PROCESS FOR THE PREPARATION OF BASIC ANTIBIOTIC-INORGANIC ACID ADDITION SALTS AND INTERMEDIATE OXALATES
    2.
    发明公开
    PROCESS FOR THE PREPARATION OF BASIC ANTIBIOTIC-INORGANIC ACID ADDITION SALTS AND INTERMEDIATE OXALATES 有权
    用于生产抗生素与无机酸和碱加成盐,草酸盐中间体

    公开(公告)号:EP1201665A1

    公开(公告)日:2002-05-02

    申请号:EP00948257.1

    申请日:2000-07-27

    申请人: Eisai Co., Ltd.

    摘要: The present invention provides:

    an industrially-excellent and novel process for producing a basic antibiotic·inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic·oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid:
    (wherein the ring A means the basic antibiotic; R 10 means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively);
    a novel oxalate useful as a production intermediate for producing an antibiotic·hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula:
    (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R 6 ; R 1 represents hydrogen or methyl group; R 2 and R 5 are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R 3 represents a carboxyl-protecting group; R 4 represents hydrogen, a lower alkyl group or an amino-protecting group; R 6 represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula:
    (wherein R 7 and R 8 are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and
    a process for producing its.

    摘要翻译: 本发明提供:在工业上优和新方法用于生产基本antibiotic.inorganic酸的盐,例如,优良的生产过程用于制备盐酸盐在工业上,所做的是,一个生产过程,它包括使一个基本antibiotic.oxalate (II)盐交换与碱土金属盐(III)的无机酸的:(worin环的装置的基本抗生素; R <10>表示在有机合成中使用的保护的官能基团; AK- E表示碱土金属;且B是指无机酸,分别地); 一种新颖的草酸作为生产用于在antibiotic.hydrochloride生产工业上,做了中间有用是草酸盐(II-I)由下式表示的碳代青霉烯化合物:( worin环A darstellt 3-至7- 具有元环的至少一个氮原子,且环A可与其它除R <6> R上substituiertem <1> darstellt氢或甲基; R <2>和R <5>是相同的或不同 形成,且分别darstellt氢或羟基保护基; R <3>表示羧基保护基; R <4> darstellt氢,低级烷基或氨基保护基的; R <6> darstellt(1 )氢,(2)任选被保护的羟基,氨基甲酰基,亚胺甲基,acetoimidoyl或可被由下式表示的取代基所substituiertem的低级烷基:(worin - [R <7>和R <8>是 相同或彼此和各darstellt氢,低级烷基或氨基保护基),或者(3个不同的 )氨基保护基或亚氨基保护的基团; 且m是0或1); 和用于生产其的过程。

    CEPHALOSPORIN DERIVATIVES
    3.
    发明公开
    CEPHALOSPORIN DERIVATIVES 失效
    头孢菌素VERBINDUNGEN。

    公开(公告)号:EP0329785A1

    公开(公告)日:1989-08-30

    申请号:EP87900286.3

    申请日:1986-12-26

    申请人: Eisai Co., Ltd.

    IPC分类号: C07D501/24 A61K31/545

    CPC分类号: C07D501/24

    摘要: Cephalosporin derivatives represented by general formula (I) [wherein R 1 represents a lower alkyl group, A represents (II) (wherein R 2 and R 3 may be the same or different and each represents a lower alkyl group, and R 4 represents a substituted lower alkyl group or an amino group), an optionally substituted group represented by formulae (III), (IV), (V) (wherein Rs represents a lower alkyl group] or a group of formula (VI) (wherein R 5 is the same as defined above and R 6 represents a hydroxy- lower alkyl group or a carboxyl group)] and pharmaceutically acceptable salts thereof, processes for their preparation, and antibacterial agents containing them.

    摘要翻译: 头孢菌素衍生物 式(I)是新的; 其中R1是低级烷基; A是N + R2R3R4; R2和R3是低级烷基; R4是氨基或是低级烷基选择。 substd。 氨基甲酰基,羧基,低级烷基氨基,巯基,低级烷酰基,羟基或肼基羰基; 或A可以是杂环gp。 通过季N(12 gps,特别声明包括(II)和(III)和(IV))选择。 substd。 氨基甲酰基,低级烷基二硫代,低级烷基,氨磺酰基,甲脒基或羧基; R5是低级烷基; 并且R 6是羧基或羟基 - 低级烷基。 A是pref。 (Ⅴ)(Ⅵ)(Ⅶ)或32个其他基团。 7β-(2-(5-氨基-1,2,4-噻二唑-3-基)-Z-2-甲氧基亚氨基乙酰亚胺基)-3-(E-3-(氨基甲酰基甲基咪唑基)-1-丙烯-1-酮 吡啶-3-基)-3-头孢烯-4-羧酸酯和其他8个cpds。 氨基和羧基保护的(I,A =卤素)与叔丁基的反应。 胺,然后脱保护。

    CEPHALOSPORIN DERIVATIVES
    5.
    发明授权
    CEPHALOSPORIN DERIVATIVES 失效
    头孢菌素联系*。

    公开(公告)号:EP0329785B1

    公开(公告)日:1994-11-30

    申请号:EP87900286.3

    申请日:1986-12-26

    申请人: Eisai Co., Ltd.

    IPC分类号: C07D501/24 A61K31/545

    CPC分类号: C07D501/24

    摘要: Cephalosporin derivatives represented by general formula (I), (wherein R1 represents a lower alkyl group, A represents (II) (wherein R2 and R3 may be the same or different and each represents a lower alkyl group, and R4 represents a substituted lower alkyl group or an amino group), an optionally substituted group represented by formulae (III), (IV), (V) (wherein R5 represents a lower alkyl group) or a group of formula (VI) (wherein R5 is the same as defined above and R6 represents a hydroxy-lower alkyl group or a carboxyl group)) and pharmaceutically acceptable salts thereof, processes for their preparation, and antibacterial agents containing them.

    PYRROLIDINE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
    8.
    发明公开
    PYRROLIDINE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 审中-公开
    PYRRIDIDDEDIVAT UND VERFAHREN ZU DESSEN HERSTELLUNG

    公开(公告)号:EP1375479A1

    公开(公告)日:2004-01-02

    申请号:EP02708748.5

    申请日:2002-04-01

    申请人: Eisai Co., Ltd.

    IPC分类号: C07D207/12

    CPC分类号: C07D207/12

    摘要: The present invention provides a compound which has cytokine production inhibitory activity and is useful for the treatment of diseases which is associated with cytokine. The compound is represented by the following general formula (I) [wherein A represents a cyclic group which may be substituted; the partial structure -D---E- represents a group represented by -CH 2 CH 2 - or -CH=CH-; W reprensents a group represented by -CH 2 -, - CH z CH 2 -, -CH=CH- or -CH=; the partial structure >X---Y- represents a group represented by >CH-(CH 2 ) n -, >C=CH-, >CH-CH 2 -CH(OH)-, >CH-CH 2 -C (=O) -, >CH-O- or >CH-O-CO-, provided that when W is -CH=, then X---Y- represents C-(CH 2 ) p -; Z represents a divalent aliphatic hydrocarbon group; R 1 and R 2 , which may be the same or different, each represents a hydrogen atom, or a hydroxyl, alkoxy or alkoxyalkoxy group; m is an integer of 0 or 1] .

    摘要翻译: 本发明提供具有细胞因子产生抑制活性的化合物,可用于治疗与细胞因子相关的疾病。 该化合物由以下通式(I)表示:其中A表示可被取代的环状基团; 部分结构-D --- E-表示由-CH 2 CH 2 - 或-CH = CH-表示的基团; W代表-CH 2 - , - CH 3 CH 2 - , - CH = CH-或-CH =表示的基团。 部分结构> X --- Y-表示由CH-(CH 2)n - ,> C = CH-,> CH-CH 2 -CH(OH) - ,> CH-CH 2 -C(= O)表示的基团 ) - ,> CH-O-或> CH-O-CO-,条件是当W为-CH =时,则X --- Y-表示C-(CH 2)p - ; Z表示二价脂族烃基; R 1和R 2可以相同或不同,各自表示氢原子,或羟基,烷氧基或烷氧基烷氧基; m是0或1Ü的整数。