MX2014006209A - Radioligandos marcados con fluor-18 y carbono-11 para la formacion de imagenes por tomografia de emision de positrones para proteina cinasa 2 de repeticion rica en leucina (lrrk2). - Google Patents

Radioligandos marcados con fluor-18 y carbono-11 para la formacion de imagenes por tomografia de emision de positrones para proteina cinasa 2 de repeticion rica en leucina (lrrk2).

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Publication number
MX2014006209A
MX2014006209A MX2014006209A MX2014006209A MX2014006209A MX 2014006209 A MX2014006209 A MX 2014006209A MX 2014006209 A MX2014006209 A MX 2014006209A MX 2014006209 A MX2014006209 A MX 2014006209A MX 2014006209 A MX2014006209 A MX 2014006209A
Authority
MX
Mexico
Prior art keywords
pet
lrrk2
imaging
positron emission
emission tomography
Prior art date
Application number
MX2014006209A
Other languages
English (en)
Other versions
MX353254B (es
Inventor
Bryan K Chan
Anthony Estrada
Zachary Kevin Sweeney
Jan Marik
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 MX2014006209A publication Critical patent/MX2014006209A/es
Publication of MX353254B publication Critical patent/MX353254B/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • 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
    • A61K51/0453Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physics & Mathematics (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Se describe un método para la formación de imágenes por tomografía de emisión de positrones (PET) de LRRK2 en el tejido de un sujeto, el método comprende: administrar un compuesto de fórmula (I), fórmula (II) o fórmula (III), o una sal farmacéuticamente aceptable del mismo al sujeto, en donde el compuesto incluye al menos un marcador de C11 o F18 sobre el mismo; permitir que el compuesto penetre en el tejido del sujeto; y tomar una imagen PET del SNC o tejido cerebral del sujeto.
MX2014006209A 2011-11-30 2012-11-28 Radioligandos marcados con fluor-18 y carbono-11 para la formacion de imagenes por tomografia de emision de positrones para proteina cinasa 2 de repeticion rica en leucina (lrrk2). MX353254B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161565324P 2011-11-30 2011-11-30
US201261720870P 2012-10-31 2012-10-31
PCT/EP2012/073770 WO2013079496A1 (en) 2011-11-30 2012-11-28 Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2

Publications (2)

Publication Number Publication Date
MX2014006209A true MX2014006209A (es) 2014-08-08
MX353254B MX353254B (es) 2018-01-05

Family

ID=47297200

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014006209A MX353254B (es) 2011-11-30 2012-11-28 Radioligandos marcados con fluor-18 y carbono-11 para la formacion de imagenes por tomografia de emision de positrones para proteina cinasa 2 de repeticion rica en leucina (lrrk2).

Country Status (12)

Country Link
US (1) US9139566B2 (es)
EP (1) EP2785381B1 (es)
JP (1) JP6148248B2 (es)
KR (1) KR101996699B1 (es)
CN (1) CN104093426B (es)
BR (1) BR112014012822A8 (es)
CA (1) CA2856002C (es)
ES (1) ES2580406T3 (es)
HK (1) HK1197192A1 (es)
MX (1) MX353254B (es)
RU (1) RU2650641C2 (es)
WO (1) WO2013079496A1 (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103038230B (zh) * 2010-06-04 2016-05-25 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂的氨基嘧啶衍生物
LT3124483T (lt) * 2010-11-10 2019-09-25 Genentech, Inc. Pirazolo aminopirimidino dariniai, kaip lrrk2 moduliatoriai
AR089182A1 (es) * 2011-11-29 2014-08-06 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
BR112014027117B1 (pt) * 2012-05-03 2022-09-06 Genentech, Inc Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composição
WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
EA029774B1 (ru) 2014-01-29 2018-05-31 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Соединения
CA2937430A1 (en) 2014-01-29 2015-08-06 Glaxosmithkline Intellectual Property Development Limited Compounds
US11214565B2 (en) 2015-11-20 2022-01-04 Denali Therapeutics Inc. Compound, compositions, and methods
PE20240221A1 (es) 2016-06-16 2024-02-16 Denali Therapeutics Inc Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos
CN106588884B (zh) * 2016-11-10 2019-04-09 浙江大学 2-多取代芳环-嘧啶类衍生物及制备和医药用途
EP3582771A4 (en) * 2017-02-17 2020-12-30 Yale University RADIOACTIVELY LABELED MEDICINAL PRODUCTS AND THE METHOD OF MANUFACTURING AND USING THEREOF
CN107827870B (zh) * 2017-10-24 2019-11-08 江苏仁明生物科技有限公司 一种正电子药物[18f]fpmmp及其制备方法与中间体
AU2018392599A1 (en) 2017-12-20 2020-07-09 Denali Therapeutics Inc. Process for the preparation of pyrimidinyl-4-aminopyrazole compounds
EP3966207B1 (en) 2019-05-10 2023-11-01 Deciphera Pharmaceuticals, LLC Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof
JP2022531932A (ja) 2019-05-10 2022-07-12 デシフェラ・ファーマシューティカルズ,エルエルシー ヘテロアリールアミノピリミジンアミドオートファジー阻害剤およびその使用方法
MX2021015628A (es) 2019-06-17 2022-04-18 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso.
CN111138439B (zh) * 2020-01-17 2021-06-25 厦门大学 氟代吡咯并嘧啶类化合物及其制备方法和应用
CN111732548B (zh) * 2020-06-11 2022-06-17 浙江大学 N2-氨甲酰芳环-2-氨基嘧啶类衍生物及其医药用途
CN111646978B (zh) * 2020-06-11 2021-12-21 浙江大学 N2-取代烷氧芳环-2-氨基嘧啶类衍生物及应用
WO2022084210A1 (en) 2020-10-20 2022-04-28 F. Hoffmann-La Roche Ag Combination therapy of pd-1 axis binding antagonists and lrrk2 inhitibors
CN115819405A (zh) * 2022-12-20 2023-03-21 沪渝人工智能研究院 嘧啶氨基吡唑衍生物及其作为富亮氨酸重复激酶2抑制剂的应用

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US4448763A (en) * 1980-11-10 1984-05-15 The University Of Kentucky Research Foundation Alteration of gallium biodistribution using indium complexes for enhanced early imaging
WO2007149789A2 (en) * 2006-06-22 2007-12-27 Applera Corporation Conversion of target specific amplification to universal sequencing
US20100322858A1 (en) * 2006-08-23 2010-12-23 Board Of Regents, The University Of Texas System Radiohaloimatinibs and Methods of Their Synthesis and Use in PET Imaging of Cancers
WO2009127642A2 (en) * 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
AR074209A1 (es) * 2008-11-24 2010-12-29 Boehringer Ingelheim Int Derivados de pirimidina utiles para el tratamiento del cancer
ES2512727T3 (es) 2009-09-29 2014-10-24 Glaxo Group Limited Nuevos compuestos
CN103038230B (zh) * 2010-06-04 2016-05-25 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂的氨基嘧啶衍生物
LT3124483T (lt) 2010-11-10 2019-09-25 Genentech, Inc. Pirazolo aminopirimidino dariniai, kaip lrrk2 moduliatoriai

Also Published As

Publication number Publication date
CA2856002C (en) 2020-10-13
ES2580406T3 (es) 2016-08-23
KR20140097470A (ko) 2014-08-06
US20130156700A1 (en) 2013-06-20
JP2015500216A (ja) 2015-01-05
BR112014012822A2 (pt) 2017-06-13
JP6148248B2 (ja) 2017-06-14
RU2650641C2 (ru) 2018-04-16
KR101996699B1 (ko) 2019-07-04
EP2785381B1 (en) 2016-05-18
CN104093426A (zh) 2014-10-08
MX353254B (es) 2018-01-05
BR112014012822A8 (pt) 2017-07-11
CN104093426B (zh) 2019-06-28
CA2856002A1 (en) 2013-06-06
EP2785381A1 (en) 2014-10-08
HK1197192A1 (en) 2015-01-09
RU2014125211A (ru) 2016-01-27
US9139566B2 (en) 2015-09-22
WO2013079496A1 (en) 2013-06-06

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