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    Sphingosine analogues
    1.
    发明授权
    Sphingosine analogues 失效
    鞘氨醇类似物

    公开(公告)号：US06235912B1

    公开(公告)日：2001-05-22

    申请号：US09380647

    申请日：1999-10-15

    申请人： Kazutoh Takesako ,  Toru Kurome ,  Naoyuki Awazu ,  Ikunoshin Kato

    发明人： Kazutoh Takesako ,  Toru Kurome ,  Naoyuki Awazu ,  Ikunoshin Kato

    IPC分类号： C07C23100

    CPC分类号： C07D307/33 ,  C07C215/10 ,  C07C215/24 ,  C07C229/22 ,  C07C229/30 ,  C07C237/08 ,  C07C237/22 ,  C07C251/08 ,  C07C271/22 ,  C07D263/06 ,  Y02P20/55

    摘要： The present invention aims to provide a novel sphingosine analogue, which is useful as an intermediate for syntheses of novel lipid derivatives such as sphingolipid derivatives and the like that can regulate the effects of sphingolipid. The present invention relates to a sphingosine analogue represented by the general formula (I) described below. In the formula, as for Q1, Q2 and Q3, Q1 and Q2, which are the same or different each other, are hydrogen, alkyl groups having 1-4 of carbon atoms, acyl groups having 2-5 of carbon atoms, or protecting groups of the amino group, and Q3 is a hydrogen or a protecting group of the hydroxyl group; or Q2 and Q3 make up an isopropylidene group and Q1 is a hydrogen or a protecting group of the amino group. Q4 and Q5, which are the same or different each other, are hydroxyl groups, acyl groups having 2-5 of carbon atoms, —O—Q6, or hydrogen; or Q4 and Q5 make up a covalent bond. Q6 is a protecting group of the hydroxyl group. X1 is —COOH, —CONH2, —CO—Q7, —CH2OH, or —CH2O—Q8. Q7 is a protecting group of the carboxyl group, and Q8 is a protecting group of the hydroxyl group.

    摘要翻译： 本发明的目的在于提供一种新颖的鞘氨醇类似物，其可用作合成新型脂质衍生物的中间体，例如可以调节鞘脂的作用的鞘脂衍生物等。本发明涉及一般的鞘氨醇类似物 在该式中，对于Q1，Q2和Q3，Q1和Q2彼此相同或不同，为氢，具有1-4个碳原子的烷基，酰基具有2- 5个碳原子或氨基的保护基，Q3为氢或羟基的保护基; 或Q2和Q3构成异亚丙基，Q 1为氢或氨基的保护基。 Q4和Q5彼此相同或不同，是羟基，具有2-5个碳原子的酰基，-O-Q6或氢; 或Q4和Q5构成共价键。 Q6是羟基的保护基。 X 1是-COOH，-CONH 2，-CO-Q 7，-CH 2 OH或-CH 2 O-Q 8。 Q7是羧基的保护基，Q8是羟基的保护基。

    Sphingosine derivatives and medicinal composition
    3.
    发明授权
    Sphingosine derivatives and medicinal composition 失效
    鞘氨醇衍生物和药用组合物

    公开(公告)号：US06239297B1

    公开(公告)日：2001-05-29

    申请号：US09508462

    申请日：2000-04-28

    申请人： Kazutoh Takesako ,  Toru Kurome ,  Naoyuki Awazu ,  Ikunoshin Kato

    发明人： Kazutoh Takesako ,  Toru Kurome ,  Naoyuki Awazu ,  Ikunoshin Kato

    IPC分类号： C07C23300

    CPC分类号： C07C219/06 ,  C07C229/08 ,  C07C235/12 ,  C07C237/12 ,  C07C237/22

    摘要： The present invention intends to provide a derivative of sphingosine analogue that is able to regulate the functions of sphigolipid, and its pharmaceutical compositions. The present invention is the derivatives of sphingosine analogues represented by the general formula (I) described below. In the formula, R1 and R2, which are the same or different each other, are hydrogen, alkyl groups having 1-4 carbon atoms, or acyl groups having 2-5 carbon atoms. R3 and R4, which are the same or different each other, are hydrogen or hydroxyl groups; or R3 and R4 make up a covalent bond. X1 is —(CH2)n—CO—NH—CH(R5)—R6 or —(CH2)m—O—CO—CH(R7)—R8.

    摘要翻译： 本发明旨在提供能够调节鞘脂类功能的鞘氨醇类似物的衍生物及其药物组合物。本发明是由下述通式（I）表示的鞘氨醇类似物的衍生物。在式中， R 1和R 2彼此相同或不同，为氢，具有1-4个碳原子的烷基或具有2-5个碳原子的酰基。 R3和R4彼此相同或不同，是氢或羟基; 或R3和R4组成共价键。 X1是 - （CH2）n-CO-NH-CH（R5）-R6或 - （CH2）m-O-CO-CH（R7）-R8。

    Physiologically active substances TKR2449, process for producing the same, and microorganism
    4.
    发明授权
    Physiologically active substances TKR2449, process for producing the same, and microorganism 失效
    生理活性物质TKR2449，其生产方法和微生物

    公开(公告)号：US06303350B1

    公开(公告)日：2001-10-16

    申请号：US09445543

    申请日：2000-03-07

    申请人： Kazutoh Takesako ,  Mitsuhiro Ueno ,  Naoyuki Awazu ,  Yoko Uno ,  Ikunoshin Kato

    发明人： Kazutoh Takesako ,  Mitsuhiro Ueno ,  Naoyuki Awazu ,  Yoko Uno ,  Ikunoshin Kato

    IPC分类号： C12P1302

    CPC分类号： C07C235/76 ,  C12P13/02 ,  Y10S435/911

    摘要： The present invention has for its object to provide novel biologically active substances which is of value as a therapeutic agent for fungal infections and immune disorders. This invention is related to a biologically active substance TKR2449 analog(s) which is represented by the following general formula (A); (In the formula, R1, R2 and R3 are the same or differ each other, and each represents hydrogen or an alkyl group of carbon number of 1 to 4. R4 is a linear or branched alkyl or alkenyl group of carbon number of 1 to 8.).

    摘要翻译： 本发明的目的是提供新的生物活性物质，其作为真菌感染和免疫疾病的治疗剂是有价值的。 本发明涉及由以下通式（A）表示的生物活性物质TKR2449类似物：（式中，R 1，R 2和R 3相同或不同，各自表示氢或 碳数为1〜4的烷基.R 4为碳原子数为1〜8的直链或支链烷基或烯基。

    Process for systhesizing cyclic peptides
    5.
    发明授权
    Process for systhesizing cyclic peptides 失效
    环肽杂交的方法

    公开(公告)号：US5633346A

    公开(公告)日：1997-05-27

    申请号：US450539

    申请日：1995-05-25

    申请人： Toru Kurome ,  Kazutoh Takesako ,  Ikunoshin Kato ,  Kaoru Inami ,  Tetsuo Shiba

    发明人： Toru Kurome ,  Kazutoh Takesako ,  Ikunoshin Kato ,  Kaoru Inami ,  Tetsuo Shiba

    IPC分类号： A61K38/00 ,  A61P31/04 ,  A61P31/10 ,  C07K1/06 ,  C07K1/113 ,  C07K11/02 ,  A61K38/12

    CPC分类号： C07K11/02 ,  A61K38/00

    摘要： A process is provided for the total synthesis of a cyclic peptide, which is useful as antifungal drug, and novel compounds prepared by the synthesis method. The cyclic peptide is represented by the following formula (I): ##STR1## wherein X1, X2, X4 and X7 are independently N-methyl-.alpha.-amino acid or .alpha.-hydroxy acid,provided that at least one of X1, X2, X4 and X7 is an .alpha.-hydroxy acid;X3, X6 and X8 are independently .alpha.-amino acid;X5 is a cyclic amino acid;X9 is an N-methyl-.alpha.-amino acid or .alpha.-hydroxy acid substituted by a hydroxy group;and the dotted lines represent intramolecular hydrogen bonds.The process includes cyclizing a corresponding linear peptide between X5 and X6 via a peptide bond.

    摘要翻译： 提供了可用作抗真菌药物的环肽的全合成方法和通过合成方法制备的新化合物。 环肽由下式（I）表示：其中X 1，X 2，X 4和X 7独立地是N-甲基-α-氨基酸或α-羟基酸，条件是X1中的至少一个 ，X2，X4和X7是α-羟基酸; X3，X6和X8独立地是α-氨基酸; X5是环状氨基酸; X 9是被羟基取代的N-甲基-α-氨基酸或α-羟基酸; 虚线表示分子内氢键。 该方法包括通过肽键在X5和X6之间环化相应的线性肽。

    Antibiotic TKR2999, process for the preparation thereof and microbe
    8.
    发明授权
    Antibiotic TKR2999, process for the preparation thereof and microbe 失效
    抗生素TKR2999，其制备方法和微生物

    公开(公告)号：US06333305B1

    公开(公告)日：2001-12-25

    申请号：US09582025

    申请日：2000-08-02

    申请人： Kazutoh Takesako ,  Naoyuki Awazu ,  Mitsuhiro Ueno ,  Yoshimi Onishi ,  Ikunoshin Kato

    发明人： Kazutoh Takesako ,  Naoyuki Awazu ,  Mitsuhiro Ueno ,  Yoshimi Onishi ,  Ikunoshin Kato

    IPC分类号： A01N3718

    CPC分类号： C12R1/645 ,  A61K38/00 ,  C07K4/06 ,  C12P21/02

    摘要： The antibiotic TKR2999 having the physicochemical properties described below and its pharmacologically acceptable salt: (1) FAB-MS m/z 971 [M+H)]+, (2) the molecular formula: C44H78N10O14, and high-resolution FAB-MS m/z 971.5776 [M+H]+, (3) the ultraviolet absorption spectrum in methanol has an end absorption, (4) the infrared absorption spectrum by KBr method shows the major absorption wave numbers at 3320, 2920, 1680, 1540, 1210, 1140, 840, 800, and 720 cm−1, (5) aspartic acid, threonine, serine, glycine, alanine, &bgr;-alanine, and ornithine are detected by the amino acid analysis using ninhydrin reaction, and (6) the solubility is that it is soluble in methanol, and practically insoluble in hexane, chloroform, and water.

    摘要翻译： 具有下述物理化学性质的抗生素TKR2999及其药理学上可接受的盐：（1）FAB-MS m / z 971 [M + H]] +，（2）分子式：C44H78N10O14和高分辨率FAB-MS m / z 971.5776 [M + H] +，（3）甲醇中的紫外吸收光谱具有终点吸收，（4）通过KBr方法的红外吸收光谱显示3320,2920,1680,1540,1210的主要吸收波数 ，1140,840,800和720cm -1，（5）通过使用茚三酮反应的氨基酸分析检测天冬氨酸，苏氨酸，丝氨酸，甘氨酸，丙氨酸，β-丙氨酸和鸟氨酸，和（6）溶解度 它是溶于甲醇，几乎不溶于己烷，氯仿和水。

    Cyclic peptides
    10.
    发明授权
    Cyclic peptides 失效
    循环肽

    公开(公告)号：US5633345A

    公开(公告)日：1997-05-27

    申请号：US433067

    申请日：1995-05-03

    申请人： Toru Kurome ,  Kazutoh Takesako ,  Ikunoshin Kato ,  Kaoru Inami ,  Tetsuo Shiba

    发明人： Toru Kurome ,  Kazutoh Takesako ,  Ikunoshin Kato ,  Kaoru Inami ,  Tetsuo Shiba

    IPC分类号： A61K38/00 ,  A61P31/04 ,  A61P31/10 ,  C07K1/06 ,  C07K1/113 ,  C07K11/02 ,  A61K38/12

    CPC分类号： C07K11/02 ,  A61K38/00

    摘要： To provide a process for the total synthesis of a cyclic peptide, which is useful as antifungal drug, and novel compounds prepared by the synthesis method. A process for synthesizing a cyclic peptide represented by the following formula (I): ##STR1## wherein X1, X2, X4 and X7 are independently N-methyl-.alpha.-amino acid or .alpha.-hydroxy acid,provided that at least one of X1, X2, X4 and X7 is a .alpha.-hydroxy acid;X3, X6 and X8 are independently .alpha.-amino acid;X5 is a cyclic amino acid;X9 is a N-methyl-.alpha.-amino acid or .alpha.-hydroxy acid substituted by a hydroxy group;and the dotted lines represent intramolecular hydrogen bonds;which process comprises cyclizing a corresponding linear peptide between X5 and X6 via a peptide bond, and a novel compound represented by the formula (I).

    摘要翻译： 提供可用作抗真菌药物的环肽的全合成方法和通过合成方法制备的新型化合物。 用于合成由下式（I）表示的环肽的方法：其中X 1，X 2，X 4和X 7独立地是N-甲基-α-氨基酸或α-羟基酸，条件是至少 X1，X2，X4和X7之一是α-羟基酸; X3，X6和X8独立地是α-氨基酸; X5是环状氨基酸; X 9是被羟基取代的N-甲基-α-氨基酸或α-羟基酸; 虚线表示分子内氢键; 该方法包括通过肽键在X5和X6之间环化相应的线性肽，和由式（I）表示的新型化合物。