N-(4-butylphenyl)pyridine-3-carboxamide | 75075-27-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(4-butylphenyl)pyridine-3-carboxamide
• CAS: 75075-27-3
• 化学式: C₁₆H₁₈N₂O
• 分子量: 254.33
• InChiKey: UGTKORWNEHKRJF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] 2-AMINO-NICOTINAMIDE DERIVATIVES AND THEIR USE AS VEGF-RECEPTOR TYROSINE KINASE INHIBITORS<br/>[FR] DERIVES DE 2-AMINO-NICOTINAMIDE ET LEUR UTILISATION COMME INHIBITEURS DE TYROSINE KINASE DU RECEPTEUR VEGF
  申请人：NOVARTIS AG

  公开号：WO2001055114A1

  公开（公告）日：2001-08-02

  The invention relates to the use of 2-amino-nicotinamide derivatives of formula (I) wherein n is from 1 up to and including 6; W is O or S; R1 and R3 represent independently of each other hydrogen, lower alkyl or lower acyl; R2 represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; R and R' are independently of each other hydrogen or lower alkyl; X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptale salt of such a compound, alone or in combination with one or more other pharmaceutically active compounds for the preparation of a pharmaceutical composition for use for therapy of a disease which responds to an inhibition of the VEGF-receptor tyrosine kinase activity; and to new 2-amino-nicotinamide derivatives of formula (I) and processes for the preparation thereof.

  本发明涉及使用式(I)的2-氨基烟酰胺衍生物，其中n为1至6，包括1和6；W为O或S；R1和R3各自独立地表示氢、低级烷基或低级酰基；R2表示环烷基、芳基或含有一个或多个环氮原子和0、1或2个异原子的单环或双环杂芳基，所述异原子独立地选自氧和硫的群，每种基团都未取代或单取代或多取代；R和R'各自独立地表示氢或低级烷基；X表示芳基或含有一个或多个环氮原子和0、1或2个异原子的单环或双环杂芳基，所述异原子独立地选自氧和硫的群，每种基团都未取代或单取代或多取代；或其N-氧化物，其可能的互变异构体或其药学上可接受的盐，单独或与一种或多种其他药物活性化合物结合，用于制备用于治疗对VEGF受体酪氨酸激酶活性抑制有反应的疾病的药物组合物；以及式(I)的新2-氨基烟酰胺衍生物及其制备方法。
• 2-AMINO-NICOTINAMIDE DERIVATIVES AND THEIR USE AS VEGF-RECEPTOR TYROSINE KINASE INHIBITORS
  申请人：Novartis AG

  公开号：EP1259487A1

  公开（公告）日：2002-11-27
• COMBINATION OF A VEGF RECEPTOR INHIBITOR WITH A CHEMOTHERAPEUTIC AGENT
  申请人：Novartis AG

  公开号：EP1682181A2

  公开（公告）日：2006-07-26
• [EN] COMBINATION OF A VEGF RECEPTOR INHIBITOR WITH A CHEMOTHERAPEUTIC AGENT<br/>[FR] POLYTHERAPIE COMBINANT UN INHIBITEUR DES RECEPTEURS DU FACTEUR VEGF AVEC UN AGENT CHIMIOTHERAPEUTIQUE
  申请人：NOVARTIS AG

  公开号：WO2005027972A2

  公开（公告）日：2005-03-31

  The present invention relates to a combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis. The patient is treated with a VEGF inhibitor compound; and one or more chemotherapeutic agents.