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6 条记录 (耗时 0.016 秒)

    36-derivatives of rifamycins and their use as antimicrobial agents
    1.
    发明授权
    36-derivatives of rifamycins and their use as antimicrobial agents 失效
    利福霉素36衍生物及其作为抗微生物剂的用途

    公开(公告)号：US5786350A

    公开(公告)日：1998-07-28

    申请号：US792035

    申请日：1997-01-31

    申请人： Emilio Occelli ,  Sergio Lociuro ,  Romeo Ciabatti ,  Maurizio Denaro

    发明人： Emilio Occelli ,  Sergio Lociuro ,  Romeo Ciabatti ,  Maurizio Denaro

    IPC分类号： A61K31/34 ,  A61K31/395 ,  A61K31/429 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61P31/04 ,  C07D213/80 ,  C07D498/08 ,  C07D498/18 ,  C07D519/00 ,  C07D491/08

    CPC分类号： C07D213/80

    摘要： Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C.sub.1 -C.sub.8)alkyl, halo, hydroxy, (C.sub.1 -C.sub.4)acyloxy, (C.sub.1-C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1-C.sub.4)alkylamino and substituted 4-oxo-3-pyridinyl carbonyloxy of formula (1) obtained by reacting rifamycin with suitably substituted malonic acid. The compounds of the invention are antimicrobial agents mainly active against gram positive bacteria and fastidious gram negative bacteria showing the considerable antimicrobial activity against the rifamypicin resistant microbial strains.

    摘要翻译： PCT No.PCT / EP94 / 01428 Sec。 371日期1996年1月22日 102（e）日期1996年1月22日PCT提交1994年5月5日PCT公布。 出版物WO94 / 28002 （Ia）式（I）和（Ia）的利福霉素抗生素衍生物在位置36具有选自（C1-C8）的取代基， 烷基，卤素，羟基，（C1-C4）酰氧基，（C1-C4）烷氧基，（C1-C4）烷硫基，（C1-C4）烷基氨基，二（C1-C4）烷基氨基和取代的4-氧代-3-吡啶基 通过使利福霉素与适当取代的丙二酸反应获得的式（1）的羰基氧基。 本发明的化合物是主要对革兰氏阳性细菌有活性的抗微生物剂和对耐赖菌素抗性微生物菌株具有相当大的抗菌活性的革兰氏阴性细菌。

    2,4,6-Trisubstituted-2,3-dihydro-benzofuran derivatives
    3.
    发明授权
    2,4,6-Trisubstituted-2,3-dihydro-benzofuran derivatives 失效
    2,4,6-三取代-2,3-二氢苯并呋喃衍生物

    公开(公告)号：US4143055A

    公开(公告)日：1979-03-06

    申请号：US890158

    申请日：1978-03-27

    申请人： Emilio Occelli

    发明人： Emilio Occelli

    IPC分类号： C07D307/79

    CPC分类号： C07D307/79 ,  Y10S514/916

    摘要： New 2,4,6-trisubstituted-2,3-dihydro-benzofuran derivatives of the following general formula ##STR1## wherein R is selected from hydrogen or methyl; one of R.sub.1 and R.sub.2 represents hydroxy, (C.sub.1-4)alkoxy or (C.sub.2-4)alkanoyloxy, and the other one is selected from cyano, carboxy, carbo(C.sub.1-4)alkoxy, carbamoyl and a --NR.sub.3 R.sub.4 group, wherein R.sub.3 and R.sub.4 independently represent hydrogen (C.sub.1-4)alkyl, (C.sub.2-4)alkanoyl, carbo(C.sub.1-4)alkoxy, carbobenzyloxy, carbamoyl, mono- and di-(C.sub.1-4)alkylamino-(C.sub.1-4)alkyl, benzenesulfonyl, toluenesulfonyl, (C.sub.1-4)alkylsulfonyl or phenacylsulfonyl; and salts therewith of pharmaceutically acceptable acids. The compounds have antinflammatory, analgesic and antipyretic utility.

    Reserpine derivatives
    5.
    发明授权
    Reserpine derivatives 失效
    利血平衍生物

    公开(公告)号：US3978065A

    公开(公告)日：1976-08-31

    申请号：US473024

    申请日：1974-05-24

    申请人： Emilio Occelli ,  Luigi Fontanella ,  Giangiacomo Nathansohn

    发明人： Emilio Occelli ,  Luigi Fontanella ,  Giangiacomo Nathansohn

    IPC分类号： A61K31/475 ,  A61P9/12 ,  C07D459/00

    CPC分类号： C07D459/00

    摘要： New reserpine-like compounds of the general formula ##SPC1##Wherein R is a member of the class consisting of hydrogen, lower alkyl, lower alkenyl and acyl; R.sub.1 is selected from hydrogen and lower alkyl, and R.sub.2 is hydrogen or lower alkyl. The new reserpine-like compounds are useful anti-hypertensive agents.

    摘要翻译： 新的利血平样化合物，通式为WHEREIN R是由氢，低级烷基，低级烯基和酰基组成的一类成员; R1选自氢和低级烷基，R2是氢或低级烷基。 新的利血平样化合物是有用的抗高血压药物。

    3,6-disubstituted triazolo [3,4-A]phthalazine derivatives
    6.
    发明授权
    3,6-disubstituted triazolo [3,4-A]phthalazine derivatives 失效
    3,6-二取代三唑并[3,4-A]酞嗪衍生物

    公开(公告)号：US4783461A

    公开(公告)日：1988-11-08

    申请号：US629658

    申请日：1984-07-11

    申请人： Emilio Occelli ,  Giorgio Tarzia

    发明人： Emilio Occelli ,  Giorgio Tarzia

    IPC分类号： A61K31/50 ,  A61K31/535 ,  A61P25/20 ,  C07D237/32 ,  C07D237/34 ,  C07D487/04 ,  A61K31/55

    CPC分类号： C07D487/04 ,  C07D237/32 ,  C07D237/34

    摘要： The present invention is directed to new 3,6-disubstituted-1,2,4-triazolo[3,4-a]phthalazine derivatives of formula I ##STR1## wherein R represents phenyl or substituted phenyl, n is 1 or 2, R.sup.1 is an amino group of formula NR.sup.4 R.sup.5, or an alkoxy of cycloalkoxy group of formula OR.sup.6, and R.sup.2 and R.sup.3 represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, to the process for their preparation and to the pharmaceutical compositions containing them. The compounds of the present invention are as active as anti-anxiety substances.

    摘要翻译： 本发明涉及式I的新的3,6-二取代-1,2,4-三唑并[3,4-a]酞嗪衍生物其中R表示苯基或取代的苯基，n为1或2，R 1 是式NR4R5的氨基或式OR6的环烷氧基的烷氧基，R2和R3表示氢，卤素，（C1-C4）烷基或（C1-C4）烷氧基，其制备方法和 含有它们的药物组合物。 本发明的化合物与抗焦虑物质一样有活性。