trans 1-(4-Isopropyl-cyclohexylamino)-4-[2-methoxy-(pyridin-4-yl)-methyl]-phthalazine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: trans 1-(4-Isopropyl-cyclohexylamino)-4-[2-methoxy-(pyridin-4-yl)-methyl]-phthalazine
• 英文别名: 4-[(2-methoxypyridin-4-yl)methyl]-N-(4-propan-2-ylcyclohexyl)phthalazin-1-amine
• 化学式: C₂₄H₃₀N₄O
• 分子量: 390.5
• InChiKey: SCVSKBOXACFBBW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  59.9
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Phthalazine derivatives with angiogenesis inhibiting activity
  申请人：——

  公开号：US20040180899A1

  公开（公告）日：2004-09-16

  The invention relates to new phthalazine derivatives of formula (I), wherein R 1 and R 2 : a) are independently in each case a lower alkyl; b) together form a bridge of subformula (I*), wherein the bond is achieved via the two terminal C atoms and m is 0 to 4; or c) together form a bridge of subformula (I**), wherein one or two of the ring members T 1 , T 2 , T 3 and T 4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T 1 and T 4 ; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; X is imino, oxa, or thia; Y is hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or unsubstituted or substituted cycloalkyl; and wherein the bonds characterized in subformula (I*) by a wavy line are either single or double bonds; to an N-oxide of a compound of formula I; a tautomer or mixture of tautomers of a compound of formula (I) of an N-oxide thereof; and a pharmaceutically acceptable salt of a compound of formula (I), of an N-oxide or of a tautomer or mixture of tautomers thereof; processes for their preparation and pharmaceutical uses. 1

  本发明涉及公式（I）的新的邻二氮杂菲衍生物，其中R1和R2：a）各自独立地为较低的烷基；b）共同形成子公式（I *）的桥梁，其中通过两个末端C原子实现键合，并且m为0到4；或c）共同形成子公式（I **）的桥梁，其中环成员T1、T2、T3和T4中的一个或两个是氮，其余的分别为CH，并且通过原子T1和T4实现键合；A、B、D、E和T各自独立地为N或CH，但至少一个且不超过三个基团为N；X为亚胺基、氧杂基或硫杂基；Y为氢、取代或未取代的芳基、取代或未取代的杂芳基、或未取代或取代的环烷基；在子公式（I *）中由波浪线表示的键可以是单键或双键；以及公式（I）化合物的N-氧化物，公式（I）化合物的互变异构体或其N-氧化物的混合物；以及公式（I）化合物的药学上可接受的盐，其N-氧化物或其互变异构体或其混合物的制备方法和药物用途。
• Phthalazine Derivatives with Angiogenesis Inhibiting Activity
  申请人：Bold Guido

  公开号：US20090076003A1

  公开（公告）日：2009-03-19

  The invention relates to new phthalazine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment of a disease, especially of a disease that responds to the inhibition of tyrosine kinases, more especially the inhibition of the vascular endothelial growth factor (VEGF) receptor kinase, preferably the treatment of a proliferative disease, such as a tumour disease.

  本发明涉及新的邻苯二酸咪唑衍生物，其制备方法，其在人或动物体内治疗过程中的应用，其单独或与一种或多种其他药物活性化合物结合使用治疗疾病，特别是对酪氨酸激酶抑制的反应疾病，更特别是对血管内皮生长因子（VEGF）受体激酶抑制的反应疾病，优选是治疗增殖性疾病，如肿瘤疾病的治疗。
• PHTHALAZINE DERIVATIVES WITH ANGIOGENESIS INHIBITING ACTIVITY
  申请人：Novartis AG

  公开号：EP1387836A1

  公开（公告）日：2004-02-11
• US7399761B2
  申请人：——

  公开号：US7399761B2

  公开（公告）日：2008-07-15
• US8034814B2
  申请人：——

  公开号：US8034814B2

  公开（公告）日：2011-10-11