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1. 发明申请

US20130029878A1 Method for Assaying Histone Methylation Enzyme Activity 有权
标题翻译：分析组蛋白甲基化酶活性的方法
公开(公告)号：US20130029878A1
公开(公告)日：2013-01-31
申请号：US13639334
申请日：2011-04-15
申请人： Norikazu Nishino , Yasushi Takemoto , Akihiro Ito , Minoru Yoshida
发明人： Norikazu Nishino , Yasushi Takemoto , Akihiro Ito , Minoru Yoshida
IPC分类号： G01N21/64 , C40B30/08 , C07K2/00 , G01N21/78
CPC分类号： C12Q1/37 , C07D311/18 , C07D311/82 , C07D473/32 , C12Q1/48 , G01N33/6875 , G01N2500/00 , Y02P20/55
摘要： Provided are a method for measuring histone methyltransferase activity, a method for screening for compounds that inhibit histone methyltransferase activity, a reagent kit for measuring histone methyltransferase activity, and a kit for screening for compounds that inhibit histone methyltransferase activity. A substrate compound represented by general formula (I): R1—X—K—R2 (I), or a salt thereof, wherein R1 represents a hydrogen atom or a protecting group for an amino terminus; X represents a peptide consisting of 0 or 1 or more amino acid residues; K represents a lysine residue; and R2 represents a dye label linked via an amide bond to the carbonyl terminus of a lysine residue, wherein the cleavage of the amide bond by peptidase changes the fluorescence property or chromogenic property of the dye label, and the methylation of the ε amino group of the lysine residue by the histone methyltransferase decreases susceptibility to peptidase, is used.
摘要翻译：提供了测定组蛋白甲基转移酶活性的方法，用于筛选抑制组蛋白甲基转移酶活性的化合物的方法，用于测定组蛋白甲基转移酶活性的试剂盒和用于筛选抑制组蛋白甲基转移酶活性的化合物的试剂盒。由通式（I）表示的底物化合物：R1-X-K-R2（I）或其盐，其中R1表示氢原子或氨基末端的保护基; X表示由0或1个或更多个氨基酸残基组成的肽; K表示赖氨酸残基; R2表示通过酰胺键与赖氨酸残基的羰基末端连接的染料标记，其中通过肽酶切割酰胺键改变染料标记的荧光性质或显色性质，以及染料标记的甲基化。使用组蛋白甲基转移酶的赖氨酸残基的氨基降低对肽酶的易感性。

2. 发明授权

US09012166B2 Method for assaying histone methylation enzyme activity 有权
标题翻译：测定组蛋白甲基化酶活性的方法
公开(公告)号：US09012166B2
公开(公告)日：2015-04-21
申请号：US13639334
申请日：2011-04-15
申请人： Norikazu Nishino , Yasushi Takemoto , Akihiro Ito , Minoru Yoshida
发明人： Norikazu Nishino , Yasushi Takemoto , Akihiro Ito , Minoru Yoshida
IPC分类号： G01N21/78 , C12Q1/37 , C12Q1/48 , G01N33/68 , C07D311/18 , C07D311/82 , C07D473/32
CPC分类号： C12Q1/37 , C07D311/18 , C07D311/82 , C07D473/32 , C12Q1/48 , G01N33/6875 , G01N2500/00 , Y02P20/55
摘要： Provided are a method for measuring histone methyltransferase activity, a method for screening for compounds that inhibit histone methyltransferase activity, a reagent kit for measuring histone methyltransferase activity, and a kit for screening for compounds that inhibit histone methyltransferase activity. A substrate compound represented by general formula (I): R1-X-K-R2 (I), or a salt thereof, wherein R1 represents a hydrogen atom or a protecting group for an amino terminus; X represents a peptide consisting of 0 or 1 or more amino acid residues; K represents a lysine residue; and R2 represents a dye label linked via an amide bond to the carbonyl terminus of a lysine residue, wherein the cleavage of the amide bond by peptidase changes the fluorescence property or chromogenic property of the dye label, and the methylation of the ε amino group of the lysine residue by the histone methyltransferase decreases susceptibility to peptidase, is used.
摘要翻译：提供了测定组蛋白甲基转移酶活性的方法，用于筛选抑制组蛋白甲基转移酶活性的化合物的方法，用于测定组蛋白甲基转移酶活性的试剂盒和用于筛选抑制组蛋白甲基转移酶活性的化合物的试剂盒。由通式（I）表示的底物化合物：R1-X-K-R2（I）或其盐，其中R1表示氢原子或氨基末端的保护基; X表示由0或1个或更多个氨基酸残基组成的肽; K表示赖氨酸残基; R2表示通过酰胺键与赖氨酸残基的羰基末端连接的染料标记，其中通过肽酶切割酰胺键改变染料标记的荧光性质或显色性质，以及染料标记的甲基化。使用组蛋白甲基转移酶的赖氨酸残基的氨基降低对肽酶的易感性。

3. 发明授权

US06399568B1 Cyclic tetrapeptide derivatives and medicinal use thereof 失效
标题翻译：环状四肽衍生物及其医药用途
公开(公告)号：US06399568B1
公开(公告)日：2002-06-04
申请号：US09486783
申请日：2000-03-01
申请人： Norikazu Nishino , Minoru Yoshida , Sueharu Horinouchi , Yasuhiko Komatsu , Tsutomu Mimoto
发明人： Norikazu Nishino , Minoru Yoshida , Sueharu Horinouchi , Yasuhiko Komatsu , Tsutomu Mimoto
IPC分类号： A61K3812
CPC分类号： C07K5/126 , A61K38/00
摘要： 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.
摘要翻译：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。

4. 发明授权

US08158587B2 Compound having histone deacetylase-inhibiting activity, and pharmaceutical composition comprising the compound as an active ingredient 有权
标题翻译：具有组蛋白脱乙酰酶抑制活性的化合物和包含该化合物作为活性成分的药物组合物
公开(公告)号：US08158587B2
公开(公告)日：2012-04-17
申请号：US12440180
申请日：2007-07-30
申请人： Norikazu Nishino , Minoru Yoshida , Junichi Nakagawa
发明人： Norikazu Nishino , Minoru Yoshida , Junichi Nakagawa
IPC分类号： A61K38/12
CPC分类号： C07K5/126 , A61K38/00
摘要： A novel compound having histone deacetylase-inhibiting activity which is a cyclic tetrapeptide derivative represented by the general formula (1) given below and a pharmaceutical composition comprising such compound as an active ingredient. (In the formula, the cyclic tetrapeptide moiety has a known structure; R1 and R2 each independently represents an alkylene group containing 1 to 6 carbon atoms, which may be branched; X represents a group or bond selected from among —CO—, —O—, —S— or —SO—; Y represents a hydrogen or halogen atom, a phenyl group (including a substituted form), a pyridyl group (including a substituted form), an alkyl group (including a halogen-substituted form; hereinafter the same shall apply) containing 1 to 6 carbon atoms, an alkyloxy group containing 1 to 6 carbon atoms, an alkylcarbonyl group containing 1 to 6 carbon atoms, an alkyloxycarbonyl group containing 1 to 6 carbon atoms, an alkylthio group containing 1 to 6 carbon atoms, an alkylthiocarbonyl group containing 1 to 6 carbon atoms or a mono- or dialkylamino group containing 1 to 6 carbon atoms; when Y is a phenyl group (including a substituted form) or a pyridyl group (including a substituted form), it may form a further cyclic structure bound to R2.)
摘要翻译：具有组蛋白脱乙酰酶抑制活性的新化合物，其为下述通式（1）表示的环状四肽衍生物，以及含有作为活性成分的化合物的药物组合物。（式中，环状四肽部分具有已知的结构; R 1和R 2各自独立地表示可以是支链的含有1〜6个碳原子的亚烷基; X表示选自-CO - ， - O - ， - S-或-SO-; Y表示氢或卤原子，苯基（包括取代基），吡啶基（包括取代基），烷基（包括卤素取代基同样适用）含有1至6个碳原子，含有1至6个碳原子的烷氧基，含有1至6个碳原子的烷基羰基，含有1至6个碳原子的烷氧基羰基，含1至6个碳原子的烷硫基原子，含有1〜6个碳原子的烷硫基羰基或含有1〜6个碳原子的单或二烷基氨基;当Y为苯基（包括取代基）或吡啶基（包括取代基）时，形成进一步的循环 c结构绑定到R2。）

5. 发明授权

US07662778B2 Histone deacetylase inhibitor and process for producing the same 失效
标题翻译：组蛋白脱乙酰酶抑制剂及其制备方法
公开(公告)号：US07662778B2
公开(公告)日：2010-02-16
申请号：US10561298
申请日：2004-06-18
申请人： Minoru Yoshida , Norikazu Nishino
发明人： Minoru Yoshida , Norikazu Nishino
IPC分类号： A61K38/00
CPC分类号： C07K5/126
摘要： HDAC inhibitor of the general formula (1) exhibits strong inhibitory activity against various subtype HDACs. The compound is useful as a medicinal agent for the treatment or prevention of HDAC 1, 4 and 6-related diseases. There is further provided a process for producing the compound which is capable of readily synthesizing various types of compounds and is promising in the contribution to the development of HDAC inhibitor having novel properties, etc.
摘要翻译：通式（1）的HDAC抑制剂对各种亚型HDAC具有强烈的抑制活性。该化合物可用作治疗或预防HDAC 1,4和6相关疾病的药物。进一步提供一种能够容易地合成各种化合物并且有助于对具有新性能的HDAC抑制剂的发展的贡献的化合物的制备方法等。

6. 发明授权

US07488712B2 Histone deacetylase inhibitors and methods for producing the same 失效
标题翻译：组蛋白脱乙酰酶抑制剂及其制备方法
公开(公告)号：US07488712B2
公开(公告)日：2009-02-10
申请号：US10505380
申请日：2003-02-20
申请人： Minoru Yoshida , Norikazu Nishino , Sueharu Horinouchi
发明人： Minoru Yoshida , Norikazu Nishino , Sueharu Horinouchi
IPC分类号： A61K38/00
CPC分类号： C07K5/126 , A61K38/00
摘要： Compounds represented by formula (1) have strong inhibitory activity that is selective towards HDAC1 and HDAC4. Therefore, the compounds of the present invention are useful as pharmaceutical agents for treating or preventing diseases caused by HDAC1 and HDAC4.
摘要翻译：由式（1）表示的化合物具有对HDAC1和HDAC4具有选择性的强抑制活性。因此，本发明的化合物可用作治疗或预防HDAC1和HDAC4引起的疾病的药剂。

7. 发明申请

US20070185071A1 Histone deacetylase inhibitor and process for producing the same 失效
标题翻译：组蛋白脱乙酰酶抑制剂及其制备方法
公开(公告)号：US20070185071A1
公开(公告)日：2007-08-09
申请号：US10561298
申请日：2004-06-18
申请人： Minoru Yoshida , Norikazu Nishino
发明人： Minoru Yoshida , Norikazu Nishino
IPC分类号： A61K31/555
CPC分类号： C07K5/126
摘要： HDAC inhibitors represented by formula (1) show strong inhibitory activity against various subtypes of HDACs. The compounds of the present invention find utility as pharmaceutical agents for treating or preventing diseases associated with HDAC 1, 4, and 6. The methods for producing the compounds of the present invention enable easy and simple synthesis of various types of these compounds, and are expected to contribute to the development of HDAC inhibitors having novel properties and the like.
摘要翻译：由式（1）表示的HDAC抑制剂显示出对各种HDACs亚型的强抑制活性。本发明的化合物可用作治疗或预防与HDAC 1,4和6有关的疾病的药物。本发明化合物的制备方法能容易和简单地合成各种类型的这些化合物，并且是预期有助于开发具有新颖性质等的HDAC抑制剂。

8. 发明申请

US20050277583A1 Histone deacetylase inhibitors and process for producing the same 失效
标题翻译：组蛋白脱乙酰酶抑制剂及其制备方法
公开(公告)号：US20050277583A1
公开(公告)日：2005-12-15
申请号：US10505380
申请日：2003-02-20
申请人： Minoru Yoshida , Norikazu Nishino , Saeharu Horinouchi
发明人： Minoru Yoshida , Norikazu Nishino , Saeharu Horinouchi
IPC分类号： A61K38/00 , A61P17/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07K5/12 , A61K38/12
CPC分类号： C07K5/126 , A61K38/00
摘要： Compounds represented by formula (1) have strong inhibitory activity that is selective towards HDAC1 and HDAC4. Therefore, the compounds of the present invention are useful as pharmaceutical agents for treating or preventing diseases caused by HDAC1 and HDAC4.
摘要翻译：由式（1）表示的化合物具有对HDAC1和HDAC4具有选择性的强抑制活性。因此，本发明的化合物可用作治疗或预防HDAC1和HDAC4引起的疾病的药剂。

9. 发明申请

US20090275728A1 COMPOUND HAVING HISTONE DEACETYLASE-INHIBITING ACTIVITY, AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUND AS AN ACTIVE INGREDIENT 有权
标题翻译：具有组蛋白脱羧酶抑制活性的化合物和包含化合物作为活性成分的药物组合物
公开(公告)号：US20090275728A1
公开(公告)日：2009-11-05
申请号：US12440180
申请日：2007-07-30
申请人： Norikazu Nishino , Minoru Yoshida , Junichi Nakagawa
发明人： Norikazu Nishino , Minoru Yoshida , Junichi Nakagawa
IPC分类号： C07K5/12
CPC分类号： C07K5/126 , A61K38/00
摘要： A novel compound having histone deacetylase-inhibiting activity which is a cyclic tetrapeptide derivative represented by the general formula (1) given below and a pharmaceutical composition comprising such compound as an active ingredient. (In the formula, the cyclic tetrapeptide moiety has a known structure; R1 and R2 each independently represents an alkylene group containing 1 to 6 carbon atoms, which may be branched; X represents a group or bond selected from among —CO—, —O—, —S— or —SO—; Y represents a hydrogen or halogen atom, a phenyl group (including a substituted form), a pyridyl group (including a substituted form), an alkyl group (including a halogen-substituted form; hereinafter the same shall apply) containing 1 to 6 carbon atoms, an alkyloxy group containing 1 to 6 carbon atoms, an alkylcarbonyl group containing 1 to 6 carbon atoms, an alkyloxycarbonyl group containing 1 to 6 carbon atoms, an alkylthio group containing 1 to 6 carbon atoms, an alkylthiocarbonyl group containing 1 to 6 carbon atoms or a mono- or dialkylamino group containing 1 to 6 carbon atoms; when Y is a phenyl group (including a substituted form) or a pyridyl group (including a substituted form), it may form a further cyclic structure bound to R2.)
摘要翻译：具有组蛋白脱乙酰酶抑制活性的新化合物，其为下述通式（1）表示的环状四肽衍生物，以及含有作为活性成分的化合物的药物组合物。（式中，环状四肽部分具有已知的结构; R 1和R 2各自独立地表示可以是支链的含有1〜6个碳原子的亚烷基; X表示选自-CO - ， - O - ， - S-或-SO-; Y表示氢或卤原子，苯基（包括取代基），吡啶基（包括取代基），烷基（包括卤素取代基同样适用）含有1至6个碳原子，含有1至6个碳原子的烷氧基，含有1至6个碳原子的烷基羰基，含1至6个碳原子的烷氧基羰基，含1至6个碳原子的烷硫基原子，含有1〜6个碳原子的烷硫基羰基或含有1〜6个碳原子的单或二烷基氨基;当Y为苯基（包括取代基）或吡啶基（包括取代基）时，形成一个进一步的循环结构 d到R2）

10. 发明授权

US06825317B2 Cyclic tetrapeptide derivatives and pharmaceutical uses thereof 失效
标题翻译：环状四肽衍生物及其药物用途
公开(公告)号：US06825317B2
公开(公告)日：2004-11-30
申请号：US09945237
申请日：2001-08-31
申请人： Norikazu Nishino , Minoru Yoshida , Sueharu Horinouchi , Yasuhiko Komatsu
发明人： Norikazu Nishino , Minoru Yoshida , Sueharu Horinouchi , Yasuhiko Komatsu
IPC分类号： C07K752
CPC分类号： C07K5/126 , A61K38/00
摘要： 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.
摘要翻译：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。

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