Possibly substituted 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo-[4.3.0]-nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolin carboxylic acids and their derivatives
    1.
    发明授权
    Possibly substituted 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo-[4.3.0]-nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolin carboxylic acids and their derivatives 有权
    可取代的8-氰基-1-环丙基-7-(2,8-二氮杂双环[4.3.0] - 壬烷-8-基)-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸 酸及其衍生物

    公开(公告)号:US06323213B1

    公开(公告)日:2001-11-27

    申请号:US09125191

    申请日:1998-08-13

    CPC classification number: C07D471/04 A01N43/90

    Abstract: The present invention relates to novel optionally substituted 8-cyano-1-cyclo-propyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids and their derivatives, of the general formula (I) in which R1 represents hydrogen, C1-C4-alkyl which is optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethylamino, or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, R2 represents hydrogen, benzyl, C1-C3-alkyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, radicals having the structures —CH═CH—COOR3, —CH2CH2COOR3, —CH2CH2CN, —CH2CH2COCH3 or —CH2COCH3, in which R3 represents methyl or ethyl, or a radical of the general structure R4—(NH—CHR5—CO)n—, in which R4 represents hydrogen, C1-C3-alkyl or the radical —COO-tert-butyl, R5 represents hydrogen, C1-C4-alkyl, hydroxyalkyl, aminoalkyl, thioalkyl, carboxyalkyl or benzyl and n is 1 or 2, and Y is oxygen or sulfur, the process for their preparation and their use in antibacterial compositions.

    Abstract translation: 本发明涉及新的任选取代的8-氰基-1-环丙基-7-(2,8-二氮杂双环[4.3.0]壬烷-8-基)-6-氟-1,4-二氢-4- 甲氧基,氨基,甲基氨基或二甲基氨基取代的C 1 -C 4 - 烷基,或(5-甲基-2-羟基喹啉羧酸)或其衍生物,其中R 1表示氢, 氧代-1,3-二氧杂环戊烯-4-基)甲基,R 2表示氢,苄基,C 1 -C 3 - 烷基,(5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基)甲基, 结构-CH = CH-COOR 3,-CH 2 CH 2 COOR 3,-CH 2 CH 2 CN,-CH 2 CH 2 COCH 3或-CH 2 COCH 3,其中R 3表示甲基或乙基,或通式结构R4-(NH-CHR5-CO)n - 的基团,其中R4 代表氢,C 1 -C 3 - 烷基或-COO-叔丁基,R 5表示氢,C 1 -C 4 - 烷基,羟基烷基,氨基烷基,硫代烷基,羧基烷基或苄基,n是1或2,Y是氧或硫, 其制备方法及其在抗菌组合物中的应用。

    Promoting production of useful livestock with silylated
aminophenylethylamine derivatives
    3.
    发明授权
    Promoting production of useful livestock with silylated aminophenylethylamine derivatives 失效
    促进用甲硅烷基化氨基苯乙胺衍生物生产有用的家畜

    公开(公告)号:US4806667A

    公开(公告)日:1989-02-21

    申请号:US937759

    申请日:1986-12-04

    CPC classification number: C07F7/1852 A23K20/111

    Abstract: A method for promoting production of useful livestock comprising administering to such livestock an amount effective therefor of a monosilylated aminopheylethylamine derivative of the formula ##STR1## in which X and Y are identical or different and represent hydrogen or CN,R.sup.2 represents hydrogen or methyl,R.sup.3 represents t-butyl, isopropyl, monofluoro-t-butyl or 1-cyclohexyl-ethyl, andR.sup.4, R.sup.5 and R.sup.6 denote a straight-chain or branched alkyl rdical,or a physiologically tolerated salt thereof.Those compounds wherein R.sup.3 is monofluoro-t-butyl or 1-cyclohexyl-ethyl are new, as is its intermediate ##STR2##

    Abstract translation: 一种用于促进有用牲畜生产的方法,其包括向所述家畜施用一种有效量的式“IMAGE”的单甲硅烷基化氨基乙基乙胺衍生物,其中X和Y相同或不同,代表氢或CN,R2代表氢或甲基,R3 代表叔丁基,异丙基,一氟叔丁基或1-环己基 - 乙基,R 4,R 5和R 6表示直链或支链烷基或其生理上耐受的盐。 其中R3是单氟叔丁基或1-环己基乙基的那些化合物是新的,它的中间体是“IMAGE”

    Efomycin G and it's use as yield promoter in animals
    7.
    发明授权
    Efomycin G and it's use as yield promoter in animals 失效
    Efomycin G,它用作动物的产量促进剂

    公开(公告)号:US4927810A

    公开(公告)日:1990-05-22

    申请号:US22915

    申请日:1987-03-06

    Abstract: An animal growth promoter, efomycin G, is obtained by culturing Streptomycetes strain BS 1261. Efomycin G has the following properties:(a) The empirical formula: C.sub.53 H.sub.86 O.sub.18(b) The mass spectrum (fast atom bombardment) Molecular weight+Na.sup.+ : 1033(c) The .sup.1 H-nuclear magnetic resonance spectrum, stated in parts per million, shown in FIG. 1.(d) The .sup.13 C-nuclear magnetic resonance spectrum, stated in parts per million shown in FIG. 2, with chemical shifts of the CC-NMR signals as follows:______________________________________ 170.0 77.9 65.9 32.9 7.0 145.4 73.4 48.5 19.4 144.7 71.2 43.6 19.1 131.9 70.6 41.9 16.8 121.1 70.1 41.1 16.7 99.6 69.9 38.8 15.1 99.5 66.9 38.5 13.4 93.6 66.5 36.2 9.0 93.3 66.4 33.0 8.9 ______________________________________ (ppm values are relative to tetramethylsilane at 0 ppm) (e) A UV absorption maximum at 251-254 nm in methanolic solution(f) The structure according to FIG. 3.

    Abstract translation: 通过培养链霉菌菌株BS1261获得动物生长促进剂efomycin G。Efomycin G具有以下性质:(a)经验式:C53H86O18(b)质谱(快速原子轰击)分子量+ Na +:1033( c)1H-核磁共振谱,以百万分之几表示,如图1所示。 (d)13C-核磁共振谱,以图1所示的百万分之几表示。 2,CC-NMR信号的化学位移如下:-170.0 77.9 65.9 32.9 7.0 -145.4 73.4 48.5 19.4 -144.7 71.2 43.6 19.1 -131.9 70.6 41.9 16.8 -121.1 70.1 41.1 16.7 -99.6 69.9 38.8 15.1 -99.5 66.9 38.5 13.4 -93.6 66.5 36.2 9.0 -93.3 66.4 33.0 8.9 - (ppm值相对于四甲基硅烷在0ppm) - (e)在甲醇溶液中在251-254nm处的UV吸收最大值(f)根据图1的结构。 3。

    Novel arylethanolamines for promoting livestock production
    8.
    发明授权
    Novel arylethanolamines for promoting livestock production 失效
    用于促进畜牧生产的新型芳基乙醇胺

    公开(公告)号:US4845262A

    公开(公告)日:1989-07-04

    申请号:US89691

    申请日:1987-08-25

    CPC classification number: C07C255/00 A23K20/111

    Abstract: The growth of livestock is promoted by the novel arylethanolamines of the formula ##STR1## in which R.sup.1 represents cyano,R.sup.2 represents amino, alkylamino or acylamino,R.sup.3 represents hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, hydroxymethyl, nitro or methylsulphonylmethyl,R.sup.4 represents hydrogen, alkyl or acyl,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents alkyl,n represents 1, 2 or 3,R.sup.7 represents the radicals --COR.sup.9, --O-alkylene-COR.sup.9, -alkylene-R.sup.10 or --O-alkylene-R.sup.10,R.sup.8 represents hydrogen, alkyl or halogen,R.sup.9 represents hydroxyl, alkoxy or the radical --NR.sup.11 R.sup.12,R.sup.10 represents hydroxyl, alkoxy or the radical NR.sup.11 R.sup.12,R.sup.11 represents hydrogen or alkyl, andR.sup.12 represents hydrogen or alkyl,and the physiologically acceptable salts thereof.

    Abstract translation: 通过式(I)的新型芳基乙醇胺促进家畜的生长,其中R1代表氰基,R2代表氨基,烷基氨基或酰氨基,R3代表氢,卤素,烷基,卤代烷基,烷氧基,卤代烷氧基,羟基甲基,硝基 或甲基磺酰基甲基,R 4表示氢,烷基或酰基,R 5表示氢或烷基,R 6表示烷基,n表示1,2或3,R 7表示基团-COR 9,-O-亚烷基-CON 9, - 亚烷基-R 10或-O - 亚烷基-R 10,R 8表示氢,烷基或卤素,R 9表示羟基,烷氧基或基团-NR 11 R 12,R 10表示羟基,烷氧基或基团NR 11 R 12,R 11表示氢或烷基,R 12表示氢或烷基, 其可接受的盐。

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