赖色甘酯 | 110816-79-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 赖色甘酯
• 中文别名: 乙基5-[2-[(2S)-2,6-二氨基己酰基]氧基-3-(2-乙氧羰基-4-氧代苯并吡喃-5-基)氧基丙氧基]-4-氧代苯并吡喃-2-羧酸酯
• 英文名称: Cromoglicate lisetil
• 英文别名: ethyl 5-[2-[(2S)-2,6-diaminohexanoyl]oxy-3-(2-ethoxycarbonyl-4-oxochromen-5-yl)oxypropoxy]-4-oxochromene-2-carboxylate
• CAS: 110816-79-0
• 化学式: C₃₃H₃₆N₂O₁₂
• 分子量: 652.6
• InChiKey: NGJJDHCBOKNREV-FQEVSTJZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  47
• 可旋转键数：
  19
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  202
• 氢给体数：
  2
• 氢受体数：
  14

反应信息

• 作为产物：
  描述：

  2--1,3-bis(2-ethoxycarbonylchromon-5-yloxy)propane 、 盐酸 生成 赖色甘酯
  参考文献：
  名称：

  TAMAKI, SATOSHI;KITAGAWA, MASARU;TSUDA, HIROKAZU;NISHIZAWA, SUSUMU;KAKEYA+

  摘要：

  DOI：

文献信息

• Bile acid containing prodrugs with enhanced bioavailabilty
  申请人：——

  公开号：US20030212051A1

  公开（公告）日：2003-11-13

  Many compounds have poor bioavailability or variable bioavailability because of poor absorption of the compound in the small intestine. Conjugation of the compound with bile acid to form a prodrug will increase the bioavailibility of the compound and/or reduce the bioavailability variability of the compound because of the active transport of the prodrug by the intestinal bile acid transporter and because of increased lipophilic nature of the prodrug. A linker group can be used between the bile acid and the compound. One example of a bile acid containing prodrug is acyclovir valylchenodeoxycholate, where valine is the linker group. Another example of this prodrug is atenolol cholic acid amide.

  许多化合物由于在小肠中吸收不良而具有较差的生物利用度或生物利用度变异性。将化合物与胆酸结合形成前药会增加化合物的生物利用度和/或减少化合物的生物利用度变异性，因为前药通过肠道胆酸转运体的主动转运以及前药的增加亲脂性质。胆酸和化合物之间可以使用连接基团。胆酸含有前药的一个例子是乙酰环磷酸腺苷瓜氨酸胆酸酯，其中瓜氨酸是连接基团。这种前药的另一个例子是阿托伐他胆酸酰胺。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Methods for treating asthmatic conditions
  申请人：Wyeth

  公开号：US20030149029A1

  公开（公告）日：2003-08-07

  This invention provides methods for treating in mammals asthma and asthmatic conditions using substituted indole compounds of the general formula: 1 and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A 2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

  本发明提供了一种使用通式为1的取代吲哚化合物及其药学上可接受的盐形式，治疗哮喘和哮喘症状的哺乳动物的方法，并且提供了使用这些化合物作为各种磷脂酶酶活性抑制剂的方法，特别是磷脂酶A2酶的方法，以及用于医疗治疗、预防和抑制疼痛和炎症的方法。
• Inhibitors of cytosolic phospholipase A2
  申请人：McKew C. John

  公开号：US20070004719A1

  公开（公告）日：2007-01-04

  This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A 2 enzymes (cPLA 2 ), more particularly including inhibitors of cytosolic phospholipase A 2 alpha enzymes (cPLA 2 α). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.

  该发明提供了化学抑制剂，用于抑制各种磷脂酶酶活性，特别是细胞质磷脂酶A2酶（cPLA2），更特别地包括细胞质磷脂酶A2α酶（cPLA2α）的抑制剂。在某些实施例中，抑制剂具有公式I，其中组成变量如本文所定义。
• Inhibitors of Cytosolic Phospholipase A2
  申请人：McKew John C.

  公开号：US20100022536A1

  公开（公告）日：2010-01-28

  This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A 2 enzymes (cPLA 2 ), more particularly including inhibitors of cytosolic phospholipase A 2 alpha enzymes (cPLA 2 α). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.

  该发明提供了化学抑制剂，用于抑制各种磷脂酶酶的活性，特别是细胞质磷脂酶A2酶（cPLA2），更特别地包括细胞质磷脂酶A2α酶（cPLA2α）的抑制剂。在某些实施例中，抑制剂具有公式I：其中组分变量如此处所定义。