KR101770531B1 - 타우-펫-리간드로서의 다이아자카르바졸 유도체 - Google Patents

타우-펫-리간드로서의 다이아자카르바졸 유도체 Download PDF

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KR101770531B1
KR101770531B1 KR1020167008013A KR20167008013A KR101770531B1 KR 101770531 B1 KR101770531 B1 KR 101770531B1 KR 1020167008013 A KR1020167008013 A KR 1020167008013A KR 20167008013 A KR20167008013 A KR 20167008013A KR 101770531 B1 KR101770531 B1 KR 101770531B1
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formula
compound
tau
fluoro
rti
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KR20160047552A (ko
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루카 고비
헨너 크너스트
마티아스 쾨르너
디터 무리
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에프. 호프만-라 로슈 아게
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • 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
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/28—Neurological disorders
    • G01N2800/2814—Dementia; Cognitive disorders
    • G01N2800/2821—Alzheimer

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (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)
KR1020167008013A 2013-10-08 2014-10-06 타우-펫-리간드로서의 다이아자카르바졸 유도체 Active KR101770531B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13187764 2013-10-08
EP13187764.9 2013-10-08
PCT/EP2014/071283 WO2015052105A1 (en) 2013-10-08 2014-10-06 Diazacarbazole derivatives as tau-pet-ligands

Publications (2)

Publication Number Publication Date
KR20160047552A KR20160047552A (ko) 2016-05-02
KR101770531B1 true KR101770531B1 (ko) 2017-08-22

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KR1020167008013A Active KR101770531B1 (ko) 2013-10-08 2014-10-06 타우-펫-리간드로서의 다이아자카르바졸 유도체

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US (2) US10004817B2 (OSRAM)
EP (1) EP3055308B1 (OSRAM)
JP (1) JP6194416B2 (OSRAM)
KR (1) KR101770531B1 (OSRAM)
CN (1) CN105358558B (OSRAM)
AR (1) AR097931A1 (OSRAM)
AU (1) AU2014333996B2 (OSRAM)
CA (1) CA2917191C (OSRAM)
CL (1) CL2016000728A1 (OSRAM)
CR (1) CR20150663A (OSRAM)
DK (1) DK3055308T3 (OSRAM)
EA (1) EA028483B1 (OSRAM)
ES (1) ES2657121T3 (OSRAM)
HR (1) HRP20180049T1 (OSRAM)
HU (1) HUE035413T2 (OSRAM)
IL (1) IL243249A0 (OSRAM)
LT (1) LT3055308T (OSRAM)
MA (1) MA38935B1 (OSRAM)
MX (1) MX373153B (OSRAM)
MY (1) MY190196A (OSRAM)
NO (1) NO3055308T3 (OSRAM)
PE (1) PE20160159A1 (OSRAM)
PH (1) PH12016500249A1 (OSRAM)
PL (1) PL3055308T3 (OSRAM)
PT (1) PT3055308T (OSRAM)
RS (1) RS56777B1 (OSRAM)
SG (1) SG11201602786UA (OSRAM)
SI (1) SI3055308T1 (OSRAM)
TW (1) TWI513698B (OSRAM)
UA (1) UA116164C2 (OSRAM)
WO (1) WO2015052105A1 (OSRAM)
ZA (1) ZA201509013B (OSRAM)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT2247558T (lt) 2008-02-14 2022-04-11 Eli Lilly And Company Nauji vizualizavimo agentai neurologinės disfunkcijos aptikimui
NO3055308T3 (OSRAM) 2013-10-08 2018-04-21
SI3143011T1 (sl) 2014-05-13 2021-08-31 F. Hoffmann-La Roche Ag Devterirane heterociklične spojine in njihova uporaba kot kontrastna sredstva
CA2973648C (en) 2015-02-02 2023-09-26 Ucb Biopharma Sprl 9h-pyrrolo-dipyridine derivatives
EP3118202A1 (en) 2015-07-15 2017-01-18 AC Immune S.A. Dihydropyridopyrrole derivatives as tau-pet-ligands
EP3322707A1 (en) 2015-07-15 2018-05-23 AC Immune SA Novel imaging compounds
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
IL264239B (en) * 2016-07-22 2022-08-01 Ac Immune Sa Compounds for imaging tau protein aggregates
WO2018024642A1 (en) 2016-08-02 2018-02-08 Ucb Biopharma Sprl 9h-pyrrolo-dipyridine derivatives
WO2018024643A1 (en) 2016-08-02 2018-02-08 Ucb Biopharma Sprl 9h-pyrrolo-dipyridine derivatives
CN109689653B (zh) * 2016-09-09 2022-04-12 豪夫迈·罗氏有限公司 用于制备2-(6-硝基吡啶-3-基)-9H-二吡啶并[2，3-b；3’，4’-d]吡咯的方法
JP7260552B2 (ja) * 2018-01-24 2023-04-18 エーシー・イミューン・エス・アー Ｐｅｔ画像化のための診断用組成物、診断用組成物を製造するための方法及び診断におけるその使用
US20210038747A1 (en) * 2018-01-24 2021-02-11 Ac Immune Sa Novel method of preparing an imaging compound
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

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
US20110182812A1 (en) 2009-03-23 2011-07-28 Siemens Medical Solutions Usa, Inc. Imaging Agents for Detecting Neurological Disorders

Family Cites Families (7)

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Publication number Priority date Publication date Assignee Title
US8932557B2 (en) * 2008-02-14 2015-01-13 Eli Lilly And Company Imaging agents for detecting neurological dysfunction
US20110124654A1 (en) 2008-06-11 2011-05-26 Huifen Chen Diazacarbazoles and methods of use
EP2323697A2 (en) * 2008-07-24 2011-05-25 Siemens Medical Solutions USA, Inc. Imaging agents useful for identifying ad pathology
EP2411057B1 (en) * 2009-03-23 2020-05-06 Eli Lilly and Company Imaging agents for detecting neurological disorders
US20110183938A1 (en) * 2009-12-16 2011-07-28 Genentech, Inc. 1,7-diazacarbazoles and methods of use
US20150368244A1 (en) * 2011-01-31 2015-12-24 Genentech, Inc. Diazacarbazoles and methods of use
NO3055308T3 (OSRAM) * 2013-10-08 2018-04-21

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
US20110182812A1 (en) 2009-03-23 2011-07-28 Siemens Medical Solutions Usa, Inc. Imaging Agents for Detecting Neurological Disorders

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Publication number Publication date
CR20150663A (es) 2016-01-27
CA2917191A1 (en) 2015-04-16
LT3055308T (lt) 2018-02-12
HUE035413T2 (en) 2018-05-02
MA38935A1 (fr) 2016-04-29
CA2917191C (en) 2021-08-10
AU2014333996B2 (en) 2018-03-15
CL2016000728A1 (es) 2016-11-11
PH12016500249B1 (en) 2016-05-16
MY190196A (en) 2022-04-04
EA201690515A1 (ru) 2016-07-29
PT3055308T (pt) 2018-01-18
EP3055308A1 (en) 2016-08-17
TW201520212A (zh) 2015-06-01
AR097931A1 (es) 2016-04-20
MA38935B1 (fr) 2016-12-30
UA116164C2 (uk) 2018-02-12
IL243249A0 (en) 2016-02-29
PH12016500249A1 (en) 2016-05-16
NO3055308T3 (OSRAM) 2018-04-21
NZ714831A (en) 2021-09-24
US11058781B2 (en) 2021-07-13
MX2016002234A (es) 2016-06-06
AU2014333996A1 (en) 2015-12-24
PL3055308T3 (pl) 2018-03-30
US20180326099A1 (en) 2018-11-15
ES2657121T3 (es) 2018-03-01
JP6194416B2 (ja) 2017-09-06
EP3055308B1 (en) 2017-11-22
SG11201602786UA (en) 2016-05-30
SI3055308T1 (en) 2018-03-30
US10004817B2 (en) 2018-06-26
MX373153B (es) 2020-04-21
JP2016534979A (ja) 2016-11-10
KR20160047552A (ko) 2016-05-02
WO2015052105A1 (en) 2015-04-16
RS56777B1 (sr) 2018-04-30
PE20160159A1 (es) 2016-03-18
EA028483B1 (ru) 2017-11-30
US20160220712A1 (en) 2016-08-04
CN105358558B (zh) 2017-09-26
CN105358558A (zh) 2016-02-24
DK3055308T3 (en) 2018-01-22
ZA201509013B (en) 2016-10-26
HK1215574A1 (zh) 2016-09-02
TWI513698B (zh) 2015-12-21
HRP20180049T1 (hr) 2018-02-09

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