CN104379585B - 18f-标记的叶酸/抗叶酸剂类似物 - Google Patents

18f-标记的叶酸/抗叶酸剂类似物 Download PDF

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Publication number
CN104379585B
CN104379585B CN201380024067.2A CN201380024067A CN104379585B CN 104379585 B CN104379585 B CN 104379585B CN 201380024067 A CN201380024067 A CN 201380024067A CN 104379585 B CN104379585 B CN 104379585B
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independently
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folate
diagnostic imaging
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CN104379585A (zh
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R·施布利
R·莫泽
C·M·穆勒
S·M·艾梅塔美
T·贝特泽尔
V·格罗恩
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Merck et Cie
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/02Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/06Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G01N33/60Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances involving radioactive labelled substances
    • 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201380024067.2A 2012-05-08 2013-05-08 18f-标记的叶酸/抗叶酸剂类似物 Active CN104379585B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12167126 2012-05-08
EP12167126.7 2012-05-08
PCT/EP2013/059584 WO2013167653A1 (en) 2012-05-08 2013-05-08 18f-labelled folate/antifolate analogues

Publications (2)

Publication Number Publication Date
CN104379585A CN104379585A (zh) 2015-02-25
CN104379585B true CN104379585B (zh) 2018-07-06

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US (1) US10357576B2 (https=)
EP (1) EP2864329B1 (https=)
JP (1) JP6198814B2 (https=)
KR (1) KR102116000B1 (https=)
CN (1) CN104379585B (https=)
AU (1) AU2013258027B2 (https=)
CA (1) CA2870124C (https=)
DK (1) DK2864329T3 (https=)
EA (1) EA201401225A1 (https=)
ES (1) ES2703627T3 (https=)
IL (1) IL235476B (https=)
PL (1) PL2864329T3 (https=)
PT (1) PT2864329T (https=)
SG (1) SG11201406481TA (https=)
TR (1) TR201819802T4 (https=)
WO (1) WO2013167653A1 (https=)
ZA (1) ZA201407266B (https=)

Families Citing this family (12)

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Publication number Priority date Publication date Assignee Title
KR101646577B1 (ko) * 2014-08-14 2016-08-09 원광대학교산학협력단 엽산수용체 표적용 화합물 또는 이의 약학적으로 허용가능한 염과, 이를 유효성분으로 포함하는 암 예방, 진단 또는 치료용 조성물
JP7204662B2 (ja) * 2017-03-20 2023-01-16 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 異性体的に純粋な18f-標識されたテトラヒドロ葉酸
EP3671511B1 (en) 2018-12-19 2022-07-06 Rohde & Schwarz GmbH & Co. KG Communication system and method
DE102019110904B4 (de) * 2019-04-26 2022-01-20 Helmholtz-Zentrum Dresden - Rossendorf E. V. N-(4-methoxy-7-morpholinobenzo[d]thiazol-2-yl)-acetamid-Derivate und deren Verwendung
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
SMT202500271T1 (it) 2020-07-02 2025-09-12 Incyte Corp Composti di urea triciclici come inibitori di v617f di jak2
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
CN119173514A (zh) 2022-03-17 2024-12-20 因赛特公司 作为jak2 v617f抑制剂的三环脲化合物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101646670A (zh) * 2007-04-11 2010-02-10 默克阿泼洛发股份公司 18f-标记的叶酸酯

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2007128036A (ru) 2004-12-23 2009-01-27 Пердью Рисерч Фаундейшн (Us) Способ получения изображения позитронно-эмиссионной томографией
JP4503039B2 (ja) 2006-04-27 2010-07-14 三洋電機株式会社 回路装置
US8586595B2 (en) 2007-02-07 2013-11-19 Purdue Research Foundation Positron emission tomography imaging method
WO2008125615A1 (en) 2007-04-11 2008-10-23 Merck Eprova Ag 18 f-labelled folates
CA2670363C (en) 2007-04-11 2015-07-21 Merck Eprova Ag 18f-labelled folates
US20100143249A1 (en) 2007-04-11 2010-06-10 Merck Eprova Ag Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy
SG195545A1 (en) 2008-10-10 2013-12-30 Merck & Cie 18f-labelled folates as pet radiotracers

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101646670A (zh) * 2007-04-11 2010-02-10 默克阿泼洛发股份公司 18f-标记的叶酸酯

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
Folic Acid Analogs. Modifications in the Benzene-Ring Region. 1. 2’-and 3’-Azafolic Acids;Eugene C. Roberts, et al.;《Journal of Medicinal Chemistry》;19711231;第14卷(第2期);第125-130页 *
Folic Acid Analogs. Modifications in the Benzene-Ring Region. 2. Thiazole Analogs;Eugene C. Roberts, et al.;《Journal of Medicinal Chemistry》;19721231;第15卷(第12期);第1310-1312页 *
Folic Acid Analogs. Modifications in the Benzene-Ring Region. 5. 2’, 6’-Diazafolic Acid (1,2);Eugene C. Roberts, et al.;《Journal of Heterocyclic Chemistry》;19740831;第11卷;第547-550页 *
Synthesis of N-([2-([(2-Amino-3,4-dihydro-4-oxo-6-pteridinyl) methyl]amino)-5-pyrazinyl]carbonyl)-L-glutamic Acid (2’,5’-Diazafolic Acid);Yu-uji Nakahara, et al.;《Journal of Heterocyclic Chemistry》;19751031;第12卷;第1073-1074页 *
THE SYNTHESIS AND BIOLOGICAL ACTIVITY OF A SERIES OF 2,4-DIAMINOPYRIDO[2,3-D] PYRIMIDINE BASED ANTIFOLATES AS ANTINEOPLASTIC AND ANTIARTHRITIC AGENTS;Lynn S. Gossett, et al.;《Bioorganic & Medicinal Chemistry Letters》;19991231;第9卷;第75-78,页 *

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Publication number Publication date
DK2864329T3 (en) 2019-01-21
ES2703627T3 (es) 2019-03-11
US10357576B2 (en) 2019-07-23
KR20150010970A (ko) 2015-01-29
EP2864329B1 (en) 2018-09-26
US20150125390A1 (en) 2015-05-07
SG11201406481TA (en) 2014-11-27
CA2870124A1 (en) 2013-11-14
EP2864329A1 (en) 2015-04-29
TR201819802T4 (tr) 2019-01-21
CA2870124C (en) 2021-02-16
AU2013258027A1 (en) 2014-11-13
IL235476A0 (en) 2014-12-31
CN104379585A (zh) 2015-02-25
HK1202548A1 (en) 2015-10-02
IL235476B (en) 2019-09-26
JP2015516405A (ja) 2015-06-11
JP6198814B2 (ja) 2017-09-20
ZA201407266B (en) 2016-09-28
PL2864329T3 (pl) 2019-03-29
WO2013167653A1 (en) 2013-11-14
PT2864329T (pt) 2019-01-10
KR102116000B1 (ko) 2020-05-29
AU2013258027B2 (en) 2017-11-30
EA201401225A1 (ru) 2015-04-30

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