MX2016016384A - Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares. - Google Patents

Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares.

Info

Publication number
MX2016016384A
MX2016016384A MX2016016384A MX2016016384A MX2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A
Authority
MX
Mexico
Prior art keywords
aggregates
tau
alzheimer
imaging
pyridines
Prior art date
Application number
MX2016016384A
Other languages
English (en)
Inventor
James Mulhearn
Yaode Wang
M Walji Abbas
Hostetler Eric
GRESHOCK Thomas
Li Jing
P Moore Keith
Bennacef Idriss
Selnick Harold
Yang Kun
Fu Jianmin
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of MX2016016384A publication Critical patent/MX2016016384A/es

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    • 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
    • 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
    • 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)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente invención se refiere a compuestos de pirrolopiridina de fórmula (I) (ver Fórmula) o sus sales farmacéuticamente aceptables, que pueden ser adecuadas para la obtención de imágenes de agregados de tau, agregados de hojas b, agregados de beta-amiloide o agregados de alfa-sinucleína y, por tanto, son útiles en la unión y formación de imágenes de agregados de tau en pacientes de Alzheimer; más específicamente, esta invención se refiere a un método de utilización de los compuestos de esta invención como trazadores en las imágenes de tomografía por emisión de positrones (PET) para estudiar los depósitos de tau en el cerebro in vivo para permitir el diagnóstico de la enfermedad de Alzheimer y otras enfermedades neurodegenerativas caracterizadas por patología tau; la invención se refiere además a un método para medir la eficacia clínica de agentes terapéuticos para la enfermedad de Alzheimer y otras enfermedades neurodegenerativas caracterizadas por patología tau.
MX2016016384A 2014-06-13 2015-06-09 Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares. MX2016016384A (es)

Applications Claiming Priority (2)

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
PCT/US2015/034794 WO2015191506A2 (en) 2014-06-13 2015-06-09 Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles

Publications (1)

Publication Number Publication Date
MX2016016384A true MX2016016384A (es) 2017-05-01

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016016384A MX2016016384A (es) 2014-06-13 2015-06-09 Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares.

Country Status (15)

Country Link
US (2) US9808542B2 (es)
EP (1) EP3154970B1 (es)
JP (1) JP6513107B2 (es)
KR (1) KR102478430B1 (es)
CN (1) CN106661018B (es)
AU (1) AU2015274843B2 (es)
BR (1) BR112016028345B1 (es)
CA (1) CA2948528C (es)
DK (1) DK3154970T3 (es)
ES (1) ES2763095T3 (es)
HU (1) HUE048395T2 (es)
MX (1) MX2016016384A (es)
PL (1) PL3154970T3 (es)
RU (1) RU2695373C2 (es)
WO (2) WO2015188368A1 (es)

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BR112019024878A2 (pt) * 2017-06-02 2020-06-16 Fujifilm Toyama Chemical Co., Ltd. Agente para prevenção ou tratamento de tauopatia
SG11201911519UA (en) 2017-06-02 2020-01-30 Fujifilm Toyama Chemical Co Ltd AGENT FOR REDUCING AMOUNT OF AMYLOID ß PROTEIN
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
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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
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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
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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
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Also Published As

Publication number Publication date
KR20170016481A (ko) 2017-02-13
JP2017521387A (ja) 2017-08-03
WO2015191506A3 (en) 2016-02-04
WO2015191506A2 (en) 2015-12-17
CA2948528A1 (en) 2015-12-17
CN106661018A (zh) 2017-05-10
CN106661018B (zh) 2019-07-19
RU2019115483A (ru) 2019-06-13
AU2015274843B2 (en) 2018-11-22
AU2015274843A1 (en) 2016-11-10
DK3154970T3 (da) 2020-01-20
EP3154970A2 (en) 2017-04-19
EP3154970B1 (en) 2019-11-06
CA2948528C (en) 2022-05-31
BR112016028345B1 (pt) 2022-11-29
BR112016028345A8 (pt) 2021-06-29
KR102478430B1 (ko) 2022-12-15
BR112016028345A2 (pt) 2017-08-22
JP6513107B2 (ja) 2019-05-15
US10022461B2 (en) 2018-07-17
WO2015188368A1 (en) 2015-12-17
US9808542B2 (en) 2017-11-07
US20170119912A1 (en) 2017-05-04
ES2763095T3 (es) 2020-05-27
RU2016150404A3 (es) 2018-11-30
PL3154970T3 (pl) 2020-04-30
US20180071412A1 (en) 2018-03-15
RU2016150404A (ru) 2018-07-18
RU2695373C2 (ru) 2019-07-23
EP3154970A4 (en) 2017-11-15
HUE048395T2 (hu) 2020-08-28

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