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4-cyano-3-methyl-1-phenyl-5-{3-(4-chlorobenzenesulfonyl)ureido}-(1H)-pyrazole

中文名称
——
中文别名
——
英文名称
4-cyano-3-methyl-1-phenyl-5-{3-(4-chlorobenzenesulfonyl)ureido}-(1H)-pyrazole
英文别名
SM-19712;SM19712 free acid;1-(4-chlorophenyl)sulfonyl-3-(4-cyano-5-methyl-2-phenylpyrazol-3-yl)urea
4-cyano-3-methyl-1-phenyl-5-{3-(4-chlorobenzenesulfonyl)ureido}-(1H)-pyrazole化学式
CAS
——
化学式
C18H14ClN5O3S
mdl
——
分子量
415.86
InChiKey
CWLFPWRNPQXWLD-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    3.7
  • 重原子数:
    28
  • 可旋转键数:
    4
  • 环数:
    3.0
  • sp3杂化的碳原子比例:
    0.06
  • 拓扑面积:
    125
  • 氢给体数:
    2
  • 氢受体数:
    5

文献信息

  • SULFONYLUREIDOPYRAZOLE DERIVATIVES
    申请人:SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
    公开号:EP0885890A1
    公开(公告)日:1998-12-23
    A sulfonylureidopyrazole derivative of formula (1) or (2) is disclosed. The derivative has an inhibitory activity on endothelin converting enzyme, and is useful for treating or preventing various cardiac failures, tracheal constrictions, nervous disorders, parasecretion, vascular disorders, various ulcers and the like.
    公开了一种化学式(1)或(2)的磺酰脲吡唑衍生物。该衍生物对内皮素转化酶具有抑制活性,可用于治疗或预防各种心脏衰竭、气管收缩、神经紊乱、副分泌、血管紊乱、各种溃疡等疾病。
  • 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。
  • Stabilized oral pharmaceutical composition
    申请人:——
    公开号:US20030105144A1
    公开(公告)日:2003-06-05
    An orally deliverable pharmaceutical composition is provided comprising an aminosulfonyl-comprising drug, for example a selective cyclooxygenase-2 inhibitory drug such as celecoxib, and a solvent liquid comprising a polyethylene glycol and one or more free radical-scavenging antioxidants. At least a substantial part of the drug is in dissolved form in the solvent liquid. The composition has rapid-onset properties and is useful in treatment of cyclooxygenase-2 mediated conditions and disorders.
    一种可口服给药的药物组合物由含氨磺酰的药物(例如塞来昔布等选择性环氧化酶-2抑制剂)和含聚乙二醇及一种或多种自由基清除抗氧化剂的溶剂液组成。至少有相当一部分药物以溶解形式存在于溶剂液中。该组合物具有快速起效的特性,可用于治疗环氧化酶-2 介导的病症和紊乱。
  • Oral dosage form of a sulfonamide prodrug
    申请人:——
    公开号:US20030100595A1
    公开(公告)日:2003-05-29
    A pharmaceutical composition that is substantially free of water comprises at least one orally deliverable dosage unit comprising a therapeutically effective amount of a sulfonamide prodrug and, where the prodrug is readily degradable ex vivo, has means to inhibit such degradation prior to oral administration. Illustratively the prodrug is parecoxib or a water-soluble salt thereof, and the composition has means to inhibit conversion of the parecoxib to valdecoxib. A method of treating or preventing a COX-2 mediated disorder in a subject comprises (a) dissolving at least one dosage unit of such a composition in a pharmaceutically acceptable aqueous vehicle to form a solution, and (b) orally administering the solution to the subject before substantial precipitation of insoluble matter occurs in the solution.
    一种基本上不含水的药物组合物包含至少一个口服给药剂量单位,其中含有治疗有效量的磺胺原药,如果原药在体内外容易降解,则在口服给药前具有抑制这种降解的方法。举例来说,原药是帕瑞昔布或其水溶性盐,组合物具有抑制帕瑞昔布转化为缬癸昔布的方法。一种治疗或预防受试者 COX-2 介导的疾病的方法包括:(a)将至少一个剂量单位的这种组合物溶解在药学上可接受的水性载体中以形成溶液,和(b)在溶液中出现大量不溶物沉淀之前将溶液口服给受试者。
  • Compounds with NEP/MP-inhibitory activity and uses thereof
    申请人:Solvay Pharmaceuticals GmbH
    公开号:US20040162345A1
    公开(公告)日:2004-08-19
    Compounds having combined, particularly concurrent, inhibitory activity on neutral endopeptidase (NEP) and on a novel metalloprotease designated IGS5, or of a pharmaceutically acceptable salt or solvate or biolabile ester thereof, and related methods for treating and for the manufacture of a pharmaceutical composition for a mammal, preferably a larger mammal such as a human, suffering from or being susceptible to a disease or condition which can be alleviated or inhibited by combined or concurrent inhibition of NEP and IGS5. Treatments for diseases or conditions where big-ET-1 levels are elevated, or where ET-1 is upregulated, where such diseases or conditions can be alleviated or inhibited by combined or concurrent inhibition of NEP and IGS5.
    对中性内肽酶(NEP)和一种被命名为IGS5的新型金属蛋白酶或其药学上可接受的盐或溶解物或生物可降解酯具有联合、特别是并发抑制活性的化合物,以及用于治疗和制造药物组合物的相关方法,该药物组合物用于哺乳动物,最好是较大的哺乳动物,如人类,患有或易患可通过联合或并发抑制NEP和IGS5而减轻或抑制的疾病或病症。治疗big-ET-1水平升高或ET-1上调的疾病或病症,这些疾病或病症可通过联合或同时抑制NEP和IGS5而减轻或抑制。
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