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    • 6. 发明授权
    • Pyrazine derivatives, their preparation and medicaments containing them
    • 吡嗪衍生物,其制剂和含有它们的药物
    • US06399613B1
    • 2002-06-04
    • US09483984
    • 2000-01-14
    • Georges BashiardesJean-Christophe CarryMichel EversBruno FilocheSerge Mignani
    • Georges BashiardesJean-Christophe CarryMichel EversBruno FilocheSerge Mignani
    • A61K3150
    • C07D213/81C07D213/38C07D213/82C07D241/12C07D241/24
    • The invention concerns pyrazine derivatives of formula (1) in which a pharmaceutical composition comprising at least one compound of formula: in which R represents a nitrogen atom, R1 and R3 each represent the same radical selected from the group consisting of —CO—NR5R6, —CO—N(CH(CH2OH)2)2, —CO—N(CH2OH)2, —CO—N(CH2—CH(CH2OH)2)2, —CO—N(CH2—(CHOH)n—CH2OH)2 in which n is equal to 0, 1, 2, 3 or 4, —CH2—O—R6, —NR5—CO—R6, —CH2—NR5R6, —CH2—N(CH2OH)2, —CH2—N(CH2—(CHOH)y—CH2OH)2 in which y is equal to 0, 1, 2, 3 or 4, —CH2—N(CH(CH2OH)2)2 and —CH2—N(CH2—CH(CH2OH)2)2 and R2 and R4 each represents a hydrogen atom, R5 represents a hydrogen atom or an alkyl radical, R6 represents a radical —CH2—(CHOH)m—CH2OH in which m is equal to 0, 1, 2, 3 or 4, -alk-O-alk-CH2OH, -alk-O-alk, —CH(CH2OH)2, —C(CH2OH)3, —C(CH3) (CH2OH)2, —CH2—CH(CH2OH)2 or —CH(CH2OH)—(CHOH)x—CH2OH in which x is equal to 1, 2, 3 or 4, alk represents an alkyl radical, the alkyl radicals containing, unless otherwise stated, 1 to 6 carbon atoms in a straight or branched chain, stereoisomers thereof and salts thereof with an inorganic or organic acid and their preparation.
    • 本发明涉及式(1)的吡嗪衍生物,其中包含至少一种下式的化合物的药物组合物:其中R表示氮原子,R1和R3各自表示选自-CO-NR5R6, - CO-N(CH(CH 2 OH)2)2,-CO-N(CH 2 OH)2,-CO-N(CH 2 -CH(CH 2 OH)2)2,-CO-N(CH 2 - (CHOH)n -CH 2 OH) 2,其中n等于0,1,2,3或4,-CH 2 -O-R 6,-NR 5 -CO-R 6,-CH 2 -NR 5 R 6,-CH 2 -N(CH 2 OH)2,-CH 2 -N( CH 2 - (CHOH)y -CH 2 OH)2,其中y等于0,1,2,3或4,-CH 2 -N(CH(CH 2 OH)2)2和-CH 2 -N(CH 2 -CH(CH 2 OH) 2)2,R 2和R 4各自表示氢原子,R 5表示氢原子或烷基,R 6表示基团-CH 2 - (CHOH)m -CH 2 OH,其中m等于0,1,2,3或 4,-alk-O-烷基-CH 2 OH,-OCO-烷基,-CH(CH 2 OH)2,-C(CH 2 OH)3,-C(CH 3)(CH 2 OH)2,-CH 2 -CH(CH 2 OH)2 或-CH(CH 2 OH) - (CHOH)x-CH 2 OH,其中x等于1,2,3或4,alk表示烷基,除非另有说明,烷基含有1至6个碳原子 其直链或支链的立体异构体和其与无机或有机酸的盐及其制备方法。
    • 9. 发明授权
    • Polyhydroxyalkylpyrazine derivatives, their preparation and the medicaments comprising them
    • 聚羟基烷基吡嗪衍生物,其制备方法和包含它们的药物
    • US06362185B1
    • 2002-03-26
    • US09483939
    • 2000-01-14
    • Georges BashiardesJean-Christophe CarryMichel EversBruno FilocheSerge Mignani
    • Georges BashiardesJean-Christophe CarryMichel EversBruno FilocheSerge Mignani
    • A61K314965
    • A61K31/495C07D241/12
    • The present invention relates to medicaments comprising at least one compound of formula: wherein either R1 represents a —CH(Ra)—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 represents a —CHOH—CHF—CHOH—CH2OH chain and R2 represents a —CH2—CHF—CHOH—CH2OH chain, or R1 represents a —CHOH—CHOH—CHOH—Rb chain and R2 represents a —CH2—CHOH—CHOH—Rb chain, or R1 represents a —CH2—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 and R2 are identical and each represent a —(CHOH)n—CH2OH chain in which n is equal to 1, 2, 3 or 4, Ra represents an alkoxy radical (1-6 C in a straight or branched chain) or a fluorine atom, and Rb represents a carboxyl, —CO—NH2 or —CH2—NH2 radical, or one of their stereoisomers or their salts with an inorganic or organic acid, to novel compounds of formula (I) and to their preparation.
    • 本发明涉及包含至少一种下式的化合物的药物:其中R1表示-CH(Ra)-CHOH-CHOH-CH2OH链,R2表示-CH2-CHOH-CHOH-CH2OH链,或R1表示-CHOH- CHF-CHOH-CH2OH链,R2表示-CH2-CHF-CHOH-CH2OH链,或R1表示-CHOH-CHOH-CHOH-Rb链,R2表示-CH2-CHOH-CHOH-Rb链,或R1表示 -CH 2 -CHOH-CHOH-CH 2 OH链,R 2表示-CH 2 -CHOH-CHOH-CH 2 OH链,或R 1和R 2相同,各自表示其中n等于1的 - (CHOH)n -CH 2 OH链, 2,3或4中,Ra表示烷氧基(直链或支链中1-6C)或氟原子,Rb表示羧基,-CO-NH2或-CH2-NH2基,或其立体异构体或 它们与无机或有机酸的盐,与式(I)的新型化合物及其制备。