JP2016216377A5 - - Google Patents

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JP2016216377A5
JP2016216377A5 JP2015099697A JP2015099697A JP2016216377A5 JP 2016216377 A5 JP2016216377 A5 JP 2016216377A5 JP 2015099697 A JP2015099697 A JP 2015099697A JP 2015099697 A JP2015099697 A JP 2015099697A JP 2016216377 A5 JP2016216377 A5 JP 2016216377A5
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dry powder
powder inhaler
compound
formula
pulmonary fibrosis
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JP6915956B2 (en
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ヒトの肺線維症の治療のための方法において使用するための、式（I）
Figure 2016216377
 の化合物であって、
前記方法は、前記肺線維症を治療するのに有効な量の前記式（I）の化合物をヒトの肺組織の最も狭い部分に１日１回投与することを含む、化合物。 Formula (I) for use in a method for the treatment of human pulmonary fibrosis
Figure 2016216377
 A compound of
The method comprises administering once a day an amount of the compound of formula (I) effective to treat the pulmonary fibrosis to the narrowest part of human lung tissue. 前記式（I）の化合物は、遊離形態としてのビス（３−デオキシ−３−（３−フルオロフェニル−１Ｈ−１，２，３−トリアゾール−１−イル）−β−Ｄ−ガラクトピラノシル）スルファンである、請求項１に記載の化合物。   The compound of formula (I) is bis (3-deoxy-3- (3-fluorophenyl-1H-1,2,3-triazol-1-yl) -β-D-galactopyranosyl in free form 2. The compound of claim 1 which is sulfane. 前記肺線維症は特発性肺線維症（ＩＰＦ）である、請求項１又は２に記載の化合物。   The compound according to claim 1 or 2, wherein the pulmonary fibrosis is idiopathic pulmonary fibrosis (IPF). 前記投与は乾燥粉体吸入器によって行われる、請求項１〜３のいずれか１項に記載の化合物。   4. A compound according to any one of claims 1 to 3, wherein the administration is performed by a dry powder inhaler. 前記投与は、ＲＳ０１ Ｍｏｎｏｄｏｓｅ Ｄｒｙ Ｐｏｗｄｅｒ Ｉｎｈａｌｅｒ（Ｐｌａｓｔｉａｐｅ）等の単回投与用乾燥粉体吸入器よって行われる、請求項１〜４のいずれか１項に記載の化合物。   5. A compound according to any one of claims 1 to 4, wherein the administration is performed by a single dose dry powder inhaler such as RS01 Monodose Dry Powder Inhaler (Plastiape). 前記肺組織の最も狭い部分は細気管支及び肺胞である、請求項１〜５のいずれか１項に記載の化合物。   6. A compound according to any one of claims 1 to 5, wherein the narrowest parts of the lung tissue are bronchioles and alveoli. 前記１日１回量は０．１５〜５０ｍｇ、例えば０．１５〜１．５ｍｇ、１．５〜３ｍｇ、３〜５ｍｇ、５〜７ｍｇ、７〜８ｍｇ、８〜１０ｍｇ、１０〜２０ｍｇ、２０〜５０ｍｇである、請求項１〜６のいずれか１項に記載の化合物。   The daily dose is 0.15 to 50 mg, for example 0.15 to 1.5 mg, 1.5 to 3 mg, 3 to 5 mg, 5 to 7 mg, 7 to 8 mg, 8 to 10 mg, 10 to 20 mg, 20 to 20 mg. The compound according to any one of claims 1 to 6, which is 50 mg. 前記１日１回量は１．５〜１０ｍｇ、例えば３〜７ｍｇである、請求項７に記載の化合物。   8. A compound according to claim 7, wherein the once daily dose is 1.5 to 10 mg, for example 3 to 7 mg. 請求項１〜８のいずれか１項に記載の式（I）の化合物と、任意に薬学的に許容可能な添加剤とを含む、薬学的組成物。   9. A pharmaceutical composition comprising a compound of formula (I) according to any one of claims 1-8 and optionally a pharmaceutically acceptable additive. 式（I）
Figure 2016216377
 の化合物を備える乾燥粉体吸入器デバイスに関し、
前記乾燥粉体吸入器デバイスは、肺線維症を治療するのに有効な量の前記式（I）の化合物をヒトの肺組織の最も狭い部分に１日１回投与するためのものである、乾燥粉体吸入器デバイス。 Formula (I)
Figure 2016216377
 A dry powder inhaler device comprising:
The dry powder inhaler device is for once a day administration of an amount of the compound of formula (I) effective to treat pulmonary fibrosis to the narrowest part of human lung tissue; Dry powder inhaler device. 前記式（I）の化合物は、遊離形態としてのビス（３−デオキシ−３−（３−フルオロフェニル−１Ｈ−１，２，３−トリアゾール−１−イル）−β−Ｄ−ガラクトピラノシル）スルファンである、請求項１０に記載の乾燥粉体吸入器デバイス。   The compound of formula (I) is bis (3-deoxy-3- (3-fluorophenyl-1H-1,2,3-triazol-1-yl) -β-D-galactopyranosyl in free form 11. The dry powder inhaler device according to claim 10, which is a sulfane. 前記肺線維症は特発性肺線維症（ＩＰＦ）である、請求項１０又は１１に記載の乾燥粉体吸入器デバイス。   12. A dry powder inhaler device according to claim 10 or 11, wherein the pulmonary fibrosis is idiopathic pulmonary fibrosis (IPF). 前記デバイスは、ＲＳ０１ Ｍｏｎｏｄｏｓｅ Ｄｒｙ Ｐｏｗｄｅｒ Ｉｎｈａｌｅｒ（Ｐｌａｓｔｉａｐｅ）等の単回投与用乾燥粉体吸入器である、請求項１０〜１２のいずれか１項に記載の乾燥粉体吸入器デバイス。   13. The dry powder inhaler device according to any one of claims 10 to 12, wherein the device is a single dose dry powder inhaler such as RS01 Monodose Dry Powder Inhaler (Plastiape). 前記１日１回量は０．１５〜５０ｍｇ、例えば０．１５〜１．５ｍｇ、１．５〜３ｍｇ、３〜５ｍｇ、５〜７ｍｇ、７〜８ｍｇ、８〜１０ｍｇ、１０〜２０ｍｇ、２０〜５０ｍｇである、請求項１０〜１３のいずれか１項に記載の乾燥粉体吸入器デバイス。   The daily dose is 0.15 to 50 mg, for example 0.15 to 1.5 mg, 1.5 to 3 mg, 3 to 5 mg, 5 to 7 mg, 7 to 8 mg, 8 to 10 mg, 10 to 20 mg, 20 to 20 mg. 14. A dry powder inhaler device according to any one of claims 10 to 13 which is 50 mg. 前記１日１回量は１．５〜１０ｍｇ、例えば３〜７ｍｇである、請求項１４に記載の乾燥粉体吸入器デバイス。   15. A dry powder inhaler device according to claim 14, wherein the once daily dose is 1.5 to 10 mg, for example 3 to 7 mg. 前記肺組織の最も狭い部分は細気管支及び肺胞である、請求項１０〜１５のいずれか１項に記載の乾燥粉体吸入器デバイス。   16. A dry powder inhaler device according to any one of claims 10 to 15, wherein the narrowest parts of the lung tissue are bronchioles and alveoli.
JP2015099697A 2015-05-15 2015-05-15 Treatment of pulmonary fibrosis once daily Active JP6915956B2 (en)

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JP2016216377A JP2016216377A (en) 2016-12-22
JP2016216377A5 true JP2016216377A5 (en) 2018-05-17
JP6915956B2 JP6915956B2 (en) 2021-08-11

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104755088A (en) * 2012-10-31 2015-07-01 格莱克特生物技术公司 Galactoside inhibitor of galectin-3 and its use for treating pulmonary fibrosis

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