RU2695373C2 - Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков - Google Patents

Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков Download PDF

Info

Publication number
RU2695373C2
RU2695373C2 RU2016150404A RU2016150404A RU2695373C2 RU 2695373 C2 RU2695373 C2 RU 2695373C2 RU 2016150404 A RU2016150404 A RU 2016150404A RU 2016150404 A RU2016150404 A RU 2016150404A RU 2695373 C2 RU2695373 C2 RU 2695373C2
Authority
RU
Russia
Prior art keywords
mmol
pyrrolo
pyridine
pyridin
optionally substituted
Prior art date
Application number
RU2016150404A
Other languages
English (en)
Russian (ru)
Other versions
RU2016150404A (ru
RU2016150404A3 (enExample
Inventor
Аббас М. ВАЛДЖИ
Эрик ХОСТЕТЛЕР
Томас ГРЕШОК
Цзин Ли
Кит П. МУР
Идрисс БЕННАСЕФ
Джеймс МАЛХИРН
Харолд СЕЛНИК
Яодэ ВАН
Кунь ЯН
Цзяньминь Фу
Original Assignee
Мерк Шарп И Доум Корп.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Мерк Шарп И Доум Корп. filed Critical Мерк Шарп И Доум Корп.
Publication of RU2016150404A publication Critical patent/RU2016150404A/ru
Publication of RU2016150404A3 publication Critical patent/RU2016150404A3/ru
Application granted granted Critical
Publication of RU2695373C2 publication Critical patent/RU2695373C2/ru

Links

Images

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
    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Hospice & Palliative Care (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
RU2016150404A 2014-06-13 2015-06-09 Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков RU2695373C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2014/079834 WO2015188368A1 (en) 2014-06-13 2014-06-13 Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles
CNPCT/CN2014/079834 2014-06-13
PCT/US2015/034794 WO2015191506A2 (en) 2014-06-13 2015-06-09 Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles

Related Child Applications (1)

Application Number Title Priority Date Filing Date
RU2019115483A Division RU2788916C2 (ru) 2014-06-13 2015-06-09 Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков

Publications (3)

Publication Number Publication Date
RU2016150404A RU2016150404A (ru) 2018-07-18
RU2016150404A3 RU2016150404A3 (enExample) 2018-11-30
RU2695373C2 true RU2695373C2 (ru) 2019-07-23

Family

ID=54832744

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2016150404A RU2695373C2 (ru) 2014-06-13 2015-06-09 Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков

Country Status (15)

Country Link
US (2) US9808542B2 (enExample)
EP (1) EP3154970B1 (enExample)
JP (1) JP6513107B2 (enExample)
KR (1) KR102478430B1 (enExample)
CN (1) CN106661018B (enExample)
AU (1) AU2015274843B2 (enExample)
BR (1) BR112016028345B1 (enExample)
CA (1) CA2948528C (enExample)
DK (1) DK3154970T3 (enExample)
ES (1) ES2763095T3 (enExample)
HU (1) HUE048395T2 (enExample)
MX (1) MX375282B (enExample)
PL (1) PL3154970T3 (enExample)
RU (1) RU2695373C2 (enExample)
WO (2) WO2015188368A1 (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2894994C (en) 2012-12-21 2019-11-12 National Institute Of Radiological Sciences Compounds for imaging tau proteins that accumulate in brain
EP3487545A1 (en) 2016-07-22 2019-05-29 AC Immune S.A. Compounds for imaging tau protein aggregates
CN115650982A (zh) 2016-07-22 2023-01-31 Ac免疫有限公司 用于成像tau蛋白聚集体的化合物
EP3636262A4 (en) 2017-06-02 2020-06-10 FUJIFILM Toyama Chemical Co., Ltd. AGENT FOR PREVENTING OR TREATING ALZHEIMER-LIKE DEMENTIA
US11660287B2 (en) 2017-06-02 2023-05-30 Fujifilm Toyama Chemical Co., Ltd. Agent for preventing or treating spinocerebellar ataxia
MX393052B (es) 2017-06-02 2025-03-24 Fujifilm Toyama Chemical Co Ltd Agente para prevenir o tratar atrofia cerebral.
BR112019024983A2 (pt) 2017-06-02 2020-06-23 Fujifilm Toyama Chemical Co., Ltd. Agente para reduzir a quantidade de proteína b amiloide
WO2018221731A1 (ja) * 2017-06-02 2018-12-06 富山化学工業株式会社 タウオパチー予防または治療剤
EP3705121B1 (en) 2017-10-30 2023-08-30 FUJIFILM Toyama Chemical Co., Ltd. Emopamil binding protein binding agent and use thereof
EP3743423A1 (en) 2018-01-24 2020-12-02 AC Immune SA 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
WO2019192533A1 (zh) * 2018-04-04 2019-10-10 深圳福沃药业有限公司 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
JP7293343B2 (ja) * 2018-05-09 2023-06-19 アプリノイア セラピューティクス リミテッド ヘテロアリール化合物及びその使用
US12448374B2 (en) 2018-06-07 2025-10-21 Disarm Therapeutics, Inc. Inhibitors of SARM1
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
EP3897670A4 (en) 2018-12-19 2022-09-07 Disarm Therapeutics, Inc. MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS
KR20220100921A (ko) 2019-11-13 2022-07-18 아프리노이아 테라퓨틱스 리미티드 타우 단백질 응집체를 분해하기 위한 화합물 및 이의 용도
US20220008563A1 (en) * 2020-07-10 2022-01-13 The Regents Of The University Of California Radiolabelled and nonradiolabelled pegylated compounds and uses thereof
WO2022031946A1 (en) * 2020-08-06 2022-02-10 Chdi Foundation, Inc. Heterobiaryl compounds and imaging agents for imaging huntingtin protein
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2135497C1 (ru) * 1993-11-17 1999-08-27 Зенека Лимитед Пирролопиридины или их сельскохозяйственно-приемлемые соли, гербицидная композиция и способ подавления нежелательной растительности
US20080027044A1 (en) * 2006-06-13 2008-01-31 Kim Lewis Prodrug antibiotic screens
WO2009022961A1 (en) * 2007-05-15 2009-02-19 Astrazeneca Ab Pyrrolopyridine derivatives and their use as bace inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5635727B2 (ja) * 2004-10-07 2014-12-03 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法
WO2008103615A1 (en) 2007-02-21 2008-08-28 Kalypsys, Inc. Isoquinolines useful as inducible nitric oxide synthase inhibitors
WO2009155024A1 (en) * 2008-05-30 2009-12-23 Merck & Co., Inc. Novel substituted indoles
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
GB201004311D0 (en) * 2010-03-15 2010-04-28 Proximagen Ltd New enzyme inhibitor compounds
CN103298474B (zh) 2010-11-10 2016-06-29 无限药品股份有限公司 杂环化合物及其用途
CA2825599C (en) 2011-02-01 2021-07-13 The Board Of Trustees Of The University Of Illinois 4-methyl-n-hydroxybenzamide compounds as histone deacetylase (hdac) inhibitors
US8684313B2 (en) 2011-02-02 2014-04-01 Ocean Rodeo Sports Inc. Inflatable kite with leading edge swept forwards at wingtip
WO2013040183A1 (en) * 2011-09-16 2013-03-21 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Beta-amyloid imaging agents, methods of manufacture, and methods of use thereof
EP2855477A4 (en) * 2012-05-29 2015-11-18 Merck Sharp & Dohme ISOTOPICALLY MARKED 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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2135497C1 (ru) * 1993-11-17 1999-08-27 Зенека Лимитед Пирролопиридины или их сельскохозяйственно-приемлемые соли, гербицидная композиция и способ подавления нежелательной растительности
US20080027044A1 (en) * 2006-06-13 2008-01-31 Kim Lewis Prodrug antibiotic screens
WO2009022961A1 (en) * 2007-05-15 2009-02-19 Astrazeneca Ab Pyrrolopyridine derivatives and their use as bace inhibitors

Also Published As

Publication number Publication date
AU2015274843A1 (en) 2016-11-10
JP2017521387A (ja) 2017-08-03
CN106661018A (zh) 2017-05-10
BR112016028345B1 (pt) 2022-11-29
ES2763095T3 (es) 2020-05-27
EP3154970A4 (en) 2017-11-15
AU2015274843B2 (en) 2018-11-22
RU2019115483A (ru) 2019-06-13
DK3154970T3 (da) 2020-01-20
CN106661018B (zh) 2019-07-19
EP3154970B1 (en) 2019-11-06
BR112016028345A8 (pt) 2021-06-29
US9808542B2 (en) 2017-11-07
CA2948528A1 (en) 2015-12-17
MX2016016384A (es) 2017-05-01
WO2015191506A3 (en) 2016-02-04
US20170119912A1 (en) 2017-05-04
HUE048395T2 (hu) 2020-08-28
KR102478430B1 (ko) 2022-12-15
US20180071412A1 (en) 2018-03-15
WO2015191506A2 (en) 2015-12-17
RU2016150404A (ru) 2018-07-18
EP3154970A2 (en) 2017-04-19
RU2016150404A3 (enExample) 2018-11-30
PL3154970T3 (pl) 2020-04-30
WO2015188368A1 (en) 2015-12-17
MX375282B (es) 2025-03-06
CA2948528C (en) 2022-05-31
KR20170016481A (ko) 2017-02-13
US10022461B2 (en) 2018-07-17
BR112016028345A2 (pt) 2017-08-22
JP6513107B2 (ja) 2019-05-15

Similar Documents

Publication Publication Date Title
RU2695373C2 (ru) Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков
EP2300481B1 (en) Novel substituted azabenzoxazoles
KR101099303B1 (ko) 신규한 벤조이미다졸 유도체 및 이를 함유하는 약제학적조성물
JP6579670B2 (ja) ９ｈ−ピロロ−ジピリジン誘導体
CA3145305A1 (en) Indazoles and azaindazoles as lrrk2 inhibitors
CA2741668A1 (en) Novel substituted azabenzoxazoles
CA2725934A1 (en) Novel substituted indoles
RU2788916C2 (ru) Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков
KR101418078B1 (ko) ｍＧｌｕＲ5 길항제로서의 2-(치환된에티닐)퀴놀린 유도체