure 4), which can be obtained by use of the inventive preparation pro- cess, a pharmaceutical composition comprising one or more of the inventive crystal salt forms in particular in the treatment of a disease or condition in which modulation of inflammatory cells is beneficial, a disease or condition concerning bones or joints and/or the gastro-intestinal tract.

  本发明涉及磺胺嘧啶的新晶体盐形式，特别是D(-)-N-甲基葡萄糖胺（美格胺）盐晶型A（见图1），磺胺嘧啶的哌嗪盐晶型A（见图2）和磺胺嘧啶的二乙胺盐晶型B（见图4），可以通过使用本发明的制备过程获得，包括一种药物组合物，该组合物包括本发明的一种或多种晶体盐形式，特别用于治疗炎症细胞调节有益的疾病或病况，涉及骨骼或关节和/或胃肠道的疾病或病况。
• [EN] PHARMACEUTICAL COMPOSITIONS WITH IMPROVED DISSOLUTION<br/>[FR] COMPOSITIONS PHARMACEUTIQUES A DISSOLUTION AMELIOREE
  申请人：TRANSFORM PHARMACEUTICALS INC

  公开号：WO2004000284A1

  公开（公告）日：2003-12-31

  The invention relates to methods of screening mixtures containing a pharmaceutical compound an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a recrystallization/precipitation retardant and an optional enhancer.

  本发明涉及筛选包含药物化合物和赋形剂的混合物的方法，以识别延缓固态成核的药物化合物/赋形剂组合的特性。该发明还涉及通过将药物与再结晶/沉淀抑制剂和可选增效剂结合，来增加低溶解度药物在胃液条件下的溶解度、溶出性和生物利用度。
• Pharmaceutical compositions with improved dissolution
  申请人：Tawa Mark

  公开号：US20060134198A1

  公开（公告）日：2006-06-22

  The invention relates to methods of screening mixtures containing a pharmaceutical compound and an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a precipitation retardant and an optional enhancer.

  本发明涉及筛选混合物的方法，该混合物含有药物化合物和赋形剂，以识别药物化合物/赋形剂组合的性质，以延缓固态成核。本发明还涉及通过将药物与沉淀抑制剂和可选增效剂结合，在胃液条件下增加低溶解度药物的溶解度、溶出度和生物利用度的方法。