7-hydroxy-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one | 94193-53-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 7-hydroxy-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one
• 英文别名: 6-hydroxy-4,3a-dihydroimidazolidino[2,1-b]quinazolin-2-one；7-Hydroxy-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-one；7-hydroxy-3,5-dihydro-1H-imidazo[2,1-b]quinazolin-2-one
• CAS: 94193-53-0
• 化学式: C₁₀H₉N₃O₂
• 分子量: 203.2
• InChiKey: FNAHBRBEEQQVHH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  64.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  7-hydroxy-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one 生成 7-(2-hydroxyethyl)oxy-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-one
  参考文献：
  名称：

  [EN] DIHYDROPYRIDINE COMPOUNDS HAVING SIMULTANEOUS ABILITY TO BLOCK L-TYPE CALCIUM CHANNELS AND TO INHIBIT PHOSPHODIESTERASE TYPE 3 ACTIVITY
  [FR] COMPOSES DE DIHYDROPYRIDINE PRESENTANT A LA FOIS LA CAPACITE DE BLOQUER DES CANAUX CALCIQUES DE TYPE L ET LA CAPACITE D'INHIBER L'ACTIVITE DE TYPE 3 DE LA PHOSPHODIESTERASE

  摘要：

  本发明提供了具有对PDE-3和L型钙通道具有抑制活性的化合物。本发明还提供了包含这些化合物的药物组合物以及使用这些化合物治疗心血管疾病、中风、癫痫、眼科疾病或偏头痛的方法。

  公开号：

  WO2004033444A1
• 作为产物：
  描述：

  2-oxo-4,3a-dihydroimidazolidino[2,1-b]quinazolin-6-yl acetic acid 生成 7-hydroxy-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one
  参考文献：
  名称：

  [EN] DIHYDROPYRIDINE COMPOUNDS HAVING SIMULTANEOUS ABILITY TO BLOCK L-TYPE CALCIUM CHANNELS AND TO INHIBIT PHOSPHODIESTERASE TYPE 3 ACTIVITY
  [FR] COMPOSES DE DIHYDROPYRIDINE PRESENTANT A LA FOIS LA CAPACITE DE BLOQUER DES CANAUX CALCIQUES DE TYPE L ET LA CAPACITE D'INHIBER L'ACTIVITE DE TYPE 3 DE LA PHOSPHODIESTERASE

  摘要：

  本发明提供了具有对PDE-3和L型钙通道具有抑制活性的化合物。本发明还提供了包含这些化合物的药物组合物以及使用这些化合物治疗心血管疾病、中风、癫痫、眼科疾病或偏头痛的方法。

  公开号：

  WO2004033444A1

文献信息

• (2-Oxo-1,2,3,5-tetrahydroimidazo-[2,1-B]quinazolinyl) oxyalkylamides
  申请人：Syntex (U.S.A.) Inc.

  公开号：US04690925A1

  公开（公告）日：1987-09-01

  Compounds according to the formula ##STR1## , its optical isomers, or a pharmaceutically acceptable salt thereof wherein: m and n are integers of 1 to 6; R.sub.1 is hydrogen or alkyl of 1 to 4 carbons; R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group; R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or .alpha.-amino acid side chains; R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl; R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.6, halo, --NH.sub.2, --N(R.sub.6).sub.2, --NHCOR.sub.6, --COOH, or --COO(R.sub.6) group wherein R.sub.6 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an --NH.sub.2, --N(R.sub.6).sub.2, --NHCOR.sub.6, --COOH, or --COOR.sub.6 group wherein R.sub.6 is lower alkyl; Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy; and Z is --OR.sub.7 or --NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or lower alkyl.

  根据公式 ##STR1## 的化合物，其光学异构体或药物可接受的盐，其中：m和n是1至6的整数；R.sub.1是1至4碳的氢或烷基；R.sub.2是氢或R.sub.1和R.sub.2结合形成氧代基；R.sub.3是氢、1至6碳的烷基、苯基、苄基、羟基低级烷基及其1至6碳原子的脂肪酰基或7至12碳原子的芳基酰基、氨基甲基、羧基烷基、烷氧羰基烷基或α-氨基酸侧链；R.sub.4是氢、1至6碳的烷基、苄基或羟基低级烷基；R.sub.5是氢、1至6碳原子的烷基、3至8碳原子的环烷基或4至12碳原子的环烷基低级烷基，其中环烷基环未取代或取代有低级烷基、低级烷氧基、--OH、--OCOR.sub.6、卤、--NH.sub.2、--N(R.sub.6).sub.2、--NHCOR.sub.6、--COOH或--COO(R.sub.6)基团，其中R.sub.6是低级烷基；苯基或苯基低级烷基，其中苯基未取代或取代有1个或多个低级烷基、卤或低级烷氧基或一个--NH.sub.2、--N(R.sub.6).sub.2、--NHCOR.sub.6、--COOH或--COOR.sub.6基团，其中R.sub.6是低级烷基；Y是氢、1至4碳原子的烷基、卤或低级烷氧基；Z是--OR.sub.7或--NR.sub.7 R.sub.8，其中R.sub.7和R.sub.8独立地是氢或低级烷基。
• Cardiotonic compounds with inhibitory activity against beta-adrenergic receptors and phosphodiesterase
  申请人：Hamilton Gregory

  公开号：US20070117978A1

  公开（公告）日：2007-05-24

  The present invention provides compounds possessing inhibitory activity against (3-adrenergic receptors and phosphodiesterase (PDE), including type 3 phosphodiesterase (PDE-3). The present invention further provides pharmaceutical compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for regulating calcium homeostasis, for treating a disease, disorder or condition in which disregulation of calcium homeostasis is implicated and for treating cardiovascular disease, stroke, epilepsy, an ophthalmic disorder or migraine.

  本发明提供了具有抑制(3-肾上腺素受体和磷酸二酯酶(PDE)活性的化合物，包括3型磷酸二酯酶(PDE-3)。本发明还提供了包含这些化合物的制药组合物，制备这些化合物的方法，以及使用这些化合物调节钙离子稳态，治疗涉及钙离子稳态失调的疾病、紊乱或状况，以及治疗心血管疾病、中风、癫痫、眼科疾病或偏头痛的方法。
• Controlled release compositions of agents that reduce circulating levels of platelets and methods therefor
  申请人：Glidden Paul F.

  公开号：US20090324710A1

  公开（公告）日：2009-12-31

  Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

  提供了预防和治疗方法，用于通过给予药剂，包括anagrelide和anagrelide衍生物，将循环血小板数量降至低于正常水平或低于正常水平，以抑制血管闭塞事件，包括栓塞。提供了包含这些药剂的方法和制药制剂。
• Compounds with mixed pde-inhibitory and beta-adrenergic antagonist or partial agonist activity for treatment of heart failure
  申请人：Hamilton S. Gregory

  公开号：US20070060748A1

  公开（公告）日：2007-03-15

  This invention provides compounds that possess inhibitory activity against β-adrenergic receptors and phosphodiesterase PDE, including phosphodiesterase 3 (PDE3). This invention further provides pharmaceutical compositions comprising such compounds; methods of using such compounds for treating cardiovascular disease, stroke, epilepsy, ophthalmic disorder or migraine; and methods of preparing pharmaceutical compositions and compounds that possess inhibitory activity against β-adrenergic receptors and PDE.

  本发明提供了一种具有对β-肾上腺素能受体和磷酸二酯酶PDE，包括磷酸二酯酶3（PDE3）的抑制活性的化合物。本发明还提供了包含这些化合物的药物组合物；使用这些化合物治疗心血管疾病、中风、癫痫、眼科疾病或偏头痛的方法；以及制备具有对β-肾上腺素能受体和PDE抑制活性的药物组合物和化合物的方法。
• Compounds having simultaneous ability to block L-type calcium channels and to inhibit phosphodiesterase type 3 activity
  申请人：Hamilton S. Gregory

  公开号：US20070066619A1

  公开（公告）日：2007-03-22

  The present invention provides compounds that possess inhibitory activity against PDE-3 and L-type calcium channels. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating cardiovascular disease, stroke, epilepsy, ophthalmic disorder or migraine.

  本发明提供了具有对 PDE-3 和 L 型钙通道抑制活性的化合物。本发明还提供了包含这些化合物的药物组合物以及使用这些化合物治疗心血管疾病、中风、癫痫、眼科疾病或偏头痛的方法。