RU2324686C2 - ПРОИЗВОДНЫЕ ТИОФЛАВИНА, СВЯЗЫВАЮЩИЕ АМИЛОИД, СПОСОБ ОБНАРУЖЕНИЯ in vivo ОТЛОЖЕНИЙ АМИЛОИДА И СПОСОБ РАСПОЗНАВАНИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА - Google Patents
ПРОИЗВОДНЫЕ ТИОФЛАВИНА, СВЯЗЫВАЮЩИЕ АМИЛОИД, СПОСОБ ОБНАРУЖЕНИЯ in vivo ОТЛОЖЕНИЙ АМИЛОИДА И СПОСОБ РАСПОЗНАВАНИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА Download PDFInfo
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- RU2324686C2 RU2324686C2 RU2003108256/04A RU2003108256A RU2324686C2 RU 2324686 C2 RU2324686 C2 RU 2324686C2 RU 2003108256/04 A RU2003108256/04 A RU 2003108256/04A RU 2003108256 A RU2003108256 A RU 2003108256A RU 2324686 C2 RU2324686 C2 RU 2324686C2
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- Prior art keywords
- amyloid
- compound
- disease
- group
- alzheimer
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- 238000001514 detection method Methods 0.000 title claims abstract 3
- 238000001727 in vivo Methods 0.000 title claims abstract 3
- 238000000034 method Methods 0.000 title claims 10
- 208000024827 Alzheimer disease Diseases 0.000 title claims 9
- 208000037259 Amyloid Plaque Diseases 0.000 title abstract 3
- NRYGFMAOIPXXBW-UHFFFAOYSA-N 2-phenyl-3,4-dihydro-2h-thiochromene Chemical class C1CC2=CC=CC=C2SC1C1=CC=CC=C1 NRYGFMAOIPXXBW-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 28
- 125000000217 alkyl group Chemical group 0.000 claims abstract 10
- 210000004556 brain Anatomy 0.000 claims abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 6
- 238000012800 visualization Methods 0.000 claims abstract 4
- 201000010099 disease Diseases 0.000 claims abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 2
- 231100000252 nontoxic Toxicity 0.000 claims abstract 2
- 230000003000 nontoxic effect Effects 0.000 claims abstract 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims abstract 2
- 230000002285 radioactive effect Effects 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 210000001638 cerebellum Anatomy 0.000 claims 6
- 230000008021 deposition Effects 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 108700028369 Alleles Proteins 0.000 claims 1
- 108010060159 Apolipoprotein E4 Proteins 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 210000005013 brain tissue Anatomy 0.000 claims 1
- 238000010494 dissociation reaction Methods 0.000 claims 1
- 230000005593 dissociations Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000010253 intravenous injection Methods 0.000 claims 1
- OEOPVJYUCSQVMJ-UHFFFAOYSA-N n,n-dimethyl-4-(6-methyl-1,3-benzothiazol-2-yl)aniline Chemical compound C1=CC(N(C)C)=CC=C1C1=NC2=CC=C(C)C=C2S1 OEOPVJYUCSQVMJ-UHFFFAOYSA-N 0.000 claims 1
- GGFYWXBSNMOKOK-UHFFFAOYSA-N n-methyl-4-(6-methyl-1,3-benzothiazol-2-yl)aniline Chemical compound C1=CC(NC)=CC=C1C1=NC2=CC=C(C)C=C2S1 GGFYWXBSNMOKOK-UHFFFAOYSA-N 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 238000002603 single-photon emission computed tomography Methods 0.000 claims 1
- 238000004611 spectroscopical analysis Methods 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000003325 tomography Methods 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003550 marker Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 0 CC1C=C(*)C=C2NC(C3=CCC(**)C=C3)=*C12 Chemical compound CC1C=C(*)C=C2NC(C3=CCC(**)C=C3)=*C12 0.000 description 2
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Classifications
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
- C07D277/66—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Medicinal Preparation (AREA)
- Magnetic Resonance Imaging Apparatus (AREA)
- Nuclear Medicine (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22760100P | 2000-08-24 | 2000-08-24 | |
| US60/227,601 | 2000-08-24 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2003108256A RU2003108256A (ru) | 2004-11-27 |
| RU2324686C2 true RU2324686C2 (ru) | 2008-05-20 |
Family
ID=22853739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2003108256/04A RU2324686C2 (ru) | 2000-08-24 | 2001-08-24 | ПРОИЗВОДНЫЕ ТИОФЛАВИНА, СВЯЗЫВАЮЩИЕ АМИЛОИД, СПОСОБ ОБНАРУЖЕНИЯ in vivo ОТЛОЖЕНИЙ АМИЛОИДА И СПОСОБ РАСПОЗНАВАНИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА |
Country Status (18)
| Country | Link |
|---|---|
| US (5) | US20020133019A1 (enExample) |
| EP (2) | EP2264018B1 (enExample) |
| JP (2) | JP5022554B2 (enExample) |
| CN (1) | CN1285582C (enExample) |
| AU (3) | AU2001286702B2 (enExample) |
| BR (1) | BRPI0113470B8 (enExample) |
| CA (1) | CA2419420C (enExample) |
| CY (1) | CY1113311T1 (enExample) |
| DK (2) | DK1334091T3 (enExample) |
| ES (2) | ES2536449T3 (enExample) |
| HU (2) | HU230581B1 (enExample) |
| LT (1) | LTC1334091I2 (enExample) |
| NO (1) | NO330176B1 (enExample) |
| PL (1) | PL215711B1 (enExample) |
| PT (2) | PT2264018E (enExample) |
| RU (1) | RU2324686C2 (enExample) |
| SI (1) | SI1334091T1 (enExample) |
| WO (1) | WO2002016333A2 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2766139C2 (ru) * | 2016-03-11 | 2022-02-08 | Ац Иммуне Са | Бициклические соединения для диагностики и лечения |
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| JP4853936B2 (ja) | 2000-08-21 | 2012-01-11 | ザ ジェネラル ホスピタル コーポレイション | 神経変性状態の診断方法 |
| US7270800B2 (en) | 2000-08-24 | 2007-09-18 | University Of Pittsburgh | Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
| SI1334091T1 (sl) | 2000-08-24 | 2013-01-31 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Derivati tioflavina in njihova uporaba pri diagnozi in terapiji pri Alzheimerjevi bolezni |
| JP2004518488A (ja) * | 2000-11-02 | 2004-06-24 | コーネル リサーチ ファンデーション インコーポレーテッド | インビボ多光子診断的な神経変性疾患の検出および撮像 |
| JP2004524289A (ja) * | 2000-12-22 | 2004-08-12 | アストラゼネカ・アクチエボラーグ | 治療化合物 |
| GB0106953D0 (en) | 2001-03-20 | 2001-05-09 | Univ Aberdeen | Neufofibrillary labels |
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| US6774248B2 (en) | 2001-12-18 | 2004-08-10 | Wyeth | Substituted 2-phenyl benzofurans as estrogenic agents |
| EP1820806A1 (en) * | 2006-02-16 | 2007-08-22 | Crossbeta Biosciences B.V. | Affinity regions |
| WO2003099206A2 (en) | 2002-05-21 | 2003-12-04 | Bristol-Myers Squibb Company | Indole compounds useful as impdh inhibitors |
| AU2003242233A1 (en) * | 2002-06-12 | 2003-12-31 | Bf Research Institute, Inc. | Probe compound for image diagnosis of disease with amyloid accumulation, compound for staining age spots/diffuse age spots, and remedy for disease with amyloid accumulation |
| EP1380290A1 (en) * | 2002-07-09 | 2004-01-14 | Universitair Medisch Centrum Utrecht | Cross-beta structure pathway and its therapeutic relevance |
| US20070003552A1 (en) * | 2002-07-09 | 2007-01-04 | Gebbink Martijn F B | Cross-beta structure comprising amyloid binding proteins and methods for detection of the cross-beta structure, for modulating cross-beta structures fibril formation and for modulating cross-beta structure-mediated toxicity and method for interfering with blood coagulation |
| AU2003261834A1 (en) * | 2002-08-30 | 2004-05-04 | Bf Research Institute, Inc. | Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein |
| CN101413143B (zh) | 2002-12-19 | 2013-09-18 | 斯克里普斯研究学院 | 稳定甲状腺素运载蛋白和抑制甲状腺素运载蛋白错折叠的组合物和方法 |
| GB0229686D0 (en) | 2002-12-20 | 2003-01-29 | Amersham Plc | Solid-phase fluorination of benzothiazoles |
| CA2438032C (en) * | 2003-03-14 | 2013-05-07 | University Of Pittsburgh | Benzothiazole derivative compounds, compositions and uses |
| ES2393921T3 (es) * | 2003-03-14 | 2013-01-02 | University Of Pittsburgh - Of The Commonwealthsystem Of Higher Education | Compuestos derivados de BENZOTIAZOL, composiciones y usos |
| GB0307855D0 (en) * | 2003-04-04 | 2003-05-14 | Novartis Ag | Organic compounds |
| US20040223912A1 (en) * | 2003-05-07 | 2004-11-11 | Montalto Michael Christopher | Compositions and methods for non-invasive imaging of soluble beta-amyloid |
| WO2004100998A2 (en) | 2003-05-07 | 2004-11-25 | General Electric Company | Compositions and methods for non-invasive imaging of soluble beta-amyloid |
| WO2005016384A1 (ja) * | 2003-08-13 | 2005-02-24 | Bf Research Institute, Inc. | アミロイド蓄積性疾患のプローブ、アミロイド染色剤、アミロイド蓄積性疾患の治療および予防薬、ならびに神経原線維変化の診断プローブおよび染色剤 |
| WO2005016888A1 (ja) * | 2003-08-13 | 2005-02-24 | Bf Research Institute, Inc. | アミロイド蓄積性疾患のプローブ、アミロイド染色剤、アミロイド蓄積性疾患の治療および予防薬、ならびに神経原線維変化の診断プローブおよび染色剤 |
| US8236282B2 (en) | 2003-08-22 | 2012-08-07 | University of Pittsburgh—of the Commonwealth System of Higher Education | Benzothiazole derivative compounds, compositions and uses |
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