4-(1,3-oxazol-5-yl)phenylhydrazine hydrochloride | 297757-05-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-(1,3-oxazol-5-yl)phenylhydrazine hydrochloride
• 英文别名: [4-(1,3-Oxazol-5-yl)phenyl]hydrazine;hydrochloride
• CAS: 297757-05-2
• 化学式: C₉H₉N₃O*ClH
• 分子量: 211.651
• InChiKey: OSWLDVZOJXPCGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.05
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  64.1
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1,6-dihydro-1,2,3,6-tetraaza-as-indacene-7,8-dione 、 4-(1,3-oxazol-5-yl)phenylhydrazine hydrochloride 生成 1,6-dihydro[1,2,3]triazolo[4,5-e]indole-7,8-dione 8{N-[4-(1,3-oxazol-5-yl)phenyl]hydrazone} 、 1,6-dihydro[1,2,3]triazolo[4,5-e]indole-7,8-dione 8{N-[4-(1,3-oxazol-5-yl)phenyl]hydrazone}
  参考文献：
  名称：

  3-(anilinomethylene) oxindoles

  摘要：

  本发明一般涉及新型胺取代的噁二酮化合物和组合物。这些化合物和组合物作为药理学药剂在治疗由于一般蛋白激酶激活的信号通路的抑制或拮抗而减轻的疾病或症状方面具有实用性，特别是在涉及异常细胞增殖的病理过程中，如肿瘤生长。具体而言，本发明涉及一系列取代的噁二酮化合物，其表现出蛋白酪氨酸激酶和蛋白丝氨酸/苏氨酸激酶抑制作用，并且在通过抑制与肿瘤相关的血管生成抑制肿瘤生长方面是有用的。

  公开号：

  US06350747B1

文献信息

• Substituted oxindole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors and compositions and methods of treating chemotherapy and radiation therapy side effects
  申请人：——

  公开号：US20030069430A1

  公开（公告）日：2003-04-10

  Compounds of formula (I): wherein X is N, CH, CCF 3 , or C(C 1-12 aliphatic); R 4 is sulfonic acid, C 1-12 aliphatic-sulfonyl, sulfonyl-C 1-12 aliphatic, C 1-12 aliphatic-sulfonyl-C 1-6 aliphatic, C 1-6 aliphatic-amino, R 7 -sulfonyl, R 7 sulfonyl-C 1-12 aliphatic, R 7 -aminosulfonyl, R 7 aminosulfonyl-C 1-12 aliphatic, R 7 -sulfonylamino, R 7 -sulfonylamino-C 1-12 aliphatic, aminosulfonylamino, di-C 1-12 aliphatic amino, di-C 1-12 aliphatic aminocarbonyl, di-C 1-12 aliphatic aminosulfonyl, di-C 1-12 aliphatic amino, di-C 1-12 aliphatic aminocarbonyl, di-C 1-12 aliphatic aminosulfonyl-C 1-12 aliphatic, (R 8 ) 1-3 -Arylamino, (R 8 ) 1-3 -Arylsulfonyl, (R 8 ) 1-3 -Aryl-aminosulfonyl, (R 8 ) 1-3 -Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R 5 is hydrogen; and further wherein R 4 and R 5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

  化合物的公式（I）：其中X为N，CH，CCF3或C（C1-12脂肪族）; R4为磺酸，C1-12脂肪族磺酰基，磺酰基-C1-12脂肪族，C1-12脂肪族磺酰基-C1-6脂肪族，C1-6脂肪族氨基，R7-磺酰基，R7磺酰基-C1-12脂肪族，R7-氨基磺酰基，R7氨基磺酰基-C1-12脂肪族，R7-磺酰胺基，R7-磺酰胺基-C1-12脂肪族，氨基磺酰胺基，二C1-12脂肪族氨基，二C1-12脂肪族氨基甲酰基，二C1-12脂肪族氨基磺酰基，二C1-12脂肪族氨基，二C1-12脂肪族氨基甲酰基，二C1-12脂肪族氨基磺酰基-C1-12脂肪族，（R8）1-3-芳基氨基，（R8）1-3-芳基磺酰基，（R8）1-3-芳基氨基磺酰基，（R8）1-3-芳基磺酰胺基，Het-氨基，Het-磺酰基，Het-氨基磺酰基，氨基亚氨基，或氨基亚氨基磺酰基，R5为氢; 进一步地，其中R4和R5可选择地连接以形成融合环，包括它们的制药配方以及它们在治疗中的应用，特别是在CDK2活性介导的疾病治疗中，例如由癌症化疗或放疗引起的脱发。
• 3-(Anilinomethylene)oxindoles
  申请人：——

  公开号：US20020099071A1

  公开（公告）日：2002-07-25

  1 Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.

  公式（I）中的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，A，D，X，Y和Z的含义如权利要求中所定义，具有蛋白酪氨酸激酶和蛋白丝氨酸/苏氨酸激酶抑制活性。
• Compounds
  申请人：——

  公开号：US20040191210A1

  公开（公告）日：2004-09-30

  1 Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.

  化合物式（I）其中R1，R2，R3，R4，R5，R6，R7，R8，A，D，X，Y和Z的含义如权利要求所定义，表现出蛋白酪氨酸激酶和蛋白质丝氨酸/苏氨酸激酶抑制活性。
• Hydrazone derivative
  申请人：Kawagoe Keiichi

  公开号：US20060276433A1

  公开（公告）日：2006-12-07

  A compound represented by the following formula (I): wherein R 1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R 2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R 3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof.

  以下是式子（I）所代表的化合物： 其中，R1代表氢、芳基（可能带有取代基）、饱和或不饱和的5-至7-成员杂环基（可能带有取代基）等； R2代表氢、芳基（可能带有取代基）、饱和或不饱和的5-至7-成员杂环基（可能带有取代基）等； R3代表氢等； Ar代表从芳香族碳氢化合物衍生的二价基团等； X代表单键、线性或支链烷基，具有1至3个碳原子，可能带有取代基等； G代表卤素、饱和或不饱和的5-或6-成员环烃基（可能带有取代基）、饱和或不饱和的5-至7-成员杂环基（可能带有取代基）等，其盐或溶剂化物；以及用于抑制淀粉样蛋白或类淀粉样蛋白的聚集和/或沉积的药剂，包括该化合物、其盐或溶剂化物。
• HYDRAZONE DERIVATIVE
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1612204A1

  公开（公告）日：2006-01-04

  A compound represented by the following formula (I): wherein R1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof

  下式(I)所代表的化合物： 其中 R1 代表氢、可能具有取代基的芳基、可能具有取代基的饱和或不饱和 5 至 7 元杂环基团等；R2 代表氢、可能具有取代基的芳基、可能具有取代基的饱和或不饱和 5 至 7 元杂环基团等；R3 代表氢等。Ar 代表衍生自芳香烃的二价基团等；X 代表具有 1 至 3 个碳原子的单键、线性或支链亚烷基（可具有取代基）等；G 代表卤素、饱和或不饱和的 5 或 6 元环状烃基（可具有取代基）、饱和或不饱和的 5 至 7 元杂环基（可具有取代基）等、一种抑制淀粉样蛋白或类淀粉样蛋白聚集和/或沉积的制剂，其中包括该化合物、其盐或其溶液。