2-[2-ethoxy-5-(4-ethoxycarbonylpiperidino-sulphonyl)phenyl]-8-n-propylpyrido[3,2-d]pyrimidin-4(3H)-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 2-[2-ethoxy-5-(4-ethoxycarbonylpiperidino-sulphonyl)phenyl]-8-n-propylpyrido[3,2-d]pyrimidin-4(3H)-one
• 英文别名: 2-[2-ethoxy-5-(4-ethoxycarbonylpiperidinosulfonyl)phenyl]-8-n-propylpyrido [3,2-d]pyrimidin-4(3H)-one；2-[2-Ethoxy-5-(4-ethoxycarbonylpiperidinosulphonyl)phenyl]-8-n-propylpyrido[3,2-d]pyrimidin-4(3H)-one；ethyl 1-[4-ethoxy-3-(4-oxo-8-propyl-3H-pyrido[3,2-d]pyrimidin-2-yl)phenyl]sulfonylpiperidine-4-carboxylate
• 化学式: C₂₆H₃₂N₄O₆S
• 分子量: 528.629
• InChiKey: XXEKNQTZGSHWOS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  37
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  136
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  2-[2-ethoxy-5-(4-ethoxycarbonylpiperidino-sulphonyl)phenyl]-8-n-propylpyrido[3,2-d]pyrimidin-4(3H)-one 在 吡啶 、 氢氧化钾 作用下， 以 乙醇 、 水 为溶剂， 以8%的产率得到2-[5-(4-Carboxypiperidinosulphonyl)-2-ethoxyphenyl]-8-n-propylpyrido[3,2-d]pyrimidin-4(3H)-one
  参考文献：
  名称：

  Method of treating a patient having precancerous lesions with phenyl

  摘要：

  苯基环氨基嘧啶酮的衍生物对于治疗患有癌前病变的患者是有用的。这些化合物还可用于抑制肿瘤细胞的生长。

  公开号：

  US06060477A1

文献信息

• Methods and compositions for nucleic acid delivery
  申请人：Johns Hopkins University

  公开号：US20020094326A1

  公开（公告）日：2002-07-18

  The present provides methods and compositions that enable effective delivery of nucleic acids to desired cells, including to a solid organ such as a mammalian heart. The methods and compositions enable effective gene transfer and subsequent expression to a majority of cells throughout a solid organ such as the heart. Methods and compositions of the invention preferably provide enhanced vascular permeability that enables increased gene transfer to targeted cells, but without significant degradation or injury to endothelial cell layers.

  本文提供了一种方法和组合物，可以有效地将核酸传递到所需的细胞，包括哺乳动物心脏等固体器官。这些方法和组合物可以实现有效的基因转移，并随后在固体器官（如心脏）的大多数细胞中表达。本发明的方法和组合物最好提供增强的血管通透性，从而使基因转移到靶向细胞的数量增加，但不会对内皮细胞层造成显著的降解或损伤。
• Methods for prevention and treatment of gastrointestinal disorders
  申请人：——

  公开号：US20020128171A1

  公开（公告）日：2002-09-12

  Disclosed are methods for preventing or treating a gastrointestinal (GI) disorder in a mammal such as a human patient. In one embodiment, the methods include administering to the mammal a therapeutically effective amount of a compound that modulates a nitric oxide (NO) signaling pathway, particularly in GI neurons. Methods of the invention are particularly useful for the treatment (including prophylactic treatment) of diabetic gastropathies and other GI disorders.

  本发明涉及一种预防或治疗哺乳动物（例如人类患者）胃肠道（GI）疾病的方法。在一种实施例中，该方法包括向哺乳动物（特别是GI神经元）中投与治疗效果的化合物，该化合物调节一氧化氮（NO）信号通路的数量。本发明的方法对于治疗（包括预防性治疗）糖尿病性胃病和其他GI疾病特别有用。
• cGMP PDE 5 Inhibitors for inhalation in the treatment of sexual dysfunction
  申请人：——

  公开号：US20010055570A1

  公开（公告）日：2001-12-27

  Treatment of sexual dysfunction by inhalation of a cGMP PDE 5 inhibitor, especially 5-[2-ethoxy-5-(4-methylpiperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one, 4-phenylmethylamino-6-chloro-2-(1-imidazolyl) quinazoline, 4-phenylmethylamino-6-chloro-2-(3-pyridyl) quinazoline, 1,3-dimethyl-6-(2-propoxy-5-methanesulfonylamidophenyl)-1,5-dihydropyrazolo[3,4-d]pyrimidin-4-one or 1-cyclopentyl-3-ethyl-6-(3-ethoxy-4-pyridyl)-pyrazolo[3,4-d]pyrimidin-4-one.

  通过吸入cGMP PDE 5抑制剂治疗性功能障碍，特别是5-[2-乙氧基-5-(4-甲基哌嗪磺酰基)苯基]-1-甲基-3-正丙基-1,6-二氢-7H-吡唑并[4,3-d]嘧啶-7-酮、4-苯甲基氨基-6-氯-2-(1-咪唑基)喹唑啉、4-苯甲基氨基-6-氯-2-(3-吡啶基)喹唑啉、1,3-二甲基-6-(2-丙氧基-5-甲烷磺酰胺基苯基)-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮或1-环戊基-3-乙基-6-(3-乙氧基-4-吡啶基)-吡唑并[3,4-d]嘧啶-4-酮。
• cGMP PDE 5 inhibitors for inhalation in the treatment of sexual dysfunction
  申请人：——

  公开号：US20040214831A1

  公开（公告）日：2004-10-28

  Treatment of sexual dysfunction by inhalation of a cGMP PDE 5 inhibitor, especially 5-[2-ethoxy-5-(4-methylpiperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one, 4-phenylmethylamino-6-chloro-2-(1-imidazolyl) quinazoline, 4-phenylmethylamino-6-chloro-2-(3-pyridyl) quinazoline, 1,3-dimethyl-6-(2-propoxy-5-methanesulfonylamidophenyl)-1,5-dihydropyrazolo[3,4-d]pyrimidin-4-one or 1-cyclopentyl-3-ethyl-6-(3-ethoxy-4-pyridyl)-pyrazolo[3,4-d]pyrimidin-4-one.

  通过吸入cGMP PDE 5抑制剂治疗性功能障碍，特别是5-[2-乙氧基-5-(4-甲基哌嗪磺酰基)苯基]-1-甲基-3-正丙基-1,6-二氢-7H-吡唑并[4,3-d]嘧啶-7-酮，4-苯甲氨基-6-氯-2-(1-咪唑基)喹唑啉，4-苯甲氨基-6-氯-2-(3-吡啶基)喹唑啉，1,3-二甲基-6-(2-丙氧基-5-甲磺酰胺基苯基)-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮或1-环戊基-3-乙基-6-(3-乙氧基-4-吡啶基)-吡唑并[3,4-d]嘧啶-4-酮。
• Pyridopyrimidinone antianginal agents
  申请人：Pfizer Inc.

  公开号：US05591742A1

  公开（公告）日：1997-01-07

  Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl CN or CONR.sup.4 R.sup.5 ; R.sup.2 is C.sub.2 -C.sub.4 alkyl; R.sup.3 is SO.sub.2 NR.sup.6 R.sup.7, NO.sub.2, NH.sub.2, NHCOR.sup.8 NHSO.sub.2 R.sup.8 or N(SO.sub.2 R.sup.8).sub.2 ; R.sup.4 and R.sup.5 are each independently selected from H and C.sub.1 -C.sub.4 alkyl; R.sup.6 and R.sup.7 are each independently selected from H and C.sub.1 -C.sub.4 alkyl optionally substituted with CO.sub.2 R.sup.9, OH, pyridyl 5-isoxazolin-3-onyl, morpholino or 1-imidazolidin-2-onyl; or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino, 1-pyrazolyl or 4-(NR.sup.10)-1-piperazinyl group wherein any of said groups may optionally be substituted with one or two substituents selected from C.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.9, NH.sub.2 and OH; R.sup.8 is C.sub.1 -C.sub.4 alkyl or pyridyl; R.sup.9 is H or C.sub.1 -C.sub.4 alkyl; and R.sup.10 is H, C.sub.1 -C.sub.4 alkyl or (hydroxy) C.sub.2 -C.sub.3 alkyl; are selected cGMP PDE inhibitors useful in the treatment of, inter alia, cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis.

  化合物的公式为##STR1##以及药学上可接受的盐，其中R.sup.1是H，C.sub.1-C.sub.4烷基CN或CONR.sup.4 R.sup.5; R.sup.2是C.sub.2-C.sub.4烷基; R.sup.3是SO.sub.2 NR.sup.6 R.sup.7，NO.sub.2，NH.sub.2，NHCOR.sup.8 NHSO.sub.2 R.sup.8或N（SO.sub.2 R.sup.8）.sub.2; R.sup.4和R.sup.5各自独立地选自H和C.sub.1-C.sub.4烷基; R.sup.6和R.sup.7各自独立地选自H和C.sub.1-C.sub.4烷基，可选地被CO.sub.2 R.sup.9，OH，吡啶基5-异噁唑啉-3-酰基，吗啉或1-咪唑啉-2-酰基替代; 或与它们连接的氮原子一起形成吡咯啉基，哌啶基，吗啉，1-吡唑基或4-（NR.sup.10）-1-哌嗪基，其中任何所述基团都可以可选地被一个或两个选自C.sub.1-C.sub.4烷基，CO.sub.2 R.sup.9，NH.sub.2和OH的取代基所替代; R.sup.8是C.sub.1-C.sub.4烷基或吡啶基; R.sup.9是H或C.sub.1-C.sub.4烷基; R.sup.10是H，C.sub.1-C.sub.4烷基或（羟基）C.sub.2-C.sub.3烷基; 被选为cGMP PDE抑制剂，用于治疗心血管疾病，如心绞痛、高血压、心力衰竭和动脉硬化等。