1-[4-(1-Methyl-1H-pyrazolo[3,4-c]pyridin-4-yl)-phenyl]-3-phenyl-urea | 1032943-11-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-[4-(1-Methyl-1H-pyrazolo[3,4-c]pyridin-4-yl)-phenyl]-3-phenyl-urea
• 英文别名: 1-[4-(1-methylpyrazolo[3,4-c]pyridin-4-yl)phenyl]-3-phenylurea
• CAS: 1032943-11-5
• 化学式: C₂₀H₁₇N₅O
• 分子量: 343.388
• InChiKey: FNPBYQXVBUWBBG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  71.8
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  4-(1-甲基-1H-吡唑并[3,4-c]吡啶-4-基)-苯胺 、 异氰酸苯酯 以 二氯甲烷 为溶剂， 以provided 29 mg of the analytically pure product (0.084 mmol, 17% yield)的产率得到1-[4-(1-Methyl-1H-pyrazolo[3,4-c]pyridin-4-yl)-phenyl]-3-phenyl-urea
  参考文献：
  名称：

  3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same.

  摘要：

  本发明涉及符合通式(I)的3-H-吡唑吡啶类化合物： 其中A、B、D、E、Ra、R1、R2、R3、R4、R5和q如权利要求中所定义的，并且涉及其盐、N-氧化物、溶剂合物和前药，涉及包含所述3-H-吡唑吡啶类化合物的制药组合物，制备所述3-H-吡唑吡啶类化合物的方法，有用于所述方法的中间化合物，以及有用于制备用于治疗失调血管生长的疾病或伴随失调血管生长的疾病的制药组合物的3-H-吡唑吡啶类化合物的用途，其中所述化合物有效地干扰Tie2信号传导。

  公开号：

  US20090062273A1

文献信息

• 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP1932845A1

  公开（公告）日：2008-06-18

  The invention relates to 3-H-pyrazolopyridines according to the general formula (I) : in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said 3-H-pyrazolopyridine compounds, to methods of preparing said 3-H-pyrazolopyridines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.

  本发明涉及3-H-吡唑吡啶，其通式（I）如下：其中A、B、D、E、Ra、R1、R2、R3、R4、R5和q如权利要求中所定义，以及其盐，N-氧化物，溶剂合物和前药，制备上述3-H-吡唑吡啶的方法，以及将其用于制造治疗失调血管生长疾病或伴随失调血管生长的疾病的药物组合物的用途，其中该化合物有效地干扰Tie2信号传导。
• N-[4-(1-H-pyrazolo[3,4-c]pyridin-4-yl)phenyl]-N'-[(hetero)aryl]-urea compounds, pharmaceutical compositions comprising them, their preparation and their use as Tie2-kinase inhibitors
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2042500A1

  公开（公告）日：2009-04-01

  The invention relates to 3-H-pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said 3-H-pyrazolopyridine compounds, to methods of preparing said 3-H-pyrazolopyridines, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said 3-H-pyrazolopyridines, as well as to uses of said 3-H-pyrazolopyridines for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.

  本发明涉及通式（I）的 3-H-吡唑并吡啶： 其中 A、B、D、E、Ra、R1、R2、R3、R4、R5 和 q 如权利要求书中所定义，及其盐类、N-氧化物、溶剂和原药，涉及包含所述 3-H-吡唑并吡啶化合物的药物组合物，涉及制备所述 3-H-吡唑并吡啶的方法，涉及在所述方法中有用的中间化合物、所述中间化合物在制备所述 3-H-吡唑并吡啶化合物中的用途，以及所述 3-H-吡唑并吡啶化合物在制造药物组合物中的用途，所述药物组合物用于治疗血管生长失调疾病或伴随血管生长失调的疾病，其中所述化合物可有效干扰 Tie2 信号。
• 3-H-PYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2125808A2

  公开（公告）日：2009-12-02
• [EN] 3-H-PYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME<br/>[FR] 3-H-PYRAZOLOPYRIDINES ET LEURS SELS, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, PROCEDES DE PREPARATION ET UTILISATIONS ASSOCIES
  申请人：BAYER SCHERING PHARMA AG

  公开号：WO2008071456A2

  公开（公告）日：2008-06-19

  [EN] The invention relates to 3-H-pyrazolopyridines according to the general formula (I) in which A, B, D, E, R^a, R¹, R², R³, R⁴, R⁵ and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said 3-H-pyrazolopyridine compounds, to methods of preparing said 3-H-pyrazolopyridines, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said 3-H-pyrazolopyridines, as well as to uses of said 3-H-pyrazolopyridines for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
  [FR] L'invention concerne des 3-H-pyrazolopyridines de formule générale (I), dans laquelle A, B, D, E, R^a, R¹, R², R³, R⁴, R⁵ et q sont tels que définis dans les revendications, ainsi que leurs sels, N-oxydes, solvates et promédicaments. L'invention concerne également des compositions pharmaceutiques contenant lesdits composés 3-H-pyrazolopyridines, des procédés de préparation de ces 3-H-pyrazolopyridines, des composés intermédiaires utiles dans lesdits procédés, les utilisations de ces composés intermédiaires dans la préparation des 3-H-pyrazolopyridines, ainsi que les utilisations de ces 3-H-pyrazolopyridines dans la fabrication d'une composition pharmaceutique destinée à traiter les maladies induites par un dérèglement de la croissance vasculaire ou les maladies s'accompagnant d'un dérèglement de la croissance vasculaire, les composés selon l'invention interférant efficacement avec la signalisation de Tie2.
• 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same.
  申请人：HARTUNG Ingo

  公开号：US20090062273A1

  公开（公告）日：2009-03-05

  The invention relates to 3-H-pyrazolopyridines according to the general formula (I): in which A, B, D, E, R a , R 1 , R 2 , R 3 , R 4 , R 5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said 3-H-pyrazolopyridine compounds, to methods of preparing said 3-H-pyrazolopyridines, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said 3-H-pyrazolopyridines, as well as to uses of said 3-H-pyrazolopyridines for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.

  本发明涉及符合通式(I)的3-H-吡唑吡啶类化合物： 其中A、B、D、E、Ra、R1、R2、R3、R4、R5和q如权利要求中所定义的，并且涉及其盐、N-氧化物、溶剂合物和前药，涉及包含所述3-H-吡唑吡啶类化合物的制药组合物，制备所述3-H-吡唑吡啶类化合物的方法，有用于所述方法的中间化合物，以及有用于制备用于治疗失调血管生长的疾病或伴随失调血管生长的疾病的制药组合物的3-H-吡唑吡啶类化合物的用途，其中所述化合物有效地干扰Tie2信号传导。