1,2-dihydro-2,2,4-trimethyl-5H-chromeno[3,4-f]quinoline

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: 1,2-dihydro-2,2,4-trimethyl-5H-chromeno[3,4-f]quinoline
• 英文别名: 2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinoline；2,2,4-trimethyl-1,5-dihydrochromeno[3,4-f]quinoline
• 化学式: C₁₉H₁₉NO
• 分子量: 277.366
• InChiKey: CNWLUDPVYBPOSX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  8-nitro-6H-benzo[c]chromen-6-one 在 三乙基硅烷 、 三氟化硼乙醚 、 碘 、 二异丁基氢化铝 、 tin(ll) chloride 作用下， 以 二氯甲烷 、 乙酸乙酯 、 甲苯 为溶剂， 反应 22.0h， 生成 1,2-dihydro-2,2,4-trimethyl-5H-chromeno[3,4-f]quinoline
  参考文献：
  名称：

  Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore

  摘要：

  A series of 1,2-dihydrochromeno[3,4-f]quinoline derivatives was synthesized and tested in biological assays to evaluate the nonsteroidal progesterone receptor modulator pharmacophore (4) as antiprogestins. A number of potent analogues were identified by modification of the substituents at the D-ring. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00256-7

文献信息

• [EN] GLUCOCORTICOID RECEPTOR MODULATOR COMPOUNDS AND METHODS- UTILITY<br/>[FR] COMPOSES MODULATEURS DE RECEPTEURS DE GLUCOCORTICOIDE ET PROCEDES
  申请人：LIGAND PHARM INC

  公开号：WO2005082909A1

  公开（公告）日：2005-09-09

  Provided herein are compounds of Formula (I) and pharmaceutically acceptable derivatives thereof. Certain of such compounds are selective glucocorticoid receptor modulators and/or selective glucocorticoid binding agents. Also provided are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.

  本文提供了式（I）的化合物及其药用可接受的衍生物。其中某些化合物是选择性糖皮质激素受体调节剂和/或选择性糖皮质激素结合剂。还提供了制备和使用这些化合物的方法，包括但不限于使用这些化合物治疗各种疾病。
• Glucocortiocoid-selective antinflammatory agents
  申请人：Abbott Laboratories and Ligand Pharmaceuticals Incorporated

  公开号：US20030073703A1

  公开（公告）日：2003-04-17

  Compounds having Formula I 1 are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.

  具有I1式的化合物对于部分或完全对抗、抑制、激动或调节糖皮质激素受体，并治疗哺乳动物的免疫、自身免疫和炎症性疾病是有用的。此外，还揭示了包含I式化合物的制药组合物和抑制哺乳动物的免疫或自身免疫疾病的方法。
• Steroid receptor modulator compounds and methods
  申请人：——

  公开号：US20040186132A1

  公开（公告）日：2004-09-23

  Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

  本文披露了高亲和力、高选择性的非类固醇化合物，可作为类固醇受体调节剂。同时也披露了包含这些化合物的药物组合物，以及使用这些化合物和组合物治疗需要类固醇受体激动剂或拮抗剂治疗的患者的方法，还包括制备这些化合物的中间体和制备类固醇受体调节剂化合物的方法。
• Methods for the preparation of coumarine derivatives
  申请人：LIGAND PHARMACEUTICALS INCORPORATED

  公开号：EP1041071A1

  公开（公告）日：2000-10-04

  Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

  本发明公开了对类固醇受体具有高亲和力、高选择性调节作用的非类固醇化合物。还公开了含有此类化合物的药物组合物、使用所公开化合物和组合物治疗需要类固醇受体激动剂或拮抗剂治疗的患者的方法、制备化合物时有用的中间体以及制备类固醇受体调节剂化合物的工艺。
• 5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators
  作者：Lin Zhi、Christopher M Tegley、James P Edwards、Sarah J West、Keith B Marschke、Marco M Gottardis、Dale E Mais、Todd K Jones

  DOI：10.1016/s0960-894x(98)00608-8

  日期：1998.12

  A series of nonsteroidal human progesterone receptor (hPR) agonists, 5-alkyl 1,2-dihydrochromeno[3,4-f]quinolines, was synthesized and evaluated in cotransfection and competitive receptor binding assays. The 5-alkyl substitution was shown to be responsible for the agonist activity and substitution at C9 dramatically enhanced the potency. A number of analogues in this series showed activities similar to or better than progesterone in the cotransfection and binding assays and analogue 15 exhibited similar in vivo activity as medroxyprogesterone acetate (MPA) in murine uterine wet weight/mammary gland morphology assays. (C) 1998 Elsevier Science Ltd. All rights reserved.