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    Crystalline substance of cefditoren pivoxyl and the production of the same
    1.
    发明授权
    Crystalline substance of cefditoren pivoxyl and the production of the same 有权
    头孢托仑的新型结晶物质及其生产

    公开(公告)号：US06441162B2

    公开(公告)日：2002-08-27

    申请号：US09854462

    申请日：2001-05-15

    申请人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    发明人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    IPC分类号： C07D50124

    CPC分类号： C07D501/00

    摘要： A crystalline substance of Cefditoren pivoxyl is provided which has a high purity and enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving an amorphous form of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous form well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.

    摘要翻译： 提供了新戊酸头孢托仑的结晶物质，其具有高纯度和增强的储存热稳定性。 这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，该方法包括将无定形形式的新戊酰氧基头孢托仑溶解在能够将所述无定形形式溶解在其中的无水第一有机溶剂中，以及将所得溶液的第一有机溶剂组分 通过具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后浓缩至15℃以下。 减压下等。 由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。 从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。

    Crystalline substance of cefditoren pivoxyl and the production of the same
    8.
    发明授权
    Crystalline substance of cefditoren pivoxyl and the production of the same 有权
    头孢托仑的新型结晶物质及其生产

    公开(公告)号：US06294669B1

    公开(公告)日：2001-09-25

    申请号：US09269109

    申请日：1999-03-19

    申请人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    发明人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    IPC分类号： C07D50124

    CPC分类号： C07D501/00

    摘要： As a novel substance is provided such a new, crystalline substance of Cefditoren povoxyl which has a high purity and an enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving amorphous substance of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous substance well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.

    摘要翻译： 作为一种新物质，提供了这样一种具有高纯度和增加的储存热稳定性的新型头孢托仑聚氧乙烯醚的结晶物质。 这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，所述方法包括将能够将所述无定形物质溶解在其中的无水的第一有机溶剂中溶解新戊酰氧基甲基头孢托仑的无定形物质，以及将所得溶液的第一有机溶剂组分置换为 将具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后在15℃以下浓缩 减压等。 由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。 从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。

    Process for the selective preparation of Z-isomers of 3-2(substituted vinyl)cephalosporins
    9.
    发明授权
    Process for the selective preparation of Z-isomers of 3-2(substituted vinyl)cephalosporins 有权
    选择性制备3-2（取代乙烯基）头孢菌素的Z-异构体的方法

    公开(公告)号：US06288223B1

    公开(公告)日：2001-09-11

    申请号：US09446380

    申请日：2000-02-18

    申请人： Yumiko Okada ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Hiroyuki Iwasawa ,  Yasushi Murai ,  Katsuharu Iinuma

    发明人： Yumiko Okada ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Hiroyuki Iwasawa ,  Yasushi Murai ,  Katsuharu Iinuma

    IPC分类号： C07D50104

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： There can be produced, at a high selectivity and in a high yield, the Z-isomer of a 7-N-unsubstituted or substituted-amino-3-[2-(4-substituted or unsubstituted-thiazol-5-yl) vinyl]-3-cephem-4-carboxylic acid or an ester thereof having the general formula (IV) wherein R1 denotes a hydrogen atom, a mono-valent amino-protecting group or a 2-(2-N-protected or unprotected aminothiazol-4-yl)- 2-alkoxyiminoacetyl group, R2 denotes a hydrogen atom, or R1 and R2 as taken together mean one di-valent amino-protecting group, R3 denotes a hydrogen atom, pivaloyloxymethyl group or a carboxyl-protecting group and R8 denotes an alkyl group and so on, by a process comprising reacting a 7-N-unsubstituted or substituted-amino-3-[(tri-substituted-phosphoranylidene) methyl]-3-cephem-4-carboxylic acid or an ester thereof having the general formula (I) wherein R1, R2 and R3 each have the same meanings as defined above, and R4 denotes a lower alryl group or an aryl group, with a 4-substituted or unsubstituted-thiazol-5-carbaldehyde in a mixed solvent consisting of a mixture of one or more chlorinated hydrocarbon solvent(s) with one or more lower alkanol(s) at a low temperature of +5° C. or below. According to the processes of this invention, the production of such E-isomer of the compound (IV) that is of lower antibacterial activity than that of the Z-isomer can be suppressed remarkedly. Further, the Z-isomer of a high purity can be produced efficiently in a facile way.

    摘要翻译： 可以以高选择性和高产率制备7-N-未取代或取代的氨基-3- [2-（4-取代或未取代的 - 噻唑-5-基）乙烯基的Z-异构体 ] - 3-头孢烯-4-羧酸或其具有通式（IV）的酯，其中R 1表示氢原子，一价氨基保护基或2-（2-N-保护或未保护的氨基噻唑-2-基） 4-烷氧基亚氨基乙酰基，R 2表示氢原子，或者R 1和R 2一起表示一个二价氨基保护基，R 3表示氢原子，新戊酰氧基甲基或羧基保护基，R 8表示 烷基等，通过包括使7-N - 未取代的或取代的氨基-3 - [（三取代的亚正膦基）甲基] -3-头孢烯-4-羧酸或其酯具有 通式（I）其中R1，R2和R3各自具有与上述相同的含义，R4表示低级烯丙基或芳基，具有4-取代或未取代的t 在一个或多个氯化烃溶剂与一种或多种低级链烷醇的混合物中，在+ 5℃或更低的低温下混合的混合溶剂中， 根据本发明的方法，能够显着抑制抗Z活性降低的化合物（Ⅳ）的这种E-异构体的生产。 此外，可以以简便的方式有效地制备高纯度的Z-异构体。

    Antifungal compound and process for producing the same
    10.
    发明授权
    Antifungal compound and process for producing the same 失效
    抗真菌化合物及其制备方法

    公开(公告)号：US07250389B1

    公开(公告)日：2007-07-31

    申请号：US09601655

    申请日：1999-02-08

    申请人： Osamu Sakanaka ,  Koichi Mitomo ,  Takayoshi Tamura ,  Yasushi Murai ,  Katsuharu Iinuma ,  Takeshi Teraoka ,  Kikuko Kuzuhara ,  Haruki Mikoshiba ,  Makoto Taniguchi

    发明人： Osamu Sakanaka ,  Koichi Mitomo ,  Takayoshi Tamura ,  Yasushi Murai ,  Katsuharu Iinuma ,  Takeshi Teraoka ,  Kikuko Kuzuhara ,  Haruki Mikoshiba ,  Makoto Taniguchi

    IPC分类号： A01N504/14 ,  C07D405/00

    CPC分类号： C07D405/12 ,  A01N43/24 ,  A01N43/40 ,  A01N43/54 ,  C07D321/00 ,  Y02P20/55

    摘要： Disclosed are novel compounds useful for prevention or control of diseases derived from fungi, a process for producing the same, and novel antifungal agents using the novel compounds. The compounds useful for prevention and treatment of diseases derived from fungi according to the present invention include novel compounds represented by formula (I). The compounds represented by formula (I) have potent antifungal activity against diseases derived from fungi, and do not have phytotoxicity to mammals and agricultural and garden plants, from which diseases should be eliminated, and, even when applied to agricultural and garden plants, have high photostability. wherein R1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl; R2 represents a hydrogen atom, an aromatic carboxylic acid residue, or a protective group of amino; and R3 represents a hydrogen atom, nitro, amino, acylamino, or N,N-dialkylamino, excluding the case where, when R1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl with R3 representing a hydrogen atom, R2 represents a 3-hydroxypicolinic acid residue, 3-hydroxy-4-methoxypicolinic acid residue, or a 3,4-dimethoxypicolinic acid residue.

    摘要翻译： 公开了可用于预防或控制来自真菌的疾病的新化合物，其制备方法和使用该新化合物的新型抗真菌剂。 用于预防和治疗根据本发明的真菌的疾病的化合物包括由式（I）表示的新化合物。 由式（I）表示的化合物对从真菌衍生的疾病具有有效的抗真菌活性，并且对哺乳动物和农业和园艺植物没有植物毒性，应从其中消除疾病，甚至在应用于农业和花园植物时也具有 高光稳定性 其中R 1表示异丁酰基，二酰基，异戊酰基或2-甲基丁酰基; R 2表示氢原子，芳族羧酸残基或氨基的保护基; 并且R 3表示氢原子，硝基，氨基，酰氨基或N，N-二烷基氨基，不同之处在于当R 1表示异丁酰基时，二酰基，异戊酰基， 或代表氢原子的R 3的2-甲基丁酰基，R 2表示3-羟基吡啶甲酸残基，3-羟基-4-甲氧基吡啶甲酸残基，或3- 4-二甲氧基吡啶甲酸残余物。