3-(Hydroxymethyl)-6-nitro-2,3-dihydro-1,4-benzodioxin-5-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并二恶烷
• 英文名称: 3-(Hydroxymethyl)-6-nitro-2,3-dihydro-1,4-benzodioxin-5-ol
• 化学式: C9H9NO6
• 分子量: 227.17
• InChiKey: OVGRHQFLFKQEDH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  105
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• USE OF PHOSPHORDIESTERASE INHIBITORS IN THE TREATMENT OF PROSTATIC DISEASES
  申请人：——

  公开号：US20020025969A1

  公开（公告）日：2002-02-28

  The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy-phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline; g) 1-methyl-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo (3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy)-2 -carboxy-2,3-didehydro-chronan-4-one (FPL-557212) k) quinazolines and their trimethoxy derivatives; l) Pyrazolopyrimidones; as well as pharmacologically compatible salts thereof, quinazolines and their trimethoxy derivatives, pyrazolopyrimidones or compatible salts thereof, in local and systemic administration

  本发明涉及使用磷酸二酯酶 I、IV 和 V 抑制剂来预防和治疗前列腺疾病，特别是 使用以下药物 a) 2-(2-丙氧基苯基)-8-氮杂嘌呤-6-酮（扎普那司特）； b) 双嘧达莫 c) 1-(3-氯苯胺基)-4-苯基酞嗪（M5445） d) 2-(N-(4-羧基哌啶-6-氯-4-(3,4-(甲基内二氧基)苄基)氨基)喹唑啉（E 4021，ER 21355）； e) 2,3-二氢-8-羟基-7-硝基-1,4-苯并二恶烷-2-甲醇，α-硝酸盐（E 4701）； f) 4-((3,4-(甲基内二氧基)苄基)氨基)-6,7,8-三甲氧基喹唑啉； g) 1-甲基-3-丙基-6-(5-(N-(4-甲基吗啉基)磺酰基)-2-乙氧基苯基)吡唑[4,5]嘧啶-4(5H)one（西地那非） i) 1-环戊基-3-甲基-6-(4-吡啶基)吡唑并(3,4-d)嘧啶-4(5H)-酮(WIN 58237)； j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy)-2 -carboxy-2,3-didehydro-chronan-4-one (FPL-557212) k) 喹唑啉类及其三甲氧基衍生物； l) 吡唑嘧啶酮类； 喹唑啉类及其三甲氧基衍生物； l) 吡唑嘧啶酮类；以及它们的药理相容盐，喹唑啉类及其三甲氧基衍生物、吡唑嘧啶酮类或它们的相容盐，可局部和全身给药
• Use of phosphordiesterase inhibitors in the treatment of prostatic diseases
  申请人：Wolf-Georg Forssmann

  公开号：US20030199517A1

  公开（公告）日：2003-10-23

  The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy-phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxy-quinazoline; g) 1-methly-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo (3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy)-2-carboxy-2,3-didehydro-chronan-4-one (FPL-557212); k) quinazolines and their trimethoxy derivatives; l) Pyrazolopyrimidones; as well as pharmacologically compatible salts thereof, quinazolines and their trimethoxy derivatives, pyrazolopyrimidones or compatible salts thereof, in local and systemic administration.

  本发明涉及使用磷酸二酯酶 I、IV 和 V 抑制剂来预防和治疗前列腺疾病，特别是 使用以下药物 a) 2-(2-丙氧基苯基)-8-氮杂嘌呤-6-酮（扎普那司特）； b) 双嘧达莫 c) 1-(3-氯苯胺基)-4-苯基酞嗪（M5445） d) 2-(N-(4-羧基哌啶-6-氯-4-(3,4-(甲基内二氧基)苄基)氨基)喹唑啉（E 4021，ER 21355）； e) 2,3-二氢-8-羟基-7-硝基-1,4-苯并二恶烷-2-甲醇，α-硝酸盐（E 4701）； f) 4-((3,4-(甲基内二氧基)苄基)氨基)-6,7,8-三甲氧基-喹唑啉； g) 1-甲基-3-丙基-6-(5-(N-(4-甲基吗啉基)磺酰基)-2-乙氧基苯基)吡唑[4,5]嘧啶-4(5H)-1（西地那非） i) 1-环戊基-3-甲基-6-(4-吡啶基)吡唑并(3,4-d)嘧啶-4(5H)-酮(WIN 58237)； j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy)-2-carboxy-2,3-didehydro-chronan-4-one (FPL-557212); k) 喹唑啉类及其三甲氧基衍生物； l) 吡唑嘧啶酮类； 以及它们的药理相容盐、 l) 吡唑嘧啶酮；以及它们的药理相容盐，可局部或全身给药。
• US8106061B2
  申请人：——

  公开号：US8106061B2

  公开（公告）日：2012-01-31
• US8791124B2
  申请人：——

  公开号：US8791124B2

  公开（公告）日：2014-07-29
• [EN] USE OF PHOSPHORDIESTERASE INHIBITORS IN THE TREATMENT OF PROSTATIC DISEASES<br/>[FR] UTILISATION D'INHIBITEURS DE LA PHOSPHORDIESTERASE DANS LE TRAITEMENT DE MALADIES DE LA PROSTATE
  申请人：FORSSMANN, Wolf-Georg

  公开号：WO1999002161A1

  公开（公告）日：1999-01-21

  (EN) The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy- phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8- hydroxy-7-nitro-1, 4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy) benzyl)amino)-6, 7,8-trimethoxy-quinazoline; g) 1-methyl-3-propyl-6- (5-(N-(4-methylmorpholino) sulfonyl)-2-ethoxyphenyl)pyrazole [4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6- (4-pyridinyl)pyrazolo(3, 4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3- hydroxy-2-propyl-phenoxy) -2-hydroxy-propoxy)-2-carboxy-2, 3-didehydro-chronan-4-one (FPL-557212); k) quinazolines and their trimethoxy derivatives; l) Pyrazolopyrimidones; as well as pharmacologically compatible salts thereof, quinazolines and their trimethoxy derivatives, pyrazolopyrimidones or compatible salts thereof, in local and systemic administration.(FR) L'invention concerne l'utilisation d'inhibiteurs de la phosphordiestérase I, IV et V pour la prévention et le traitement de maladies de la prostate, plus particulièrement l'utilisation de a) 2- (2-propoxy-phényl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophénylamino)-4-phénylphtalazine (M5445); d) 2-(N-(4-carboxypipéridine-6-chloro-4-(3,4-(méthylène-dioxy)benzyl)amino)qinazoline (E 4021, ER 21355); e) 2,3-dihydro-8- hydroxy-7-nitro-1, 4-benzodioxine-2-méthanol, alpha-nitrate (E 4701); f) 4-((3,4-(méthylènedioxy) benzyl)amino)-6, 7,8-triméthoxy-quinazoline; g) 1-méthyl-3-propyl-6- (5-(N-(4-méthylmorpholino) sulfonyl)-2-éthoxyphényl)pyrazole [4,5]pyrimidine-4(5H)one (sildenafil); i) 1-cyclopentyl-3-méthyl-6- (4-pyridinyl)pyrazolo (3, 4-d)pyrimidine-4(5H)one (WIN 58237); j) 7-(3-(4-acétyl-3- hydroxy-2-propyl-phénoxy) -2-hydroxy-propoxy)-2-carboxy-2, 3-didéhydro-chromane-4-one (FPL-557212); k) quinazolines et leur dérivés triméthoxy; l) pyrazolopyrimidones; ainsi que leurs sels pharmaceutiquement compatibles, des quinazolines et leur dérivés triméthoxy, des pyrazolopyrimidones ou leurs sels compatibles pour une administration locale et par voie générale.