AR062726A1 - Composiciones que comprenden compuestos marcados con 18f y metodos relacionados - Google Patents

Composiciones que comprenden compuestos marcados con 18f y metodos relacionados

Info

Publication number
AR062726A1
AR062726A1 ARP070103993A ARP070103993A AR062726A1 AR 062726 A1 AR062726 A1 AR 062726A1 AR P070103993 A ARP070103993 A AR P070103993A AR P070103993 A ARP070103993 A AR P070103993A AR 062726 A1 AR062726 A1 AR 062726A1
Authority
AR
Argentina
Prior art keywords
anion
heteroaryl
aryl
alkyl
group
Prior art date
Application number
ARP070103993A
Other languages
English (en)
Inventor
Detief Sulzle
Thomas Brumby
Lutz Lehmann
Timo Stellfeld
Ananth Srinivasan
Simon Ametamey
Original Assignee
Bayer Schering Pharma Ag
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
Priority claimed from EP06090166A external-priority patent/EP1897885A1/en
Priority claimed from EP07090079A external-priority patent/EP1985624A3/en
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR062726A1 publication Critical patent/AR062726A1/es

Links

Classifications

    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/655Somatostatins
    • C07K14/6555Somatostatins at least 1 amino acid in D-form
    • 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
    • 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
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • 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
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/57545Neuropeptide Y

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Genetics & Genomics (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

Uso de tales compuestos como agentes de diagnostico por imágenes. Reivindicacion 1: Un compuesto caracterizado porque es de la formula química general (1) en donde G se selecciona entre el grupo que comprende -Cl, -Br, -I, -NO, -NO2, -NR4COCF3, - NR4SO2CF3, -N(R4)SO2R5, -N(CF3)2, -NHCSNHR4, -N(SO2R5)2 , -N(O)=NCONH2, -NR4CN, -NHCSR5, -N:::C, -N=C(CF3)2, -N=NCF3, -N=NCN, -NR4COR4, -NR4COOR5, -OSO2CF3 -OSO2C6H5, -OCOR5, -ONO2, -OSO2R5, -O-C=CH2, -OCF2CF3, -OCOCF3, -OCN, -OCF3, -C:::N, - C(NO2)3, -COOR4, -CONR4R5, -C(S)NH2, -CH=NOR4, -CH2SO2R4, -COCF3, -CF3, -CF2Cl-CBr3, -CClF2, -CCl3, -CF2CF3, -C:::CR4, -CH=NSO2CF3, -CH2CF3, -COR5, -CH=NOR5, -CH2CONH2, -CSNHR5, -CH=NNHCSNH2, -CH=NNHCONHNH2, -C:::C-CF3, -CF=CFCF3, -CF2-CF2-CF3, - CR4(CN)2, -COCF2CF2CF3, -C(CF3)3, -C(CN)3,CR4=C(CN)2, -1-pirrilo, -C(CN)=C(CN)2, -C-piridilo, -COC6H5, -COOC6H5, -SOCF3, -SO2CF3, -SCF3, -SO2CN, -SCOCF3, -SOR5, -S(OR5), -SC:::CR4, -SO2R5, -SSO2R5, -SR5, -SSR4, -SO2CF2CF3, -SCF2CF3, -S(CF3)=NSO2CF3, -SO2C6H5, -SO2N(R5)2, -SO2C(CF3)3, -SC(CF3)3, -SO(CF3)=NSO2CF3, -S(O)(=NH)CF3, -S(O)(=NH)R5, -S-C=CH2, -SCOR5, -SOC6H5, -P(O)C3F7, -PO(OR5)2, -PO(N(R5)2)2, -P(N(R5)2)2, -P(O)R52, y -PO(OR5)2 u otro grupo aceptor de electrones en donde el sustituyente respectivo puede estar en posicion orto, para o meta con respecto al grupo K, Q es hidrogeno, alquilo inferior ramificado o no ramificado, arilo, heteroarilo, -O-(alquilo C1-4), -CN, - halogeno, -SO2-R4, -NO2 o un arilo condensado o heteroarilo condensado en donde el sustituyente respectivo puede estar en posicion orto, para o meta con respecto al grupo K, en donde R4 es hidrogeno o alquilo inferior ramificado o no ramificado y R5 es alquilo inferior ramificado o no ramificado, L es un enlace, -CO-, SO2, -(CH2)d-CO-, -SO-, -C:::C-CO-, -[CH2]m-E-[CH2]n-CO-, -[CH2]m-E-[CH2]n-SO2, -C(=O)-O-, -NR10-, -O-, -(S)p-, -C(=O)NR12-, -C(=S)NR12-, -C(=S)O-, cicloalquilo C1-6, alquenilo, heterocicloalquilo, arilo sustituido o no sustituido o heteroarilo sustituido o no sustituido, aralquilo, heteroaralquilo, alquiloxi, ariloxi, aralquiloxi, -SO2NR13-, -NR13SO2-, -NR13C (=O)O-, -NR13C(=O)NR12-, -NH-NH- y -NH-O-, en donde d es un entero entre 1 y 6, m y n, en forma independiente, son cualquier entero entre 0 y 5, E es un enlace, -S-, -O- o -NR9-, en donde R9 es H, alquilo C1-10, arilo, heteroarilo o aralquilo, p es cualquier entero entre 1 y 3, R10 y R12, en forma independiente, se seleccionan del grupo que comprende H, alquilo C1-10, arilo, heteroarilo o aralquilo y R13 H, alquilo C1-6, arilo, cicloalquilo, heterocicloalquilo, heteroarilo, aralquilo o heteroaralquilo sustituido o no sustituido, de cadena lineal o ramificada, Y es un enlace o un espaciador, U es un agente direccionador, X es CF3S(O)2O-, C4F9S(O)2O-, anion yoduro, anion bromuro, anion cloruro, anion perclorato (ClO4-), anion fosfato, anion trifluoroacetato (CF3-C(O)O-), o el anion de otra sal de un ácido inorgánico u orgánico, K es N+(R1) (R2) (R3) X- o W, en donde R1, R2 y R3 se seleccionan en forma independiente entre sí entre el grupo que comprende alquilo y aralquilo sustituido o insustituido, W es un isotopo de fluor, y una sal aceptable para uso farmacéutico de un ácido inorgánico u orgánico del mismo, un hidrato, complejo, éster, amida, solvato y prodroga del mismo.
ARP070103993A 2006-09-08 2007-09-10 Composiciones que comprenden compuestos marcados con 18f y metodos relacionados AR062726A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06090166A EP1897885A1 (en) 2006-09-08 2006-09-08 Compounds and methods for F labelled agents
EP07090079A EP1985624A3 (en) 2007-04-23 2007-04-23 Single step method of radiofluorination of biologically active compounds or biomolecules

Publications (1)

Publication Number Publication Date
AR062726A1 true AR062726A1 (es) 2008-11-26

Family

ID=39031005

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070103993A AR062726A1 (es) 2006-09-08 2007-09-10 Composiciones que comprenden compuestos marcados con 18f y metodos relacionados

Country Status (20)

Country Link
US (1) US8557776B2 (es)
EP (5) EP3056509A1 (es)
JP (2) JP5603074B2 (es)
KR (1) KR20090058553A (es)
AR (1) AR062726A1 (es)
AU (1) AU2007294124A1 (es)
BR (1) BRPI0716554A2 (es)
CA (2) CA2662449A1 (es)
CL (1) CL2007002620A1 (es)
CO (1) CO6150196A2 (es)
CR (1) CR10654A (es)
IL (4) IL197363A0 (es)
MA (1) MA30780B1 (es)
MX (1) MX2009002492A (es)
NO (1) NO20091428L (es)
PE (1) PE20080850A1 (es)
RU (1) RU2009112716A (es)
TN (1) TN2009000063A1 (es)
TW (1) TW200829277A (es)
WO (1) WO2008028688A2 (es)

Families Citing this family (14)

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CA2662449A1 (en) 2006-09-08 2008-03-13 Bayer Schering Pharma Aktiengesellschaft Compounds and methods for 18f labeled agents
EP2146753A2 (en) * 2007-03-01 2010-01-27 Bayer Schering Pharma Aktiengesellschaft 18f fluoro-benzoyl labelled biological active compounds as diagnostic imaging agents as well as benzotriazol-1-yloxy-benzoyl , 2,5-dioxo-pyrrolidin-1-yloxy)benzoyl and trimethylammonio-benzoyl precursers thereof
GB201013808D0 (en) 2010-08-18 2010-09-29 Ge Healthcare Ltd Peptide radiotracer compositions
WO2012094334A1 (en) * 2011-01-04 2012-07-12 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services One-step 18f labeling of biological substrates and uses of 18f labeled biological substrates
JP2014526952A (ja) * 2011-06-09 2014-10-09 ジーイー・ヘルスケア・リミテッド 蒸留装置及び方法
CN105308056B (zh) * 2013-03-15 2018-03-20 癌靶技术有限责任公司 18f‑标记的靶向psma的pet成像剂
GB201314936D0 (en) 2013-08-21 2013-10-02 Ge Healthcare Ltd Radiolabelling method
GB201322456D0 (en) 2013-12-18 2014-02-05 Ge Healthcare Ltd Radiotracer compositions and methods
EP3582771A4 (en) * 2017-02-17 2020-12-30 Yale University RADIOACTIVELY LABELED MEDICINAL PRODUCTS AND THE METHOD OF MANUFACTURING AND USING THEREOF
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CA3097568A1 (en) * 2018-04-20 2019-10-24 The General Hospital Corporation Acetylated prodrugs for delivery across the blood-brain barrier
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WO2022246118A2 (en) * 2021-05-20 2022-11-24 The Regents Of The University Of California Pet imaging tracers

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Also Published As

Publication number Publication date
TN2009000063A1 (en) 2010-08-19
EP2455105A3 (en) 2012-09-05
EP2289564A3 (en) 2012-11-14
EP2455105B1 (en) 2016-02-17
US20080292548A1 (en) 2008-11-27
AU2007294124A1 (en) 2008-03-13
EP3056509A1 (en) 2016-08-17
EP2279759A3 (en) 2013-04-17
EP2063918A2 (en) 2009-06-03
EP2279759A2 (en) 2011-02-02
TW200829277A (en) 2008-07-16
IL211033A0 (en) 2011-04-28
JP5722966B2 (ja) 2015-05-27
JP2014028813A (ja) 2014-02-13
NO20091428L (no) 2009-06-03
US8557776B2 (en) 2013-10-15
WO2008028688A2 (en) 2008-03-13
MX2009002492A (es) 2009-08-28
IL211526A0 (en) 2011-05-31
IL211527A0 (en) 2011-05-31
WO2008028688A3 (en) 2008-11-13
BRPI0716554A2 (pt) 2013-09-24
IL197363A0 (en) 2011-08-01
EP2063918B1 (en) 2014-02-26
KR20090058553A (ko) 2009-06-09
CO6150196A2 (es) 2010-04-20
JP2010503618A (ja) 2010-02-04
CL2007002620A1 (es) 2008-05-30
CA2858907A1 (en) 2008-03-13
CR10654A (es) 2009-04-14
EP2455105A2 (en) 2012-05-23
PE20080850A1 (es) 2008-09-02
JP5603074B2 (ja) 2014-10-08
MA30780B1 (fr) 2009-10-01
CA2662449A1 (en) 2008-03-13
RU2009112716A (ru) 2010-10-20
EP2289564A2 (en) 2011-03-02

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