N-(3,4-bis-trifluoromethyl-phenyl)-nicotinamide | 62315-04-2

• 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-(3,4-bis-trifluoromethyl-phenyl)-nicotinamide
• 英文别名: N-[3,4-Bis(trifluoromethyl)phenyl]pyridine-3-carboxamide
• CAS: 62315-04-2
• 化学式: C₁₄H₈F₆N₂O
• 分子量: 334.221
• InChiKey: HDGGCTJQKRSAAY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  8

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
• COMBINATIONS OF A VEGF RECEPTOR INHIBITOR WITH OTHER THERAPEUTIC AGENTS
  申请人：Novartis AG

  公开号：EP1667721A2

  公开（公告）日：2006-06-14
• [EN] COMBINATIONS OF A VEGF RECEPTOR INHIBITOR WITH OTHER THERAPEUTIC AGENTS<br/>[FR] COMBINAISONS D'UN INHIBITEUR DU RECEPTEUR DU VEGF ET D'AUTRES AGENTS THERAPEUTIQUES
  申请人：NOVARTIS AG

  公开号：WO2005027973A2

  公开（公告）日：2005-03-31

  The invention relates to a combination therapy for treating patients suffering from diseases characterized by cell proliferation and infiltration of inflammatory cells, coronary diseases, hypertension, renal diseases, diabetes, or ocular diseases and conditions. The patient is treated with a combination of: (a) a VEGF inhibitor compound; and (b) one or more second therapeutic agents selected from the group consisting of: i. angiostatic steroids; ii. photosensitizers; iii. implants containing corticosteroids; iv. AT1 receptor antagonists; V. ACE inhibitors; vi. cyclooxygenase inhibitors; vii. IGF-IR inhibitors; viii. mTOR kinase inhibitors; ix. somatostatin receptor antagonists; X. P13K inhibitors; A. Raf kinase inhibitors; xii. PKC inhibitors; xiii. integrin antagonists; xiv. endogenous anti-anglogenic molecules; and xv. PEDF and analogs.