AU2015274843B2 - Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles - Google Patents

Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles Download PDF

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Publication number
AU2015274843B2
AU2015274843B2 AU2015274843A AU2015274843A AU2015274843B2 AU 2015274843 B2 AU2015274843 B2 AU 2015274843B2 AU 2015274843 A AU2015274843 A AU 2015274843A AU 2015274843 A AU2015274843 A AU 2015274843A AU 2015274843 B2 AU2015274843 B2 AU 2015274843B2
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mmol
pyrrolo
pyridin
aryl
synthesis
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AU2015274843A1 (en
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Idriss BENNACEF
Jianmin Fu
Thomas Greshock
Eric Hostetler
Jing Li
Keith P. Moore
James Mulhearn
Harold Selnick
Abbas M. Walji
Yaode Wang
Kun Yang
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Merck Sharp and Dohme LLC
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0455Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • 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)
AU2015274843A 2014-06-13 2015-06-09 Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles Active AU2015274843B2 (en)

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
AUPCT/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

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AU2015274843A1 AU2015274843A1 (en) 2016-11-10
AU2015274843B2 true AU2015274843B2 (en) 2018-11-22

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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)

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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
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
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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
RU2019115483A (ru) 2019-06-13
DK3154970T3 (da) 2020-01-20
RU2695373C2 (ru) 2019-07-23
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

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