4-(4-benzyloxy-2,5-dimethyl-phenyl)-1,2,3,6-tetrahydro-pyridine | 648897-88-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 4-(4-benzyloxy-2,5-dimethyl-phenyl)-1,2,3,6-tetrahydro-pyridine
• 英文别名: 4-[4-(Benzyloxy)-2,5-dimethylphenyl]-1,2,3,6-tetrahydropyridine；4-(2,5-dimethyl-4-phenylmethoxyphenyl)-1,2,3,6-tetrahydropyridine
• CAS: 648897-88-5
• 化学式: C₂₀H₂₃NO
• 分子量: 293.409
• InChiKey: UHLBHZOETOLSGU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA<br/>[FR] DERIVES D'ARYL PIPERIDINE UTILISES COMME INDUCTEURS D'EXPRESSION DES RECEPTEURS DES LIPOPROTEINES DE BASSE DENSITE (LDL) PERMETTANT DE TRAITER L'HYPERCHOLESTEROLEMIE
  申请人：GLAXO GROUP LTD

  公开号：WO2004006923A1

  公开（公告）日：2004-01-22

  This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression. and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy. wherein Ar1 is substituted, by at least one R1 group selected from: -O(CRaRb)nC(O)NRXRy, -O(CH2)nCN, -O(CH2)nO(CH2)mOR2, -O(CH2)nCO2R2, -OS02NRxRy, -OSO2(CH2)pCH3, -(CRaRb)nC(O)NRXRy, -(CH2)nCN, -(CH2)nO(CH2)mOR2, -(CH2)nCO2R2, -(CH2)nC(O)R2, - SO2NRxRy, -SO2(CH2)pCH3, -CH=CHC(O)NRxRy, -CH=CHCN, -CH=CHCO2R2, -CO2R2, - C(O)R2, -C(O)NRxRy and C2-5alkenyl.

  这项发明涉及促进低密度脂蛋白受体（LDL-r）表达的新化合物，以及它们的制备方法、含有它们的药物组合物和它们的医疗用途。更具体地说，这项发明涉及式（I）的新芳香基哌啶及其在治疗中的应用。其中Ar1被至少一个R1基团取代，所述R1基团选自：-O(CRaRb)nC(O)NRXRy，-O(CH2)nCN，-O( )nO( )mOR2，-O( )nCO2R2，-OS02NRxRy，-OSO2( )pCH3，-(CRaRb)nC(O)NRXRy，-( )nCN，-( )nO( )mOR2，-( )nCO2R2，-( )nC(O)R2，-SO2NRxRy，-SO2( )pCH3，-CH=CHC(O)NRxRy，-CH=CHCN，-CH=CHCO2R2，-CO2R2，-C(O)R2，-C(O)NRxRy和C2-5烯基。