ES2867814T3 - Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes - Google Patents

Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes Download PDF

Info

Publication number
ES2867814T3
ES2867814T3 ES15725253T ES15725253T ES2867814T3 ES 2867814 T3 ES2867814 T3 ES 2867814T3 ES 15725253 T ES15725253 T ES 15725253T ES 15725253 T ES15725253 T ES 15725253T ES 2867814 T3 ES2867814 T3 ES 2867814T3
Authority
ES
Spain
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
individual
deuterated
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
ES15725253T
Other languages
English (en)
Spanish (es)
Inventor
Jan Marik
Joseph P Lyssikatos
Simon Williams
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche 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
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of ES2867814T3 publication Critical patent/ES2867814T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P25/28—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
    • 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
ES15725253T 2014-05-13 2015-05-12 Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes Active ES2867814T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461992717P 2014-05-13 2014-05-13
PCT/EP2015/060447 WO2015173225A1 (en) 2014-05-13 2015-05-12 Deuterated heterocyclic compounds and their use as imaging agents

Publications (1)

Publication Number Publication Date
ES2867814T3 true ES2867814T3 (es) 2021-10-20

Family

ID=53269446

Family Applications (1)

Application Number Title Priority Date Filing Date
ES15725253T Active ES2867814T3 (es) 2014-05-13 2015-05-12 Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes

Country Status (21)

Country Link
US (4) US10076581B2 (enExample)
EP (2) EP3143011B1 (enExample)
JP (2) JP6529986B2 (enExample)
KR (2) KR102618139B1 (enExample)
CN (2) CN106459059B (enExample)
AU (2) AU2015261008B2 (enExample)
CA (1) CA2948721C (enExample)
DK (1) DK3143011T3 (enExample)
ES (1) ES2867814T3 (enExample)
HR (1) HRP20210641T1 (enExample)
HU (1) HUE053939T2 (enExample)
IL (3) IL280791B2 (enExample)
LT (1) LT3143011T (enExample)
MX (2) MX376163B (enExample)
PL (1) PL3143011T3 (enExample)
PT (1) PT3143011T (enExample)
RS (1) RS61810B1 (enExample)
RU (1) RU2696492C2 (enExample)
SG (2) SG11201609281UA (enExample)
SI (1) SI3143011T1 (enExample)
WO (1) WO2015173225A1 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX376163B (es) 2014-05-13 2025-03-07 Hoffmann La Roche Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes.
EP3487545A1 (en) 2016-07-22 2019-05-29 AC Immune S.A. Compounds for imaging tau protein aggregates
WO2018015549A1 (en) 2016-07-22 2018-01-25 Ac Immune S.A. Compounds for imaging tau protein aggregates
MX2019005007A (es) * 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
AU2018346597B2 (en) 2017-10-06 2023-07-13 Forma Therapeutics, Inc. Inhibiting Ubiquitin Specific Peptidase 30
WO2019145291A1 (en) 2018-01-24 2019-08-01 Ac Immune Sa Gamma-carboline compounds for the detection of tau aggregates
EP3743426A1 (en) 2018-01-24 2020-12-02 AC Immune SA Azacarboline compounds for the detection of tau aggregates
WO2019169111A1 (en) 2018-03-02 2019-09-06 The Trustees Of The University Of Pennsylvania [1,2,4]triazolo[1,5-a]pyrimidine compounds and use in stabilizing microtubules
IL278291B2 (en) 2018-05-17 2023-10-01 Forma Therapeutics Inc Condensed bicyclic compounds are useful as ubiquitin-specific peptidase 30 inhibitors
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
JP7337174B2 (ja) 2018-09-18 2023-09-01 ニカング セラピューティクス, インコーポレイテッド Srcホモロジー-2ホスファターゼ阻害剤としての三置換ヘテロアリール誘導体
EP4218934B1 (en) 2018-10-05 2025-06-18 Forma Therapeutics, Inc. Inhibiting ubiquitin-specific protease 30 (usp30)
LT3860998T (lt) 2018-10-05 2024-06-25 Annapurna Bio Inc. Junginiai ir kompozicijos, skirti gydyti būkles, susijusias su apj receptoriaus aktyvumu
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
JP7119978B2 (ja) * 2018-12-20 2022-08-17 オムロン株式会社 制御装置およびプログラム
CA3138873C (en) * 2019-05-09 2024-01-09 Kyle Bradley Pascual CLAGG Synthesis of labeled imidazo[1,2-a]pyrimidines
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
CN113526526A (zh) * 2021-07-12 2021-10-22 苏州大学 氘代氨制备方法及以其作为氘源参与的氘代反应
WO2023028591A1 (en) 2021-08-27 2023-03-02 Genentech, Inc. Methods of treating tau pathologies
EP4536358A1 (en) 2022-06-13 2025-04-16 Genentech Inc. Methods of delaying or preventing the onset of alzheimer's disease using crenezumab
WO2025155625A1 (en) * 2024-01-16 2025-07-24 Eli Lilly And Company Novel compounds for tau imaging
CN118957609B (zh) * 2024-07-23 2025-09-09 无锡绿能电合科技有限公司 一种氟代芳环的氘代方法

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD76515A (enExample) *
DE76515C (de) F. MORA in Mailand Verfahren zur Herstellung imitirter Ledertapete aus Baumwollstoff
EP1340759A1 (en) 2002-02-28 2003-09-03 Sanofi-Synthelabo 1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-(pyrimidin-4-yl)-imidazo[1,2-a]pyrimidin-5(1H)-one derivatives
US6875784B2 (en) 2002-10-09 2005-04-05 Pharmacia & Upjohn Company Antimibicrobial [3.1.0.] bicyclic oxazolidinone derivatives
PL1999109T3 (pl) * 2006-03-30 2012-05-31 Univ Pennsylvania Pochodne styrylopirydyny i ich zastosowanie do wiązania i obrazowania blaszek amyloidowych
JP5647519B2 (ja) 2007-09-13 2014-12-24 コンサート ファーマシューティカルズ インコーポレイテッド 重水素化カテコールおよびベンゾ[d][1,3]ジオキソールおよびその誘導体の合成
US8932557B2 (en) 2008-02-14 2015-01-13 Eli Lilly And Company Imaging agents for detecting neurological dysfunction
EP2599763A1 (en) 2008-02-14 2013-06-05 Siemens Molecular Imaging, Inc. Novel imaging agents for detecting neurological dysfunction
US20100144657A1 (en) 2008-12-09 2010-06-10 Auspex Pharmaceuticals, Inc. PHENYLPIPERIDINE MODULATORS OF mu-OPIOID RECEPTORS
US8691187B2 (en) 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
CN102438660A (zh) 2009-03-23 2012-05-02 美国西门子医疗解决公司 用于检测神经障碍的显像剂
EP2450332A1 (en) * 2010-10-22 2012-05-09 Bayer Pharma Aktiengesellschaft Compounds for use in Imaging, diagnosing and/or treatment of diseases of the central nervous system (F-D2-Deprenyl)
KR20140003438A (ko) * 2010-11-15 2014-01-09 카톨리에케 유니버시테이트 루벤 항바이러스성 축합 헤테로사이클릭 화합물
JP5976206B2 (ja) * 2012-05-22 2016-08-23 イーライ リリー アンド カンパニー 神経機能障害を検出するための造影剤
AU2014333996B2 (en) * 2013-10-08 2018-03-15 F. Hoffmann-La Roche Ag Diazacarbazole derivatives as tau-pet-ligands
MX376163B (es) 2014-05-13 2025-03-07 Hoffmann La Roche Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes.

Also Published As

Publication number Publication date
BR112016026443A8 (pt) 2021-07-06
CA2948721A1 (en) 2015-11-19
CN110483522A (zh) 2019-11-22
IL248692A0 (en) 2017-01-31
MX2016014615A (es) 2017-03-06
IL280791A (en) 2021-04-29
LT3143011T (lt) 2021-05-10
IL280791B2 (en) 2024-03-01
JP2019147825A (ja) 2019-09-05
PT3143011T (pt) 2021-04-26
US20200297875A1 (en) 2020-09-24
JP2017515856A (ja) 2017-06-15
IL271631A (en) 2020-02-27
KR20170002639A (ko) 2017-01-06
HUE053939T2 (hu) 2021-08-30
MX376163B (es) 2025-03-07
CN106459059B (zh) 2019-09-24
RU2696492C2 (ru) 2019-08-02
SG10201805628TA (en) 2018-08-30
US20230218782A1 (en) 2023-07-13
NZ726208A (en) 2023-11-24
CN110483522B (zh) 2022-05-03
US10076581B2 (en) 2018-09-18
AU2019203369A1 (en) 2019-06-06
US20190201561A1 (en) 2019-07-04
RU2016147742A (ru) 2018-06-18
BR112016026443A2 (pt) 2017-08-15
MX2020010847A (es) 2021-07-16
PL3143011T3 (pl) 2021-07-19
AU2015261008A1 (en) 2016-11-17
MX384604B (es) 2025-03-14
HRP20210641T1 (hr) 2021-05-28
IL280791B1 (en) 2023-11-01
US12214058B2 (en) 2025-02-04
JP6681498B2 (ja) 2020-04-15
EP3143011A1 (en) 2017-03-22
IL248692B (en) 2020-01-30
RS61810B1 (sr) 2021-06-30
AU2019203369B2 (en) 2020-06-04
KR102530129B1 (ko) 2023-05-10
KR102618139B1 (ko) 2023-12-27
SG11201609281UA (en) 2016-12-29
US11504440B2 (en) 2022-11-22
CA2948721C (en) 2023-03-28
RU2016147742A3 (enExample) 2018-10-08
NZ764181A (en) 2023-11-24
JP6529986B2 (ja) 2019-06-12
WO2015173225A1 (en) 2015-11-19
KR20230035445A (ko) 2023-03-13
DK3143011T3 (da) 2021-05-03
EP3901145A1 (en) 2021-10-27
EP3143011B1 (en) 2021-03-03
US10675367B2 (en) 2020-06-09
AU2015261008B2 (en) 2019-02-14
CN106459059A (zh) 2017-02-22
SI3143011T1 (sl) 2021-08-31
US20160250358A1 (en) 2016-09-01
IL271631B (en) 2021-05-31

Similar Documents

Publication Publication Date Title
EP3143011B1 (en) Deuterated heterocyclic compounds and their use as imaging agents
EP3856261A1 (en) Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of psma-expressing cancers
JP2012514007A (ja) トシラート前駆体からの18f−放射性標識スチリルピリジンおよびその安定性医薬組成物の合成
Nguyen et al. IBETA: a new aβ plaque positron emission tomography imaging agent for Alzheimer’s disease
Ahn et al. Preclinical evaluation of [18F] FP-CIT, the radiotracer targeting dopamine transporter for diagnosing Parkinson’s disease: pharmacokinetic and efficacy analysis
ES2864825T3 (es) Derivados de azetidina para la obtención de imágenes Tau
AU2009309339C1 (en) Use of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide as a biomarker of peripheral benzodiazepine receptor levels
JPWO2020045638A1 (ja) 放射性イミダゾチアジアゾール誘導体化合物
RU2791900C1 (ru) Дейтрированные гетероциклические соединения и их применение в качестве средств визуализации
HK40014375B (en) Deuterated heterocyclic compounds and their use as imaging agents
Pang et al. Using 18F-ML-10 PET/CT imaging to detect atherosclerosis lesions and apoptotic processes in mice
Nguyen et al. [124I] BETA, a new beta-amyloid plaque PET imaging agent for Alzheimer's disease
HK40014375A (en) Deuterated heterocyclic compounds and their use as imaging agents
HK1228902B (en) Deuterated heterocyclic compounds and their use as imaging agents
BR112016026443B1 (pt) Compostos heterocíclicos deuterados, seus usos, e composição farmacêutica
HK1228902A1 (en) Deuterated heterocyclic compounds and their use as imaging agents