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1. 发明授权

US5698670A 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。

2. 发明授权

US5633346A Process for systhesizing cyclic peptides 失效
标题翻译：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。

3. 发明授权

US5633345A Cyclic peptides 失效
标题翻译：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。

4. 发明授权

US6111145A Cyclopentenone derivative 失效
标题翻译：环戊烯酮衍生物
公开(公告)号：US6111145A
公开(公告)日：2000-08-29
申请号：US419221
申请日：1999-10-15
申请人： Eiji Kobayashi , Nobuto Koyama , Ikunoshin Kato , Kaoru Inami , Tetsuo Shiba
发明人： Eiji Kobayashi , Nobuto Koyama , Ikunoshin Kato , Kaoru Inami , Tetsuo Shiba
IPC分类号： C07C45/71 , C07C49/753 , C07C49/105 , A61K31/12
CPC分类号： C07C49/753 , C07C45/71
摘要： A cyclopentenone derivative represented by the following formula [I] or an optically active substance or a salt thereof. ##STR1## (In the formula, R.sub.1 and R.sub.2 are same or different and each of them is straight or branched alkyl group, straight or branched alkenyl group, aromatic group, aromatic-aliphatic group or H with a proviso that the case where R.sub.1 =R.sub.2 =H, or R.sub.1 =benzyl group and R.sub.2 =H is excluded.)
摘要翻译：由下式[I]表示的环戊烯酮衍生物或光学活性物质或其盐。（式中，R 1，R 2相同或不同，分别为直链或支链烷基，直链或支链烯基，芳香族基，芳香族 - 脂肪族基或H，条件是R1 = R2 = H ，或R 1 =苄基，并且R 2 = H被排除。

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