CO6220852A2 - Marcacion radioactiva por fluoracion de aziridinas - Google Patents

Marcacion radioactiva por fluoracion de aziridinas

Info

Publication number
CO6220852A2
CO6220852A2 CO09071219A CO09071219A CO6220852A2 CO 6220852 A2 CO6220852 A2 CO 6220852A2 CO 09071219 A CO09071219 A CO 09071219A CO 09071219 A CO09071219 A CO 09071219A CO 6220852 A2 CO6220852 A2 CO 6220852A2
Authority
CO
Colombia
Prior art keywords
aryl
sulfonyl
substituted
unsubstituted
phenyl
Prior art date
Application number
CO09071219A
Other languages
English (en)
Inventor
Ananth Srinivasan
Thomas Brumby
Timo Stellfeld
Keith Graham
Ulrike Rohn
Jessica Becaud
Linjing Mu
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 EP07090001A external-priority patent/EP1944288A1/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 CO6220852A2 publication Critical patent/CO6220852A2/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/19Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • 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
    • C07B59/001Acyclic or carbocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D203/00Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D203/04Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D203/06Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D203/08Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D203/00Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D203/04Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D203/06Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D203/22Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • C07D203/24Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • 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
    • 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
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

1.- Un compuesto que comprende un anillo de aziridina apropiadamente activado con fines de marcación, en el cual un radical agente de direccionamiento está unido, ya sea directamente o a través de un conector apropiado, al anillo de aziridina o a un anillo carbocíclico o heterociclico de cinco miembros que está fusionado al anillo de aziridina.2.- El compuesto de acuerdo con la reivindicación 1 que responde a la Fórmula química general Ien el cual R representa Ts, 2,4,6-triisopropil-fenil-sulfonilo, 3,4-dimetoxi-fenil-sulfonilo, fenil-sulfonilo no sustituido, fenil-sulfonilo sustituido con 1 - 5 porciones R2, Ns, Cbz, Bz, Bn, Boc, Fmoc, metoxicarbonilo, etoxi-carbonilo, aliloxicarbonilo, Tr o acilo; en donde R2 representa hidrógeno, alquilo C1-C6 sustituido o no sustituido, lineal o ramificado, ciclo-alquilo, heterocicloalquilo, arilo, heteroarilo, aralquilo o heteroaralquilo, OH, OR3, NH2, NHR3, N(R3)2, SH, SR3, halógeno, NO2, C(=O)R3, C(=O)OR3, C(=O)NHR3 o C(=O)(NR3)2, en donde R3 representa hidrógeno, alquilo C1-C6, arilo, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, aralquilo o heteroaralquilo sustituido o no sustituido, lineal o ramificado;R1 y R4, en forma independiente, se seleccionan entre el grupo que comprende hidrógeno, alquilo C1-C6, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, aralquilo y heteroaralquilo sustituido y no sustituido o lineal o ramificado; L representa un conector adecuado para acoplar con el radical agente de direccionamiento, B representa el radical agente de direccionamiento, 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.
CO09071219A 2007-01-09 2009-07-09 Marcacion radioactiva por fluoracion de aziridinas CO6220852A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07090001A EP1944288A1 (en) 2007-01-09 2007-01-09 Radiolabelling via fluorination of aziridines
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
CO6220852A2 true CO6220852A2 (es) 2010-11-19

Family

ID=38941926

Family Applications (1)

Application Number Title Priority Date Filing Date
CO09071219A CO6220852A2 (es) 2007-01-09 2009-07-09 Marcacion radioactiva por fluoracion de aziridinas

Country Status (24)

Country Link
US (1) US20090022664A1 (es)
EP (1) EP2099747A1 (es)
JP (1) JP2010522140A (es)
KR (1) KR20090096716A (es)
AR (1) AR062856A1 (es)
AU (1) AU2007343454A1 (es)
BR (1) BRPI0720884A2 (es)
CA (1) CA2674408A1 (es)
CL (1) CL2007002673A1 (es)
CO (1) CO6220852A2 (es)
CR (1) CR10917A (es)
DO (1) DOP2009000173A (es)
EC (1) ECSP099505A (es)
MA (1) MA31175B1 (es)
MX (1) MX2009007395A (es)
NO (1) NO20092813L (es)
PA (1) PA8747801A1 (es)
PE (1) PE20081661A1 (es)
RU (1) RU2009130455A (es)
SV (1) SV2009003328A (es)
TN (1) TN2009000233A1 (es)
TW (1) TW200829275A (es)
UY (1) UY30594A1 (es)
WO (1) WO2008083729A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8784774B2 (en) 2011-09-16 2014-07-22 General Electric Company Labeled molecular imaging agents and methods of use
US9468692B2 (en) 2014-01-23 2016-10-18 General Electric Company Labeled molecular imaging agents and methods of use
US9468693B2 (en) 2014-01-23 2016-10-18 General Electric Company Labeled molecular imaging agents and methods of use
NL2014828B1 (en) * 2015-05-20 2017-01-31 Out And Out Chemistry S P R L Method of performing a plurality of synthesis processes of preparing a radiopharmaceutical in series, a device and cassette for performing this method.

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3954994A (en) * 1968-10-03 1976-05-04 Pfizer Inc. Intermediates for preparing hipolipemic agents and method of lowering the blood lipid level in mammals with said agents
JPS5810380B2 (ja) * 1975-01-31 1983-02-25 三共株式会社 ペプチドノ セイホウ
US6015790A (en) * 1997-10-06 2000-01-18 Basf Aktiengesellschaft Methods and compositions for treating rheumatoid arthritis
ATE453627T1 (de) * 1999-07-21 2010-01-15 Univ Pennsylvania Herstellung von verbindungen zur bestimmung der hypoxie
SE9903998D0 (sv) * 1999-11-03 1999-11-03 Astra Ab New compounds
US6894057B2 (en) * 2002-03-08 2005-05-17 Warner-Lambert Company Oxo-azabicyclic compounds
AU2003249532A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 4-hydroxyquinoline derivatives as matrix metalloproteinase inhibitors
GB0222909D0 (en) * 2002-10-03 2002-11-13 Astrazeneca Ab Novel process and intermediates
US6875784B2 (en) * 2002-10-09 2005-04-05 Pharmacia & Upjohn Company Antimibicrobial [3.1.0.] bicyclic oxazolidinone derivatives
CN1212307C (zh) * 2003-07-23 2005-07-27 中国科学院上海有机化学研究所 一种合成β-氟胺化合物的方法
EP1799637A1 (en) * 2004-09-23 2007-06-27 Amgen, Inc Substituted sulfonamidopropionamides and methods of use
JP2008535839A (ja) * 2005-04-07 2008-09-04 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤

Also Published As

Publication number Publication date
PA8747801A1 (es) 2009-08-26
TN2009000233A1 (en) 2010-10-18
NO20092813L (no) 2009-09-22
CA2674408A1 (en) 2008-07-17
WO2008083729A1 (en) 2008-07-17
CR10917A (es) 2009-08-27
EP2099747A1 (en) 2009-09-16
MX2009007395A (es) 2009-07-17
JP2010522140A (ja) 2010-07-01
TW200829275A (en) 2008-07-16
AU2007343454A1 (en) 2008-07-17
DOP2009000173A (es) 2010-10-31
PE20081661A1 (es) 2009-01-18
AR062856A1 (es) 2008-12-10
US20090022664A1 (en) 2009-01-22
KR20090096716A (ko) 2009-09-14
BRPI0720884A2 (pt) 2014-03-25
RU2009130455A (ru) 2011-02-20
MA31175B1 (fr) 2010-02-01
ECSP099505A (es) 2009-08-28
UY30594A1 (es) 2008-09-02
CL2007002673A1 (es) 2008-07-18
SV2009003328A (es) 2009-12-14

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