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    • 18. 发明授权
    • PHOSPHORAMIDATE DERIVATIVES
    • 磷酰胺衍生物
    • EP1709056B1
    • 2009-06-17
    • EP05701927.5
    • 2005-01-18
    • University College Cardiff Consultants Limited
    • MCGUIGAN, ChristopherCARANGIO, AntonellaCATERSON, BruceHUGHES, Clare, ElizabethCURTIS, Clare Louise
    • C07H11/04A61K31/7024A61P29/00
    • C07H11/04Y02P20/55
    • The present invention provides a phosphoramidate compound comprising the structure (I) Formula (I)wherein: X comprises a monosaccharide group comprising the structure (II) or (III),8Formula (II) , (III) B and B are independently selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R is selected from the group consisting of -H, protecting groups and monovalent hydrocarbon radicals; R and R are independently selected from the group consisting of -H and monovalent hydrocarbon radicals, or R2 and R3 together form an alkylene or heteroalkylene chain so as to provide, together with the C atom to which they are attached, a cyclic system; R is selected from the group consisting of -H and monovalent hydrocarbon radicals; R -R are independently selected from the group consisting of -H, -OH, N3, halogen, -SH,-OR , -SR , -NHR , -NR 2 and group Formula (1) wherein B" is selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R -R are independently selected and are as defined above, wherein R and R are independently selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R , and wherein R is selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R , wherein R is selected from the group consisting of -H and monovalent hydrocarbon radicals; or a pharmaceutically acceptable derivative or metabolite of a compound of formula (I). The present invention also provides processes for the production of (I) and uses thereof.
    • 本发明提供了包含结构(I)式(I)的氨基磷酸酯化合物,其中:X包含包含结构(II)或(III)的单糖基团,式(II),(III)B和B独立地选自 由-O - , - CH 2 - 和键组成的基团,优选-O-; R 1选自-H,保护基和单价烃基; R 2和R 3独立地选自-H和一价烃基,或者R 2和R 3一起形成亚烷基或亚杂烷基链,从而与它们所连接的C原子一起提供 ,一个循环系统; R 4选自-H和一价烃基; R 5 -R 12独立地选自-H,-OH,N 3,卤素,-SH,-OR 13,-SR 13',-NHR 14, - NR 14 2和式(1)的基团,其中B“选自-O - , - CH 2 - 和键,优选-O-; R 1 -R 4独立地选自 如上所定义,其中R 13和R 13'独立地选自-H,一价烃基,保护基和-C(O)R 15,并且其中R 14和R 14独立地选自-H, 选自-H,一价烃基,保护基和-C(O)R 15,其中R 15选自-H和一价烃基;或药学上可接受的基团 (I)化合物的衍生物或代谢物,本发明还提供了用于生产(I)的方法及其用途。
    • 19. 发明公开
    • NOVEL K04-0144 SUBSTANCES AND PROCESS FOR PRODUCTION THEREOF
    • NOVEL K04-0144物质及其生产方法
    • EP2019147A1
    • 2009-01-28
    • EP06732665.2
    • 2006-05-16
    • THE KITASATO INSTITUTE
    • TOMODA, HiroshiKIM, Yong-pilHANAKI, HideakiMATSUMOTO, AtsukoTAKAHASHI, YokoOMURA, Satoshi
    • C12P19/26C07H11/04A61K31/7024A61P31/04
    • C07H11/04C07C323/59C12P13/02C12P19/26C12P19/44C12R1/465
    • Amicroorganism represented by a strain K04-0144 belonging to Streptomyces sp. having ability to produce K04-0144 substance is cultured in the medium, and the isolated K04-0144A substance, K04-0144B substance and K04-0144C substance therefrom have strong antibacterial activities against Gram-positive bacteria including methicillin-resistant Streptococcus aureus (MRSA), consequently these are useful as the therapeutic agents for infectious disease caused by MRSA as well as infectious diseases caused by multidrug including β-lactam antibiotics resistant bacteria. Further, similarly, since the novel K04-0144D substance isolated from the cultured liquid has the action for enhancing the effect of β-lactam antibiotics, which are utilized as the antibacterial agents, in combination with them, it is useful as the therapeutic agent for infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and multidrug including β-lactam antibiotics resistant bacteria.
    • 由属于链霉菌属的菌株K04-0144代表的微生物。 在培养基中培养具有产生K04-0144物质的能力,并且分离出的K04-0144A物质,K04-0144B物质和K04-0144C物质对包括耐甲氧西林金黄色葡萄球菌(MRSA)在内的革兰氏阳性菌具有强的抗菌活性, 因此它们可用作由MRSA引起的感染性疾病的治疗剂以及由包括β-内酰胺抗生素抗性细菌在内的多种药物引起的感染性疾病。 此外,类似地,由于从培养液中分离出的新型K04-0144D物质具有提高作为抗菌剂使用的β-内酰胺抗生素的效果的作用,因此与它们组合使用时,可用作 由耐甲氧西林金黄色葡萄球菌(MRSA)引起的传染病和包括β-内酰胺抗生素耐药细菌在内的多种药物。