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8 条记录 (耗时 0.016 秒)

    Process for systhesizing cyclic peptides
    2.
    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。

    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。

    Cyclic peptides
    4.
    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。

    Sphingosine analogues
    6.
    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。

    Aureobasidins
    7.
    发明授权
    Aureobasidins 失效

    公开(公告)号：US5698670A

    公开(公告)日：1997-12-16

    申请号：US505255

    申请日：1995-08-16

    申请人： Toru Kurome ,  Tetsuya Inoue ,  Kazutoh Takesako ,  Kaoru Inami ,  Ikunoshin Kato

    发明人： Toru Kurome ,  Tetsuya Inoue ,  Kazutoh Takesako ,  Kaoru Inami ,  Ikunoshin Kato

    IPC分类号： A61K38/00 ,  C07K11/02 ,  A61K38/12 ,  C07K5/00

    CPC分类号： C07K11/02 ,  A61K38/00

    摘要： This invention relates to Aureobasidins useful as an antifungal agent having broader spectrum. The compound according to this invention includes a cyclic depsipeptide consisting of one hydroxy acid residue having A.sup.1, 3 amino acid residues having C.sup.1, F.sup.1 and H.sup.1, respectively, 4 N-methylamino acid residues having B.sup.1, D.sup.1, G.sup.1 and I.sup.1, respectively, and 1 cyclic amino acid residue having E.sup.1. The typical compound includes one wherein A.sup.1 is CH.sub.3 CH.sub.2 CH(CH.sub.3)--, B.sup.1 is (CH.sub.3).sub.2 CH--, C.sup.1 is benzyl, cyclohexylmethyl, p-fluorobenzyl, benzyloxymethyl, benzyloxybenzyl, methoxybenzyl, cyclohexylmethyloxybenzyl or the like, D.sup.1 is methyl, benzyl, hydroxymethyl or the like, E.sup.1 is --(CH.sub.2).sub.3 --, F.sup.1 is CH.sub.3 CH.sub.2 CH(CH.sub.3)--, G.sup.1 is (CH.sub.3).sub.2 CH--, H.sup.1 is (CH.sub.3).sub.2 CHCH.sub.2 -- and I.sup.1 is (CH.sub.3).sub.2 C(OH)--. The compound according to this invention has an excellent activity against not only Candida but also Cryptococcus and Aspergillus.

    摘要翻译： PCT No.PCT / JP94 / 02201 Sec。 371日期：1995年8月16日 102（e）日期1995年8月16日PCT 1994年12月26日PCT公布。 出版物WO95 / 18147 日期1995年7月6日本发明涉及可用作具有更宽光谱的抗真菌剂的Aureobasidins。 根据本发明的化合物包括由一个具有A1的羟基酸残基，具有C1，F1和H1的3个氨基酸残基，分别具有B1，D1，G1和I1的4个N-甲基氨基酸残基的环状缩肽，以及 1个具有E1的环状氨基酸残基。 典型的化合物包括其中A 1为CH 3 CH 2 CH（CH 3） - ，B 1为（CH 3）2 CH-，C 1为苄基，环己基甲基，对氟苄基，苄氧基甲基，苄氧基苄基，甲氧基苄基，环己基甲氧基苄基等的化合物，D1为甲基，苄基， 等等，E1是 - （CH 2）3 - ，F1是CH 3 CH 2 CH（CH 3） - ，G 1是（CH 3）2 CH-，H 1是（CH 3）2 CHCH 2 - 且I 1是（CH 3）2 C（OH） - 。 根据本发明的化合物对假丝酵母不仅具有优异的活性，而且对隐球菌和曲霉也具有优异的活性。