5-{5-[4-(2-hydroxyethyl)piperazin-1-ylsulphonyl]-2-n-propoxyphenyl}-3-n-propyl-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-{5-[4-(2-hydroxyethyl)piperazin-1-ylsulphonyl]-2-n-propoxyphenyl}-3-n-propyl-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
• 英文别名: 5-{5-[4-(2-hydroxyethyl)piperazin-1-ylsulfonyl]-2-n-propoxyphenyl}-3-n-propyl-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one；5-[5-[4-(2-hydroxyethyl)piperazin-1-yl]sulfonyl-2-propoxyphenyl]-3-propyl-2-(pyridin-2-ylmethyl)-6H-pyrazolo[4,3-d]pyrimidin-7-one
• 化学式: C₂₉H₃₇N₇O₅S
• 分子量: 595.723
• InChiKey: DGERVXVPEYEJJF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  42
• 可旋转键数：
  12
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  151
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• 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。
• Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterase (cGMP-PDE5) for the treatment of sexual dysfunction
  申请人：Pfizer Inc

  公开号：US20040180944A1

  公开（公告）日：2004-09-16

  1 Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R 1 is C 1 to C 3 alkyl substituted with C 3 to C 6 cycloalkyl, CONR 5 R 6 or a N-linked heterocyclic group; (CH 2 ) n Het or (CH 2 ) n Ar, R 2 is C 1 to C 6 alkyl; R 3 is C 1 to C 6 alkyl optionally substituted with C 1 to C 4 alkoxy; R 4 is SO 2 NR 7 R 8 ; R 5 and R 6 are each independently selected from H and C 1 to C 4 alkyl optionally substituted with C 1 to C 4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R 7 and R 8 , together with the nitrogen atom to which they are attached, form a 4-R 10 -piperazinyl group; R 10 is H or C 1 to C 4 alkyl optionally substituted with OH, C 1 to C 4 alkoxy or CONH 2 ; Het is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.

  式（IA）和（IB）化合物或其药学上或兽医学上可接受的盐，或者是任一实体的药学上或兽医学上可接受的溶剂化合物，其中R1是C1到C3烷基，其上取代了C3到C6环烷基，CONR5R6或N-连接的杂环基；（CH2）nHet或（CH2）nAr，R2是C1到C6烷基；R3是C1到C6烷基，可选地取代了C1到C4烷氧基；R4是SO2NR7R8；R5和R6各自独立地选择自H和C1到C4烷基，可选地取代自C1到C4烷氧基，或者与它们所连接的氮原子一起形成一个5-或6-成员的杂环基；R7和R8与它们所连接的氮原子一起形成一个4-R10-哌嗪基团；R10是H或C1到C4烷基，可选地取代自OH、C1到C4烷氧基或CONH2；Het是可选地取代的C-连接的5-或6-成员的杂环基；Ar是可选地取代的苯基；n为0或1；这些化合物是强效和选择性的cGMP PDE5抑制剂，可用于治疗男性勃起功能障碍和女性性功能障碍等疾病。
• Pharmaceutical compositions for treating nitrate-induced tolerance
  申请人：Pfizer Limited

  公开号：EP1022026A2

  公开（公告）日：2000-07-26

  The present invention relates to methods for treating nitrate-induced tolerance in a mammal by administering a nitrate-induced tolerance treating amount of a compound of formulae (I), (II), (III) (IV), (V), (VI), (VII), (VIII), (IX), (XA) or (XB) as defined herein, or the pharmaceutically acceptable salts, prodrugs, polymorphs, hydrates, solvates, active metabolites or stereoisomers thereof. The invention also relates to pharmaceutical compositions for the treatment of nitrate-induced tolerance in a mammal comprising a nitrate-induced tolerance treating amount of a compound of formulae (I), (II), (III) (lV), (V), (VI), (VII), (VIII), (IX), (XA) or (XB) as defined herein, or the pharmaceutically acceptable salts, prodrugs, polymorphs, hydrates, solvates, active metabolites or stereoisomers thereof, and a pharmaceutically acceptable vehicle, diluent or carrier. The invention further relates to methods of preventing nitrate-induced tolerance in a mammal comprising administering a nitrate-induced tolerance preventing amount of a cGMP PDE inhibitor.

  本发明涉及通过施用本文定义的式(I)、(II)、(III)(IV)、(V)、(VI)、(VII)、(VIII)、(IX)、(XA)或(XB)化合物或其药学上可接受的盐、原药、多晶型物、水合物、溶解物、活性代谢物或立体异构体的硝酸盐诱导的耐受性治疗量来治疗哺乳动物的硝酸盐诱导的耐受性的方法。本发明还涉及用于治疗哺乳动物硝酸盐诱导耐受性的药物组合物，其包含硝酸盐诱导耐受性治疗量的式(I)、(II)、(III)(lV)、(V)、(VI)、(VII)、(VIII)、(IX)、(XA)或(XB)，或其药学上可接受的盐、原药、多晶型物、水合物、溶解物、活性代谢物或立体异构体，以及药学上可接受的载体、稀释剂或载体。本发明还涉及防止哺乳动物产生硝酸盐耐受性的方法，包括施用一定量的 cGMP PDE 抑制剂，以防止产生硝酸盐耐受性。
• PYRAZOLOPYRIMIDINONES WHICH INHIBIT TYPE 5 CYCLIC GUANOSINE 3',5'-MONOPHOSPHATE PHOSPHODIESTERASE (cGMP PDE5) FOR THE TREATMENT OF SEXUAL DYSFUNCTION
  申请人：Pfizer Limited

  公开号：EP0977756A1

  公开（公告）日：2000-02-09