2-penem-3-carboxylic acid derivatives and use
    3.
    发明授权
    2-penem-3-carboxylic acid derivatives and use 失效
    2-青霉烯-3-羧酸衍生物和用途

    公开(公告)号:US4639441A

    公开(公告)日:1987-01-27

    申请号:US582152

    申请日:1984-02-24

    摘要: Compounds of formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups;R.sup.2 represents a hydrogen atom, a group of formula ##STR2## (in which R.sup.5 and R.sup.6 each represents an alkyl group, an aralkyl group or an aryl group, or R.sup.5 and R.sup.6 together represent a nitrogen-containing heterocyclic group) or a group of formula ##STR3## (in which R.sup.7 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted amino group, a cyclic amino group, a hydroxy group, an alkoxy group, an aryloxy group, an aralkyloxy group, a substituted or unsubstituted hydrazino group or a guanidino group, and A' represents a bivalent saturated aliphatic hydrocarbon group); andR.sup.3 represents a carboxy group or a protected carboxy group; and pharmaceutically acceptable salts thereof are valuable antibiotics and may be prepared from the corresponding 1-(protected carboxymethyl)-4-alkylthio-azetidin-2-one.

    摘要翻译: 式(I)化合物:其中:R1表示氢原子,烷基,烷氧基或各种取代的烷基; R 2表示氢原子,式(IMAGE)(其中R 5和R 6各自表示烷基,芳烷基或芳基,或R 5和R 6一起代表含氮杂环基团)的基团 式中,R 7表示氢原子,取代或未取代的烷基,取代或未取代的氨基,环状氨基,羟基,烷氧基,芳氧基,芳烷氧基,取代的 或未取代的肼基或胍基,A'表示二价饱和脂族烃基)。 并且R 3表示羧基或保护的羧基; 和其药学上可接受的盐是有价值的抗生素,并且可以由相应的1-(保护的羧甲基)-4-烷硫基 - 氮杂环丁-2-酮制备。

    Carbapenem compounds, and compositions containing them
    5.
    发明授权
    Carbapenem compounds, and compositions containing them 失效
    碳青霉烯化合物和含有它们的组合物

    公开(公告)号:US4552873A

    公开(公告)日:1985-11-12

    申请号:US407914

    申请日:1982-08-13

    CPC分类号: C07D477/20 C07D207/12

    摘要: Compounds of formula (I): ##STR1## [wherein: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups;R.sup.2 represents a group of formula ##STR2## in which ##STR3## represents an alicyclic amine group having from 4 to 8 ring atoms, optionally having a single double bond, optionally containing an additional hetero-atom and optionally having an oxo group on the ring;X represents a hydrogen atom, an alkyl group, an alkoxy group, an alkylthio group, an alkylsulphinyl group, an alkylsulphonyl group, a hydroxy group, a halogen atom or various substituted alkyl groups;Y represents a hydrogen atom, an alkyl group, an aliphatic acyl group or an acylimidoyl group; andR.sup.3 represents a carboxy group or a protected carboxy group]and pharmaceutically acceptable salts thereof have valuable antibacterial activity, especially in vivo.

    摘要翻译: 式(I)的化合物:其中:R1表示氢原子,烷基,烷氧基或各种取代的烷基; R2代表一组式(IMAGE),其中表示具有4至8个环原子的脂环族胺基,任选具有单个双键,任选地含有另外的杂原子并且任选地在环上具有氧代基 ; X表示氢原子,烷基,烷氧基,烷硫基,烷基亚磺酰基,烷基磺酰基,羟基,卤素原子或各种取代的烷基; Y表示氢原子,烷基,脂肪族酰基或酰亚氨基; 和R3表示羧基或保护的羧基]及其药学上可接受的盐具有有价值的抗菌活性,特别是在体内。

    Radicicol derivatives, their preparation and their anti-tumor activity
    10.
    发明授权
    Radicicol derivatives, their preparation and their anti-tumor activity 失效
    蓝霉素衍生物,其制备及其抗肿瘤活性

    公开(公告)号:US5597846A

    公开(公告)日:1997-01-28

    申请号:US311518

    申请日:1994-09-23

    CPC分类号: C07D493/04

    摘要: A compound of the formula ##STR1## in which: R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen atoms and groups of formula R.sup.3 --CO--, wherein R.sup.3 represents a group selected from the group consisting of unsubstituted alkyl groups having from 9 to 20 carbon atoms; substituted alkyl groups having from 10 to 20 carbon atoms; unsubstituted alkenyl groups having from 9 to 20 carbon atoms; substituted alkenyl group having from 10 to 20 carbon atoms; unsubstituted alkynyl groups having from 8 to 10 carbon atoms; and substituted alkynyl groups having from 8 to 10 carbon atoms wherein R.sup.1 and R.sup.2 are not both hydrogen atoms or acetyl groups. The compounds have antitumor activity.

    摘要翻译: 式(Ia)化合物,其中:R 1和R 2独立地选自氢原子和式R3-CO-基团,其中R3代表选自具有9个 至20个碳原子; 具有10-20个碳原子的取代烷基; 具有9至20个碳原子的未取代的烯基; 具有10至20个碳原子的取代的烯基; 具有8至10个碳原子的未取代的炔基; 和具有8至10个碳原子的取代的炔基,其中R 1和R 2不是氢原子或乙酰基。 该化合物具有抗肿瘤活性。