CA2973648C - 9h-pyrrolo-dipyridine derivatives - Google Patents

9h-pyrrolo-dipyridine derivatives Download PDF

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Publication number
CA2973648C
CA2973648C CA2973648A CA2973648A CA2973648C CA 2973648 C CA2973648 C CA 2973648C CA 2973648 A CA2973648 A CA 2973648A CA 2973648 A CA2973648 A CA 2973648A CA 2973648 C CA2973648 C CA 2973648C
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Prior art keywords
pyrrolo
methyl
methoxy
mmol
optionally substituted
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CA2973648A
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English (en)
French (fr)
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CA2973648A1 (en
Inventor
Joel Mercier
Laurent Provins
Celine VERMEIREN
Yogesh Anil Sabnis
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UCB Biopharma SRL
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UCB Biopharma SRL
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    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-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
    • 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
    • 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
    • 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
    • A61K51/0463Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CA2973648A 2015-02-02 2016-01-29 9h-pyrrolo-dipyridine derivatives Active CA2973648C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15153448.4 2015-02-02
EP15153448 2015-02-02
PCT/EP2016/051993 WO2016124508A1 (en) 2015-02-02 2016-01-29 9h-pyrrolo-dipyridine derivatives

Publications (2)

Publication Number Publication Date
CA2973648A1 CA2973648A1 (en) 2016-08-11
CA2973648C true CA2973648C (en) 2023-09-26

Family

ID=52477553

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2973648A Active CA2973648C (en) 2015-02-02 2016-01-29 9h-pyrrolo-dipyridine derivatives

Country Status (17)

Country Link
US (3) US20180022748A1 (enExample)
EP (1) EP3253762B1 (enExample)
JP (1) JP6579670B2 (enExample)
KR (1) KR102621513B1 (enExample)
CN (1) CN107207508B (enExample)
AU (1) AU2016214537B2 (enExample)
BR (1) BR112017016311A2 (enExample)
CA (1) CA2973648C (enExample)
CL (1) CL2017001923A1 (enExample)
DK (1) DK3253762T3 (enExample)
EA (1) EA036518B1 (enExample)
ES (1) ES2875734T3 (enExample)
IL (1) IL253381B (enExample)
MX (1) MX378155B (enExample)
MY (1) MY191590A (enExample)
SG (1) SG11201705727TA (enExample)
WO (1) WO2016124508A1 (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009102498A1 (en) 2008-02-14 2009-08-20 Siemens Medical Solutions Usa, Inc. Novel imaging agents for detecting neurological dysfunction
WO2016124508A1 (en) * 2015-02-02 2016-08-11 Ucb Biopharma Sprl 9h-pyrrolo-dipyridine derivatives
JP7059270B2 (ja) * 2016-07-22 2022-04-25 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
SG11201811311VA (en) 2016-07-22 2019-01-30 Ac Immune Sa Compounds for imaging tau protein aggregates
ES2847903T3 (es) * 2016-09-09 2021-08-04 Hoffmann La Roche Procedimiento para la preparación de 2-(6-nitropiridin-3-il)-9H-dipirido[2,3-b;3',4'-d]pirrol
AU2017367872B2 (en) * 2016-11-01 2022-03-31 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
JPWO2018221728A1 (ja) 2017-06-02 2020-04-02 富士フイルム富山化学株式会社 アルツハイマー型認知症予防または治療剤
CN110691595A (zh) 2017-06-02 2020-01-14 富士胶片富山化学株式会社 β-淀粉样蛋白量减少剂
JP7133547B2 (ja) 2017-06-02 2022-09-08 富士フイルム富山化学株式会社 脊髄小脳変性症予防または治療剤
JP7370859B2 (ja) * 2017-06-02 2023-10-30 富士フイルム富山化学株式会社 タウオパチー予防または治療剤
CN116473962A (zh) 2017-06-02 2023-07-25 富士胶片富山化学株式会社 脑萎缩预防或治疗剂
WO2019088083A1 (ja) 2017-10-30 2019-05-09 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
US20210041447A1 (en) * 2018-01-24 2021-02-11 Ac Immune Sa Azacarboline compounds for the detection of tau aggregates
CN111868062B (zh) * 2018-01-24 2023-07-07 Ac免疫有限公司 制备显像化合物的方法
CN114867727B (zh) 2019-07-17 2025-02-21 阿尔维纳斯运营股份有限公司 Tau蛋白靶向化合物及相关使用方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1268771A (en) 1968-03-15 1972-03-29 Glaxo Lab Ltd Azacarbazoles
WO2008132454A1 (en) * 2007-04-26 2008-11-06 Ge Healthcare Limited Carbolines and their use as imaging agents
WO2009102498A1 (en) * 2008-02-14 2009-08-20 Siemens Medical Solutions Usa, Inc. Novel imaging agents for detecting neurological dysfunction
CN102325752B (zh) * 2008-12-19 2015-02-04 百时美施贵宝公司 咔唑和咔啉激酶抑制剂
CA2873963C (en) * 2012-05-22 2017-04-11 Eli Lilly And Company Carboline and carbazole based imaging agents for detecting neurological dysfunction
US20160115162A1 (en) 2013-05-31 2016-04-28 The General Hospital Corporation Radiosynthesis of Tau Radiopharmaceuticals
WO2015010263A1 (en) * 2013-07-24 2015-01-29 Telefonaktiebolaget L M Ericsson(Publ) Method and apparautus relating to reception of radio signals
PT3055308T (pt) * 2013-10-08 2018-01-18 Hoffmann La Roche Resumo
US10662193B2 (en) * 2014-01-21 2020-05-26 Ac Immune Sa Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyloid-like proteins
WO2016124508A1 (en) * 2015-02-02 2016-08-11 Ucb Biopharma Sprl 9h-pyrrolo-dipyridine derivatives

Also Published As

Publication number Publication date
JP2018503673A (ja) 2018-02-08
US20210047326A1 (en) 2021-02-18
MY191590A (en) 2022-06-30
IL253381A0 (en) 2017-09-28
MX378155B (es) 2025-03-10
ES2875734T3 (es) 2021-11-11
JP6579670B2 (ja) 2019-09-25
EP3253762B1 (en) 2021-05-05
KR102621513B1 (ko) 2024-01-04
IL253381B (en) 2020-10-29
EA036518B1 (ru) 2020-11-18
CN107207508B (zh) 2020-02-28
AU2016214537A1 (en) 2017-08-03
DK3253762T3 (da) 2021-07-19
BR112017016311A2 (pt) 2018-03-27
CL2017001923A1 (es) 2018-02-16
US20220213103A1 (en) 2022-07-07
KR20170113607A (ko) 2017-10-12
EP3253762A1 (en) 2017-12-13
WO2016124508A1 (en) 2016-08-11
AU2016214537B2 (en) 2018-05-10
EA201791733A1 (ru) 2018-01-31
US12006316B2 (en) 2024-06-11
US11312716B2 (en) 2022-04-26
MX2017009505A (es) 2017-11-02
US20180022748A1 (en) 2018-01-25
SG11201705727TA (en) 2017-08-30
CN107207508A (zh) 2017-09-26
CA2973648A1 (en) 2016-08-11

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