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Semifluorinated compounds and their compositions

A composition, CH2 technology, applied in the direction of drug combination, drug delivery, halogenated hydrocarbon active ingredients, etc.

Active Publication Date: 2019-11-05
NOVALIQ GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, the formula CF 3 -(CF 2 ) 5 -CH(CH 3 )-(CH 2 ) 5 -CH 3 of semifluorinated alkanes and containing CF 3 (CF 2 ) 5 (CH 2 ) 7 CH 3 and CF 3 -(CF 2 ) 5 -CH(CH 3 )-(CH 2 ) 5 -CH 3 Compositions have not been described, especially for ophthalmic applications

Method used

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  • Semifluorinated compounds and their compositions
  • Semifluorinated compounds and their compositions
  • Semifluorinated compounds and their compositions

Examples

Experimental program
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Effect test

Embodiment

[0051] CF 3 -(CF 2 ) 5 -CH(CH 3 )-(CH 2 ) 5 -CH 3 (2-perfluorohexyl-octane, C 14 f 13 h 17 ) preparation

[0052] Compound CF 3 -(CF 2 ) 5 -CH(CH 3 )-(CH 2 ) 5 -CH 3 It can be prepared by radical addition of perfluorohexyl iodide to 1-octene in the presence of a radical initiator (this paper mixes perfluorohexyl iodide with 1-octene and a radical initiator which is AIBN, and the resulting solution was maintained at 80°C for 30 minutes and cooled), and then treated with a hydride (ie, LiAlH 4 ) or reduction of the resulting iodine adduct by hydrogenation (ie catalytic hydrogenation in the presence of a catalyst such as Pd / C) to form 2-perfluorohexyl-octane, which is then purified by fractional distillation.

[0053] CF 3 -(CF 2 ) 5 -CH(CH 3 )-(CH 2 ) 5 -CH 3 : 1 H-NMR (CDCl 3 ,400MHz):2.17-2.33(m,1H,CH),1.67-1.77(m,2H,CH 2 ),1.25-1.40(m,8H,CH 2 ),1.15(d,3H,CH 3 ),0.9(t,3H,CH 3 )

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Abstract

The present invention is directed to compositions comprising semifluorinated compounds and their use as medicaments for topical administration to the eye.

Description

[0001] This application is a divisional application of the invention application with the filing date of September 29, 2016, the application number of 201680056188.9, and the title of "semifluorinated compounds and their compositions". technical field [0002] The present invention is in the field of compositions comprising semifluorinated compounds and their use in ophthalmic administration. Background technique [0003] Semifluorinated alkanes are compounds comprising at least one non-fluorinated hydrocarbon segment and at least one perfluorinated hydrocarbon segment. Describes the general formula as CF 3 (CF 2 ) n (CH 2 ) m CH 3 straight-chain, unbranched semifluorinated alkanes, where n and m are integers representing the number of carbon atoms in each segment, for use in various applications, such as commercially for spreading and recoating the retina, as vitreous humor Long-term tamponade for surrogate (H. Meinert et al., European Journal of Ophthalmology, Vol. 1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/02A61P27/02
CPCA61K31/02A61P27/02A61K9/08A61K9/0048A61F9/0008A61K2300/00
Inventor 拉尔夫·格里伦恩伯杰弗兰克·洛施尔迪特尔·谢勒哈特穆特·沃斯
Owner NOVALIQ GMBH