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1. 发明申请

US20180318301A1 FORMULATIONS OF AZAINDOLE COMPOUNDS 审中-公开
公开(公告)号：US20180318301A1
公开(公告)日：2018-11-08
申请号：US16036044
申请日：2018-07-16
申请人： Vertex Pharmaceuticals Incorporated
发明人： Eric Arthur Simone , Tapan Sanghvi , Alamelu Banda , Katherine Stavropoulos
IPC分类号： A61K31/506 , A61K31/351 , A61K31/16 , A61K9/20 , A61K45/06 , A61K31/4965 , A61K31/497
CPC分类号： A61K31/506 , A61K9/2095 , A61K31/16 , A61K31/351 , A61K31/4965 , A61K31/497 , A61K45/06
摘要： A pharmaceutical composition comprises: a) 5 wt % to 95 wt % of a HCl salt of Compound (1).xH2O by the weight of the pharmaceutical composition, wherein x is from 0 to 3; and b) 5 wt % to 95 wt % of a filler by the weight of the pharmaceutical composition.Another pharmaceutical composition comprises: a) 1 mg/mL to 20 mg/mL of Compound (1) in water; and b) 0.01 M to 0.1 M of a pharmaceutically acceptable pH modifier. A method of preparing a pharmaceutical composition, comprising providing a mixture of Compound (1) that includes the HCl salt of Compound (1).xH2O and the filler. Another method of preparing a pharmaceutical composition comprises mixing the HCl salt of Compound-(1).xH2O and the pH modifier to form 1 mg/mL to 20 mg/mL of Compound (1) in water. Methods of reducing the amount of influenza viruses, inhibiting the replication of influenza viruses, and treating influenza each independently employ such pharmaceutical compositions.

2. 发明申请

US20160250213A1 FORMULATIONS OF AZAINDOLE COMPOUNDS 审中-公开
标题翻译：唑烷化合物的配方
公开(公告)号：US20160250213A1
公开(公告)日：2016-09-01
申请号：US15150497
申请日：2016-05-10
申请人： Vertex Pharmaceuticals Incorporated
发明人： Eric Arthur Simone , Tapan Sanghvi , Alamelu Banda , Katherine Stavropoulos
IPC分类号： A61K31/506 , A61K31/4965 , A61K31/16 , A61K31/351 , A61K9/20 , A61K45/06
CPC分类号： A61K31/506 , A61K9/2095 , A61K31/16 , A61K31/351 , A61K31/4965 , A61K31/497 , A61K45/06
摘要： A pharmaceutical composition comprises: a) 5 wt % to 95 wt % of a HCl salt of Compound (1).xH2O by the weight of the pharmaceutical composition, wherein x is from 0 to 3; and b) 5 wt % to 95 wt % of a filler by the weight of the pharmaceutical composition. Another pharmaceutical composition comprises: a) 1 mg/mL to 20 mg/mL of Compound (1) in water; and b) 0.01 M to 0.1 M of a pharmaceutically acceptable pH modifier. A method of preparing a pharmaceutical composition, comprising providing a mixture of Compound (1) that includes the HCl salt of Compound (1).xH2O and the filler. Another method of preparing a pharmaceutical composition comprises mixing the HCl salt of Compound (1).xH2O and the pH modifier to form 1 mg/mL to 20 mg/mL of Compound (1) in water. Methods of reducing the amount of influenza viruses, inhibiting the replication of influenza viruses, and treating influenza each independently employ such pharmaceutical compositions.
摘要翻译：药物组合物包含：a）药物组合物重量的5重量％至95重量％的化合物（1）的HCl盐，其中x为0至3; 和b）以药物组合物的重量计5重量％至95重量％的填料。另一药物组合物包括：a）1mg / mL至20mg / mL化合物（1）的水溶液; 和b）0.01M至0.1M的药学上可接受的pH调节剂。一种制备药物组合物的方法，包括提供化合物（1）的混合物，其包括化合物（1）的HCl盐与所述填充剂。制备药物组合物的另一种方法包括将化合物（1）xH 2 O的HCl盐与pH调节剂混合以在水中形成1mg / mL至20mg / mL的化合物（1）。减少流感病毒的数量，抑制流感病毒的复制，以及流感病毒各自独立地使用这种药物组合物的方法。

3. 发明申请

US20210008072A1 FORMULATIONS OF AZAINDOLE COMPOUNDS 有权
公开(公告)号：US20210008072A1
公开(公告)日：2021-01-14
申请号：US17038749
申请日：2020-09-30
申请人： Vertex Pharmaceuticals Incorporated
发明人： Eric Arthur Simone , Tapan Sanghvi , Alamelu Banda , Katherine Stavropoulos
IPC分类号： A61K31/506 , A61K45/06 , A61K31/497 , A61K9/20 , A61K31/16 , A61K31/351 , A61K31/4965
摘要： A pharmaceutical composition comprises: a) 5 wt % to 95 wt % of a HCl salt of Compound (1).xH2O by the weight of the pharmaceutical composition, wherein x is from 0 to 3; and b) 5 wt % to 95 wt % of a filler by the weight of the pharmaceutical composition. Another pharmaceutical composition comprises: a) 1 mg/mL to 20 mg/mL of Compound (1) in water; and b) 0.01 M to 0.1 M of a pharmaceutically acceptable pH modifier. A method of preparing a pharmaceutical composition, comprising providing a mixture of Compound (1) that includes the HCl salt of Compound (1).xH2O and the filler. Another method of preparing a pharmaceutical composition comprises mixing the HCl salt of Compound (1).xH2O and the pH modifier to form 1 mg/mL to 20 mg/mL of Compound (1) in water. Methods of reducing the amount of influenza viruses, inhibiting the replication of influenza viruses, and treating influenza each independently employ such pharmaceutical compositions.

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