JP2009531404A5 - - Google Patents
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- Publication number
- JP2009531404A5 JP2009531404A5 JP2009502206A JP2009502206A JP2009531404A5 JP 2009531404 A5 JP2009531404 A5 JP 2009531404A5 JP 2009502206 A JP2009502206 A JP 2009502206A JP 2009502206 A JP2009502206 A JP 2009502206A JP 2009531404 A5 JP2009531404 A5 JP 2009531404A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- alkyl
- carboaryl
- aliphatic
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 26
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 13
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 13
- 125000001931 aliphatic group Chemical group 0.000 claims 13
- 125000005488 carboaryl group Chemical group 0.000 claims 13
- 102000019355 Synuclein Human genes 0.000 claims 11
- 108050006783 Synuclein Proteins 0.000 claims 11
- -1 diaminophenothiazine compound Chemical class 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 238000004220 aggregation Methods 0.000 claims 6
- 230000002776 aggregation Effects 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 5
- KPYHKEZPEDJERZ-UHFFFAOYSA-N 10h-phenothiazine-1,2-diamine Chemical class C1=CC=C2NC3=C(N)C(N)=CC=C3SC2=C1 KPYHKEZPEDJERZ-UHFFFAOYSA-N 0.000 claims 3
- 229940126534 drug product Drugs 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 206010012289 Dementia Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000032859 Synucleinopathies Diseases 0.000 claims 2
- 125000000129 anionic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 102000003802 alpha-Synuclein Human genes 0.000 claims 1
- 108090000185 alpha-Synuclein Proteins 0.000 claims 1
- 230000000890 antigenic effect Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 239000003153 chemical reaction reagent Substances 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 claims 1
- 229960003638 dopamine Drugs 0.000 claims 1
- 239000000975 dye Substances 0.000 claims 1
- 150000002500 ions Chemical class 0.000 claims 1
- 238000002372 labelling Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000004393 prognosis Methods 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78670006P | 2006-03-29 | 2006-03-29 | |
| US60/786,700 | 2006-03-29 | ||
| PCT/GB2007/001105 WO2007110629A1 (en) | 2006-03-29 | 2007-03-28 | Inhibitors of protein aggregation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009531404A JP2009531404A (ja) | 2009-09-03 |
| JP2009531404A5 true JP2009531404A5 (enExample) | 2010-05-13 |
| JP5654748B2 JP5654748B2 (ja) | 2015-01-14 |
Family
ID=38068838
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009502206A Active JP5654748B2 (ja) | 2006-03-29 | 2007-03-28 | タンパク質凝集の阻害物質 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US8263589B2 (enExample) |
| EP (1) | EP2004155B1 (enExample) |
| JP (1) | JP5654748B2 (enExample) |
| CN (2) | CN103735554B (enExample) |
| AU (1) | AU2007231126B2 (enExample) |
| CA (1) | CA2645946C (enExample) |
| DK (1) | DK2004155T3 (enExample) |
| ES (1) | ES2667002T3 (enExample) |
| MY (1) | MY153198A (enExample) |
| PL (1) | PL2004155T3 (enExample) |
| PT (1) | PT2004155T (enExample) |
| SI (1) | SI2004155T1 (enExample) |
| WO (1) | WO2007110629A1 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7790881B2 (en) | 2004-09-23 | 2010-09-07 | Wista Laboratories Ltd. | Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC) |
| PL2004155T3 (pl) | 2006-03-29 | 2018-08-31 | Wista Laboratories Ltd. | Inhibitory agregacji białek |
| CN109384741B (zh) | 2006-03-29 | 2023-01-06 | 维斯塔实验室有限公司 | 3,7-二氨基-10h-吩噻嗪化合物盐及其用途 |
| FR2903696B1 (fr) | 2006-07-12 | 2011-02-11 | Provence Technologies | Procede de purification de composes diaminophenothiazium |
| CN101820884B (zh) * | 2007-06-19 | 2013-08-28 | 维斯塔实验室有限公司 | 用于治疗轻度认知缺损的吩噻嗪化合物 |
| SI2205245T1 (sl) * | 2007-10-03 | 2015-10-30 | Wista Laboratories Ltd. | Terapevtska uporaba diaminofenotiazinov |
| AU2016202982B2 (en) * | 2009-09-24 | 2017-09-21 | TauRx Therapeutics Management Ltd | Crystalline methylthionium chloride (methylene blue) hydrates |
| ES2689029T3 (es) * | 2009-09-24 | 2018-11-08 | Wista Laboratories Ltd. | Hidratos de cloruro de metiltioninio cristalinos - Parte 2 |
| US8828986B2 (en) | 2011-04-20 | 2014-09-09 | Prosetta Antiviral Inc. | Antiviral compounds |
| US8785434B2 (en) | 2010-04-30 | 2014-07-22 | Prosetta Antiviral Inc. | Antiviral compounds |
| WO2012106363A2 (en) | 2011-01-31 | 2012-08-09 | Intellect Neurosciences Inc. | Treatment of tauopathies |
| EA025033B1 (ru) | 2011-02-11 | 2016-11-30 | Уиста Лэборэтэриз Лтд. | Диаминиевые соли фенотиазина и их применение |
| CN102690244A (zh) * | 2011-03-22 | 2012-09-26 | 中国科学院上海生命科学研究院 | 调节α-突触核蛋白积聚的物质及其制药用途 |
| GB201317702D0 (en) * | 2013-10-07 | 2013-11-20 | Wista Lab Ltd | Methods of chemical synthesis of diaminophenothiazinium compounds including methylthioninium chloride (MTC) |
| EP3207925A1 (en) * | 2016-02-22 | 2017-08-23 | Universität Wien | Compound for use in the prevention and treatment of neurodegenerative diseases |
| ES2804541T3 (es) * | 2015-11-30 | 2021-02-08 | Univ Wien | Compuesto para su uso en la prevención y el tratamiento de enfermedades neurodegenerativas |
| CN106046027B (zh) * | 2016-06-30 | 2019-03-05 | 广东工业大学 | 一种含吡咯并吩噻嗪-1,3-二酮衍生物及其制备方法与应用 |
| AU2017301966B2 (en) * | 2016-07-25 | 2022-09-22 | TauRx Therapeutics Management Ltd | Administration and dosage of diaminophenothiazines |
| EP3589616A1 (en) | 2017-02-28 | 2020-01-08 | Universitat Autònoma de Barcelona | (nitro-phenyl)-nitropyridine compounds for treating synucleinopathies |
| FR3063495B1 (fr) * | 2017-03-02 | 2019-04-05 | Provepharm Life Solutions | Procede de preparation de l’iodure de 3,7-bis(dimethylamino)phenothiazine-5-ylium |
| WO2018226589A1 (en) | 2017-06-05 | 2018-12-13 | Board Of Trustees Of Michigan State University | Small molecule proteosome activators and uses thereof |
| WO2019025424A1 (en) | 2017-08-04 | 2019-02-07 | Universitat Autonoma De Barcelona | COMPOUNDS FOR TREATING SYNUCLEINOPATHIES |
| US12071649B1 (en) | 2017-12-03 | 2024-08-27 | Nitrase Therapeutics, Inc. | Identification of modulators of nitration and therapeutic uses thereof |
| WO2019161917A1 (en) | 2018-02-23 | 2019-08-29 | Universitat Autonoma De Barcelona | 4-substituted 1-ethenylsulfonyl-2-nitrobenzene compounds for treating synucleinopathies |
| EP3826639B1 (en) | 2018-07-26 | 2024-08-21 | WisTa Laboratories Ltd. | Optimised dosage of diaminophenothiazines in populations |
| CN113874078B (zh) | 2019-04-05 | 2025-05-06 | Tauc3生物制品有限公司 | 抗tauc3抗体及其应用 |
| MY209608A (en) * | 2019-04-10 | 2025-07-24 | Genting Taurx Diagnostic Centre Sdn Bhd | Adaptive neurological testing method |
| EP4061807A1 (en) * | 2019-11-19 | 2022-09-28 | Modag GmbH | Novel compounds for the diagnosis, treatment and prevention of diseases associated with the aggregation of alpha-synuclein |
| EP4531863A1 (en) | 2022-05-31 | 2025-04-09 | WisTa Laboratories Ltd. | Treatment of neurodegenerative disorders utilising methylthioninium (mt)-containing compounds |
| AU2024231880A1 (en) | 2023-03-03 | 2025-09-11 | Taurx Therapeutics Management Ltd. | Diaminophenothiazine for the treatment of microvascular brain disease disease |
| WO2024263638A2 (en) * | 2023-06-20 | 2024-12-26 | Yeefan Med Inc | Pharmaceutical composition and uses thereof |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE569430A (enExample) | 1957-07-17 | |||
| US4309255A (en) | 1980-09-10 | 1982-01-05 | International Business Machines Corporation | Electrochromic recording paper |
| US4622395A (en) | 1984-10-01 | 1986-11-11 | Minnesota Mining And Manufacturing Company | Phenoxazine and phenothiazine dyes and leuco forms thereof |
| US4647525A (en) | 1984-10-01 | 1987-03-03 | Minnesota Mining And Manufacturing Company | Stabilized leuco phenazine dyes and their use in an imaging system |
| GB8724412D0 (en) | 1987-10-19 | 1987-11-25 | Medical Res Council | Protein |
| US5571666A (en) | 1988-10-28 | 1996-11-05 | Oklahoma Medical Research Foundation | Thiazine dyes used to inactivate HIV in biological fluids |
| US5220009A (en) | 1990-05-03 | 1993-06-15 | Yeda Research And Development Company Limited | Phenothiazinium salts and their use for disinfecting aqueous effluents |
| JPH0725786A (ja) | 1990-05-16 | 1995-01-27 | Univ Rockefeller | アルツハイマー病を伴うアミロイドーシスの治療 |
| WO1993003369A1 (en) | 1991-08-01 | 1993-02-18 | Voorheis Paul H | Diagnostic method for alzheimer's disease |
| WO1993003177A1 (en) | 1991-08-09 | 1993-02-18 | Massachusetts Institute Of Technology | Novel tau/neurofilament protein kinases |
| WO1993011231A1 (en) | 1991-12-06 | 1993-06-10 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Tools for the diagnosis and treatment of alzheimer's disease |
| JPH06289015A (ja) | 1993-03-30 | 1994-10-18 | Sunstar Inc | フェノチアジン系色源体安定化組成物 |
| GB9316727D0 (en) | 1993-08-12 | 1993-09-29 | Inst Of Psychiatry | Models of alzheimers's disease |
| GB9317193D0 (en) | 1993-08-18 | 1993-10-06 | Zeneca Ltd | Method |
| WO1996004915A1 (en) | 1994-08-08 | 1996-02-22 | Albert Einstein College Of Medicine Of Yeshiva University | Methods for treating and/or preventing alzheimer's disease using phenothiazines and/or thioxanthenes |
| DE4430091A1 (de) | 1994-08-25 | 1996-02-29 | Bayer Ag | Verwendung von N-substituierten Phenothiazinen |
| GB9506197D0 (en) | 1995-03-27 | 1995-05-17 | Hoffmann La Roche | Inhibition of tau-tau association. |
| US5804601A (en) | 1995-04-10 | 1998-09-08 | Takeda Chemical Industries, Ltd. | Aromatic hydroxamic acid compounds, their production and use |
| US5693638A (en) | 1996-02-23 | 1997-12-02 | Myers; Daniel | Method of treating a migraine headache |
| US6333322B1 (en) | 1996-03-13 | 2001-12-25 | Eisai Co., Ltd. | Nitrogen-containing tricyclic compounds and drugs containing the same |
| WO1999062548A1 (en) | 1998-06-01 | 1999-12-09 | Advanced Research And Technology Institute | Methods and compositions for diagnosing tauopathies |
| FR2788436A1 (fr) | 1999-01-14 | 2000-07-21 | Pf Medicament | Composition d'un derive de phenothiazine |
| EP1248518A2 (en) | 2000-01-21 | 2002-10-16 | PHARMACIA & UPJOHN COMPANY | Transgenic mouse model of human neurodegenerative disease |
| GB0017060D0 (en) * | 2000-07-11 | 2000-08-30 | Hunter Fleming Ltd | Production, stabilisation and use of reduced forms of pharmaceutical compounds |
| GB0100119D0 (en) | 2001-01-03 | 2001-02-14 | Univ Aberdeen | Materials and methods relating to protein aggregation in neurodegenerative disease |
| GB0101049D0 (en) * | 2001-01-15 | 2001-02-28 | Univ Aberdeen | Materials and methods relating to protein aggregation in neurodegenerative disease |
| WO2002076381A2 (en) * | 2001-03-15 | 2002-10-03 | Proteotech, Inc. | Proanthocyanidins for the treatment of amyloid and alpha-synuclein diseases |
| GB0106953D0 (en) | 2001-03-20 | 2001-05-09 | Univ Aberdeen | Neufofibrillary labels |
| WO2003000714A2 (en) * | 2001-06-22 | 2003-01-03 | Panacea Pharmaceuticals, Inc. | Compositions and methods for preventing protein aggregation in neurodegenerative diseases |
| GB0117326D0 (en) | 2001-07-16 | 2001-09-05 | Univ Aberdeen | Napthoquinone-type inhibitors of protein aggregation |
| US20030217370A1 (en) | 2002-05-16 | 2003-11-20 | Giasson Benoit I. | Transgenic animal expressing alpha-synuclein and uses thereof |
| JP3867639B2 (ja) * | 2002-07-31 | 2007-01-10 | 株式会社デンソー | 混成集積回路装置 |
| US6953974B2 (en) | 2003-08-26 | 2005-10-11 | Texas Instruments Incorporated | EEPROM device and method for providing lower programming voltage |
| GB0322756D0 (en) | 2003-09-29 | 2003-10-29 | Univ Aberdeen | Methods of chemical synthesis |
| AU2004295148A1 (en) | 2003-11-28 | 2005-06-16 | Photopharmica Limited | Developments in biologically active methylene blue derivatives (2) |
| DE602005016537D1 (de) * | 2004-03-31 | 2009-10-22 | Anges Mg Inc | Testverfahren zur identifizierung eines kandidatenarzneistoffs |
| GB0420963D0 (en) | 2004-09-21 | 2004-10-20 | Reneuron Ltd | Hepatocyte |
| US7790881B2 (en) | 2004-09-23 | 2010-09-07 | Wista Laboratories Ltd. | Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC) |
| PT1799662E (pt) | 2004-09-23 | 2013-07-09 | Wista Lab Ltd | Métodos de síntese química e purificação de compostos de diaminofenotiazínio incluindo cloreto de metiltionínio (mtc) |
| WO2006122546A1 (de) | 2005-05-18 | 2006-11-23 | Forschungsverbund Berlin E.V. | Nicht-peptidische inhibitoren der akap-pka-wechselwirkung |
| US20070116757A1 (en) | 2005-11-08 | 2007-05-24 | Collegium Pharmaceutical, Inc. | Methylene Blue Derivatives |
| PL2004155T3 (pl) | 2006-03-29 | 2018-08-31 | Wista Laboratories Ltd. | Inhibitory agregacji białek |
| CN109384741B (zh) | 2006-03-29 | 2023-01-06 | 维斯塔实验室有限公司 | 3,7-二氨基-10h-吩噻嗪化合物盐及其用途 |
-
2007
- 2007-03-28 PL PL07712961T patent/PL2004155T3/pl unknown
- 2007-03-28 DK DK07712961.7T patent/DK2004155T3/en active
- 2007-03-28 EP EP07712961.7A patent/EP2004155B1/en active Active
- 2007-03-28 AU AU2007231126A patent/AU2007231126B2/en active Active
- 2007-03-28 US US12/294,605 patent/US8263589B2/en active Active
- 2007-03-28 SI SI200732019T patent/SI2004155T1/en unknown
- 2007-03-28 MY MYPI20083823A patent/MY153198A/en unknown
- 2007-03-28 JP JP2009502206A patent/JP5654748B2/ja active Active
- 2007-03-28 PT PT77129617T patent/PT2004155T/pt unknown
- 2007-03-28 CA CA2645946A patent/CA2645946C/en active Active
- 2007-03-28 CN CN201310556670.7A patent/CN103735554B/zh active Active
- 2007-03-28 WO PCT/GB2007/001105 patent/WO2007110629A1/en not_active Ceased
- 2007-03-28 CN CN200780020257.1A patent/CN101460157B/zh active Active
- 2007-03-28 ES ES07712961.7T patent/ES2667002T3/es active Active
-
2011
- 2011-01-21 US US13/011,797 patent/US8710051B2/en active Active
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2014
- 2014-04-09 US US14/248,730 patent/US9174954B2/en active Active