JP2008540389A5 - - Google Patents
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- JP2008540389A5 JP2008540389A5 JP2008509500A JP2008509500A JP2008540389A5 JP 2008540389 A5 JP2008540389 A5 JP 2008540389A5 JP 2008509500 A JP2008509500 A JP 2008509500A JP 2008509500 A JP2008509500 A JP 2008509500A JP 2008540389 A5 JP2008540389 A5 JP 2008540389A5
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- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 25
- 125000004122 cyclic group Chemical group 0.000 claims description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 5
- 125000002950 monocyclic group Chemical group 0.000 claims description 5
- 125000002619 bicyclic group Chemical group 0.000 claims description 3
- 125000000165 tricyclic carbocycle group Chemical group 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- -1 N-methylpiperidin-4-yl Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000002843 carboxylic acid group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000004185 ester group Chemical group 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 150000003568 thioethers Chemical class 0.000 claims 2
- BLWWHQCJSVHDJK-QFIPXVFZSA-N (2s)-2-[[3-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetic acid Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC(CN[C@H](C(O)=O)C=2C=CC=CC=2)=C1 BLWWHQCJSVHDJK-QFIPXVFZSA-N 0.000 claims 1
- GFQLAZSQPSUKKD-SFHVURJKSA-N (2s)-2-[[3-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-3-[(2-methylpropan-2-yl)oxy]propanoic acid Chemical compound CC(C)(C)OC[C@@H](C(O)=O)NCC1=CC=CC(NC(=O)CCCCCCC(=O)NO)=C1 GFQLAZSQPSUKKD-SFHVURJKSA-N 0.000 claims 1
- DPUPCCLYBOVSNL-SFHVURJKSA-N (2s)-2-[[3-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-4-methylpentanoic acid Chemical compound CC(C)C[C@@H](C(O)=O)NCC1=CC=CC(NC(=O)CCCCCCC(=O)NO)=C1 DPUPCCLYBOVSNL-SFHVURJKSA-N 0.000 claims 1
- BKOTWGYGBLTPKM-QFIPXVFZSA-N (2s)-2-[[4-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetic acid Chemical compound C1=CC(NC(=O)CCCCCCC(=O)NO)=CC=C1CN[C@H](C(O)=O)C1=CC=CC=C1 BKOTWGYGBLTPKM-QFIPXVFZSA-N 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 102000013392 Carboxylesterase Human genes 0.000 claims 1
- 108010051152 Carboxylesterase Proteins 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 1
- 235000008206 alpha-amino acids Nutrition 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 230000009702 cancer cell proliferation Effects 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- CAFYVKHSHZKTTO-MHZLTWQESA-N cyclopentyl (2s)-2-[[3-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetate Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC(CN[C@H](C(=O)OC2CCCC2)C=2C=CC=CC=2)=C1 CAFYVKHSHZKTTO-MHZLTWQESA-N 0.000 claims 1
- NJSXINSJGRZADK-QHCPKHFHSA-N cyclopentyl (2s)-2-[[3-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-3-[(2-methylpropan-2-yl)oxy]propanoate Chemical compound N([C@@H](COC(C)(C)C)C(=O)OC1CCCC1)CC1=CC=CC(NC(=O)CCCCCCC(=O)NO)=C1 NJSXINSJGRZADK-QHCPKHFHSA-N 0.000 claims 1
- QMGXAAVAXIEBEX-QHCPKHFHSA-N cyclopentyl (2s)-2-[[3-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-4-methylpentanoate Chemical compound N([C@@H](CC(C)C)C(=O)OC1CCCC1)CC1=CC=CC(NC(=O)CCCCCCC(=O)NO)=C1 QMGXAAVAXIEBEX-QHCPKHFHSA-N 0.000 claims 1
- GLNWREBYRLDPQP-MHZLTWQESA-N cyclopentyl (2s)-2-[[4-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetate Chemical compound C1=CC(NC(=O)CCCCCCC(=O)NO)=CC=C1CN[C@@H](C=1C=CC=CC=1)C(=O)OC1CCCC1 GLNWREBYRLDPQP-MHZLTWQESA-N 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002170 ethers Chemical class 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229920000155 polyglutamine Polymers 0.000 claims 1
- 108010040003 polyglutamine Proteins 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- NEAQRZUHTPSBBM-UHFFFAOYSA-N 2-hydroxy-3,3-dimethyl-7-nitro-4h-isoquinolin-1-one Chemical compound C1=C([N+]([O-])=O)C=C2C(=O)N(O)C(C)(C)CC2=C1 NEAQRZUHTPSBBM-UHFFFAOYSA-N 0.000 description 1
- 102000003964 Histone deacetylase Human genes 0.000 description 1
- 108090000353 Histone deacetylase Proteins 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229910021645 metal ion Inorganic materials 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0509223.4 | 2005-05-05 | ||
| GB0509223A GB0509223D0 (en) | 2005-05-05 | 2005-05-05 | Enzyme inhibitors |
| PCT/GB2006/001605 WO2006117549A1 (en) | 2005-05-05 | 2006-05-04 | Enzyme inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008540389A JP2008540389A (ja) | 2008-11-20 |
| JP2008540389A5 true JP2008540389A5 (https=) | 2009-07-02 |
| JP5405820B2 JP5405820B2 (ja) | 2014-02-05 |
Family
ID=34685155
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008509500A Expired - Fee Related JP5405820B2 (ja) | 2005-05-05 | 2006-05-04 | 酵素阻害剤 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US7939666B2 (https=) |
| EP (2) | EP1879895B1 (https=) |
| JP (1) | JP5405820B2 (https=) |
| KR (1) | KR101307815B1 (https=) |
| CN (1) | CN101133060B (https=) |
| AT (1) | ATE512150T1 (https=) |
| AU (1) | AU2006243065B2 (https=) |
| BR (1) | BRPI0607410A2 (https=) |
| CA (1) | CA2599411C (https=) |
| DK (1) | DK1879895T3 (https=) |
| ES (1) | ES2367369T3 (https=) |
| GB (1) | GB0509223D0 (https=) |
| IL (1) | IL185580A (https=) |
| MX (1) | MX2007010456A (https=) |
| NZ (1) | NZ560289A (https=) |
| PL (1) | PL1879895T3 (https=) |
| PT (1) | PT1879895E (https=) |
| WO (1) | WO2006117549A1 (https=) |
| ZA (1) | ZA200707091B (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1483283A4 (en) | 2002-03-13 | 2007-04-11 | Signum Biosciences Inc | MODULATION OF PROTEIN METHYLATION AND PHOSPHOPROTEIN PHOSPHATE |
| CA2601777A1 (en) | 2005-02-03 | 2006-08-10 | Signum Biosciences, Inc. | Compositions and methods for enhancing cognitive function |
| US7923041B2 (en) | 2005-02-03 | 2011-04-12 | Signum Biosciences, Inc. | Compositions and methods for enhancing cognitive function |
| AU2006243000B2 (en) * | 2005-05-05 | 2011-05-26 | Macrophage Pharma Limited | Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase |
| GB0509223D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| GB0509225D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Inhibitors of enzymatic activity |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| GB0619753D0 (en) | 2006-10-06 | 2006-11-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| SG158147A1 (en) | 2006-10-09 | 2010-01-29 | Takeda Pharmaceutical | Kinase inhibitors |
| WO2008053131A1 (en) | 2006-10-30 | 2008-05-08 | Chroma Therapeutics Ltd. | Hydroxamates as inhibitors of histone deacetylase |
| GB0803747D0 (en) | 2008-02-29 | 2008-04-09 | Martin | Enzyme and receptor modulation |
| GB0903480D0 (en) | 2009-02-27 | 2009-04-08 | Chroma Therapeutics Ltd | Enzyme Inhibitors |
| ES2736200T3 (es) * | 2009-07-22 | 2019-12-26 | Univ Illinois | Inhibidores de HDAC y métodos terapéuticos que utilizan los mismos |
| EP2516387B1 (en) * | 2009-12-21 | 2018-02-21 | Institut National de la Sante et de la Recherche Medicale (INSERM) | Inhibitors of cyclophilins for use in the prevention and/or the treatment of viral pathologies or infections |
| GB201009853D0 (en) | 2010-06-11 | 2010-07-21 | Chroma Therapeutics Ltd | HSP90 inhibitors |
| ES2402252B1 (es) * | 2011-09-26 | 2014-03-10 | Universidad De Granada | Compuesto con actividad antileishmania |
| CN103906732A (zh) * | 2011-10-28 | 2014-07-02 | 株式会社钟根堂 | 用作hdac抑制剂的异羟肟酸酯衍生物以及包含所述衍生物的药物组合物 |
| GB201211310D0 (en) | 2012-06-26 | 2012-08-08 | Chroma Therapeutics Ltd | CSF-1R kinase inhibitors |
| PL3222616T3 (pl) | 2012-10-17 | 2019-12-31 | Macrophage Pharma Limited | N-[2-{4-[6-amino-5-(2,4-difluorobenzoilo)-2-oksopirydyn-1(2h)-ylo]-3,5-difluorofenylo}etylo)-L-alaninian tert-butylu lub jego sól, hydrat lub solwat |
| CN103172540B (zh) * | 2013-03-18 | 2015-07-01 | 潍坊博创国际生物医药研究院 | 苯甘氨酸类组蛋白去乙酰酶抑制剂及其制备方法和应用 |
| TW201636329A (zh) | 2015-02-02 | 2016-10-16 | 佛瑪治療公司 | 作為ｈｄａｃ抑制劑之雙環［４，６，０］異羥肟酸 |
| PL3292116T3 (pl) | 2015-02-02 | 2022-02-21 | Valo Health, Inc. | 3-arylo-4-amidobicykliczne kwasy [4,5,0]hydroksamowe jako inhibitory hdac |
| JP6945546B2 (ja) * | 2016-03-22 | 2021-10-06 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 新規誘導体、及びカスパーゼ−２の選択的阻害剤としての使用 |
| WO2017216297A1 (en) | 2016-06-16 | 2017-12-21 | Glaxosmithkline Intellectual Property Development Limited | Dosage regimen |
| EP3472131B1 (en) | 2016-06-17 | 2020-02-19 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors |
| GB201713975D0 (en) | 2017-08-31 | 2017-10-18 | Macrophage Pharma Ltd | Medical use |
| TWI650139B (zh) * | 2017-10-11 | 2019-02-11 | 行政院原子能委員會核能硏究所 | 含有放射性同位素氟的異羥肟酸類造影劑、其製備方法及其用途 |
| WO2020013116A1 (ja) * | 2018-07-10 | 2020-01-16 | 京都薬品工業株式会社 | Ｐｔｐ－１ｂ阻害剤およびその用途 |
| CN111393404B (zh) * | 2019-01-02 | 2023-02-17 | 中国科学院上海药物研究所 | 一类苯并噻吩类化合物及其药物组合物及应用 |
| CN113121527B (zh) * | 2019-12-31 | 2024-09-06 | 上海辉启生物医药科技有限公司 | 三环类化合物及其用途 |
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| WO2005030705A1 (en) | 2003-09-24 | 2005-04-07 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| EP1677731A4 (en) * | 2003-10-09 | 2009-05-06 | Aton Pharma Inc | THIOPHENE AND BENZOTHIOPHENE DERIVATIVES OF HYDROXAMIC ACID |
| WO2005037272A1 (en) * | 2003-10-22 | 2005-04-28 | Arpida A/S | Benzimidazole derivatives and use thereof as peptide deformylase inhibitors |
| AU2006243000B2 (en) | 2005-05-05 | 2011-05-26 | Macrophage Pharma Limited | Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase |
| GB0509223D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
-
2005
- 2005-05-05 GB GB0509223A patent/GB0509223D0/en not_active Ceased
-
2006
- 2006-05-04 KR KR1020077019886A patent/KR101307815B1/ko not_active Expired - Fee Related
- 2006-05-04 DK DK06726982.9T patent/DK1879895T3/da active
- 2006-05-04 AT AT06726982T patent/ATE512150T1/de active
- 2006-05-04 NZ NZ560289A patent/NZ560289A/en not_active IP Right Cessation
- 2006-05-04 PT PT06726982T patent/PT1879895E/pt unknown
- 2006-05-04 EP EP06726982A patent/EP1879895B1/en not_active Expired - Lifetime
- 2006-05-04 US US11/918,139 patent/US7939666B2/en active Active
- 2006-05-04 WO PCT/GB2006/001605 patent/WO2006117549A1/en not_active Ceased
- 2006-05-04 JP JP2008509500A patent/JP5405820B2/ja not_active Expired - Fee Related
- 2006-05-04 ES ES06726982T patent/ES2367369T3/es not_active Expired - Lifetime
- 2006-05-04 MX MX2007010456A patent/MX2007010456A/es active IP Right Grant
- 2006-05-04 AU AU2006243065A patent/AU2006243065B2/en not_active Ceased
- 2006-05-04 PL PL06726982T patent/PL1879895T3/pl unknown
- 2006-05-04 BR BRPI0607410-3A patent/BRPI0607410A2/pt not_active Application Discontinuation
- 2006-05-04 EP EP20100176446 patent/EP2301939A1/en not_active Withdrawn
- 2006-05-04 CA CA2599411A patent/CA2599411C/en not_active Expired - Fee Related
- 2006-05-04 CN CN2006800069161A patent/CN101133060B/zh not_active Expired - Fee Related
-
2007
- 2007-08-22 ZA ZA200707091A patent/ZA200707091B/xx unknown
- 2007-08-29 IL IL185580A patent/IL185580A/en active IP Right Grant
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2010
- 2010-12-01 US US12/957,829 patent/US8686032B2/en not_active Expired - Fee Related
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2014
- 2014-02-13 US US14/179,880 patent/US9133104B2/en not_active Expired - Fee Related
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