2,4-Dimethyl-6-(4-formamino-benzolsulfonylamino)-pyrimidin | 795-13-1

• 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: 2,4-Dimethyl-6-(4-formamino-benzolsulfonylamino)-pyrimidin
• 英文别名: 2,6-Dimethyl-4-(4-formamino-benzolsulfonylamino)-pyrimidin；N⁴-Formyl-sulfisomidine；N-(2,6-dimethyl-pyrimidin-4-yl)-4-formylamino-benzenesulfonamide；2,6-dimethyl-4-(4-formamido-phenylsulfonamido)-pyrimidine；N2-Formylsulfisomidine；N-[4-[(2,6-dimethylpyrimidin-4-yl)sulfamoyl]phenyl]formamide
• CAS: 795-13-1
• 化学式: C₁₃H₁₄N₄O₃S
• 分子量: 306.345
• InChiKey: LACNPVKUGFOYFW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  109
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Prodrugs containing novel bio-cleavable linkers
  申请人：Satyam Apparao

  公开号：US20060046967A1

  公开（公告）日：2006-03-02

  The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

  本发明提供了公式(I)的化合物或其药用可接受的盐。本发明还提供了包含一个或多个公式I的化合物或其中间体以及一个或多个药用可接受的载体、车辆或稀释剂的药物组合物。本发明进一步提供了包括制备方法和使用方法在内的前药，包括释放一氧化氮的前药、双前药和相互前药，由公式I的化合物组成。
• [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。
• PRODRUGS CONTAINING NOVEL BIO-CLEAVABLE LINKERS
  申请人：Satyam Apparao

  公开号：US20060205674A2

  公开（公告）日：2006-09-14

  Abstract of the Disclosure The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one or more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

  本发明提供了式（I）的化合物或其药学上可接受的盐。本发明还提供了包括式I的一个或多个化合物或其中间体以及一个或多个药学上可接受的载体、载体或稀释剂的制药组合物。本发明还提供了制备方法和使用方法，其中包括NO释放前药、双前药和相互前药的前药，包括式I的化合物。
• BIODEGRADABLE POLYMER - BIOACTIVE MOIETY CONJUGATES
  申请人：O'Shea Michael Shane

  公开号：US20110243884A1

  公开（公告）日：2011-10-06

  The invention relates to a biodegradable polymer comprising a plurality of releasable bioactive moieties, the releasable bioactive moieties being pendant from and covalently bonded to the biodegradable polymer backbone, wherein the biodegradable polymer backbone is formed from monomeric units that are each coupled via a biodegradable moiety, and wherein the bioactive moieties are capable of being released at a rate equal to or faster than the rate of biodegradation of the polymer backbone.

  该发明涉及一种可生物降解的聚合物，其包含多个可释放的生物活性基团，这些可释放的生物活性基团悬挂在并与可生物降解的聚合物主链上共价键合，其中可生物降解的聚合物主链由通过可生物降解基团耦合的单体单元形成，而生物活性基团能够以与聚合物主链的降解速率相等或更快的速率释放出来。