3,4-diamino-1-phenyl-1H-pyrazole | 701917-05-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3,4-diamino-1-phenyl-1H-pyrazole
• 英文别名: 1-phenylpyrazole-3,4-diamine
• CAS: 701917-05-7
• 化学式: C₉H₁₀N₄
• 分子量: 174.205
• InChiKey: NAPYLWNTEWCCQN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  69.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1’-氧代-螺[环己基-1,3’(1’H)-呋喃并[3,4-c]吡啶]-4-羧酸 、 3,4-diamino-1-phenyl-1H-pyrazole 在 吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以74.2%的产率得到trans-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide
  参考文献：
  名称：

  NOVEL AZOLE DERIVATIVES

  摘要：

  公开号：

  EP1566384B1
• 作为产物：
  描述：

  4-硝基-1-苯基吡唑-3-胺 在 palladium 10% on activated carbon 氢气 作用下， 以 甲醇 为溶剂， 反应 1.5h， 以58.6%的产率得到3,4-diamino-1-phenyl-1H-pyrazole
  参考文献：
  名称：

  NOVEL AZOLE DERIVATIVES

  摘要：

  公开号：

  EP1566384B1

文献信息

• [EN] INHIBITORS OF JANUS KINASES<br/>[FR] INHIBITEURS DE JANUS KINASES
  申请人：MERCK & CO INC

  公开号：WO2010014453A1

  公开（公告）日：2010-02-04

  The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

  这项即时发明提供了抑制四种已知哺乳动物JAK激酶（JAK1、JAK2、JAK3和TYK2）的化合物。该发明还提供了包含这种抑制性化合物的组合物以及通过向需要治疗骨髓增生性疾病或癌症的患者施用该化合物来抑制JAK1、JAK2、JAK3和TYK2活性的方法。
• Novel azole derivatives
  申请人：Otake Norikazu

  公开号：US20060111380A1

  公开（公告）日：2006-05-25

  The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

  本发明涉及一种式子为(I)的化合物：其中，Az是包含单环唑或同种或不同融合唑的双环芳香环的基团；T、U、V和W独立地是亚甲基或氮，所述亚甲基可以选用取代基进行取代，且至少有两个T、U、V和W是所述亚甲基基团；而X是氮或亚甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病、神经系统疾病、遗传性疾病、代谢性疾病、生殖器或生殖系统疾病、胃肠疾病、呼吸系统疾病、炎症性疾病或青光眼等。
• Fluorinated Arylamide Derivatives
  申请人：Miller Thomas A.

  公开号：US20090012075A1

  公开（公告）日：2009-01-08

  The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

  本发明涉及一种新型的氟化芳基酰胺衍生物。这些化合物可用于治疗癌症。氟化芳基酰胺衍生物还可以抑制组蛋白去乙酰化酶，并适用于选择性诱导终末分化、阻止肿瘤细胞的生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的这些化合物在治疗具有肿瘤细胞增殖特征的患者中是有用的。本发明的这些化合物也可能在预防和治疗TRX介导的疾病中有用，例如自身免疫、过敏和炎症性疾病，以及中枢神经系统（CNS）疾病的预防和/或治疗，如神经退行性疾病。本发明还提供了包含羟酰胺衍生物的药物组合物和这些药物组合物的安全用量方案，这些方案易于遵循，并在体内产生治疗有效量的羟酰胺衍生物。
• Benzothiophene derivatives
  申请人：Hubbs Jed Lee

  公开号：US20090082308A1

  公开（公告）日：2009-03-26

  The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

  本发明涉及一类新型的苯并噻吩酰胺衍生物。这些羟肟酸化合物可用于治疗癌症。苯并噻吩酰胺化合物还可以抑制组蛋白去乙酰化酶，并适用于选择性诱导终末分化，阻止肿瘤细胞的生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有肿瘤细胞增殖特征的患者。该发明的化合物也可用于预防和治疗TRX介导的疾病，如自身免疫性、过敏性和炎症性疾病，以及中枢神经系统（CNS）疾病的预防和/或治疗，如神经退行性疾病。本发明还提供了包含羟肟酸衍生物的药物组合物和这些药物组合物的安全剂量方案，易于遵循，并在体内产生治疗有效量的羟肟酸衍生物。
• Azole derivatives
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：US07365079B2

  公开（公告）日：2008-04-29

  The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

  本发明涉及一种式子（I）的化合物：其中Az是包含单环唑或同一或不同融合唑的双环芳香环的基团；T、U、V和W独立地是甲烷或氮，所述甲烷可以被取代，而且至少有两个T、U、V和W是所述甲烷基团；X是氮或甲烷。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病、神经系统疾病、遗传疾病、代谢性疾病、生殖器或生殖系统疾病、胃肠道疾病、呼吸系统疾病、炎症性疾病或青光眼等。