CN1953749A - 1-(取代苯基)-5-甲基-2-(1h)吡啶酮(ⅰ)化合物用于制备抗器官或组织纤维化药物的应用 - Google Patents
1-(取代苯基)-5-甲基-2-(1h)吡啶酮(ⅰ)化合物用于制备抗器官或组织纤维化药物的应用 Download PDFInfo
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Abstract
Description
Claims (7)
- 权利 要 求1. 1- (取代苯基) -5-甲基 -2- (1H) 卩¾定酮(I)化合物用于制备抗器官或组织纤维化的 药物的应用;当 n=l时, 所述的取代基 R表示 F、 Cl、 Br、 I、 硝基、 垸基、 氧代烷基、 卤代垸 当 n=2时, 所述的取代基 R表示 F、 Cl、 Br、 I, 烷基、 氧代垸基、 卤代烷基。2、 根据权利要求 1所述的化合物在制备抗器官或组织纤维化药物的应用, 其特征在于 其中当 n=l时, R=F、 Br、 I; 当 n=2时, R=F、 Cl、 Br、 I, 饱和直链烃基, 氧代饱和 直链烃基、 卤代饱和直链烃基; R取代基在苯环上的位置具有邻位、 间位或对位。
- 3、根据权利要求 2所述的化合物在制备抗器官或组织纤维化药物的应用,其特征在于: 式 (I)的 1 -取代苯基 -5-甲基 -2 (1H) 吡啶酮中, n= l, R = Br, 如:1 - ( 2-溴苯基) -5-甲基 -2- (1H) Π比啶酮;1 - ( 3-溴苯基) -5-甲基 -2- (1H) 卩比啶酮;1 - ( 4-溴苯基) -5-甲基 -2- (1H) 吡啶酮; 或式 (I)的 1-取代苯基 -5-甲基 -2 (1H) 吡啶酮中, n= l, R=F, 如:1 - ( 2-氟苯基) -5-甲基 -2- (1H) 吡啶酮;1 - ( 3-氟苯基) -5-甲基 -2- (1H) 吡啶酮;1 - ( 4-氟苯基) -5-甲基 -2- (1H) 吡啶酮; 或式 (I)的 1 -取代苯基 -5-甲基 -2 (1H) 吡啶酮中, n= l, R=I, 如:1 - ( 2-碘苯基) -5-甲基 -2- (1H) 口比啶酮;1 - ( 3-碘苯基) -5-甲基 -2- (1H) 吡啶酮;1 - ( 4-碘苯基) -5-甲基 -2- (1H) 吡啶酮; 或式 (I)的 1 -取代苯基 -5-甲基 -2 (1H) 吡啶酮中, n= 2 , R=F、 Br或 Cl, 如:1 - (2,3-二溴苯基) -5 -甲基 -2 (1H) 吡啶酮;1 - (2,4-二溴苯基) -5 -甲基 -2- (1H) 吡啶酮;1 - (2,5-二溴苯基) -5 -甲基 -2- (1H) 吡啶酮;1 - (2,6-二溴苯基) -5 -甲基 -2- (1H) 吡啶酮;1 - (3,4-二溴苯基) -5 -甲基 -2- (1H) 吡啶酮;1- (3,5-二溴苯基) -5 -甲基 -2- (1H) 吡啶酮;1 - (2,3-二氯苯基) -5 -甲基 -2- (1H) 吡啶酮;1 - (2,4-二氯苯基) - 5 -甲基 -2- (1H) 吡啶酮;1 - (2,5-二氯苯基) -5 -甲基 -2- (1H) 吡啶酮;1 - (2,6-二氯苯基) -5 -甲基 -2- (1H) 吡啶酮;1 - (3,5-二氯苯基) -5 -甲基 -2_ (1H) 吡啶酮; 1- (2,3-二氟苯基) -5-甲基 -2- (1H)吡啶酮;1- (2,4-二氟苯基) -5-甲基 -2- (1H)吡啶酮;1- (2,5-二氟苯基) -5-甲基 -2- (1H)吡啶酮;1- (2,6-二氟苯基) -5-甲基 -2- (1H) 吡啶酮;1- (3,5-二氟苯基) -5-甲基 -2- (1H)吡啶酮; 或式 (I)的 1-取代苯基 -5-甲基 -2 (1H)吡啶酮中, n=l或 2, R=三氟甲基, 如:1- (2-三氟甲基苯基) -5-甲基 -2- (1H)吡啶酮;1- (4-三氟甲基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,3-三氟甲基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,4-三氟甲基苯基) -5-甲基 -2- (1H)吡啶酮;1- (2,5-三氟甲基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,6-三氟甲基苯基) -5-甲基 -2- (1H)吡啶酮;1- (3,4-三氟甲基苯基) -5國甲基 -2- (1H) 吡啶酮;1- (2,5-三氟甲基苯基) -5-甲基 -2- (1H)吡啶酮; 或式 (I)的 1-取代苯基 -5-甲基 -2 (1H)吡啶酮中, n=l或 2, R =甲基, 如:1- (2-甲基苯基) -5-甲基 -2- (1H)吡啶酮;1- (3-甲基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,3-二甲基苯基) -5-甲基 -2- (1H)吡啶酮;1- (2,4-二甲基苯基) -5-甲基 -2- (1H)吡啶酮;1- (2,5-二甲基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,6-二甲基苯基) -5-甲基 -2- (1H)吡啶酮;1- (3,4-二甲基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,5-二甲基苯基) -5-甲基國2- (1H)吡啶酮; 或式 (I)的 1-取代苯基 -5-甲基 -2 (1H)吡啶酮中, n=l或 2, 11 =甲氧基, 如:1- (2-甲氧基苯基) -5-甲基 -2- (1H)吡啶酮;1- (3-甲氧基苯基) -5-甲基 -2- (1H)吡啶酮;1- (2,3-二甲氧基苯基) -5-甲塞 -2- (1H)吡啶酮;1- (2,4-二甲氧基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,5-二甲氧基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (2,6-二甲氧基苯基) -5-甲基 -2- (1H)吡啶酮;1- (3,4-二甲氧基苯基) -5-甲基 -2- (1H) 吡啶酮;1- (3,5-二甲氧基苯基) -5-甲基 -2- (1H)吡啶酮。 '
- 4、 根据权利要求 3所述的化合物在制备抗器官或组织纤维化药物的应用, 其特征在于 优选 R为 3 -氟。
- 5、 根据权利要求 1或 2所述的化合物在制备抗器官或组织纤维化药物中的应用, 其特 征在于所说的垸基是直链或支链的具有 1-6个碳原子数的烷基, 优选 1-4个碳原子。 6、 根据权利要求 1至 5之一所述的应用, 其特征在于所说的纤维化是肾小球硬化、 肾 间质纤维化、 肝纤维化、 肺纤维化、 腹膜纤维化、 心肌纤维化、 皮肤纤维化、 手术后粘 连、 良性前列腺肥大症、 骨骼肌纤维化、 硬皮病、 阿尔茨海默病、 血管纤维化疾病。 7、 根据权利要求 6所述的应用, 其特征在于所说的肾小球硬化是由于糖尿病引起的病 变。
- 8、 根据权利要求 6所述的应用, 其特征在于所说的肾间质纤维化是由于输尿管梗阻或 糖尿病引起的病变。
- 9、 根据权利要求 6所述的应用, 其特征在于所说的肝纤维化是由于血吸虫病引起的病 变。
- 10、 根据权利要求 1~9之一所述的应用, 其特征在于给药方式为所说的化合物口服、 注射或外用给药; 或与药用辅料及其它药物做成适当的形式给药。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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CNA2005100314457A CN1846699A (zh) | 2005-04-13 | 2005-04-13 | 1-(取代苯基)-5-甲基-2-(1h) 吡啶酮(i)化合物用于制备抗除肾间质纤维化外其他器官纤维化或组织纤维化药物的应用 |
CN200510031445.7 | 2005-04-13 | ||
PCT/CN2006/000651 WO2006108354A1 (fr) | 2005-04-13 | 2006-04-11 | 5-méthyl-2-(1h)-pyridone substituée en 1 par un groupement phényle dans la fabrication de médicaments pour le traitement de la fibrose d'organes ou de tissus |
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CN1953749A true CN1953749A (zh) | 2007-04-25 |
CN1953749B CN1953749B (zh) | 2010-04-14 |
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CNA2005100314457A Pending CN1846699A (zh) | 2005-04-13 | 2005-04-13 | 1-(取代苯基)-5-甲基-2-(1h) 吡啶酮(i)化合物用于制备抗除肾间质纤维化外其他器官纤维化或组织纤维化药物的应用 |
CN2006800002161A Active CN1953749B (zh) | 2005-04-13 | 2006-04-11 | 1-(取代苯基)-5-甲基-2-(1h)吡啶酮(ⅰ)化合物用于制备抗器官或组织纤维化药物的应用 |
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CNA2005100314457A Pending CN1846699A (zh) | 2005-04-13 | 2005-04-13 | 1-(取代苯基)-5-甲基-2-(1h) 吡啶酮(i)化合物用于制备抗除肾间质纤维化外其他器官纤维化或组织纤维化药物的应用 |
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US (3) | US20090005424A9 (zh) |
EP (1) | EP1878428A4 (zh) |
JP (1) | JP2008535871A (zh) |
KR (1) | KR20080018857A (zh) |
CN (2) | CN1846699A (zh) |
AU (1) | AU2006233433A1 (zh) |
CA (1) | CA2603763A1 (zh) |
RU (1) | RU2007141892A (zh) |
TW (1) | TW200808315A (zh) |
WO (1) | WO2006108354A1 (zh) |
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CN113274389A (zh) * | 2021-07-09 | 2021-08-20 | 中南大学 | 氟非尼酮在制备治疗急性肺损伤药物中的应用 |
CN114716365A (zh) * | 2022-01-04 | 2022-07-08 | 大连理工大学 | 一类n-取代苯基-2-吡啶酮化合物或其可药用盐在治疗肺纤维化中的应用 |
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US7825133B2 (en) | 2003-11-14 | 2010-11-02 | Shanghai Genomics, Inc. | Derivatives of pyridone and the use of them |
CN1846699A (zh) * | 2005-04-13 | 2006-10-18 | 中南大学湘雅医院 | 1-(取代苯基)-5-甲基-2-(1h) 吡啶酮(i)化合物用于制备抗除肾间质纤维化外其他器官纤维化或组织纤维化药物的应用 |
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2005
- 2005-04-13 CN CNA2005100314457A patent/CN1846699A/zh active Pending
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2006
- 2006-04-11 JP JP2008505716A patent/JP2008535871A/ja active Pending
- 2006-04-11 AU AU2006233433A patent/AU2006233433A1/en not_active Abandoned
- 2006-04-11 KR KR1020077018590A patent/KR20080018857A/ko not_active Application Discontinuation
- 2006-04-11 WO PCT/CN2006/000651 patent/WO2006108354A1/zh active Application Filing
- 2006-04-11 EP EP06722303A patent/EP1878428A4/en not_active Withdrawn
- 2006-04-11 RU RU2007141892/15A patent/RU2007141892A/ru not_active Application Discontinuation
- 2006-04-11 CN CN2006800002161A patent/CN1953749B/zh active Active
- 2006-04-11 CA CA002603763A patent/CA2603763A1/en not_active Abandoned
- 2006-08-04 TW TW095128659A patent/TW200808315A/zh unknown
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2008
- 2008-09-04 US US12/204,629 patent/US20080319027A1/en not_active Abandoned
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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CN113274389A (zh) * | 2021-07-09 | 2021-08-20 | 中南大学 | 氟非尼酮在制备治疗急性肺损伤药物中的应用 |
CN114716365A (zh) * | 2022-01-04 | 2022-07-08 | 大连理工大学 | 一类n-取代苯基-2-吡啶酮化合物或其可药用盐在治疗肺纤维化中的应用 |
CN114716365B (zh) * | 2022-01-04 | 2024-03-01 | 大连理工大学 | 一类n-取代苯基-2-吡啶酮化合物或其可药用盐在治疗肺纤维化中的应用 |
Also Published As
Publication number | Publication date |
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CA2603763A1 (en) | 2006-10-19 |
KR20080018857A (ko) | 2008-02-28 |
JP2008535871A (ja) | 2008-09-04 |
AU2006233433A1 (en) | 2006-10-19 |
US20090005424A9 (en) | 2009-01-01 |
EP1878428A1 (en) | 2008-01-16 |
TW200808315A (en) | 2008-02-16 |
WO2006108354A1 (fr) | 2006-10-19 |
RU2007141892A (ru) | 2009-05-20 |
CN1953749B (zh) | 2010-04-14 |
CN1846699A (zh) | 2006-10-18 |
US20070203203A1 (en) | 2007-08-30 |
EP1878428A4 (en) | 2008-09-03 |
US20090258911A1 (en) | 2009-10-15 |
US20080319027A1 (en) | 2008-12-25 |
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