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MX2016002234A - Derivados de diazacarbazol como ligandos de tau para tomografia por emision de positrones (pet). - Google Patents

Derivados de diazacarbazol como ligandos de tau para tomografia por emision de positrones (pet).

Info

Publication number
MX2016002234A
MX2016002234A MX2016002234A MX2016002234A MX2016002234A MX 2016002234 A MX2016002234 A MX 2016002234A MX 2016002234 A MX2016002234 A MX 2016002234A MX 2016002234 A MX2016002234 A MX 2016002234A MX 2016002234 A MX2016002234 A MX 2016002234A
Authority
MX
Mexico
Prior art keywords
fluoro
aggregates
dipyrido
pyridin
tau
Prior art date
Application number
MX2016002234A
Other languages
English (en)
Other versions
MX373153B (es
Inventor
Dieter Muri
Luca Gobbi
Henner Knust
Matthias Koerner
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2016002234A publication Critical patent/MX2016002234A/es
Publication of MX373153B publication Critical patent/MX373153B/es

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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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10Organic compounds
    • 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
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • 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
    • 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/28Neurological disorders
    • G01N2800/2814Dementia; Cognitive disorders
    • G01N2800/2821Alzheimer

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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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • 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)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pathology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (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)

Abstract

La presente invención se refiere a un compuesto de fórmula general (Ver Fórmula) la que R es hidrógeno o tritio; F es Flúor o 18flúor; o a una sal de adición de ácido farmacéuticamente aceptable. Los compuestos de fórmula I incluyen 2-(6-fluoro-piridin-3-il)-9H-dipirido [2,3-b;3',4'-d]pirrol,3H-2-( 6-fluoro-piridin3-il)-9H-dipirido[2,3-b;3',4'-d]pirrol y [18F]-2-(6-fluoro-piridin-3-il)-9H-dipirido[2,3-b;3',4'-d]pirrol. Los compuestos se pueden usar para la unión y la formación de imágenes de agregados de tau y los agregados de lámina beta relacionados incluyendo entre otros agregados de beta-amiloide o agregados de alfa-sinucleína.
MX2016002234A 2013-10-08 2014-10-06 Derivados de diazacarbazol como ligandos de tau para tomografía por emisión de positrones (pet). MX373153B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13187764 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
MX2016002234A true MX2016002234A (es) 2016-06-06
MX373153B MX373153B (es) 2020-04-21

Family

ID=49301396

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016002234A MX373153B (es) 2013-10-08 2014-10-06 Derivados de diazacarbazol como ligandos de tau para tomografía por emisión de positrones (pet).

Country Status (32)

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

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2247558T (pt) 2008-02-14 2022-03-21 Lilly Co Eli Novos agentes de imagiologia para deteção de disfunção neurológica
RS56777B1 (sr) 2013-10-08 2018-04-30 Hoffmann La Roche Derivati diazakarbazola kao tau-pet-ligandi
KR102618139B1 (ko) 2014-05-13 2023-12-27 에프. 호프만-라 로슈 아게 중수소화된 헤테로사이클릭 화합물 및 이의 조영제로서의 용도
CN107207508B (zh) * 2015-02-02 2020-02-28 Ucb生物制药私人有限公司 9h-吡咯并-二吡啶衍生物
EP3118202A1 (en) 2015-07-15 2017-01-18 AC Immune S.A. Dihydropyridopyrrole derivatives as tau-pet-ligands
WO2017009454A1 (en) 2015-07-15 2017-01-19 Ac Immune S.A. Novel imaging compounds
JP7197476B2 (ja) * 2016-07-22 2022-12-27 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
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
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
HRP20210145T1 (hr) * 2016-09-09 2021-03-05 F. Hoffmann - La Roche Ag Postupak za dobivanje 2-(6-nitropiridin-3-il)-9h-dipirido[2,3-b;3',4'-d]pirola
WO2019145292A1 (en) 2018-01-24 2019-08-01 Ac Immune Sa Azacarboline compounds for the detection of tau aggregates
IL275995B2 (en) * 2018-01-24 2023-09-01 Ac Immune Sa A new method for the preparation of imaging compound
KR102789462B1 (ko) * 2018-01-24 2025-04-03 에이씨 이뮨 에스에이 Pet 이미징을 위한 진단 조성물, 진단 조성물의 제조 방법 및 진단에서의 그 용도
EP3743423A1 (en) 2018-01-24 2020-12-02 AC Immune SA Gamma-carboline compounds for the detection of tau aggregates

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2247558T (pt) * 2008-02-14 2022-03-21 Lilly Co Eli Novos agentes de imagiologia para deteção de disfunção neurológica
US8932557B2 (en) * 2008-02-14 2015-01-13 Eli Lilly And Company Imaging agents for detecting neurological dysfunction
KR101764556B1 (ko) 2008-06-11 2017-08-02 제넨테크, 인크. 디아자카르바졸 및 사용 방법
WO2010011964A2 (en) 2008-07-24 2010-01-28 Siemens Medical Solutions Usa, Inc. Imaging agents useful for identifying ad pathology
CA2756137C (en) 2009-03-23 2015-11-24 Siemens Medical Solutions Usa, Inc. Imaging agents for detecting neurological disorders
US8691187B2 (en) * 2009-03-23 2014-04-08 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
RS56777B1 (sr) * 2013-10-08 2018-04-30 Hoffmann La Roche Derivati diazakarbazola kao tau-pet-ligandi

Also Published As

Publication number Publication date
AU2014333996B2 (en) 2018-03-15
PH12016500249B1 (en) 2016-05-16
TWI513698B (zh) 2015-12-21
MA38935A1 (fr) 2016-04-29
HK1215574A1 (zh) 2016-09-02
PT3055308T (pt) 2018-01-18
HUE035413T2 (en) 2018-05-02
SG11201602786UA (en) 2016-05-30
IL243249A0 (en) 2016-02-29
WO2015052105A1 (en) 2015-04-16
HRP20180049T1 (hr) 2018-02-09
JP2016534979A (ja) 2016-11-10
CN105358558B (zh) 2017-09-26
EP3055308A1 (en) 2016-08-17
ZA201509013B (en) 2016-10-26
SI3055308T1 (en) 2018-03-30
LT3055308T (lt) 2018-02-12
AR097931A1 (es) 2016-04-20
UA116164C2 (uk) 2018-02-12
US11058781B2 (en) 2021-07-13
KR101770531B1 (ko) 2017-08-22
US10004817B2 (en) 2018-06-26
NO3055308T3 (es) 2018-04-21
PE20160159A1 (es) 2016-03-18
US20180326099A1 (en) 2018-11-15
PL3055308T3 (pl) 2018-03-30
AU2014333996A1 (en) 2015-12-24
JP6194416B2 (ja) 2017-09-06
EA028483B1 (ru) 2017-11-30
DK3055308T3 (en) 2018-01-22
CL2016000728A1 (es) 2016-11-11
RS56777B1 (sr) 2018-04-30
PH12016500249A1 (en) 2016-05-16
MX373153B (es) 2020-04-21
CN105358558A (zh) 2016-02-24
MA38935B1 (fr) 2016-12-30
CR20150663A (es) 2016-01-27
EP3055308B1 (en) 2017-11-22
EA201690515A1 (ru) 2016-07-29
CA2917191A1 (en) 2015-04-16
KR20160047552A (ko) 2016-05-02
TW201520212A (zh) 2015-06-01
CA2917191C (en) 2021-08-10
NZ714831A (en) 2021-09-24
MY190196A (en) 2022-04-04
US20160220712A1 (en) 2016-08-04
ES2657121T3 (es) 2018-03-01

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