3-[1-(6,7-diethoxy-2-morpholinoquinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H,3H)-quinazolinedione hydrochloride

• 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: 3-[1-(6,7-diethoxy-2-morpholinoquinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H,3H)-quinazolinedione hydrochloride
• 英文别名: KF24345；3-[1-(6,7-Diethoxy-2-morpholino-4-quinazolinyl)-4-piperidinyl]-1,2,3,4-tetrahydro-1,6-dimethyl-2,4-dioxoquinazoline hydrochloride；3-[1-(6,7-diethoxy-2-morpholin-4-ylquinazolin-4-yl)piperidin-4-yl]-1,6-dimethylquinazoline-2,4-dione;hydrochloride
• 化学式: C₃₁H₃₈N₆O₅*ClH
• 分子量: 611.141
• InChiKey: XORSKPONEBPJTN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.85
• 重原子数：
  43
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  101
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  苯硫酚 、 3-[1-(6,7-diethoxy-2-morpholinoquinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H,3H)-quinazolinedione hydrochloride 以 水 、 N,N-二甲基甲酰胺 为溶剂， 以49%的产率得到3-[1-(6-Ethoxy-7-hydroxy-2-morpholino-4-quinazolinyl)-4-piperidinyl]-1,2,3,4-tetrahydro-1,6-dimethyl-2,4-dioxoquinazoline
  参考文献：
  名称：

  US5948784

  摘要：

  公开号：

文献信息

• Quinazoline derivatives
  申请人：Kyowa Hakko Kogyo Co., Ltd.

  公开号：US05948784A1

  公开（公告）日：1999-09-07

  Disclosed are quinazoline derivatives represented by formula (I): wherein R.sup.1 represents hydrogen, lower alkyl, alkenyl, or aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, or the like; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 represent hydrogen, lower alkyl, lower alkoxy, aralkyloxy, or the like, or any adjoining two of them are combined to form methylenedioxy or the like; R.sup.10 represents hydrogen, lower alkyl, or the like; R.sup.11 and R.sup.12 represent hydrogen, lower alkyl, cycloalkyl, phenyl, or aralkyl, or R.sup.11 and R.sup.12 are combined together with N to form a heterocyclic group; and n represents 0, 1 or 2, and pharmaceutically acceptable salts thereof. These compounds have adenosine uptake inhibitory activity and are useful for the protection of myocardium and for the prevention or treatment of renal diseases such as nephritis and diabetic nephropathy.

  本发明涉及由式(I)表示的喹唑啉衍生物：其中R.sup.1表示氢、低碳基、烯基或芳基烷基；R.sup.2、R.sup.3、R.sup.4和R.sup.5表示氢、低碳基、低烷氧基、低烷酰基或类似物；R.sup.6、R.sup.7、R.sup.8和R.sup.9表示氢、低碳基、低烷氧基、芳基烷氧基或类似物，或其中任意相邻两个结合形成亚甲二氧基或类似物；R.sup.10表示氢、低碳基或类似物；R.sup.11和R.sup.12表示氢、低碳基、环烷基、苯基或芳基烷基，或R.sup.11和R.sup.12与N结合形成杂环基团；n表示0、1或2，以及其药学上可接受的盐。这些化合物具有腺苷摄取抑制活性，可用于心肌保护以及预防或治疗肾脏疾病，如肾炎和糖尿病肾病。
• QUINAZOLINE DERIVATIVE
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP0726267A1

  公开（公告）日：1996-08-14

  Disclosed are quinazoline derivatives represented by formula (I): wherein R1 represents hydrogen, lower alkyl, alkenyl, or aralkyl; R2, R3, R4, and R5 represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, or the like; R6, R7, R8, and R9 represent hydrogen, lower alkyl, lower alkoxy, aralkyloxy, or the like, or any adjoining two of them are combined to form methylenedioxy or the like; R10 represents hydrogen, lower alkyl, or the like; R11 and R12 represent hydrogen, lower alkyl, cycloalkyl, phenyl, or aralkyl, or R11 and R12 are combined together with N to form a heterocyclic group; and n represents 0, 1 or 2, and pharmaceutically acceptable salts thereof. These compounds have adenosine uptake inhibitory activity and are useful for the protection of myocardium and for the prevention or treatment of inflammation such as leg and foot edema.

  公开了式 (I) 所代表的喹唑啉衍生物： 其中 R1 代表氢、低级烷基、烯基或芳基；R2、R3、R4 和 R5 代表氢、低级烷基、低级烷氧基、低级烷酰基或类似物；R6、R7、R8 和 R9 代表氢、低级烷基、低级烷氧基、芳基氧基或类似物，或其中任意相邻的两个结合形成亚甲基二氧基或类似物；R10 代表氢、低级烷基或类似物；R11 和 R12 代表氢、低级烷基、环烷基、苯基或芳烷基，或 R11 和 R12 与 N 结合形成杂环基团；n 代表 0、1 或 2、 及其药学上可接受的盐类。 这些化合物具有腺苷摄取抑制活性，可用于保护心肌和预防或治疗炎症，如腿部和足部水肿。
• THERAPEUTIC AGENT FOR KIDNEY DISEASES
  申请人：KYOWA HAKKO KOGYO KABUSHIKI KAISHA

  公开号：EP0919233A1

  公开（公告）日：1999-06-02

  Disclosed is a therapeutic agent for renal disease comprising a quinazoline derivative represented by formula (I): (wherein R1 represents hydrogen, lower alkyl, alkenyl, or aralkyl; R2, R3, R4, and R5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, or the like; R6, R7, R8, and R9 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, aralkyloxy, or lower alkanoyloxy, or the like, or any adjoining two of them are combined to form methylenedioxy or the like; R10 represents hydrogen, lower alkyl, or the like; R11 and R12 are the same or different and represent hydrogen, lower alkyl, cycloalkyl, phenyl, or aralkyl, or R11 and R12 are combined together to form a heterocyclic group containing nitrogen atom; and n represents 0, 1 or 2) and pharmaceutically acceptable salts thereof as an active ingredient. This therapeutic agent is useful for the prevention or treatment of renal diseases such as nephritis and diabetic nephropathy.

  本发明公开了一种治疗肾病的药物，该药物包含由式（I）代表的喹唑啉衍生物： (其中R1代表氢、低级烷基、烯基或芳烷基；R2、R3、R4和R5相同或不同，代表氢、低级烷基、低级烷氧基、低级烷酰基或类似物；R6、R7、R8和R9相同或不同，代表氢、低级烷基、低级烷氧基、芳烷氧基或低级烷酰氧基或类似物，或其中任意相邻的两个结合成亚甲基二氧基或类似物；R10 代表氢、低级烷基或类似物；R11 和 R12 相同或不同，代表氢、低级烷基、环烷基、苯基或芳烷基，或 R11 和 R12 结合在一起形成含氮原子的杂环基团；n 代表 0、1 或 2）及其药学上可接受的盐类作为活性成分。 这种治疗剂可用于预防或治疗肾炎和糖尿病肾病等肾脏疾病。
• Methods, compositions, and kits for the treatment of ophthalmic disorders
  申请人：CombinatoRx, Inc.

  公开号：EP2218442A1

  公开（公告）日：2010-08-18

  The invention features methods, compositions and kits comprising a corticosteroid and a non-steroidal immunophilin-dependent immunosuppressant for treating an ophthalmic disorder in a patient, wherein at least one of said corticosteroid and said non-steroidal immunophilin-dependent immunosuppressant is present at a low concentration, in particular wherein said corticosteroid is prednisolone acetate and said non-steroidal immunophilin-dependent immunosuppressant is cyclosporine A.

  本发明的特征是包含皮质类固醇和非类固醇免疫嗜血素依赖性免疫抑制剂的方法、组合物和试剂盒，用于治疗患者的眼科疾病、其中，所述皮质类固醇和所述非类固醇免疫嗜血素依赖性免疫抑制剂中至少有一种以低浓度存在，特别是所述皮质类固醇为醋酸泼尼松龙，所述非类固醇免疫嗜血素依赖性免疫抑制剂为环孢素 A。
• QUINAZOLINE DERIVATIVES
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP0726267B1

  公开（公告）日：2000-11-22