会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明授权
    • 7-Oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid derivatives, their
use and preparation
    • 7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸衍生物,其用途和制备方法
    • US4377591A
    • 1983-03-22
    • US239139
    • 1981-02-27
    • Tetsuo HiraokaTakeo KobayashiNoboru IshidaShinichi Sugawara
    • Tetsuo HiraokaTakeo KobayashiNoboru IshidaShinichi Sugawara
    • C07D477/00A61K31/397A61K31/40A61P31/04C07D205/08C07D477/14C07F7/10C07F7/18C07F9/568C07D487/04
    • C07D477/14C07D205/08C07F7/10C07F7/186C07F9/5683Y02P20/55
    • 7-Oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid derivatives of formula (I): ##STR1## (in which:) R.sup.1 represents a hydrogen atom or an optionally substituted alkyl group;X represents an oxy group, a thio group, a sulphinyl group or a sulphonyl group;A represents a bivalent for trivalent saturated aliphatic hydrocarbon group;p is 1 (when A is bivalent) or 2 (when A is trivalent);R.sup.2 represents an azido, nitro or cyano group or one of the groups of formula ##STR2## m and n are the same or different and each is 0 or 1; R represents an amidino group or a group of formula R.sup.4, --N(R.sup.4).sub.2 or --YR.sup.4,B represents a group of formula ##STR3## D represents a group of formula ##STR4## (provided that, where m and n are both 1, the groups represented by B and D must be different);R.sup.4 represents a hydrogen atom or an alkyl group and, where there are 2 or more groups represented by R.sup.4, they may be the same or different, andY represents an oxygen atom or a sulphur atom; andR.sup.3 represents a carboxy group or a protected carboxy group)and pharmaceutically acceptable salts thereof are valuable antibiotics and may be prepared by a process which includes heating a corresponding phosphorus-ylide compound.
    • (I)的7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸衍生物:其中:R 1表示氢原子或任选取代的烷基 组; X表示氧基,硫基,亚磺酰基或磺酰基; A代表三价饱和脂族烃基的二价; p为1(当A为二价时)或2(当A为三价时); R 2表示叠氮基,硝基或氰基,或者式中的一个基团m和n相同或不同,各自为0或1; R表示脒基或式R4,-N(R4)2或-YR4的基团,B表示式的基团D表示式的基团(条件是,其中m和n均为 1,由B和D表示的基团必须不同); R 4表示氢原子或烷基,其中,R 2表示2个以上基团时,可以相同或不同,Y表示氧原子或硫原子。 并且R 3表示羧基或保护的羧基)及其药学上可接受的盐是有价值的抗生素,并且可以通过包括加热相应的磷内酯化合物的方法来制备。
    • 4. 发明授权
    • Penem-3-carboxylic acid derivatives
    • 甘氨酸-3-羧酸衍生物
    • US4395418A
    • 1983-07-26
    • US271010
    • 1981-06-05
    • Eiji OhkiSadao OidaAkira YoshidaTeruo HayashiShinichi Sugawara
    • Eiji OhkiSadao OidaAkira YoshidaTeruo HayashiShinichi Sugawara
    • C07D205/09C07D499/88C07F7/18C07F9/568A61K31/425C07D499/00
    • C07F7/186C07D205/09C07D499/88C07F9/5683Y02P20/55
    • Penem-3-carboxylic acid derivatives of formula (I): ##STR1## (wherein: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyalkyl group, an acyloxyalkyl group, an alkylsulphonyloxyalkyl group, an arylsulphonyloxyalkyl group or a trialkylsilyloxyalkyl group;R.sup.2 represents a hydrogen atom or an alkyl group;R.sup.3 represents a hydrogen atom, an amino-protecting group or a group of formula ##STR2## in which R.sup.5 and R.sup.6 are the same or different and each represents a hydrogen atom or an alkyl group;A represents a branched-chain alkylene group; andR.sup.4 represents a carboxy group or a protected carboxy group)and pharmaceutically acceptable salts thereof, may be prepared by heating a corresponding phosphorus-ylide compound or by reacting a corresponding azetidin-2-one with a suitable phosphorous acid triester or triamide, and have been found to have excellent antibacterial activity accompanied by a very low acute toxicity.
    • (I)的半酯-3-羧酸衍生物:其中:R1表示氢原子,烷基,烷氧基,羟烷基,酰氧基烷基,烷基磺酰氧基烷基,芳基磺酰氧基烷基 基团或三烷基甲硅烷氧基烷基; R 2表示氢原子或烷基; R 3表示氢原子,氨基保护基或式“IMAGE”基团,其中R 5和R 6相同或不同,并且各自表示氢 原子或烷基; A表示支链亚烷基; R4表示羧基或保护的羧基)及其药学上可接受的盐可以通过加热相应的磷内酯化合物或通过使相应的氮杂环丁烷 -2-酮与合适的亚磷酸三酯或三酰胺,发现具有优异的抗菌活性,伴随着非常低的急性毒性。