JP6533799B2 - 放射標識された化合物 - Google Patents

放射標識された化合物 Download PDF

Info

Publication number
JP6533799B2
JP6533799B2 JP2016571359A JP2016571359A JP6533799B2 JP 6533799 B2 JP6533799 B2 JP 6533799B2 JP 2016571359 A JP2016571359 A JP 2016571359A JP 2016571359 A JP2016571359 A JP 2016571359A JP 6533799 B2 JP6533799 B2 JP 6533799B2
Authority
JP
Japan
Prior art keywords
group
substituted
compound
mixture
salt
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2016571359A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017520540A (ja
JP2017520540A5 (enExample
Inventor
小池　竜樹
竜樹 小池
周平 池田
周平 池田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Takeda Pharmaceutical Co Ltd
Original Assignee
Takeda Pharmaceutical Co Ltd
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
Application filed by Takeda Pharmaceutical Co Ltd filed Critical Takeda Pharmaceutical Co Ltd
Publication of JP2017520540A publication Critical patent/JP2017520540A/ja
Publication of JP2017520540A5 publication Critical patent/JP2017520540A5/ja
Application granted granted Critical
Publication of JP6533799B2 publication Critical patent/JP6533799B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • 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
    • A61K51/0459—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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)
  • Nuclear Medicine (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016571359A 2014-06-09 2015-06-08 放射標識された化合物 Active JP6533799B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462009526P 2014-06-09 2014-06-09
US62/009,526 2014-06-09
PCT/JP2015/067100 WO2015190613A1 (en) 2014-06-09 2015-06-08 Radiolabeled compounds

Publications (3)

Publication Number Publication Date
JP2017520540A JP2017520540A (ja) 2017-07-27
JP2017520540A5 JP2017520540A5 (enExample) 2018-06-21
JP6533799B2 true JP6533799B2 (ja) 2019-06-19

Family

ID=53610936

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016571359A Active JP6533799B2 (ja) 2014-06-09 2015-06-08 放射標識された化合物

Country Status (6)

Country Link
US (1) US9963443B2 (enExample)
EP (1) EP3152198B1 (enExample)
JP (1) JP6533799B2 (enExample)
CN (1) CN106573916A (enExample)
CA (1) CA2951521A1 (enExample)
WO (1) WO2015190613A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA029056B1 (ru) * 2012-12-11 2018-02-28 Такеда Фармасьютикал Компани Лимитед Гетероциклическое соединение
WO2016086036A2 (en) 2014-11-25 2016-06-02 Bristol-Myers Squibb Company Methods and compositions for 18f-radiolabeling of biologics
JP6622814B2 (ja) 2014-11-25 2019-12-18 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ イメージングのための新規ｐｄ−ｌ１結合ポリペプチド
CN109562195A (zh) 2016-06-01 2019-04-02 百时美施贵宝公司 用pd-l1结合多肽进行pet成像
WO2017210335A1 (en) 2016-06-01 2017-12-07 Bristol-Myers Squibb Company Imaging methods using 18f-radiolabeled biologics
WO2020027344A1 (en) * 2018-08-03 2020-02-06 Takeda Pharmaceutical Company Limited Ch24h inhibitors for mdd use
JP7443255B2 (ja) * 2018-09-20 2024-03-05 武田薬品工業株式会社 疼痛使用のためのｃｈ２４ｈ阻害剤
CN111436396A (zh) * 2020-04-24 2020-07-24 军事科学院军事医学研究院环境医学与作业医学研究所 大鼠恐惧应激与气态污染物复合暴露模型的建立方法
CA3264698A1 (en) * 2022-08-12 2024-02-15 Emory University N-CYCLOPROPYL-1-(4-(4-(FLUORO-18F)PHENYL)PYRIMIDIN-5-YL)-N-METHYLPIPERIDINE-4-CARBOXAMIDE AND USES IN PET IMAGING
CN117756779A (zh) * 2023-09-05 2024-03-26 宁波职业技术学院 一种1-(吡啶-3-基)哌啶-4-羧酸的合成方法

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2214247C (en) 1995-03-14 2004-02-10 Praecis Pharmaceuticals Incorporated Modulators of amyloid aggregation
EP1586584A1 (en) 1996-08-27 2005-10-19 Praecis Pharmaceuticals Incorporated Modulators of beta-amyloid peptide aggregation comprising D-amino acids
EP1194449B1 (en) 1999-06-28 2010-09-22 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
AR035016A1 (es) 1999-08-25 2004-04-14 Takeda Chemical Industries Ltd Composicion de azol promotor de produccion/secrecion de neurotrofina, compuesto prodroga del mismo, composicion farmaceutica que lo comprende y uso del mismo para preparar esta ultima.
EP1283199A4 (en) 2000-05-16 2003-12-17 Takeda Chemical Industries Ltd MELANINE CONCENTRATING HORMONE ANTAGONISTS
AU2004218260A1 (en) * 2003-01-28 2004-09-16 Aventis Pharma S.A. N-aryl heteroaromatic products, compositions containing same and use thereof
US7807671B2 (en) * 2006-04-25 2010-10-05 Bristol-Myers Squibb Company Diketo-piperazine and piperidine derivatives as antiviral agents
WO2007139946A2 (en) * 2006-05-25 2007-12-06 University Of Tennessee Research Foundation Gpcr ligands identified by computational modeling
GB0903493D0 (en) * 2009-02-27 2009-04-08 Vantia Ltd New compounds
WO2010110400A1 (ja) 2009-03-26 2010-09-30 武田薬品工業株式会社 複素環化合物
CA2846122C (en) * 2011-08-22 2019-06-11 Takeda Pharmaceutical Company Limited Radiolabeled compounds and their use as radiotracers for quantitative imaging of phosphodiesterase (pde10a) in mammals
US8648079B2 (en) 2011-10-07 2014-02-11 Takeda Pharmaceutical Company Limited Heterocyclic compounds
WO2013090497A1 (en) * 2011-12-15 2013-06-20 Ge Healthcare Limited Heterocyclic compounds as imaging probes of tau pathology
WO2014061676A1 (ja) 2012-10-16 2014-04-24 武田薬品工業株式会社 複素環化合物
EA029056B1 (ru) * 2012-12-11 2018-02-28 Такеда Фармасьютикал Компани Лимитед Гетероциклическое соединение
US9624184B2 (en) 2013-04-04 2017-04-18 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2014163161A1 (ja) 2013-04-04 2014-10-09 武田薬品工業株式会社 複素環化合物
CR20160268A (es) * 2013-12-20 2016-08-16 Gilead Sciences Inc Inhibidores de la quinasa reguladora de la señal de apoptosis
US9624170B2 (en) * 2013-12-26 2017-04-18 Takeda Pharmaceutical Company Limited 4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

Also Published As

Publication number Publication date
EP3152198A1 (en) 2017-04-12
JP2017520540A (ja) 2017-07-27
US9963443B2 (en) 2018-05-08
WO2015190613A1 (en) 2015-12-17
US20170114042A1 (en) 2017-04-27
CN106573916A (zh) 2017-04-19
EP3152198B1 (en) 2019-02-27
CA2951521A1 (en) 2015-12-17

Similar Documents

Publication Publication Date Title
US9963443B2 (en) Radiolabeled compounds
EP3436444B1 (en) Heterocyclic compound
TWI888599B (zh) 取代哌啶化合物及其用途
DK2634177T3 (en) TAU IMAGE SOUND
JP6458054B2 (ja) 複素環化合物
US10968178B2 (en) IP6K inhibitors
ES2848999T3 (es) Compuestos heteroarilo para el tratamiento de enfermedades oftálmicas
EP4153583B1 (en) 1-((1h-pyrazol-4-yl)methyl)-3-(phenyl)-1,3-dihydro-2h-imidazol-2-one derivatives and related compounds as gpr139 antagonists for the treatment of depression
JP6450755B2 (ja) 複素環化合物
US20220089525A1 (en) Heterocyclic compound and use thereof
CN103889974B (zh) 放射性标记的化合物和它们在哺乳动物中作为磷酸二酯酶(pde10a)的定量成像的放射示踪剂的用途
JP2021183587A (ja) 複素環化合物
JP7591592B2 (ja) 置換ピペリジン化合物を含有する医薬
HK1261846A1 (en) Heterocyclic compound
HK1261846B (en) Heterocyclic compound
HK1188997B (en) Tau imaging probe

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180508

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180508

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190507

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190515

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20190521

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190527

R150 Certificate of patent or registration of utility model

Ref document number: 6533799

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250