Pyrido[2,3-d]pyrimidin-7-one deriv. 47

• 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: Pyrido[2,3-d]pyrimidin-7-one deriv. 47
• 英文别名: 2-anilino-8-ethyl-6-phenylpyrido[2,3-d]pyrimidin-7-one
• 化学式: C₂₁H₁₈N₄O
• 分子量: 342.4
• InChiKey: HSEYKDNBMMUBTH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  58.1
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] PYRIDO[2,3-d]PYRIMIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION<br/>[FR] PYRIDO[2,3-d]PYRIMIDINES DESTINEES A INHIBER LA PROLIFERATION CELLULAIRE INDUITE PAR LES TYROSINES KINASES
  申请人：WARNER-LAMBERT COMPANY

  公开号：WO1996034867A1

  公开（公告）日：1996-11-07

  (EN) 6-Aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, and 7-thiones o f formula (I) are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.(FR) On décrit des 6-aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, et 7-thiones, formule (I) qui sont des inhibiteurs des tyrosines kinases et sont, par conséquent, utiles dans le traitement de la prolifération cellulaires induite par ces protéines. Ces composés sont notamment utiles dans le traitement du cancer, de l'athérosclérose, de la sténose récidivante et du psoriasis.

  带有苯基的6-位的pyrido[2,3-d]pyrimidine 7-imines、7-ones和7-thiones（通用式为I）是抑制蛋白酪氨酸激酶的化合物，因此对通过这些蛋白质引发的细胞分裂具有治疗作用。这些化合物尤其适用于治疗癌症、动脉硬化、再狭窄和银屑病。
• PYRIDO[2,3-d]PYRIMIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION
  申请人：Warner-Lambert Company LLC

  公开号：EP0823908B1

  公开（公告）日：2006-11-02
• PYRIDO 2,3-d]PYRIMIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0823908A1

  公开（公告）日：1998-02-18
• US5733914A
  申请人：——

  公开号：US5733914A

  公开（公告）日：1998-03-31
• [EN] PYRIDOPYRIMIDINE DERIVATIVES<br/>[FR] DERIVES DE PYRIDOPYRIMIDINE
  申请人：GPC BIOTECH AG

  公开号：WO2005105097A2

  公开（公告）日：2005-11-10

  The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R1 represents -NR3R4, -SR3, -SO-R3, -SO2-R3, -OR3; R2, R3, and R4 are independently of each other hydrogen, -(CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR5R6, phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R5 and R6 are independently of each other hydrogen, (CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; R5 and R6 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R4 can optionally be -CO-R3, -CO-OR3, -SO2-R3, -SO2-NR5R6, -CO-NR5R6, -CS-NR5R6, -C(=NH)-R3, -C(=NH)-NR5R6; R3 and R4 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.