CN107406419B - Pet显像剂 - Google Patents

Pet显像剂 Download PDF

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Publication number
CN107406419B
CN107406419B CN201680016753.9A CN201680016753A CN107406419B CN 107406419 B CN107406419 B CN 107406419B CN 201680016753 A CN201680016753 A CN 201680016753A CN 107406419 B CN107406419 B CN 107406419B
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CN
China
Prior art keywords
methyl
pharmaceutically acceptable
acceptable salt
compound
compound according
Prior art date
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Active
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CN201680016753.9A
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English (en)
Chinese (zh)
Other versions
CN107406419A (zh
CN107406419A8 (zh
Inventor
Y·奥贝松
E·布里亚尔
B·奥伯豪泽尔
D·罗格朗
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Novartis AG
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Novartis AG
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Publication of CN107406419A publication Critical patent/CN107406419A/zh
Publication of CN107406419A8 publication Critical patent/CN107406419A8/zh
Application granted granted Critical
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Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61B—DIAGNOSIS; SURGERY; IDENTIFICATION
    • A61B6/00—Apparatus or devices for radiation diagnosis; Apparatus or devices for radiation diagnosis combined with radiation therapy equipment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61B—DIAGNOSIS; SURGERY; IDENTIFICATION
    • A61B8/00—Diagnosis using ultrasonic, sonic or infrasonic waves
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61K51/0459—Heterocyclic 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
    • 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
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medical Informatics (AREA)
  • Engineering & Computer Science (AREA)
  • Radiology & Medical Imaging (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pathology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Surgery (AREA)
  • High Energy & Nuclear Physics (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nuclear Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201680016753.9A 2015-01-20 2016-01-20 Pet显像剂 Active CN107406419B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562105336P 2015-01-20 2015-01-20
US62/105,336 2015-01-20
PCT/IB2016/050276 WO2016116875A1 (en) 2015-01-20 2016-01-20 Pet imaging agents

Publications (3)

Publication Number Publication Date
CN107406419A CN107406419A (zh) 2017-11-28
CN107406419A8 CN107406419A8 (zh) 2018-01-12
CN107406419B true CN107406419B (zh) 2020-09-11

Family

ID=55300733

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680016753.9A Active CN107406419B (zh) 2015-01-20 2016-01-20 Pet显像剂

Country Status (12)

Country Link
US (2) US10450298B2 (cg-RX-API-DMAC10.html)
EP (1) EP3247706B1 (cg-RX-API-DMAC10.html)
JP (2) JP6723264B2 (cg-RX-API-DMAC10.html)
KR (1) KR20170103960A (cg-RX-API-DMAC10.html)
CN (1) CN107406419B (cg-RX-API-DMAC10.html)
AU (1) AU2016209906A1 (cg-RX-API-DMAC10.html)
BR (1) BR112017015455A2 (cg-RX-API-DMAC10.html)
CA (1) CA2974311A1 (cg-RX-API-DMAC10.html)
EA (1) EA201791643A1 (cg-RX-API-DMAC10.html)
ES (1) ES2828715T3 (cg-RX-API-DMAC10.html)
MX (1) MX2017009452A (cg-RX-API-DMAC10.html)
WO (1) WO2016116875A1 (cg-RX-API-DMAC10.html)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20170103960A (ko) 2015-01-20 2017-09-13 노파르티스 아게 Pet 영상화제
TWI809597B (zh) * 2020-12-16 2023-07-21 美商美國禮來大藥廠 預靶向造影劑

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0224917D0 (en) * 2002-10-25 2002-12-04 Novartis Ag Organic compounds
WO2005043300A2 (en) 2003-10-20 2005-05-12 Empirix, Inc. Computer language interpretation and optimization for server testing
EP1740565A2 (en) 2004-04-28 2007-01-10 ICOS Corporation Arylphenylamino-, arylphenylamide-, and arylphenylether-sufide derivatives
WO2005121094A1 (en) 2004-06-09 2005-12-22 Pfizer Limited Piperazine and piperidine derivatives as anti-hiv-agents
CN101429161A (zh) * 2008-12-05 2009-05-13 常熟理工学院 Pet显像剂前体异喹啉甲酰胺衍生物的合成方法
JP5767205B2 (ja) * 2009-04-02 2015-08-19 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Merck Patent Gesellschaft mit beschraenkter Haftung オートタキシン阻害剤としての複素環式化合物
WO2012020567A1 (en) 2010-08-09 2012-02-16 Raqualia Pharma Inc. Acyl piperazine derivatives as ttx-s blockers
EP2606031B1 (en) * 2010-08-20 2017-09-27 Amira Pharmaceuticals, Inc. Autotaxin inhibitors and uses thereof
SI2861566T1 (sl) * 2012-06-13 2017-03-31 F. Hoffmann-La Roche Ag Novi diazaspirocikloalkan in azaspirocikloalkan
EP2935249B1 (en) 2012-12-19 2018-12-12 Novartis AG Autotaxin inhibitors
PT3022202T (pt) * 2013-07-18 2019-09-03 Novartis Ag Inibidores da autotaxina compreendendo um núcleo beteroaromático anel-benzilo-amida-ciclo
KR20170103960A (ko) 2015-01-20 2017-09-13 노파르티스 아게 Pet 영상화제

Also Published As

Publication number Publication date
US10450298B2 (en) 2019-10-22
BR112017015455A2 (pt) 2018-01-23
JP2018511648A (ja) 2018-04-26
EP3247706B1 (en) 2020-07-08
US20200017474A1 (en) 2020-01-16
WO2016116875A1 (en) 2016-07-28
CN107406419A (zh) 2017-11-28
JP2020158532A (ja) 2020-10-01
CA2974311A1 (en) 2016-07-28
MX2017009452A (es) 2017-11-08
AU2016209906A1 (en) 2017-08-03
KR20170103960A (ko) 2017-09-13
JP6723264B2 (ja) 2020-07-15
US20180273509A1 (en) 2018-09-27
US10865195B2 (en) 2020-12-15
EP3247706A1 (en) 2017-11-29
ES2828715T3 (es) 2021-05-27
EA201791643A1 (ru) 2017-11-30
CN107406419A8 (zh) 2018-01-12

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Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
CI02 Correction of invention patent application
CI02 Correction of invention patent application

Correction item: Classification number

Correct: C07D 401/12(2006.01)|C07D 413/12(2006.01)|C07B 59/00(2006.01)|A61K 31/496(2006.01)|A61K 51/04(2006.01)|A61B 6/00(2006.01)|A61B 8/00(2006.01)

False: A99Z 99/00(2006.01)

Number: 48-01

Page: The title page

Volume: 33

SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant