Title:
NOVEL SALT OF 4-(\{(4S)-1-(4-CARBAMIMIDOYLBENZOYL)-4-[4-(METHYLSULFONYL)PIPERAZIN-1-YL]-L-PROLYL\}AMINO)BENZOIC ACID, AND AND NOVEL CRYSTAL FORM OF SAID SALT
Document Type and Number:
WIPO Patent Application WO/2020/059812
Kind Code:
A1
Abstract:
4-(\{(4S)-1-(4-Carbamimidoylbenzoyl)-4-[4-(methylsulfonyl)piperazin-1-yl]-L-prolyl\}amino)benzoic acid di(4-toluenesulfonic acid) salt or dibenzenesulfonic acid salt or a crystal form of the salt has low hygroscopicity and excellent storage stability, and therefore can be used as a useful raw material for a medicine.
Inventors:
NISHIYAMA TAIHEI (JP)
NEKADO TAKAHIRO (JP)
NEKADO TAKAHIRO (JP)
Application Number:
PCT/JP2019/036806
Publication Date:
March 26, 2020
Filing Date:
September 19, 2019
Export Citation:
Assignee:
ONO PHARMACEUTICAL CO (JP)
International Classes:
C07D207/16; A61K31/40; A61P7/02; A61P9/10; A61P43/00
Domestic Patent References:
| WO2013174937A1 | 2013-11-28 | |||
| WO2013174937A1 | 2013-11-28 |
Foreign References:
| JP2015120685A | 2015-07-02 | |||
| JP2015120685A | 2015-07-02 | |||
| US5973188A | 1999-10-26 |
Other References:
STEPHEN M BERGE , LYLE D BIGHLEY , DONALD C MONKHOUSE: "Pharmaceutical Salts", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 66, no. 1, 1 January 1977 (1977-01-01), pages 1 - 19, XP002675560, ISSN: 0022-3549, DOI: 10.1002/jps.2600660104
"Kokei Seizai no seizo gijutsu ", 27 January 2003, CMC PUBLISHING CO., LTD, Tokyo JP, ISBN: 4-88231-783-4, article SHIOJI, YUSAKU: "Manufacture technology of solid tablet", pages: 9 - 4, XP009519792
BLOOD COAGULATION AND FIBRINOLYSIS, vol. 17, 2006, pages 251 - 257
SCIENCE, vol. 253, 1991, pages 909 - 912
BLOOD, vol. 102, 2003, pages 953 - 955
JOURNAL OF THROMBOSIS AND HAEMOSTASIS, vol. 3, 2005, pages 695 - 702
JOURNAL OF THROMBOSIS AND HAEMOSTASIS, vol. 4, 2006, pages 1496 - 1501
BLOOD, vol. 119, 2012, pages 2401 - 2408
BLOOD, vol. 113, 2009, pages 936 - 944
"Encyclopedia of Pharmaceutical Additives", 2000, YAKUJI NIPPO
"Kokei Seizai no seizo gijutsu ", 27 January 2003, CMC PUBLISHING CO., LTD, Tokyo JP, ISBN: 4-88231-783-4, article SHIOJI, YUSAKU: "Manufacture technology of solid tablet", pages: 9 - 4, XP009519792
BLOOD COAGULATION AND FIBRINOLYSIS, vol. 17, 2006, pages 251 - 257
SCIENCE, vol. 253, 1991, pages 909 - 912
BLOOD, vol. 102, 2003, pages 953 - 955
JOURNAL OF THROMBOSIS AND HAEMOSTASIS, vol. 3, 2005, pages 695 - 702
JOURNAL OF THROMBOSIS AND HAEMOSTASIS, vol. 4, 2006, pages 1496 - 1501
BLOOD, vol. 119, 2012, pages 2401 - 2408
BLOOD, vol. 113, 2009, pages 936 - 944
"Encyclopedia of Pharmaceutical Additives", 2000, YAKUJI NIPPO
Attorney, Agent or Firm:
AOKI, Atsushi et al. (JP)
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