达唑司特 | 76002-75-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 达唑司特
• 中文别名: 达唑奎那斯
• 英文名称: imidazo-[1,2-a]-quinoxaline-2-carboxylic acid
• 英文别名: dazoquinast；imidazo[1,2-a]quinoxaline-2-carboxylic acid
• CAS: 76002-75-0
• 化学式: C₁₁H₇N₃O₂
• 分子量: 213.195
• InChiKey: JVKYTWZLUFMIKS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.5
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  达唑司特 在 sodium hydroxide 作用下， 以 水 、 丙酮 为溶剂， 生成 sodium imidazo-[1,2-a]-quinoxaline-2-carboxylate
  参考文献：
  名称：

  Novel imidazoquinoxalines

  摘要：

  该专利描述了一种公式为##STR1##的新型咪唑喹啉类化合物，其中R选自氢、1至5个碳原子的烷基、--NH.sub.4、碱金属、碱土金属、镁、铝和非毒性、药学上可接受的胺类；X选自氢、1至5个碳原子的烷氧基和氨基甲酰基；Y和Z各自选自氢和卤素，以及它们的非毒性、药学上可接受的酸盐，具有抗过敏活性。该专利还涉及了这些化合物的制备方法。

  公开号：

  US04254123A1
• 作为产物：
  描述：

  2-氨基喹喔啉 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 反应 3.5h， 生成 达唑司特
  参考文献：
  名称：

  Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles

  摘要：

  4H-Imidazo[2,1-c][1,4]benzoxazine-2-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG, 1), 3 was less active following iv administration but unlike DSCG showed very significant oral activity. To explore the structural requirements for this activity, a range of tricyclic compounds was prepared and their activities were measured. Individual 2-carboxylic acids derived from imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles showed iv activities up to 10(3) times as potent as DSCG and many of them showed significant oral activity. From these, imidazo[1,2-a]quinoxaline-2-carboxylic acid 114 has been chosen for further development.

  DOI：

  10.1021/jm00401a009
• 作为试剂：
  描述：

  sodium hydroxide 、 咪唑并[1,2-a]喹喔啉-2-羧酸乙酯 、 水 在 乙醇 、 达唑司特 、 solid 作用下， 以 乙醇 为溶剂， 反应 1.0h， 生成 达唑司特
  参考文献：
  名称：

  Novel imidazoquinoxalines

  摘要：

  式子为##STR1##的新型咪唑喹啉化合物，其中R选择从氢、1至5个碳原子的烷基、--NH.sub.4、碱金属、碱土金属、镁、铝和无毒、药学上可接受的胺类中选取，X选择从氢、1至5个碳原子的烷氧基和氨基甲酰中选取，Y和Z分别从氢和卤素中选取，以及它们的无毒、药学上可接受的酸盐，具有抗过敏活性，以及它们的制备方法。

  公开号：

  US04254123A1

文献信息

• 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。
• Imidazo[2,1-C]quinolines, useful as antiallergic agents
  申请人：Roussel Uclaf

  公开号：US04644002A1

  公开（公告）日：1987-02-17

  Novel compounds of the formula ##STR1## wherein A is selected from the group consisting of nitrogen and .dbd.CH--, G is ##STR2## Z is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken with Y forms a carbon-carbon bond, Z' is selected from the group consisting of hydrogen and halogen, Y is hydrogen, or taken with Z is a carbon-carbon bond or taken with X is .dbd.O and X is hydrogen or taken with Y is .dbd.O, R is selected from the group consisting of hydroxymethyl, formyl, tetrazol-5-yl, N-(tetrazol-5-yl) carbamoyl, aminomethyl and carbamoyl, R.sub.1 is selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 5 carbon atoms and its non-toxic, pharmaceutically acceptable acid addition salts having antiallergic activity and their preparation.

  化合物的公式为##STR1##其中A选自由氮和.dbd.CH--的组合，G为##STR2##，Z选自1到5个碳原子的氢和烷基组成的组合或与Y形成碳-碳键，Z'选自氢和卤素的组合，Y为氢或与Z形成碳-碳键或与X形成.dbd.O，X为氢或与Y形成.dbd.O，R选自羟甲基、甲酰基、四唑-5-基、N-(四唑-5-基)氨基甲酰、氨甲基和氨基甲酰的组合，R.sub.1选自1到5个碳原子的卤素和烷氧基的组合，以及其无毒、药学上可接受的酸加合物，具有抗过敏活性，其制备方法。
• Substituted imidazo 1,2-a-quinoxaline-4-(5H)ones, their compositions and
  申请人：Roussel Uclaf

  公开号：US04474784A1

  公开（公告）日：1984-10-02

  Novel compounds of the formula ##STR1## wherein A is selected from the group consisting of nitrogen and .dbd.CH--, G is selected from the group consisting of --0--, ##STR2## Z is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken with Y forms a carbon-nitrogen or carbon-carbon bond, Z' is selected from the group consisting of hydrogen and halogen, Y is hydrogen, or taken with Z is a carbon-nitrogen or carbon-carbon bond or taken with X is .dbd.0 and X is hydrogen or taken with Y is .dbd.0, R is selected from the group consisting of hydroxymethyl, formyl, tetrazol-5-yl, N-(tetrazol-5-yl) carbamoyl, aminomethyl and carbamoyl, R.sub.1 is selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 5 carbon atoms and its non-toxic, pharmaceutically acceptable acid addition salts having anti-allergic activity and their preparation.

  该文描述的是一种新型化合物，化学式为##STR1## 其中A可选自氮和.dbd.CH--，G可选自--0--，##STR2##，Z可选自氢和1至5个碳原子的烷基，或与Y形成碳氮或碳碳键，Z'可选自氢和卤素，Y为氢，或与Z形成碳氮或碳碳键，或与X形成.dbd.0，X为氢，或与Y形成.dbd.0，R可选自羟甲基、甲酰基、四唑-5-基、N-(四唑-5-基)氨基甲酰基、氨甲基和氨基甲酰基，R.sub.1可选自氢、卤素和1至5个碳原子的烷氧基，以及其无毒、药学上可接受的酸盐，具有抗过敏活性，并提供了其制备方法。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Imidazoquinoxalines and pyrroloquinoxalines
  申请人：Roussel Uclaf

  公开号：US04333934A1

  公开（公告）日：1982-06-08

  Novel compounds of the formula ##STR1## wherein A is selected from the group consisting of nitrogen and .dbd.CH--, G is selected from the group consisting of ##STR2## Z is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken with Y forms a carbon-nitrogen or carbon-carbon bond, Z' is selected from the group consisting of hydrogen and halogen, Y is hydrogen, or taken with Z is a carbon-nitrogen or carbon-carbon bond or taken with X is .dbd.O and X is hydrogen or taken with Y is .dbd.O, R is selected from the group consisting of hydroxymethyl, formyl, tetrazol-5-yl, N-(tetrazol-5-yl) carbamoyl, aminomethyl and carbamoyl, R.sub.1 is selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 5 carbon atoms and its non-toxic, pharmaceutically acceptable acid addition salts having antiallergic activity and their preparation.

  化合物的新颖结构式为##STR1## 其中A选自氮和.dbd.CH--的群组，G选自##STR2##的群组，Z选自1到5个碳原子的氢和烷基，或与Y一起形成碳氮或碳碳键，Z'选自氢和卤素的群组，Y为氢，或与Z一起形成碳氮或碳碳键，或与X一起为.dbd.O，X为氢，或与Y一起为.dbd.O，R选自羟甲基、甲酰基、四唑-5-基、N-(四唑-5-基)氨甲酰基、氨甲基和氨基甲酰基的群组，R.sub.1选自1到5个碳原子的卤素和烷氧基的群组，以及其无毒、药学上可接受的酸盐，具有抗过敏活性，并且可以制备这些化合物。