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    Nitrogen-containing heterocyclic compounds and therapeutic agents for hyperlipidemia comprising the same
    13.
    发明授权
    Nitrogen-containing heterocyclic compounds and therapeutic agents for hyperlipidemia comprising the same 失效
    含氮杂环化合物和包含其的高脂血症治疗剂

    公开(公告)号：US06583144B2

    公开(公告)日：2003-06-24

    申请号：US10127491

    申请日：2002-04-23

    申请人： Naoto Ohkura ,  Takashi Tsuruoka ,  Takayuki Usui ,  Yukiko Hiraiwa ,  Tetsuya Matsushima ,  Masaharu Shiotani ,  Tetsutaro Niizato ,  Yuuko Nakatani ,  Shigeki Suzuki ,  Chidsuko Kuroda ,  Kiyoaki Katano

    发明人： Naoto Ohkura ,  Takashi Tsuruoka ,  Takayuki Usui ,  Yukiko Hiraiwa ,  Tetsuya Matsushima ,  Masaharu Shiotani ,  Tetsutaro Niizato ,  Yuuko Nakatani ,  Shigeki Suzuki ,  Chidsuko Kuroda ,  Kiyoaki Katano

    IPC分类号： A61K31495

    CPC分类号： C07D409/12 ,  C07D209/46 ,  C07D217/24 ,  C07D265/22 ,  C07D279/08 ,  G03F7/2049 ,  Y10S977/915

    摘要： Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia. wherein A represents group —CR1R2—(CH2)i— where R1 and R2 each represent a hydrogen atom or alkyl, —CH═CH—, —O—CH2—, or —S(O)j—CH2—; B represents a hydrogen or halogen atom; X represents —CR3R4R5, —NR6R7, —(CH2—CH═C(CH3)—CH2)p—CH2CH═C(CH3)2, alkyl, cycloalkyl, phenyl, cinnamyl, or heteroaromatic ring; Y represents —(CH2)q—, —CH═CH—, —NR8—, an oxygen atom, or a bond; Z represents carbonyl or a bond; K represents alkylene or a bond; L represents —CH═CH— or a bond; and M represents a hydrogen atom, alkyl, cycloalkyl, phenyl, heterocyclic ring, biphenyl, or diphenylmethyl.

    摘要翻译： 公开了由式（I）表示的化合物及其药学上可接受的盐和溶剂化物。 该化合物可以抑制肝脏中甘油三酯的生物合成，并可以抑制含有载脂蛋白B的脂蛋白从肝脏的分泌。 因此，它们可用于预防或治疗由高脂血症引起的高脂血症（特别是超低密度脂蛋白血症）和动脉硬化疾病如心肌梗死或胰腺炎。其中A代表基团-CR1R2-（CH2）i - 其中R1和R2各自表示氢原子或烷基，-CH = CH-，-O-CH2-或-S（O）j-CH2-; B表示氢或卤素原子; X代表-CR3R4R5，-NR6R7， - （CH2-CH = C（CH3）-CH2）p-CH2CH = C（CH3）2，烷基，环烷基，苯基，肉桂基或杂芳族环; Y表示 - （CH 2）q - ， - CH = CH - ， - NR 8 - ，氧原子或键; Z表示羰基或键; K表示亚烷基或键; L表示-CH = CH-或键; M代表氢原子，烷基，环烷基，苯基，杂环，联苯基或二苯基甲基。

    Nitrogenous heterocyclic compounds and hyperlipemia remedy containing the same
    15.
    发明授权
    Nitrogenous heterocyclic compounds and hyperlipemia remedy containing the same 失效
    含氮杂环化合物和含有相同的高脂血症药物

    公开(公告)号：US06417362B1

    公开(公告)日：2002-07-09

    申请号：US09424708

    申请日：1999-11-30

    申请人： Naoto Ohkura ,  Takashi Tsuruoka ,  Takayuki Usui ,  Yukiko Hiraiwa ,  Tetsuya Matsushima ,  Masaharu Shiotani ,  Tetsutaro Niizato ,  Yuuko Nakatani ,  Shigeki Suzuki ,  Chidsuko Kuroda ,  Kiyoaki Katano

    发明人： Naoto Ohkura ,  Takashi Tsuruoka ,  Takayuki Usui ,  Yukiko Hiraiwa ,  Tetsuya Matsushima ,  Masaharu Shiotani ,  Tetsutaro Niizato ,  Yuuko Nakatani ,  Shigeki Suzuki ,  Chidsuko Kuroda ,  Kiyoaki Katano

    IPC分类号： C07D24104

    CPC分类号： C07D409/12 ,  C07D209/46 ,  C07D217/24 ,  C07D265/22 ,  C07D279/08 ,  G03F7/2049 ,  Y10S977/915

    摘要： Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia. wherein A represents group —CR1R2—(CH2)i— where R1 and R2 each represent a hydrogen atom or alkyl, —CH═CH—, —O—CH2—, or —S(O)j—CH2—; B represents a hydrogen or halogen atom; X represents —CR3R4R5, —NR6R7, —(CH2—CH═C(CH3)—CH2)p—CH2CH═C(CH3)2, alkyl, cycloalkyl, phenyl, cinnamyl, or heteroaromatic ring; Y represents —(CH2)q—, —CH═CH—, —NR8—, an oxygen atom, or a bond; Z represents carbonyl or a bond; K represents alkylene or a bond; L represents —CH═CH— or a bond; and M represents a hydrogen atom, alkyl, cycloalkyl, phenyl, heterocyclic ring, biphenyl, or diphenylmethyl.

    摘要翻译： 公开了由式（I）表示的化合物及其药学上可接受的盐和溶剂化物。 该化合物可以抑制肝脏中甘油三酯的生物合成，并可以抑制含有载脂蛋白B的脂蛋白从肝脏的分泌。 因此，它们可用于预防或治疗由高脂血症引起的高脂血症（特别是超低密度脂蛋白血症）和动脉硬化疾病如心肌梗死或胰腺炎。其中A代表基团-CR1R2-（CH2）i - 其中R1和R2各自表示氢原子或烷基，-CH = CH-，-O-CH2-或-S（O）j-CH2-; B表示氢或卤素原子; X代表-CR3R4R5，-NR6R7， - （CH2-CH = C（CH3）-CH2）p-CH2CH = C（CH3）2，烷基，环烷基，苯基，肉桂基或杂芳族环; Y表示 - （CH 2）q - ， - CH = CH - ， - NR 8 - ，氧原子或键; Z表示羰基或键; K表示亚烷基或键; L表示-CH = CH-或键; M代表氢原子，烷基，环烷基，苯基，杂环，联苯基或二苯基甲基。

    Process for the production of a cephamycin derivative
    17.
    发明授权
    Process for the production of a cephamycin derivative 失效
    生产头孢霉素衍生物的方法

    公开(公告)号：US4302580A

    公开(公告)日：1981-11-24

    申请号：US185594

    申请日：1980-09-09

    申请人： Katsuyoshi Iwamatsu ,  Jiro Itoh ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inouye

    发明人： Katsuyoshi Iwamatsu ,  Jiro Itoh ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inouye

    IPC分类号： C07D501/04 ,  C07D501/36 ,  C07D501/57 ,  C12P35/08

    CPC分类号： C12P35/08

    摘要： A chemotherapeutic, antibacterial agent, 7.beta.-[(2D-2-amino-2-carboxy)ethylthioacetamido]-7.alpha.-methoxy-3-[(1-methyl-1H-tetrazole-5-yl)thiomethyl]-3-cephem-4-carboxylic acid is produced economically and efficiently starting from cephamycin A and/or B by a "new route" process comprising the consecutive steps of reaction of cephamycin with 5-mercapto-1-methyl-1H-tetrazole; protection of the terminal amino group thereof by acylation; protection of the two carboxyl groups thereof by esterification; replacement of the acyl group initially having attached to the 7-amino group by a halogenoacetyl group; deprotection of the blocked 4-carboxyl group; and condensation of D-cysteine with the halogenoacetyl group attaching to the 7-amino group.

    摘要翻译： 7β-[（2D-2-氨基-2-羧基）乙硫基乙酰氨基]-7α-甲氧基-3 - [（1-甲基-1H-四唑-5-基）硫代甲基] -3- 头孢霉素-4-羧酸从头孢霉素A和/或B开始通过包含头孢霉素与5-巯基-1-甲基-1H-四唑的连续步骤的“新途径”方法经济有效地产生; 通过酰化保护其末端氨基; 通过酯化保护其两个羧基; 用卤代乙酰基取代最初连接在7-氨基上的酰基; 封闭的4-羧基脱保护; 和D-半胱氨酸与连接于7-氨基的卤代乙酰基缩合。

    9-O-Alkanoyl-3
    18.
    发明授权
    9-O-Alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance and the production thereof 失效
    9-O-烷酰基-3 {41-烷酰氧基甲基-SF-837物质及其制备

    公开(公告)号：US3959256A

    公开(公告)日：1976-05-25

    申请号：US505310

    申请日：1974-09-12

    申请人： Shigeharu Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Taro Niida ,  Toyoaki Kawasaki ,  Takashi Tsuruoka

    发明人： Shigeharu Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Taro Niida ,  Toyoaki Kawasaki ,  Takashi Tsuruoka

    IPC分类号： C07H17/08

    CPC分类号： C07H17/08

    摘要： A 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is now synthetized, which is a new compound useful in that this new 9-O-alkanoyl-3"-O-alkanoyloxymethyl derivative of the SF-837 substance exhibits an antibacterial activity comparable to that of the parent SF-837 substance but is advantageously free from the unpleasant bitter taste inherent to the SF-837 substance and is hence adapted for oral administration. A process of producing the 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is also provided, which comprises hydrolysing partially and selectively a 9,2'-di-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance in an aqueous alkanol or aqueous acetone. The 9,2'-di-O-alkanoyl-3"-O-alkanopyloxymethyl-SF-837 substance may be prepared by reacting a 9,2'-di-alkanoyl- or O-mono-O-alkanoyl-3"-O-thiomethoxymethyl-SF-837 substance with an alkanoic anhydride which is exemplified by acetic anhydride or propionic anhydride in the specification.

    摘要翻译： 现在合成了9-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质，这是一种新的化合物，有用的是这种新型的9-O-烷酰基-3'-O-烷酰氧基甲基衍生物 -837物质表现出与母体SF-837物质相当的抗菌活性，但有利地没有SF-837物质固有的不愉快的苦味，因此适于口服给药。 还提供了制备9-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质的方法，其包括部分和选择性地水解9,2'-二-O-烷酰基-3'-O - 烷酰氧基甲基-SF-837物质在链烷醇水溶液或丙酮水溶液中。 9,2'-二-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质可以通过使9,2'-二烷酰基或O-单-O-烷酰基-3' 具有链烷酸酐的“-O-硫代甲氧基甲基-SF-837”物质，其例示在说明书中的乙酸酐或丙酸酐。

    1-Oxadethiacephalosporin derivatives and antibacterial use thereof
    19.
    发明授权
    1-Oxadethiacephalosporin derivatives and antibacterial use thereof 失效
    1-硫代十八烷基醚衍生物及其抗菌用途

    公开(公告)号：US4325951A

    公开(公告)日：1982-04-20

    申请号：US200410

    申请日：1980-10-24

    申请人： Shigeharu Inouye ,  Takashi Tsuruoka ,  Katsuyoshi Iwamatsu

    发明人： Shigeharu Inouye ,  Takashi Tsuruoka ,  Katsuyoshi Iwamatsu

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D505/00 ,  C07D498/04

    CPC分类号： C07D505/00 ,  Y02P20/55

    摘要： New antibacterial 1-oxadethiacephalosporin derivatives of the general formula ##STR1## wherein R is a heterocyclic group or a group --S--Het where Het denotes a heterocyclic group, Y is a hydrogen atom or a methoxy group; x and y are each an integer of 1 to 3 is produced by a process comprising condensing a 1-oxacephem compound of the formula ##STR2## wherein R, Y, y are as defined above; R' is a hydrogen atom or a carboxyl-protecting group; and Z is a halo group, with a sulfur-containing amino acid of the formula ##STR3## wherein x is as defined above, in a solvent and removing, if necessary, the residual protective group from the resultant condensation product. The new 1-oxadethiacephalosporin derivatives and the pharmaceutically acceptable salts and esters thereof exhibit high and broad "in vitro" and "in vivo" antibacterial activity, particularly against .beta.-lactamase-producing strains of gram-negative bacteria.

    摘要翻译： 其中R是杂环基的新型抗菌1-恶二硫醚类衍生物或其中Het表示杂环基的基团-S-Het，Y是氢原子或甲氧基; x和y各自为1〜3的整数，是通过下列方法制备的：其中R 1，Y，y如上所定义的式 R'是氢原子或羧基保护基; Z为卤素基，其中x如上定义，其中x如上所定义，并且如有必要，从所得缩合产物中除去残留的保护基团，其中含有式“IMAGE”的含硫氨基酸。 新的1-羟基乙硫菌醚衍生物及其药学上可接受的盐和酯在革兰氏阴性菌的β-内酰胺酶生产菌株中表现出高且广泛的“体外”和“体内”抗菌活性。

    Process for the production of a 7-methoxycephalosporine derivative
    20.
    发明授权
    Process for the production of a 7-methoxycephalosporine derivative 失效
    生产7-甲氧基头孢菌素衍生物的方法

    公开(公告)号：US4324891A

    公开(公告)日：1982-04-13

    申请号：US178604

    申请日：1980-08-15

    申请人： Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Kazuko Mizutani ,  Katsumi Kawaharajyo ,  Tadahiro Watanabe ,  Shigeharu Inouye

    发明人： Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Kazuko Mizutani ,  Katsumi Kawaharajyo ,  Tadahiro Watanabe ,  Shigeharu Inouye

    IPC分类号： C07D501/04 ,  C07D501/57

    CPC分类号： C07D501/57 ,  Y02P20/55

    摘要： A new, efficient process is provided for the production of 7.beta.-[(2D-2-amino-2-carboxy)-ethylthio-acetamido]-7.alpha.-methoxy-3-[(1-methyl-1H-tetrazole-5-yl) thiomethyl]-3-cephem-4-carboxylic acid useful as new antibacterial agent. This process is economic in using as the starting material the inexpensive, corresponding cephem compound containing no 7.alpha.-methoxy group on the cephem nucleus and comprises 7.alpha.-methoxylation of a protected derivative of the starting cephem compound with t-butyl hypochlorite and lithium methoxide, followed by inactivation of the excessive methoxylation reagents with a trialkyl phosphite and acetic acid to prevent undesired side-reactions such as oxidation of the alkylthioacetyl group of the product, and further by conventional removal of the protecting groups.

    摘要翻译： 提供了一种新的，有效的方法，用于生产7β - [（2D-2-氨基-2-羧基） - 乙硫基 - 乙酰氨基]-7α-甲氧基-3 - [（1-甲基-1H-四唑-5 - 基）硫代甲基] -3-头孢烯-4-羧酸，可用作新的抗菌剂。 该方法在起始物质中是经济的，其是在头孢烯核上不含有7个α-甲氧基的廉价相应的头孢烯化合物，并且包括起始头孢烯化合物与叔丁基次氯酸盐和甲醇锂的保护的衍生物的7α-甲氧基化 然后用亚磷酸三烷基酯和乙酸使过量的甲氧基化试剂失活，以防止不期望的副反应如产物的烷基硫代乙酰基氧化，并进一步通过常规除去保护基。