Title:
POLYCRYSTALLINE MESYLATE OF PHOSPHODIESTERASE TYPE 5 INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/209809
Kind Code:
A1
Abstract:
The present application relates to a polycrystalline mesylate of a phosphodiesterase type 5 inhibitor. The chemical name of the phosphodiesterase type 5 inhibitor is 5-[2-ethoxy-5-(4-methylpiperazin-1-yl-thiocarbonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-thione. The polycrystalline mesylate of the phosphodiesterase type 5 inhibitor comprises diffraction peaks measured at the following 2θ reflection angles in an X-ray powder diffraction pattern: 7.1750° ± 0.2°, 7.6299° ± 0.2°, 8.8588° ± 0.2°, 13.2310° ± 0.2°, 14.3754° ± 0.2°, 14.8440 ± 0.2°, 15.2941° ± 0.2°, 17.1838° ± 0.2°, 20.0314° ± 0.2°, 20.8507° ± 0.2°, 21.2839° ± 0.2° , 21.7890° ± 0.2°, 22.2594° ± 0.2°, 23.0373 ± 0.2°, 25.1243° ± 0.2°, 25.4244° ± 0.2°, 26.1530° ± 0.2°, 28.1210° ± 0.2°, 30.0135° ± 0.2°, 31.4809° ± 0.2°, 32.3619° ± 0.2°, 37.2410° ± 0.2°, 37.6388° ± 0.2°, and 40.8286° ± 0.2°. The polycrystalline mesylate of the phosphodiesterase type 5 inhibitor not only improves drug activity, but also improves water solubility and bioavailability thereof, making up for the lack of research on crystalline drug forms of phosphodiesterase type 5 inhibitors.
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Inventors:
WANG JINGLIN (CN)
WANG JINGLIN (CN)
YU RUIMEI (CN)
LIAN QIONGQIONG (CN)
WANG JINGLIN (CN)
YU RUIMEI (CN)
LIAN QIONGQIONG (CN)
Application Number:
PCT/CN2017/094467
Publication Date:
November 22, 2018
Filing Date:
July 26, 2017
Export Citation:
Assignee:
WANG JINGLIN (CN)
International Classes:
A61K31/519; C07D487/04; A61P15/08; A61P15/10
Domestic Patent References:
| WO2005077374A1 | 2005-08-25 |
Foreign References:
| CN104650093A | 2015-05-27 | |||
| CN1240134A | 2000-01-05 | |||
| CN101343275A | 2009-01-14 |
Other References:
DA, YUANFENG ET AL.: "Study on the Synthesis Technology of Sildenafil Analogues", CHINA MODERN MEDICINE, vol. 21, no. 5, 28 February 2014 (2014-02-28), pages 15 - 17, XP055589330, ISSN: 1674-4721
PHILIPPE LEBEL ET AL.: "A rapid, quantitative liquid chromatography-mass spectrometry screening method for 71 active and 11 natural erectile dysfunction ingredients present in potentially adulterated or counterfeit products", JOURNAL OF CHROMATOGRAPHY A, vol. 1343, 4 April 2014 (2014-04-04), pages 143 - 151, XP028650189, ISSN: 0021-9673, DOI: doi:10.1016/j.chroma.2014.03.078
See also references of EP 3553060A4
PHILIPPE LEBEL ET AL.: "A rapid, quantitative liquid chromatography-mass spectrometry screening method for 71 active and 11 natural erectile dysfunction ingredients present in potentially adulterated or counterfeit products", JOURNAL OF CHROMATOGRAPHY A, vol. 1343, 4 April 2014 (2014-04-04), pages 143 - 151, XP028650189, ISSN: 0021-9673, DOI: doi:10.1016/j.chroma.2014.03.078
See also references of EP 3553060A4
Attorney, Agent or Firm:
JINAN SHENGDA INTELLECTUAL PROPERTY AGENCY CO.,LTD (CN)
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