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2 - [[[2 -[(HYDROXYACETYL) AMINO]- 4 -PYRIDINYL] METHYL]THIO]- N -[4 - (TRIFLUOROMETHOXY) PHENYL]- 3 -PYRIDINECARBOXAMIDE BENZENE-SULFONATE, CRYSTAL OF SAME, POLYMORPH THEREOF, AND PROCESSES FOR PRODUCTION THEREOF
专利权人:
SANTEN PHARMACEUTICAL CO.; LTD.
发明人:
NIWA, MASASHI,DEGUCHI, HIROSHI
申请号:
MYPI 2011006369
公开号:
MY157122A
申请日:
2010.07.16
申请国别(地区):
MY
年份:
2016
代理人:
摘要:
IN THE DEVELOPMENT OF 2-[[[2-[(HYDROXYACETYL) AMINO]-4-PYRIDINYL]METHYL]THIO]-N-[4-(TRIFLUOROMETHOXY)PHENYL]-3-PYRIDINECARBOXAMIDE (COMPOUND A)), THERE EXIST SEVERAL COMPLEX PROBLEMS: (1) COMPOUND (A) OR SALTS THEREOF ARE DIFFICULT OF RECRYSTALLIZATION, SAID SALTS BEING CONSIDERABLY DIFFERENT IN STORAGE STABILITY, AND IT IS VERY DIFFICULT TO OBTAIN A SALT OF COMPOUND (A) HAVING HIGH STORAGE STABILITY; (2) IN THE CRYSTALLIZATION PROCESS OF COMPOUND (A), THE CONTROL OF POLYMORPHISM IS VERY DIFFICULT; (3) COMPOUND (A) (IN THE FREE FORM) CAUSES MINERAL DEPOSITION IN THE STOMACH WHEN ORAL- ADMINISTERED REPEATEDLY; AND SO ON. IN ORDER TO SOLVE THE PROBLEMS, STUDIES HAVE BEEN MADE WITH ATTENTION BEING PAID TO THE KINDS OF SALTS. AS A RESULT, IT HAS BEEN FOUND THAT BENZENSULFONATE (SALT) OF COMPOUND (A) HAS THE FOLLOWING PROPERTIES: (1) IN A ONE-WEEK PRELIMINARY STABILITY TEST (SEVERE TEST), BENZENSULFONATE OF COMPOUND (A) IS NOT DECOMPOSED BY LIGHT, HUMIDITY, OR OTHER FACTORS, THUS BEING UNPROBLEMATIC IN STORAGE STABILITY; (2) TWO KINDS OF CRYSTAL FORMS ARE PRSENT, AND THE CRYSTAL FORMS CAN BE SELECTIVELY PRODUCED BY A CERTAIN METHOD; AND (3) NO MINERAL DEPOSITION IN THE STOMACH IS OBSERVED EVEN AFTER FOUR-WEEK REPEATED ORAL ADMINISTRATION.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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