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AR114029A2 - Compuestos adecuados como precursores de compuestos que son útiles para obtener imágenes de depósitos amiloides, usos y procesos - Google Patents

Compuestos adecuados como precursores de compuestos que son útiles para obtener imágenes de depósitos amiloides, usos y procesos

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Publication number
AR114029A2
AR114029A2 ARP180103297A ARP180103297A AR114029A2 AR 114029 A2 AR114029 A2 AR 114029A2 AR P180103297 A ARP180103297 A AR P180103297A AR P180103297 A ARP180103297 A AR P180103297A AR 114029 A2 AR114029 A2 AR 114029A2
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AR
Argentina
Prior art keywords
compound
useful
amyloid deposits
compounds
processes
Prior art date
Application number
ARP180103297A
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English (en)
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Astrazeneca Ab
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Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR114029A2 publication Critical patent/AR114029A2/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a 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
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/76Nitrogen atoms to which a second hetero atom is attached
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
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    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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    • C07B2200/05Isotopically modified compounds, e.g. labelled
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    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

La presente se refiere a derivados que son adecuados como precursores de compuestos útiles para obtener imágenes de depósitos amiloides en pacientes vivos, a sus composiciones, a métodos de uso y a procesos para preparar dichos compuestos. Los compuestos que derivan de estos precursores son útiles en métodos de imaginología in vivo de depósitos amiloides en el cerebro para permitir el diagnóstico ante mortem de la enfermedad de Alzheimer mediante tomografía por emisión de positrones (PET) así como la medición de la eficacia clínica de agentes terapéuticos para la enfermedad de Alzheimer. Además, la presente también divulga los compuestos precursores en forma cristalina. Reivindicación 1: Un compuesto o una de sus sales, donde el compuesto es el éster terc-butílico del ácido [6-(5-etoximetoxi-benzofuran-2-il)-2-nitro-piridin-3-il]-metil-carbámico. Reivindicación 5: El compuesto o una de sus sales de acuerdo con la reivindicación 1, en una forma cristalina que comprende los picos de difracción siguientes: 11,27; 12,00; 13,51; 15,53; 16,82; 17,91; y 23,72 º2q. Reivindicación 8: El uso de acuerdo con la reivindicación 6 ó 7, donde el compuesto marcado es 2-(6-[¹⁸F]-flúor-5-metilamino-piridin-2-il)-benzofuran-5-ol o una de sus sales.
ARP180103297A 2008-08-29 2018-11-12 Compuestos adecuados como precursores de compuestos que son útiles para obtener imágenes de depósitos amiloides, usos y procesos AR114029A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US9285108P 2008-08-29 2008-08-29

Publications (1)

Publication Number Publication Date
AR114029A2 true AR114029A2 (es) 2020-07-15

Family

ID=41721733

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP090103323A AR073230A1 (es) 2008-08-29 2009-08-28 Derivados del acido benzofuran-piridin carbamico, utiles en la preparacion de compuestos marcados, proceso para prepararlos y proceso para preparar precursores de sintesis.
ARP180103297A AR114029A2 (es) 2008-08-29 2018-11-12 Compuestos adecuados como precursores de compuestos que son útiles para obtener imágenes de depósitos amiloides, usos y procesos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP090103323A AR073230A1 (es) 2008-08-29 2009-08-28 Derivados del acido benzofuran-piridin carbamico, utiles en la preparacion de compuestos marcados, proceso para prepararlos y proceso para preparar precursores de sintesis.

Country Status (22)

Country Link
US (3) US8193363B2 (es)
EP (1) EP2328891B1 (es)
JP (1) JP5613669B2 (es)
KR (1) KR101648848B1 (es)
CN (3) CN104478862B (es)
AR (2) AR073230A1 (es)
AU (1) AU2009286176B2 (es)
BR (1) BRPI0917147B8 (es)
CA (1) CA2735497C (es)
CL (1) CL2011000420A1 (es)
CO (1) CO6341628A2 (es)
EA (1) EA019093B1 (es)
EC (1) ECSP11010850A (es)
ES (1) ES2627769T3 (es)
IL (1) IL211188A0 (es)
MX (1) MX2011001918A (es)
NZ (1) NZ591446A (es)
PE (1) PE20110393A1 (es)
TW (1) TW201014848A (es)
UY (1) UY32076A (es)
WO (1) WO2010024769A1 (es)
ZA (1) ZA201102284B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8193363B2 (en) 2008-08-29 2012-06-05 Astrazeneca Ab Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits
WO2012017891A1 (ja) * 2010-08-06 2012-02-09 国立大学法人京都大学 ピリジルベンゾフラン誘導体
US10098859B2 (en) 2012-09-05 2018-10-16 Amri Ssci, Llc Cocrystals of p-coumaric acid
CA2894994C (en) 2012-12-21 2019-11-12 National Institute Of Radiological Sciences Compounds for imaging tau proteins that accumulate in brain
WO2016029146A1 (en) * 2014-08-22 2016-02-25 University Of Washington Specific inhibitors of methionyl-trna synthetase
MX2018006266A (es) * 2015-11-20 2019-05-06 Navidea Biopharmaceuticals Inc Formulaciones de benzofuranos 2-heteroaril-sustituidos.
US12116364B2 (en) 2018-05-09 2024-10-15 Aprinoia Therapeutics Inc. Heteroaryl compounds and uses thereof
KR20220100921A (ko) 2019-11-13 2022-07-18 아프리노이아 테라퓨틱스 리미티드 타우 단백질 응집체를 분해하기 위한 화합물 및 이의 용도

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GB1041525A (en) 1964-11-11 1966-09-07 Belge Produits Chimiques Sa Benzofuran derivatives and processes for preparing the same
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US8193363B2 (en) * 2008-08-29 2012-06-05 Astrazeneca Ab Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits

Also Published As

Publication number Publication date
CN104447710A (zh) 2015-03-25
CA2735497A1 (en) 2010-03-04
JP5613669B2 (ja) 2014-10-29
EA201100267A1 (ru) 2011-10-31
BRPI0917147B8 (pt) 2021-05-25
ECSP11010850A (es) 2011-03-31
KR20110045023A (ko) 2011-05-03
AU2009286176A1 (en) 2010-03-04
CN104478862B (zh) 2017-05-24
EP2328891A4 (en) 2012-07-04
MX2011001918A (es) 2011-03-24
US8653274B2 (en) 2014-02-18
US20100056796A1 (en) 2010-03-04
BRPI0917147B1 (pt) 2020-09-15
US8193363B2 (en) 2012-06-05
EA019093B1 (ru) 2014-01-30
CO6341628A2 (es) 2011-11-21
CA2735497C (en) 2016-07-19
JP2012501324A (ja) 2012-01-19
ES2627769T3 (es) 2017-07-31
US20140296534A1 (en) 2014-10-02
UY32076A (es) 2010-03-26
AR073230A1 (es) 2010-10-20
WO2010024769A1 (en) 2010-03-04
BRPI0917147A2 (pt) 2015-11-17
CN102197036A (zh) 2011-09-21
CL2011000420A1 (es) 2011-07-15
TW201014848A (en) 2010-04-16
EP2328891B1 (en) 2017-04-05
US9309267B2 (en) 2016-04-12
PE20110393A1 (es) 2011-07-15
EP2328891A1 (en) 2011-06-08
KR101648848B1 (ko) 2016-08-17
CN102197036B (zh) 2014-12-10
ZA201102284B (en) 2012-09-26
NZ591446A (en) 2012-08-31
CN104478862A (zh) 2015-04-01
IL211188A0 (en) 2011-04-28
US20120264943A1 (en) 2012-10-18
AU2009286176B2 (en) 2012-04-26

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