JP7284518B2 - テロメア結合タンパク質を阻害する化合物、及びそれを含むテロメア結合タンパク質阻害剤 - Google Patents
テロメア結合タンパク質を阻害する化合物、及びそれを含むテロメア結合タンパク質阻害剤 Download PDFInfo
- Publication number
- JP7284518B2 JP7284518B2 JP2020508284A JP2020508284A JP7284518B2 JP 7284518 B2 JP7284518 B2 JP 7284518B2 JP 2020508284 A JP2020508284 A JP 2020508284A JP 2020508284 A JP2020508284 A JP 2020508284A JP 7284518 B2 JP7284518 B2 JP 7284518B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- hydrogen
- telomere
- compound
- nucleic acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/78—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
- C07C217/80—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings
- C07C217/82—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring
- C07C217/92—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring the nitrogen atom of at least one of the amino groups being further bound to a carbon atom of a six-membered aromatic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
- C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C323/31—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
- C07C323/33—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton having at least one of the nitrogen atoms bound to a carbon atom of the same non-condensed six-membered aromatic ring
- C07C323/35—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton having at least one of the nitrogen atoms bound to a carbon atom of the same non-condensed six-membered aromatic ring the thio group being a sulfide group
- C07C323/37—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton having at least one of the nitrogen atoms bound to a carbon atom of the same non-condensed six-membered aromatic ring the thio group being a sulfide group the sulfur atom of the sulfide group being further bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Description
上記化学式中において、
R1は、酸素又は硫黄であり、
R2~R6は、互いに独立して、水素、炭素原子数が1~6のアルキル基、炭素原子数が1~6のアルコキシ基、炭素原子数が1~6のアシル基及びニトロ基から選択される。
R1は、酸素又は硫黄であり、
R2及びR4は、互いに独立して、水素又はニトロ基であり、
R3は、水素、ニトロ基、メチル基、メトキシ基又はブチル基であり、
R5は、水素、メチル基、メトキシ基又はアセチル基であり、
R6は、水素又はブチル基であることが好ましい。
なお、上記化学式中において、
R1は、酸素又は硫黄であり、
R2~R6は、互いに独立して、水素、炭素原子数が1~6のアルキル基、炭素原子数が1~6のアルコキシ基、炭素原子数が1~6のアシル基及びニトロ基から選択される。
R1は、酸素又は硫黄であり、
R2及びR4は、互いに独立して、水素又はニトロ基であり、
R3は、水素、ニトロ基、メチル基、メトキシ基又はブチル基であり、
R5は、水素、メチル基、メトキシ基又はアセチル基であり、
R6は、水素又はブチル基であることが好ましい。
・核酸A1:第一のヌクレオチド配列および第二のヌクレオチド配列(末端配列)を有する核酸一本鎖。
・核酸A2:第一のヌクレオチド配列に対応する配列および第三のヌクレオチド配列(末端配列)を有する核酸一本鎖。
・核酸B1:第二のヌクレオチド配列に対応する配列(末端配列)および第四のヌクレオチド配列を有する核酸一本鎖。
・核酸B2:第三のヌクレオチド配列に対応する配列(末端配列)および第四のヌクレオチド配列に対応する配列を有する核酸一本鎖。
95℃ 120秒 - 90℃ 30秒 - 85℃ 90秒 - 80℃ 90秒 - 77℃ 90秒 - 75℃ 90秒 - 72℃ 90秒 - 70℃ 90秒 - 67℃ 90秒 - 65℃ 90秒 - 62℃ 90秒 - 60℃ 90秒 - 57℃ 90秒 - 55℃ 90秒 - 52℃ 90秒 - 50℃ 90秒 - 47℃ 90秒 - 45℃ 90秒 - 42℃ 90秒 - 40℃ 90秒 - 37℃ 90秒 - 35℃ 90秒 - 32℃ 90秒 - 30℃ 90秒。
TLM-01-5F:
5’ FAM- AGTTGAGTTAGGGTTAGGGT TAGGGTTAGG GCAGGcggtg tctcgctcgc 3’(配列番号1)
TLM-02-3D:
5’ gcgagcgagacaccgCCTGC CCTAACCCTA ACCCTAACCC TAACTCAACT -Dabcyl 3’(配列番号2)
TLM-05:
5’AGTTGAGTTA GGGTTAGGGT TAGGGTTAGG GCAGGcacca caccattccc 3’(配列番号3)
TLM-06:
5’gggaatggtg tggtgCCTGC CCTAACCCTA ACCCTAACCC TAACTCAACT 3’(配列番号4)
なお、上記化学式中において、
R1は、酸素又は硫黄であり、
R2及びR4は、互いに独立して、水素又はニトロ基であり、
R3は、水素、ニトロ基、メチル基、メトキシ基又はブチル基であり、
R5は、水素、メチル基、メトキシ基又はアセチル基であり、
R6は、水素又はブチル基である。
Claims (13)
- 上記化学式中において、
R1は、酸素であり、
R2及びR4は、互いに独立して、水素又はニトロ基であり、
R3は、水素、ニトロ基、メチル基、メトキシ基又はブチル基であり、
R5は、水素、メチル基、メトキシ基又はアセチル基であり、
R6は、水素又はブチル基である、
ことを特徴とする請求項1に記載の化合物。 - 上記化学式中において、
R1は、酸素又は硫黄であり、
R2及びR4は、互いに独立して、水素又はニトロ基であり、
R3は、水素、ニトロ基、メチル基、メトキシ基又はブチル基であり、
R5は、水素、メチル基、メトキシ基又はアセチル基であり、
R6は、水素又はブチル基である、請求項4に記載のテロメア結合タンパク質阻害剤。 - 前記テロメア結合タンパク質は、TRF1、TRF2又はPOT1であることを特徴とする請求項4に記載のテロメア結合タンパク質阻害剤。
- 上記化学式中において、
R1は、酸素又は硫黄であり、
R2及びR4は、互いに独立して、水素又はニトロ基であり、
R3は、水素、ニトロ基、メチル基、メトキシ基又はブチル基であり、
R5は、水素、メチル基、メトキシ基又はアセチル基であり、
R6は、水素又はブチル基である、請求項8に記載の医薬組成物。 - 上記化学式中において、
R1は、酸素又は硫黄であり、
R2及びR4は、互いに独立して、水素又はニトロ基であり、
R3は、水素、ニトロ基、メチル基、メトキシ基又はブチル基であり、
R5は、水素、メチル基、メトキシ基又はアセチル基であり、
R6は、水素又はブチル基である、
ことを特徴とする請求項11に記載の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2018052087 | 2018-03-20 | ||
JP2018052087 | 2018-03-20 | ||
PCT/JP2019/010480 WO2019181714A1 (ja) | 2018-03-20 | 2019-03-14 | テロメア結合タンパク質を阻害する化合物、及びそれを含むテロメア結合タンパク質阻害剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2019181714A1 JPWO2019181714A1 (ja) | 2021-04-08 |
JP7284518B2 true JP7284518B2 (ja) | 2023-05-31 |
Family
ID=67987628
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2020508284A Active JP7284518B2 (ja) | 2018-03-20 | 2019-03-14 | テロメア結合タンパク質を阻害する化合物、及びそれを含むテロメア結合タンパク質阻害剤 |
Country Status (3)
Country | Link |
---|---|
US (1) | US20210024455A1 (ja) |
JP (1) | JP7284518B2 (ja) |
WO (1) | WO2019181714A1 (ja) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2023182897A1 (en) * | 2022-03-25 | 2023-09-28 | Politechnika Gdańska | Inhibitors of interactions between trf1-tin2 or trf2-tin2 telomeric proteins for use in anticancer therapy |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001072592A (ja) | 1999-07-01 | 2001-03-21 | Kyowa Hakko Kogyo Co Ltd | テロメラーゼ阻害剤 |
WO2001030771A1 (fr) | 1999-10-28 | 2001-05-03 | Kyowa Hakko Kogyo Co., Ltd. | Derives de thiazolidinedione |
WO2002044120A1 (en) | 2000-11-29 | 2002-06-06 | Karo Bio Ab | Compounds active at the glucocorticoid receptor iii |
JP2004524349A (ja) | 2001-03-23 | 2004-08-12 | アベンティス・ファーマ・ソシエテ・アノニム | 化学的誘導体および抗テロメラーゼ剤としてのその使用 |
WO2009093667A1 (ja) | 2008-01-22 | 2009-07-30 | Hiroshima University | 核酸結合蛋白質アッセイ法およびキット |
JP2012507504A (ja) | 2008-10-31 | 2012-03-29 | アンスティテュ・キュリ | 癌の処置用のポリ−ヘテロアリール誘導体 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH07238066A (ja) * | 1994-02-28 | 1995-09-12 | Green Cross Corp:The | ベンゼンスルホン酸誘導体、その製造法およびその用途 |
WO2017115753A1 (ja) * | 2015-12-28 | 2017-07-06 | コニカミノルタ株式会社 | 架橋化合物、有機エレクトロルミネッセンス素子材料、有機エレクトロルミネッセンス素子、表示装置及び照明装置 |
-
2019
- 2019-03-14 WO PCT/JP2019/010480 patent/WO2019181714A1/ja active Application Filing
- 2019-03-14 US US16/982,517 patent/US20210024455A1/en not_active Abandoned
- 2019-03-14 JP JP2020508284A patent/JP7284518B2/ja active Active
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001072592A (ja) | 1999-07-01 | 2001-03-21 | Kyowa Hakko Kogyo Co Ltd | テロメラーゼ阻害剤 |
WO2001030771A1 (fr) | 1999-10-28 | 2001-05-03 | Kyowa Hakko Kogyo Co., Ltd. | Derives de thiazolidinedione |
WO2002044120A1 (en) | 2000-11-29 | 2002-06-06 | Karo Bio Ab | Compounds active at the glucocorticoid receptor iii |
JP2004524349A (ja) | 2001-03-23 | 2004-08-12 | アベンティス・ファーマ・ソシエテ・アノニム | 化学的誘導体および抗テロメラーゼ剤としてのその使用 |
WO2009093667A1 (ja) | 2008-01-22 | 2009-07-30 | Hiroshima University | 核酸結合蛋白質アッセイ法およびキット |
JP2012507504A (ja) | 2008-10-31 | 2012-03-29 | アンスティテュ・キュリ | 癌の処置用のポリ−ヘテロアリール誘導体 |
Non-Patent Citations (6)
Title |
---|
Database REGISTRY,2001年,RN 352638-37-0,Retrieved from STN international [online] ;retrieved on 24 April 2019 |
城間 喜智 他,DSE-FREAT assayを応用して得られたTRF2-telomere DNA結合阻害剤,第21回日本がん分子標的治療学会学術集会プログラム・抄録集,2017年,W7-5 |
城間 喜智 他,DSE-FRET assayを用いたテロメア結合タンパク質阻害剤開発と機能解析,日本生化学会大会,2017年,2P-1435 |
城間 喜智 他,DSE-FRET法を用いて得られたテロメア結合タンパク質TRF2阻害剤,第20回日本がん分子標的治療学会学術集会プログラム・抄録集,2016年,P24-2 |
城間 喜智 他,テロメア結合タンパク質TRF2の結合阻害剤ががん細胞に及ぼす影響,第76日本癌学会学術総会抄録集,2017年,J-3119 |
城間 喜智,DSE-FRET法を用いたテロメア結合タンパク質 TRF2阻害剤の探索,第19回日本がん分子標的治療学会学術集会プログラム・抄録集,2015年,P3-3 |
Also Published As
Publication number | Publication date |
---|---|
US20210024455A1 (en) | 2021-01-28 |
WO2019181714A1 (ja) | 2019-09-26 |
JPWO2019181714A1 (ja) | 2021-04-08 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
Liu et al. | Circular RNA DOCK1 promotes bladder carcinoma progression via modulating circDOCK1/hsa‐miR‐132‐3p/Sox5 signalling pathway | |
Alekseyenko et al. | Ectopic protein interactions within BRD4–chromatin complexes drive oncogenic megadomain formation in NUT midline carcinoma | |
Zhang et al. | Breast cancer metastasis suppressor OTUD1 deubiquitinates SMAD7 | |
Bunch et al. | Transcriptional elongation requires DNA break-induced signalling | |
Malik et al. | Targeting the MLL complex in castration-resistant prostate cancer | |
Xie et al. | miR-106a promotes growth and metastasis of non-small cell lung cancer by targeting PTEN | |
Ahmed et al. | Telomerase does not counteract telomere shortening but protects mitochondrial function under oxidative stress | |
Singh et al. | MiCEE is a ncRNA-protein complex that mediates epigenetic silencing and nucleolar organization | |
Yong et al. | Ribosomal proteins RPS11 and RPS20, two stress-response markers of glioblastoma stem cells, are novel predictors of poor prognosis in glioblastoma patients | |
Sen et al. | Fibronectin induces matrix metalloproteinase-9 (MMP-9) in human laryngeal carcinoma cells by involving multiple signaling pathways | |
Isozaki et al. | Therapy-induced APOBEC3A drives evolution of persistent cancer cells | |
US20170137418A1 (en) | Small molecular probes, processes and use thereof | |
JP2008522615A (ja) | ドセタキセル耐性または感受性の測定方法 | |
JP2016506362A (ja) | 合成致死性および癌の治療 | |
Bambouskova et al. | New regulatory roles of galectin-3 in high-affinity IgE receptor signaling | |
Wang et al. | RETRACTED ARTICLE: microRNA-769 is downregulated in colorectal cancer and inhibits cancer progression by directly targeting cyclin-dependent kinase 1 | |
Gomez-Acevedo et al. | Identification of putative biomarkers for Infantile Hemangiomas and Propranolol treatment via data integration | |
JP7284518B2 (ja) | テロメア結合タンパク質を阻害する化合物、及びそれを含むテロメア結合タンパク質阻害剤 | |
Laliotis et al. | RETRACTED ARTICLE: AKT3-mediated IWS1 phosphorylation promotes the proliferation of EGFR-mutant lung adenocarcinomas through cell cycle-regulated U2AF2 RNA splicing | |
Kim et al. | The SET domain Is essential for Metnase functions in replication restart and the 5’end of SS-overhang cleavage | |
US20190147975A1 (en) | Sf3b1 suppression as a therapy for tumors harboring sf3b1 copy loss | |
EP2726869B1 (en) | Somatic mutations in atrx in brain cancer | |
CA3211847A1 (en) | Circular rnas for diagnosis of depression and prediction of response to antidepressant treatment | |
Sommer et al. | Applying a high-throughput fluorescence polarization assay for the discovery of chemical probes blocking La: RNA interactions in vitro and in cells | |
Jiang et al. | Post-GWAS functional analysis identifies CUX1 as a regulator of p16INK4a and cellular senescence |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A529 | Written submission of copy of amendment under article 34 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A5211 Effective date: 20200907 |
|
A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20220302 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20220304 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20230307 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20230324 |
|
TRDD | Decision of grant or rejection written | ||
A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20230509 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20230512 |
|
R150 | Certificate of patent or registration of utility model |
Ref document number: 7284518 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |