Heterocyclic compounds as inhibitors of beta-lactamases
    33.
    发明授权
    Heterocyclic compounds as inhibitors of beta-lactamases 有权
    杂环化合物作为β-内酰胺酶的抑制剂

    公开(公告)号:US07612087B2

    公开(公告)日:2009-11-03

    申请号:US10898754

    申请日:2004-07-26

    IPC分类号: A61K31/44 A61K31/545

    摘要: This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.

    摘要翻译: 本发明公开并要求通过抑制人或动物中的细菌β-内酰胺酶抑制细菌β-内酰胺酶和治疗细菌感染的方法,包括向所述人或所述动物施用治疗有效量的化合物或其药学上可接受的盐 式(I)单独或与β-内酰胺抗生素组合,其中所述组合可以分开施用,一起或随时间隔开。 还公开和要求保护包含式(I)化合物或式(I)化合物与治疗有效量的β-内酰胺抗生素和药学上可接受的载体的组合物的药物组合物。

    HETEROCYCLIC COMPOUNDS AS INHIBITORS OF BETA-LACTAMASES
    34.
    发明申请
    HETEROCYCLIC COMPOUNDS AS INHIBITORS OF BETA-LACTAMASES 审中-公开
    作为β-Lactamases的抑制剂的杂环化合物

    公开(公告)号:US20090215747A1

    公开(公告)日:2009-08-27

    申请号:US12434270

    申请日:2009-05-01

    IPC分类号: A61K31/55

    摘要: This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.

    摘要翻译: 本发明公开并要求通过抑制人或动物中的细菌β-内酰胺酶抑制细菌β-内酰胺酶和治疗细菌感染的方法,包括向所述人或所述动物施用治疗有效量的化合物或其药学上可接受的盐 式(I)单独或与β-内酰胺抗生素组合,其中所述组合可以分开施用,一起或随时间隔开。 还公开和要求保护包含式(I)化合物或式(I)化合物与治疗有效量的β-内酰胺抗生素和药学上可接受的载体的组合物的药物组合物。

    13-Thia-prostacycline derivatives
    36.
    发明授权
    13-Thia-prostacycline derivatives 失效
    13-前列环素衍生物

    公开(公告)号:US4425358A

    公开(公告)日:1984-01-10

    申请号:US370503

    申请日:1982-04-21

    摘要: The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.

    摘要翻译: 本发明涉及式I的新的光学活性或外消旋的13-前列环素衍生物,其中R1是氢,可药用阳离子或具有1-5个碳原子的直链或支链烷基; R2是具有4-9个碳原子的直链或支链烷基或单取代的苯氧基甲基; -A-B-是Z-或E-构型的-CH 2 -CH 2 - , - CH = CH-或-C 3 D C-; 符号X和Y之一是氢,甲基或乙基,另一个是羟基,四氢吡喃基氧基,1-乙氧基 - 乙氧基或三烷基甲硅烷氧基; 或X和Y一起形成-O-CH 2 -CH 2 -O-基团; Z是硫原子或-SO-基。 式I的化合物可以通过使式III的13-前 - 前列腺素(III)反应来制备。