KR101692090B1 - Ｐｂｒ 리간드로서의 트리시클릭 인돌 유도체 - Google Patents

Ｐｂｒ 리간드로서의 트리시클릭 인돌 유도체 Download PDF

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KR101692090B1
KR101692090B1 KR1020117025305A KR20117025305A KR101692090B1 KR 101692090 B1 KR101692090 B1 KR 101692090B1 KR 1020117025305 A KR1020117025305 A KR 1020117025305A KR 20117025305 A KR20117025305 A KR 20117025305A KR 101692090 B1 KR101692090 B1 KR 101692090B1
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vivo imaging
imaging agent
precursor compound
ethyl
formula
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KR20110133492A (ko
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해리 존 와즈워쓰
데니스 오'쉐어
조안나 마리 패쓰모어
윌리엄 존 트리그
아만다 이완
보 샨
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지이 헬쓰케어 리미티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/94—[b, c]- or [b, d]-condensed containing carbocyclic rings other than six-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations 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
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0446—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations 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
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0455—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations 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
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0468—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020117025305A 2009-03-27 2010-03-26 Ｐｂｒ 리간드로서의 트리시클릭 인돌 유도체 Active KR101692090B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US16413109P 2009-03-27 2009-03-27
US61/164,131 2009-03-27
GBGB0905328.1A GB0905328D0 (en) 2009-03-27 2009-03-27 Indole derivatives
GB0905328.1 2009-03-27
PCT/EP2010/053998 WO2010109007A2 (en) 2009-03-27 2010-03-26 Indole derivatives

Publications (2)

Publication Number Publication Date
KR20110133492A KR20110133492A (ko) 2011-12-12
KR101692090B1 true KR101692090B1 (ko) 2017-01-02

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US (2) US8790619B2 (enExample)
EP (1) EP2411362B1 (enExample)
JP (1) JP5651163B2 (enExample)
KR (1) KR101692090B1 (enExample)
CN (1) CN102448933B (enExample)
AU (1) AU2010227527B2 (enExample)
BR (1) BRPI1010261A2 (enExample)
CA (1) CA2756887C (enExample)
ES (1) ES2635310T3 (enExample)
GB (1) GB0905328D0 (enExample)
IL (1) IL215019A0 (enExample)
MX (1) MX2011010154A (enExample)
NZ (1) NZ595227A (enExample)
RU (1) RU2525196C2 (enExample)
SG (1) SG174589A1 (enExample)
WO (1) WO2010109007A2 (enExample)
ZA (1) ZA201106708B (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0905328D0 (en) 2009-03-27 2009-05-13 Ge Healthcare Ltd Indole derivatives
EP2552891B1 (en) * 2010-03-26 2018-08-08 GE Healthcare Limited Tricyclic indole derivatives as pbr ligands
GB201016038D0 (en) * 2010-09-24 2010-11-10 Ge Healthcare Ltd In vivo imaging method
GB201016411D0 (en) * 2010-09-30 2010-11-10 Ge Healthcare Ltd In vivo imaging method for cancer
GB201021263D0 (en) * 2010-12-15 2011-01-26 Ge Healthcare Ltd Solid phase extraction method
EP2694505B1 (en) * 2011-04-05 2022-04-27 Sloan-kettering Institute For Cancer Research Hsp90 inhibitors
EP2718464A1 (en) 2011-06-06 2014-04-16 Imperial Innovations Limited Methods to predict binding affinity of tspo imaging agents to tspo
ES2562656T3 (es) * 2011-09-30 2016-03-07 Ge Healthcare Limited Sistemas de calibración y normalización y métodos para sintetizadores radiofarmacéuticos
WO2014083163A1 (en) 2012-11-30 2014-06-05 Ge Healthcare Limited Zinc halide mediated cyclization process leading to tricyclic indoles
CN111362863A (zh) * 2012-11-30 2020-07-03 通用电气健康护理有限公司 三环吲哚衍生物的结晶方法
GB201312768D0 (en) * 2013-07-17 2013-08-28 Ge Healthcare Ltd Work-up procedure
GB201316766D0 (en) * 2013-09-20 2013-11-06 Ge Healthcare Uk Ltd Macrophage Imaging
GB201316764D0 (en) * 2013-09-20 2013-11-06 Ge Healthcare Ltd Novel compounds
GB201316762D0 (en) * 2013-09-20 2013-11-06 Ge Healthcare Ltd Novel compounds
WO2016087653A1 (en) 2014-12-04 2016-06-09 Ge Healthcare Limited Method of removing acetaldehyde from radioactive pharmaceuticals
CN106748802B (zh) * 2016-12-26 2018-11-13 南京理工大学 一种制备含氟仲胺的方法
CN110997068B (zh) * 2017-05-24 2022-12-06 宾夕法尼亚大学董事会 用于成像和放射疗法的经放射标记的荧光parp抑制剂
US11200669B2 (en) * 2019-11-19 2021-12-14 Uih America, Inc. Systems and methods for determining plasma input function used in positron emission tomography imaging

Citations (2)

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WO2000044751A1 (fr) 1999-01-26 2000-08-03 Sanofi-Synthelabo DERIVES DE 4-OXO-3,5-DIHYDRO-4H-PYRIDAZINO[4,5-b]INDOLE-1-CARBOXAMIDE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
WO2007057705A1 (en) 2005-11-18 2007-05-24 Hammersmith Imanet Limited Tetracyclic indole derivatives as in vivo imaging agents and having peripheralbenzodiazepine receptor affinity (pbr)

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US3939177A (en) * 1972-11-22 1976-02-17 Sterling Drug Inc. 4-Aminomethyl-9-benzyl-1,2,3,4-tetrahydrocarbazoles
US3979391A (en) * 1972-11-22 1976-09-07 Sterling Drug Inc. 1,2,3,4-Tetrahydrocarbazoles
FR2599740B1 (fr) * 1986-06-05 1988-08-12 Rhone Poulenc Sante Derives de benzo(b)thiophene de benzo(b)furannecarboxamides, leurs procedes de preparation et les medicaments les contenant
US5270030A (en) * 1988-12-29 1993-12-14 Bio-Technology General Corp. Fibrin binding domain polypeptide and method of producing
EP1043991A4 (en) 1997-11-14 2005-02-02 Lilly Co Eli TREATMENT OF ALZHEIMER DISEASE
US6281355B1 (en) * 1997-12-03 2001-08-28 Taisho Pharmaceutical Co., Ltd. Nitrogen-containing tetracyclic compounds
JPH11228539A (ja) * 1997-12-03 1999-08-24 Taisho Pharmaceut Co Ltd 含窒素四環性化合物
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GB0115927D0 (en) 2001-06-29 2001-08-22 Nycomed Amersham Plc Solid-phase nucleophilic fluorination
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JP2005527464A (ja) 2001-08-09 2005-09-15 イーライ・リリー・アンド・カンパニー ｓＰＬＡ２インヒビターとしてのシクロヘプタＢインドール誘導体
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WO2000044751A1 (fr) 1999-01-26 2000-08-03 Sanofi-Synthelabo DERIVES DE 4-OXO-3,5-DIHYDRO-4H-PYRIDAZINO[4,5-b]INDOLE-1-CARBOXAMIDE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
WO2007057705A1 (en) 2005-11-18 2007-05-24 Hammersmith Imanet Limited Tetracyclic indole derivatives as in vivo imaging agents and having peripheralbenzodiazepine receptor affinity (pbr)

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AU2010227527A1 (en) 2011-10-13
RU2011138850A (ru) 2013-05-10
US20110070161A1 (en) 2011-03-24
BRPI1010261A2 (pt) 2016-03-22
WO2010109007A3 (en) 2010-11-25
EP2411362A2 (en) 2012-02-01
JP2012521973A (ja) 2012-09-20
ZA201106708B (en) 2013-02-27
JP5651163B2 (ja) 2015-01-07
AU2010227527B2 (en) 2015-03-12
GB0905328D0 (en) 2009-05-13
IL215019A0 (en) 2011-11-30
CN102448933B (zh) 2014-07-02
NZ595227A (en) 2013-11-29
RU2525196C2 (ru) 2014-08-10
US20120020884A1 (en) 2012-01-26
ES2635310T3 (es) 2017-10-03
CN102448933A (zh) 2012-05-09
US8501153B2 (en) 2013-08-06
HK1167393A1 (en) 2012-11-30
EP2411362B1 (en) 2017-05-31
WO2010109007A2 (en) 2010-09-30
US8790619B2 (en) 2014-07-29
SG174589A1 (en) 2011-10-28
CA2756887A1 (en) 2010-09-30
CA2756887C (en) 2018-06-19
KR20110133492A (ko) 2011-12-12
MX2011010154A (es) 2011-10-21

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