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    • 7. 发明授权
    • Oligosaccharide aromatic glycoside and sulfate thereof
    • 寡糖芳香糖苷及其硫酸盐
    • US5498602A
    • 1996-03-12
    • US944077
    • 1992-09-11
    • Tadao ShojiNahoko TakahashiNaoya IkushimaToshiyuki UryuTakashi YoshidaNaoki YamamotoHideki NakashimaKaname KatsurayaKoichiro AdachiFusayo Kataoka
    • Tadao ShojiNahoko TakahashiNaoya IkushimaToshiyuki UryuTakashi YoshidaNaoki YamamotoHideki NakashimaKaname KatsurayaKoichiro AdachiFusayo Kataoka
    • A61K31/70A61K31/7028A61K31/7034A61P31/12A61P31/18C07H15/203C08B37/00C07G3/00C07H11/00
    • C07H15/203C08B37/006
    • Oligosaccharide aromatic glycoside sulfates and physiologically acceptable salts thereof, are disclosed. Further, antiviral agents having these sulfate compounds as the active components, and particularly an antiviral agent, wherein the virus is one which causes AIDS (Acquired Immune Deficiency Syndrome), are disclosed. The active components or the glycoside sulfates, and the salts thereof, are characterized by an oligosaccharide aromatic glycoside sulfate in which the hydrogen of the position-1 hydroxyl group of the terminal sugar of an oligosaccharide is substituted with a specified formula having an alkyl group consisting of 1 to 18 carbons, an oxygen or no oxygen, and an allylene group. The number of constituent monosaccharides in the oligosaccharide portion is preferably within a range of 2 to 20. Further, 10% or more of the remaining hydroxyl groups of the sugar subunits are subjected to sulfated esterification. In addition the antiviral agent exhibits low toxicity and is useful in the treatment of AIDS. Furthermore, an oligosaccharide is also disclosed as described above with the exception that it is the hydrogen atom of the position 1 hydrogen group at the terminal sugar residue which is substituted with the specified formula, also described above. However, in addition the remaining hydroxyl groups of the sugar portion of this oligosaccharide are protected by acyl groups or are present in an unprotected form. Also disclosed is a method for the production of an oligosaccharide aromatic glycoside sulfate synthesized by sulfation using a sulfating agent.
    • 公开了寡糖芳香糖苷硫酸盐及其生理上可接受的盐。 此外,公开了具有这些硫酸盐化合物作为活性成分的抗病毒剂,特别是其中病毒是引起AIDS(获得性免疫缺陷综合征)的抗病毒剂。 活性成分或糖苷硫酸盐及其盐的特征在于寡糖芳香糖苷硫酸盐,其中寡糖末端糖的位置1羟基的氢被具有烷基的特定式所取代, 1至18个碳,氧或无氧,以及烯丙基。 寡糖部分中的构成单糖的数量优选在2〜20的范围内。此外,将糖亚基的剩余羟基的10%以上进行硫酸化酯化。 此外,抗病毒剂的毒性低,可用于治疗艾滋病。 此外,还公开了如上所述的寡糖,不同之处在于它是上述也被指定式取代的末端糖残基上的1位氢原子的氢原子。 然而,此外,该寡糖的糖部分的剩余羟基由酰基保护或以未保护的形式存在。 还公开了通过使用硫酸化剂硫酸化合成的寡糖芳香族糖苷硫酸盐的制造方法。
    • 8. 发明授权
    • Piperidine derivative and pharmaceutical composition containing the same
    • 哌啶衍生物和含有其的药物组合物
    • US5179095A
    • 1993-01-12
    • US798963
    • 1991-11-26
    • Hitoshi OinumaMotosuke YamanakaKazutoshi MiyakeTomonori HoshikoNorio MinamiTadao ShojiYoshiharu DaikuKohei SawadaKenichi Nomoto
    • Hitoshi OinumaMotosuke YamanakaKazutoshi MiyakeTomonori HoshikoNorio MinamiTadao ShojiYoshiharu DaikuKohei SawadaKenichi Nomoto
    • C07D211/28C07D401/04C07D401/06C07D401/14C07D405/04C07D409/04C07D417/04C07D471/04C07D473/10
    • C07D401/04C07D211/28C07D401/06C07D401/14C07D405/04C07D409/04C07D417/04C07D471/04C07D473/10
    • A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sup.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, CH.sup.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## 1 being 1 or 2, --A--B, A being --(CH.sub.2).sub.n --, n being an integer of 1 to 5,a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkene having a double bond formed between carbon atoms adjacent to each other by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,--(CH.sub.2)k--S--, k being an integer of 2 to 5, --(CH.sub.2)p--CO--, p being an integer of 1 to 4, B being cyano, --NR.sub.4 R.sub.5, a heterocyclic ring or a condensed aromatic ring.
    • 新的哌啶化合物在治疗心律失常方面是药理学有效的,并由下式定义:其中R1是低级烷基或甲苯基,R2是氢,羟基,低级烷氧基或低级烷基,R3是氢 低级烷基,低级烯基,环烷基或环烷基烷基,X为-CO-,-CH 2 - 或-CHOH-,g为1〜3的整数,h为1〜3的整数,Y为氢 ,低级烷基,低级烯基,氰基,CH 2 COOR,R为氢或低级烷基,环烷基,环烷基烷基,A为1或2,-AB,A为 - (CH 2)n - ,n为 1至5的整数,具有1至5个碳原子的直链亚烷基,其是衍生自直接与一个或多个碳原子键合的低级烷基,苯基或羟基的直链烷烃的二价基团 通过除去与位于其两端的每个碳原子键合的氢原子构成所述烷烃,具有1至5个碳原子的直链亚烷基,其是 通过除去与位于其两端的每个碳原子键合的氢原子,通过除去彼此相邻的碳原子之间形成的双键的直链烯烃的二价基团, - (CH 2)k S - ,k为 2〜5的整数, - (CH 2)p -CO-,p为1〜4的整数,B为氰基,-NR 4 R 5,杂环或稠合芳环。