AU2016214537B2 - 9H-pyrrolo-dipyridine derivatives - Google Patents

9H-pyrrolo-dipyridine derivatives Download PDF

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Publication number
AU2016214537B2
AU2016214537B2 AU2016214537A AU2016214537A AU2016214537B2 AU 2016214537 B2 AU2016214537 B2 AU 2016214537B2 AU 2016214537 A AU2016214537 A AU 2016214537A AU 2016214537 A AU2016214537 A AU 2016214537A AU 2016214537 B2 AU2016214537 B2 AU 2016214537B2
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Prior art keywords
pyrrolo
optionally substituted
methyl
dipyridine
halogens
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AU2016214537A1 (en
Inventor
Joel Mercier
Laurent Provins
Yogesh Anil Sabnis
Celine VERMEIREN
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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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)
AU2016214537A 2015-02-02 2016-01-29 9H-pyrrolo-dipyridine derivatives Active AU2016214537B2 (en)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
AU2016214537A1 AU2016214537A1 (en) 2017-08-03
AU2016214537B2 true AU2016214537B2 (en) 2018-05-10

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AU2016214537A Active AU2016214537B2 (en) 2015-02-02 2016-01-29 9H-pyrrolo-dipyridine derivatives

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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)

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PL2247558T5 (pl) 2008-02-14 2024-10-14 Eli Lilly And Company Nowe środki obrazujące do wykrywania czynnościowych zaburzeń neurologicznych
SG11201705727TA (en) * 2015-02-02 2017-08-30 Ucb Biopharma Sprl 9h-pyrrolo-dipyridine derivatives
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
EP3487545A1 (en) 2016-07-22 2019-05-29 AC Immune S.A. 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
KR20230127371A (ko) * 2016-11-01 2023-08-31 아비나스 오퍼레이션스, 인코포레이티드 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법
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.
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
EP3636262A4 (en) 2017-06-02 2020-06-10 FUJIFILM Toyama Chemical Co., Ltd. AGENT FOR PREVENTING OR TREATING ALZHEIMER-LIKE DEMENTIA
BR112019024983A2 (pt) 2017-06-02 2020-06-23 Fujifilm Toyama Chemical Co., Ltd. Agente para reduzir a quantidade de proteína b amiloide
EP3705121B1 (en) 2017-10-30 2023-08-30 FUJIFILM Toyama Chemical Co., Ltd. Emopamil binding protein binding agent and use thereof
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
EP3743426A1 (en) * 2018-01-24 2020-12-02 AC Immune SA Azacarboline compounds for the detection of tau aggregates
EP3743423A1 (en) 2018-01-24 2020-12-02 AC Immune SA Gamma-carboline compounds for the detection of tau aggregates
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated

Citations (2)

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WO2009102498A1 (en) * 2008-02-14 2009-08-20 Siemens Medical Solutions Usa, Inc. Novel imaging agents for detecting neurological dysfunction
WO2015052105A1 (en) * 2013-10-08 2015-04-16 F. Hoffmann-La Roche Ag Diazacarbazole derivatives as tau-pet-ligands

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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
JP5557849B2 (ja) * 2008-12-19 2014-07-23 ブリストル−マイヤーズ スクイブ カンパニー カルバゾールおよびカルボリンキナーゼ阻害剤
ES2792830T3 (es) * 2012-05-22 2020-11-12 Lilly Co Eli Agentes para formación de imagen en base a carbolina y carbazol, para la detección de disfunción neurológica
US20160115162A1 (en) * 2013-05-31 2016-04-28 The General Hospital Corporation Radiosynthesis of Tau Radiopharmaceuticals
US9774356B2 (en) * 2013-07-24 2017-09-26 Telefonaktiebolaget Lm Ericsson (Publ) Method and apparatus relating to reception of radio signals
WO2015110263A1 (en) * 2014-01-21 2015-07-30 Ac Immune Sa Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyolid-like proteins
SG11201705727TA (en) * 2015-02-02 2017-08-30 Ucb Biopharma Sprl 9h-pyrrolo-dipyridine derivatives

Patent Citations (2)

* 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
WO2015052105A1 (en) * 2013-10-08 2015-04-16 F. Hoffmann-La Roche Ag Diazacarbazole derivatives as tau-pet-ligands

Also Published As

Publication number Publication date
CN107207508A (zh) 2017-09-26
CL2017001923A1 (es) 2018-02-16
CA2973648C (en) 2023-09-26
EA201791733A1 (ru) 2018-01-31
US20220213103A1 (en) 2022-07-07
JP6579670B2 (ja) 2019-09-25
MX2017009505A (es) 2017-11-02
US12006316B2 (en) 2024-06-11
BR112017016311A2 (pt) 2018-03-27
KR102621513B1 (ko) 2024-01-04
CA2973648A1 (en) 2016-08-11
MX378155B (es) 2025-03-10
ES2875734T3 (es) 2021-11-11
CN107207508B (zh) 2020-02-28
EP3253762B1 (en) 2021-05-05
EP3253762A1 (en) 2017-12-13
JP2018503673A (ja) 2018-02-08
MY191590A (en) 2022-06-30
AU2016214537A1 (en) 2017-08-03
SG11201705727TA (en) 2017-08-30
US11312716B2 (en) 2022-04-26
IL253381A0 (en) 2017-09-28
EA036518B1 (ru) 2020-11-18
US20180022748A1 (en) 2018-01-25
WO2016124508A1 (en) 2016-08-11
DK3253762T3 (da) 2021-07-19
IL253381B (en) 2020-10-29
KR20170113607A (ko) 2017-10-12
US20210047326A1 (en) 2021-02-18

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