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    • 1. 发明授权
    • Cyclic tetrapeptide derivatives and medicinal use thereof
    • 环状四肽衍生物及其医药用途
    • US06399568B1
    • 2002-06-04
    • US09486783
    • 2000-03-01
    • Norikazu NishinoMinoru YoshidaSueharu HorinouchiYasuhiko KomatsuTsutomu Mimoto
    • Norikazu NishinoMinoru YoshidaSueharu HorinouchiYasuhiko KomatsuTsutomu Mimoto
    • A61K3812
    • C07K5/126A61K38/00
    • A cyclic tetrapeptide derivative represented by the general formula (I): wherein: R11, R12, R21 and R22 independently denote a monovalent group selected from hydrogen, a linear or branched alkyl group with 6 or less carbon atoms, benzyl group, 4-methoxybenzyl group, 3-indolylmethyl group, (N-methoxy-3-indolyl) methyl group, (N-formyl-3-indolyl)methyl group, etc.; R3 denotes a divalent group selected from a linear chained hydrocarbon group with 3 or 4 carbon atoms, or the linear branched hydrocarbon group having a branched chain added to the chain, or a divalent group substituted with a heteroatom; R4 denotes a divalent chained hydrocarbon group with 4 to 6 carbon atoms, or a divalent group derived from said hydrocarbon group by addition etc. of a branched chain on said chain; and a pharmaceutically acceptable salt thereof, or an analogous cyclic tetrapeptide derivative compound; as well as a histone deacetylase enzyme inhibitor, an MHC class-I molecule expression promoting agent and a pharmaceutical composition that comprise said cyclic tetrapeptide derivative as an effective ingredient.
    • 由通式(I)表示的环状四肽衍生物:其中:R11,R12,R21和R22独立地表示选自氢,碳原子数6以下的直链或支链烷基,苄基,4-甲氧基苄基 (3-甲氧基-3-吲哚基)甲基,(N-甲酰基-3-吲哚基)甲基等。 R3表示选自具有3或4个碳原子的直链状烃基或者在该链上添加有支链的直链支链烃基或被杂原子取代的二价基团的二价基团; R4表示二价链状烃基 或含有4〜6个碳原子的二价基团,或通过所述链上的支链的加成等衍生自所述烃基的二价基团; 和其药学上可接受的盐,或类似的环状四肽衍生物化合物; 以及组蛋白脱乙酰酶酶抑制剂,MHC class I分子表达促进剂和包含所述环状四肽衍生物作为有效成分的药物组合物。
    • 2. 发明授权
    • Cyclic tetrapeptide derivatives and pharmaceutical uses thereof
    • 环状四肽衍生物及其药物用途
    • US06825317B2
    • 2004-11-30
    • US09945237
    • 2001-08-31
    • Norikazu NishinoMinoru YoshidaSueharu HorinouchiYasuhiko Komatsu
    • Norikazu NishinoMinoru YoshidaSueharu HorinouchiYasuhiko Komatsu
    • C07K752
    • C07K5/126A61K38/00
    • The present invention provides a cyclic tetrapeptide derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: wherein each of R21 and R22 independently denotes hydrogen, a linear C1-C6-alkyl group to which a non-aromatic cycloalkyl group or an optionally substituted aromatic ring may be attached, or a branched C3-C6-alkyl group to which a non-aromatic cycloalkyl group or an optionally substituted aromatic ring may be attached; and each of R1 and R3 independently denotes a linear C1-C5-alkylene group which may have a C1-C6 side chain, in which the side chain may form a condensed ring structure on the alkylene chain. The present invention also provides a histone deacetylase inhibitor, an MHC class-I molecule expression-promoting agent and a pharmaceutical composition, each of which comprises the above cyclic tetrapeptide derivative or pharmaceutically acceptable salt thereof as an active ingredient.
    • 本发明提供由以下通式(I)表示的环状四肽衍生物或其药学上可接受的盐:R21和R22独立地表示氢,非芳香族环烷基的直链C 1 -C 6 - 烷基或 可以连接任选取代的芳环,或者可以连接非芳族环烷基或任选取代的芳环的支链C 3 -C 6 - 烷基; R 1和R 3的每一个独立地表示可以具有C 1 -C 6侧链的直链C 1 -C 5亚烷基,其中侧链可以在亚烷基链上形成稠环结构。本发明还提供组蛋白脱乙酰酶抑制剂 ,MHC I类分子表达促进剂和药物组合物,其各自包含上述环状四肽衍生物或其药学上可接受的盐作为活性成分。
    • 5. 发明授权
    • Human CRM1 Protein
    • 人类CRM1蛋白
    • US5948883A
    • 1999-09-07
    • US975527
    • 1997-11-20
    • Minoru YoshidaSueharu HorinouchiKazunori Nishi
    • Minoru YoshidaSueharu HorinouchiKazunori Nishi
    • A61K38/00C07K14/47C12N15/12
    • C07K14/4703A61K38/00
    • A protein which comprises the sane or substantially the same amino acid sequence as that represented by SEQ ID NO:1, its partial peptide and their salts are disclosed. DNA encoding the protein or its partial peptide is also disclosed. The protein, its partial peptide or a salt thereof is an inhibitory factor of a transcription factor and, therefore, it is useful as medicine such as prophylactic and therapeutic drugs of, for example, tumors. The DNA is useful as a gene diagnosing drug. The antibody against the protein, etc. is also disclosed. The antibody is used for, for example, quantitative determination of the protein, etc. in a specimen fluid. The protein, etc. are also useful as a reagent for screening for compounds or their salts which promote the function of the protein, etc.
    • 公开了包含与SEQ ID NO:1所示的基本相同的氨基酸序列的蛋白质,其部分肽及其盐。 还公开了编码蛋白质或其部分肽的DNA。 蛋白质,其部分肽或其盐是转录因子的抑制因子,因此可用作例如肿瘤的预防和治疗药物等药物。 该DNA可用作诊断药物的基因。 还公开了针对蛋白质等的抗体。 抗体用于例如样品流体中蛋白质等的定量测定。 蛋白质等也可用作筛选促进蛋白质等功能的化合物或其盐的试剂。