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1. 发明申请

WO0008047A8 DEPSIPEPTIDE DERIVATIVES BEARING PIPERAZINONE RINGS 审中-公开
标题翻译：含哌嗪酮环的哌普生衍生物
公开(公告)号：WO0008047A8
公开(公告)日：2000-05-04
申请号：PCT/JP9904205
申请日：1999-08-04
申请人： NISSHIN FLOUR MILLING CO , YANAI MAKOTO , SUZUKI MASASHI , OSHIDA NORIO , KAWAMURA KOJI , HIRAMOTO SHIGERU , YASUDA ORIE , KINOSHITA NOBUHIRO , SHINGAI AKIKO , TAKASU MASAKO
发明人： YANAI MAKOTO , SUZUKI MASASHI , OSHIDA NORIO , KAWAMURA KOJI , HIRAMOTO SHIGERU , YASUDA ORIE , KINOSHITA NOBUHIRO , SHINGAI AKIKO , TAKASU MASAKO
IPC分类号： A61K38/00 , C07K5/02 , C07K5/078 , C07K5/062 , A61K31/50 , A61K38/06 , C07D241/08 , C07K5/072 , C07K5/083
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0207
摘要： Novel depsipeptide derivatives bearing piperazinone rings in the molecule, represented by general formula (1) wherein X1 is N(R4)-CO, N(R5)-CH2, CH2-CO, CH2-CH2, CH=CH, CH2-CH(OH) or CH(OH)-CH(OH); R1 is C5-C20 alkyl or alkoxy(C5-C15)alkyl(C1-C4); R2 to R5 are each hydrogen or C1-C6 alkyl; and A is (2), (3) or (4): -X2-CH(R11)-X3-CH(R12)-NH-R13. These derivatives exhibit apolipoprotein E production accelerating activities, thus being useful as remedies for nerve injury, dementia and hyperlipidemia.
摘要翻译：由通式（1）表示的分子中带有哌嗪酮环的新型缩酚酸肽衍生物，其中X1是N（R4）-CO，N（R5）-CH2，CH2-CO，CH2-CH2，CH = CH，CH2- OH）或CH（OH）-CH（OH）; R1是C5-C20烷基或烷氧基（C5-C15）烷基（C1-C4）; R2至R5各自为氢或C1-C6烷基; （2），（3）或（4）：-X2-CH（R11）-X3-CH（R12）-NH-R13。这些衍生物表现出载脂蛋白E产生促进活性，因此可用作神经损伤，痴呆和高脂血症的治疗剂。

2. 发明申请

WO1997049724A1 CYCLIC DEPSIPEPTIDES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开
标题翻译：循环阻断剂和含有它们作为活性成分的药物
公开(公告)号：WO1997049724A1
公开(公告)日：1997-12-31
申请号：PCT/JP1997002194
申请日：1997-06-25
申请人： NISSHIN FLOUR MILLING CO., LTD. , YANAI, Makoto , SUZUKI, Masashi , OSHIDA, Norio , KAWAMURA, Koji , HIRAMOTO, Shigeru , YASUDA, Orie , KINOSHITA, Nobuhiro , SHINGAI, Akiko , KANAI, Masako
发明人： NISSHIN FLOUR MILLING CO., LTD.
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Cyclic depsipeptides represented by general formula (1) or pharmacologically acceptable salts thereof, wherein R represents linear or branched C5-20 alkyl or linear or branched C5-15 alkoxymethyl; A, B, D, E and F independently represent each alanine, valine, leucine, isoleucine, phenylalanine, etc.; W and Z independently represent each aspartic acid, asparagine, glutamic acid or glutamine; and m and n independently represent each 0 or 1. These compounds are produced by the conventional methods for synthezing peptides. They are useful as apolipoprotein E production promoters, remedies for nerve injury, remedies for dementia, apolipoprotein B production inhibitors, apolipoprotein A1 production promoters and remedies for hyperlipemia.
摘要翻译：由通式（1）表示的环状缩酚酸肽或其药学上可接受的盐，其中R表示直链或支链的C 5-20烷基或直链或支链的C 5-15烷氧基甲基; A，B，D，E和F独立地表示丙氨酸，缬氨酸，亮氨酸，异亮氨酸，苯丙氨酸等; W和Z独立地表示各天冬氨酸，天冬酰胺，谷氨酸或谷氨酰胺; m和n独立地表示0或1.这些化合物通过用于合成肽的常规方法制备。它们可用作载脂蛋白E生产促进剂，神经损伤补救剂，痴呆症药物，载脂蛋白B生产抑制剂，载脂蛋白A1生产促进剂和高脂血症治疗药物。

3. 发明申请

WO1997049722A1 DEPSIPEPTIDES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开
标题翻译：其含有作为活性成分的药物和药物
公开(公告)号：WO1997049722A1
公开(公告)日：1997-12-31
申请号：PCT/JP1997002195
申请日：1997-06-25
申请人： NISSHIN FLOUR MILLING CO., LTD. , YANAI, Makoto , SUZUKI, Masashi , OSHIDA, Norio , KAWAMURA, Koji , HIRAMOTO, Shigeru , YASUDA, Orie , KINOSHITA, Nobuhiro , SHINGAI, Akiko , KANAI, Masako
发明人： NISSHIN FLOUR MILLING CO., LTD.
IPC分类号： C07K05/02
CPC分类号： C07K5/1021 , A61K38/00 , C07K5/06043 , C07K5/06052 , C07K5/06104 , C07K5/101 , C07K7/06 , C07K11/00
摘要： Depsipeptides represented by general formula (1) or pharmacologically acceptable salts thereof, wherein R1 represents linear or branched C5-20 alkyl or linear or branched C5-15 alcoxymethyl; R2 represents -A-B, -A-B-W, -A-B-W-D or -A-B-W-D-E; and R3 represents hydroxy, lower alkoxy, benzyloxy, -Z, -Z-G or -Z-G-J, wherein A, B, D, E, G and J independently represent each an amino acid residue selected from among alanine, valine, leucine, isoleucine, serine, threonine, lysine, hydroxylysine, arginine, cysteine, methionine, phenylalanine, tyrosine, aspartic acid, asparagine, glutamic acid, glutamine, etc. optionally bonded to N-(C1-4 alkyl); W and Z independently represent each an animo acid residue selected from among aspartic acid, asparagine, glutamic acid, glutamine, alanine, serine, and lysine. These depsipeptides have the effects of promoting apolipoprotein E production and are useful as remedies for nerve injury and, in particular, remedies for dementia. They are also useful as remedies for hyperlipemia.
摘要翻译：由通式（1）表示的多肽或其药理学上可接受的盐，其中R 1表示直链或支链的C 5-20烷基或直链或支链的C 5-15烷氧基甲基; R2代表-A-B，-A-B-W，-A-B-W-D或-A-B-W-D-E; 并且R 3表示羟基，低级烷氧基，苄氧基，-Z，-ZG或-ZGJ，其中A，B，D，E，G和J各自独立地表示选自丙氨酸，缬氨酸，亮氨酸，异亮氨酸，丝氨酸，任选地键合到N-（C 1-4烷基）上的苏氨酸，赖氨酸，羟赖氨酸，精氨酸，半胱氨酸，甲硫氨酸，苯丙氨酸，酪氨酸，天冬氨酸，天冬酰胺，谷氨酸，谷氨酰胺等。 W和Z独立地表示各自选自天冬氨酸，天冬酰胺，谷氨酸，谷氨酰胺，丙氨酸，丝氨酸和赖氨酸中的一个酸性残基。这些脱脂肽具有促进载脂蛋白E产生的作用，并且可用作神经损伤的补救措施，特别是用于痴呆的补救措施。它们也可用作高脂血症的补救措施。

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