BR112016028345A8 - composto, composição farmacêutica, sal farmaceuticamente aceitável de um composto, e, métodos para inibir agregação de tau em um mamífero e para avaliar depósitos de tau em um paciente - Google Patents
composto, composição farmacêutica, sal farmaceuticamente aceitável de um composto, e, métodos para inibir agregação de tau em um mamífero e para avaliar depósitos de tau em um pacienteInfo
- Publication number
- BR112016028345A8 BR112016028345A8 BR112016028345A BR112016028345A BR112016028345A8 BR 112016028345 A8 BR112016028345 A8 BR 112016028345A8 BR 112016028345 A BR112016028345 A BR 112016028345A BR 112016028345 A BR112016028345 A BR 112016028345A BR 112016028345 A8 BR112016028345 A8 BR 112016028345A8
- Authority
- BR
- Brazil
- Prior art keywords
- tau
- compound
- aggregates
- pharmaceutically acceptable
- evaluating
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 4
- 150000003839 salts Chemical class 0.000 title abstract 3
- 241000124008 Mammalia Species 0.000 title abstract 2
- 238000004220 aggregation Methods 0.000 title abstract 2
- 230000002776 aggregation Effects 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 238000003384 imaging method Methods 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- 230000004770 neurodegeneration Effects 0.000 abstract 2
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 2
- 230000007170 pathology Effects 0.000 abstract 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 102000003802 alpha-Synuclein Human genes 0.000 abstract 1
- 108090000185 alpha-Synuclein Proteins 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 238000002600 positron emission tomography Methods 0.000 abstract 1
- RDRCCJPEJDWSRJ-UHFFFAOYSA-N pyridine;1h-pyrrole Chemical class C=1C=CNC=1.C1=CC=NC=C1 RDRCCJPEJDWSRJ-UHFFFAOYSA-N 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- 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
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
-
- 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
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Physics & Mathematics (AREA)
- Optics & Photonics (AREA)
- Psychiatry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
composto, composição farmacêutica, sal farmaceuticamente aceitável de um composto, e, métodos para inibir agregação de tau em um mamífero e para avaliar depósitos de tau em um paciente. a presente invenção se refere a compostos de pirrol piridina da fórmula (i) ou seus sais farmaceuticamente aceitáveis, que podem ser adequados para formar imagem de agregados de tau, agregados de folha ß, agregados de beta-amiloide ou agregados de alfa-sinucleína, e consequentemente são usados na ligação e formação de imagem de agregados de tau em pacientes com alzheimer. mais especificamente, esta invenção se refere a um método para usar os compostos desta invenção como marcadores em formação de imagem por tomografia por emissão de pósitron (pet) para estudar depósitos de tau no cérebro in vivo, para permitir o diagnóstico de doença de alzheimer e outras doenças neurodegenerativas caracterizadas por patologia associada a tau. a invenção se refere adicionalmente a um método para avaliar a eficiência clínica de agentes terapêuticos para doença de alzheimer e outras doenças neurodegenerativas caracterizadas por patologia associada à tau.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/079834 | 2014-06-13 | ||
| PCT/CN2014/079834 WO2015188368A1 (en) | 2014-06-13 | 2014-06-13 | Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles |
| PCT/US2015/034794 WO2015191506A2 (en) | 2014-06-13 | 2015-06-09 | Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BR112016028345A2 BR112016028345A2 (pt) | 2017-08-22 |
| BR112016028345A8 true BR112016028345A8 (pt) | 2021-06-29 |
| BR112016028345B1 BR112016028345B1 (pt) | 2022-11-29 |
Family
ID=54832744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112016028345-7A BR112016028345B1 (pt) | 2014-06-13 | 2015-06-09 | Composto e composição farmacêutica |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9808542B2 (pt) |
| EP (1) | EP3154970B1 (pt) |
| JP (1) | JP6513107B2 (pt) |
| KR (1) | KR102478430B1 (pt) |
| CN (1) | CN106661018B (pt) |
| AU (1) | AU2015274843B2 (pt) |
| BR (1) | BR112016028345B1 (pt) |
| CA (1) | CA2948528C (pt) |
| DK (1) | DK3154970T3 (pt) |
| ES (1) | ES2763095T3 (pt) |
| HU (1) | HUE048395T2 (pt) |
| MX (1) | MX2016016384A (pt) |
| PL (1) | PL3154970T3 (pt) |
| RU (1) | RU2695373C2 (pt) |
| WO (2) | WO2015188368A1 (pt) |
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| AU2012397435B2 (en) | 2012-12-21 | 2017-03-30 | National Institutes For Quantum And Radiological Science And Technology | Novel compound for imaging TAU protein accumulated in the brain |
| US10865207B2 (en) | 2016-07-22 | 2020-12-15 | Ac Immune S.A. | Compounds for imaging Tau protein aggregates |
| JP7197476B2 (ja) | 2016-07-22 | 2022-12-27 | エーシー・イミューン・エス・アー | タウタンパク質凝集体を画像化するための化合物 |
| AU2018277983B2 (en) | 2017-06-02 | 2021-04-08 | Fujifilm Toyama Chemical Co., Ltd. | Amyloid-β protein level decreasing agent |
| WO2018221728A1 (ja) | 2017-06-02 | 2018-12-06 | 富山化学工業株式会社 | アルツハイマー型認知症予防または治療剤 |
| SG11201911520UA (en) * | 2017-06-02 | 2020-01-30 | Fujifilm Toyama Chemical Co Ltd | Agent for preventing or treating tauopathy |
| KR20190138696A (ko) | 2017-06-02 | 2019-12-13 | 후지필름 도야마 케미컬 가부시키가이샤 | 척수 소뇌 변성증 예방 또는 치료제 |
| MX2019014310A (es) | 2017-06-02 | 2022-06-10 | Fujifilm Toyama Chemical Co Ltd | Agente para prevenir o tratar atrofia cerebral. |
| JP7227914B2 (ja) | 2017-10-30 | 2023-02-22 | 富士フイルム富山化学株式会社 | エモパミル結合タンパク質結合剤およびその利用 |
| US11306089B2 (en) | 2018-01-24 | 2022-04-19 | Life Molecular Imaging Limited | Gamma-carboline compounds for the detection of Tau aggregates |
| EP3743426A1 (en) | 2018-01-24 | 2020-12-02 | AC Immune SA | Azacarboline compounds for the detection of tau aggregates |
| CN110343101B (zh) * | 2018-04-04 | 2022-07-12 | 青岛福沃药业有限公司 | 用于治疗乳腺癌的雌激素受体降解剂 |
| KR102017324B1 (ko) * | 2018-04-30 | 2019-09-02 | 경북대학교 산학협력단 | 신규한 asm 활성 직접 억제 화합물 2-아미노-2-(1,2,3-트리아졸-4-일)프로판-1,3-디올 유도체 및 이의 용도 |
| EP3790883A4 (en) * | 2018-05-09 | 2022-08-24 | Aprinoia Therapeutics Limited | HETEROARYL COMPOUNDS AND USES THEREOF |
| CN108676007B (zh) * | 2018-06-22 | 2020-06-26 | 厦门大学 | 放射性核素标记的苯并蝶啶类衍生物及其制备方法和应用 |
| CA3123215C (en) | 2018-12-19 | 2024-04-02 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with neuroprotective agents |
| AU2020383593A1 (en) | 2019-11-13 | 2022-06-09 | Aprinoia Therapeutics Limited | Compounds for degrading Tau protein aggregates and uses thereof |
| US20220008563A1 (en) * | 2020-07-10 | 2022-01-13 | The Regents Of The University Of California | Radiolabelled and nonradiolabelled pegylated compounds and uses thereof |
| CN112939753B (zh) * | 2020-09-15 | 2022-04-05 | 浙江大学 | 一种1-茚酮类化合物的合成方法 |
| KR102240400B1 (ko) * | 2020-11-19 | 2021-04-15 | 한국원자력연구원 | 베타-아밀로이드 검출용 수용성 화합물 |
| CN112745299B (zh) * | 2021-01-07 | 2022-01-25 | 温州大学 | 4-氰基-7,8-二氢异喹啉衍生物及其制备方法和应用 |
| TWI782769B (zh) * | 2021-10-28 | 2022-11-01 | 行政院原子能委員會核能研究所 | 一種新穎神經纖維糾結微管相關蛋白質Tau造影化合物、其製備方法及用途 |
| CN114149425A (zh) * | 2021-11-16 | 2022-03-08 | 上海应用技术大学 | 5-氟甲基吡啶衍生物和18-f同位素标记的5-氟甲基吡啶衍生物及其制备与应用 |
| CN114276259B (zh) * | 2022-01-04 | 2022-12-06 | 济川(上海)医学科技有限公司 | 一种马来酸二甲茚定关键中间体的制备方法 |
| CN115417816B (zh) * | 2022-09-05 | 2024-01-26 | 江苏南大光电材料股份有限公司 | 一种3,6-二溴-1-氯-异喹啉的制备方法 |
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| US5451566A (en) * | 1993-11-17 | 1995-09-19 | Zeneca Limited | Herbicidal pyrrolopyridine compounds |
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| TW200902499A (en) * | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
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| EP2637669A4 (en) | 2010-11-10 | 2014-04-02 | Infinity Pharmaceuticals Inc | Heterocyclic compounds and their use |
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| US8684313B2 (en) | 2011-02-02 | 2014-04-01 | Ocean Rodeo Sports Inc. | Inflatable kite with leading edge swept forwards at wingtip |
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| WO2013181075A1 (en) * | 2012-05-29 | 2013-12-05 | Merck Sharp & Dohme Corp. | Isotopically labeled biaryl urea compounds |
| CN103450152B (zh) * | 2012-06-04 | 2015-11-18 | 济南海乐医药技术开发有限公司 | 基于吲唑、吲哚或氮杂吲唑、氮杂吲哚的双芳基脲类结构抗肿瘤药物 |
| GB201304526D0 (en) | 2013-03-13 | 2013-04-24 | Proximagen Ltd | New compounds |
| GB201404498D0 (en) * | 2014-03-13 | 2014-04-30 | Proximagen Ltd | New compounds |
-
2014
- 2014-06-13 WO PCT/CN2014/079834 patent/WO2015188368A1/en active Application Filing
-
2015
- 2015-06-09 US US15/317,333 patent/US9808542B2/en active Active
- 2015-06-09 ES ES15806980T patent/ES2763095T3/es active Active
- 2015-06-09 DK DK15806980.7T patent/DK3154970T3/da active
- 2015-06-09 CA CA2948528A patent/CA2948528C/en active Active
- 2015-06-09 KR KR1020177000709A patent/KR102478430B1/ko active IP Right Grant
- 2015-06-09 JP JP2016572520A patent/JP6513107B2/ja active Active
- 2015-06-09 BR BR112016028345-7A patent/BR112016028345B1/pt active IP Right Grant
- 2015-06-09 RU RU2016150404A patent/RU2695373C2/ru active
- 2015-06-09 EP EP15806980.7A patent/EP3154970B1/en active Active
- 2015-06-09 WO PCT/US2015/034794 patent/WO2015191506A2/en active Application Filing
- 2015-06-09 AU AU2015274843A patent/AU2015274843B2/en active Active
- 2015-06-09 HU HUE15806980A patent/HUE048395T2/hu unknown
- 2015-06-09 CN CN201580031335.2A patent/CN106661018B/zh active Active
- 2015-06-09 PL PL15806980T patent/PL3154970T3/pl unknown
- 2015-06-09 MX MX2016016384A patent/MX2016016384A/es active IP Right Grant
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|---|---|
| US20180071412A1 (en) | 2018-03-15 |
| EP3154970A4 (en) | 2017-11-15 |
| WO2015191506A2 (en) | 2015-12-17 |
| US9808542B2 (en) | 2017-11-07 |
| US10022461B2 (en) | 2018-07-17 |
| US20170119912A1 (en) | 2017-05-04 |
| EP3154970B1 (en) | 2019-11-06 |
| WO2015191506A3 (en) | 2016-02-04 |
| EP3154970A2 (en) | 2017-04-19 |
| HUE048395T2 (hu) | 2020-08-28 |
| CN106661018A (zh) | 2017-05-10 |
| RU2019115483A (ru) | 2019-06-13 |
| AU2015274843A1 (en) | 2016-11-10 |
| RU2016150404A (ru) | 2018-07-18 |
| PL3154970T3 (pl) | 2020-04-30 |
| RU2695373C2 (ru) | 2019-07-23 |
| WO2015188368A1 (en) | 2015-12-17 |
| KR102478430B1 (ko) | 2022-12-15 |
| ES2763095T3 (es) | 2020-05-27 |
| DK3154970T3 (da) | 2020-01-20 |
| RU2016150404A3 (pt) | 2018-11-30 |
| KR20170016481A (ko) | 2017-02-13 |
| JP6513107B2 (ja) | 2019-05-15 |
| CN106661018B (zh) | 2019-07-19 |
| BR112016028345B1 (pt) | 2022-11-29 |
| CA2948528C (en) | 2022-05-31 |
| JP2017521387A (ja) | 2017-08-03 |
| CA2948528A1 (en) | 2015-12-17 |
| AU2015274843B2 (en) | 2018-11-22 |
| BR112016028345A2 (pt) | 2017-08-22 |
| MX2016016384A (es) | 2017-05-01 |
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