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Glukopyranosyloxypyrazolový derivát a farmaceutická kompozice s jeho obsahem a benzylpyrazolový meziprodukt
专利权人:
LTD.;KISSEI PHARMACEUTICAL CO.
发明人:
FUJIKURA HIDEKI,NISHIMURA TOSHIHIRO,KATSUNO KENJI,HIRATOCHI MASAHIRO,IYOBE AKIRA,FUJIOKA MINORU,ISAJI MASAYUKI
申请号:
CZ2002665
公开号:
CZ303372B6
申请日:
2000.08.24
申请国别(地区):
CZ
年份:
2012
代理人:
摘要:
Glukopyranosyloxypyrazolový derivát vzorce I, kde R.sup.1.n. je H nebo C.sub.1-6.n.alkyl; jeden ze symbolu Q.sup.1.n. a T.sup.1.n. je skupina vzorce A, zatímco druhý je C.sub.1-6.n.alkyl nebo halogen(C.sub.1-6.n.alkyl); a R.sup.2.n. je H, C.sub.1-6.n.alkyl, C.sub.1-6.n.alkoxy, C.sub.1-6.n.alkylthio, halogen(C.sub.1-6.n.alkyl) s 1 až 3 stejnými nebo ruznými atomy halogenu, nebo atom halogenu nebo jeho farmaceuticky prijatelná sul. Farmaceutická kompozice s obsahem tohoto derivátu a její použití jako inhibitoru lidského SGLT2 nebo pro prevenci nebo lécení diabetes nebo obezity. Benzylpyrazolový meziprodukt vzorce Va, kde R.sup.2.n.´ je C.sub.1-6.n.alkyl, C.sub.1-6.n.alkoxy, C.sub.1-6.n.alkylthio, halogen(C.sub.1-6.n.alkyl) s 1 až 3 stejnými nebo ruznými atomy halogenu, nebo atom halogenu a R.sup.3´.n. je C.sub.1-6.n.alkyl, nebo jeho sul.The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula I in which Re1 represents a hydrogen atom or an alkyl group containing 1 to 6 carbon atoms; one of the Qe1 and Te1 symbols represents a group represented by the general formula A, while the other represents an alkyl group containing 1 to 6 carbon atoms or a haloalkyl group having 1 to 6 carbon atoms in the alkyl moiety; and Re2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group containing 1 to 6 carbon atoms, an alkylthio group having 1 to 6 carbon atoms, a haloalkyl group containing 1 to 6 carbon atoms in the alkyl moiety and 1 to 3 identical or different halogen atoms, or with a halogen atom or a pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition containing the above-described derivative as well as its use as human SGLT2 inhibitor or for the treatment of diabetes mellitus or obesity. Also disclosed is a benzylpyrazole intermediate of the general formula Va in which Re2 represents an alkyl group containing 1 to 6 carbon atoms, an alkoxy group h
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