KR102530129B1 - 중수소화된 헤테로사이클릭 화합물 및 이의 조영제로서의 용도 - Google Patents

중수소화된 헤테로사이클릭 화합물 및 이의 조영제로서의 용도 Download PDF

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KR102530129B1
KR102530129B1 KR1020167034871A KR20167034871A KR102530129B1 KR 102530129 B1 KR102530129 B1 KR 102530129B1 KR 1020167034871 A KR1020167034871 A KR 1020167034871A KR 20167034871 A KR20167034871 A KR 20167034871A KR 102530129 B1 KR102530129 B1 KR 102530129B1
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KR20170002639A (ko
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잰 매릭
조셉 피 라이시카토스
시몬 윌리암스
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에프. 호프만-라 로슈 아게
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    • 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
    • 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
    • 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
    • A61P25/28—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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
KR1020167034871A 2014-05-13 2015-05-12 중수소화된 헤테로사이클릭 화합물 및 이의 조영제로서의 용도 Active KR102530129B1 (ko)

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KR1020237006997A KR102618139B1 (ko) 2014-05-13 2015-05-12 중수소화된 헤테로사이클릭 화합물 및 이의 조영제로서의 용도

Applications Claiming Priority (3)

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US201461992717P 2014-05-13 2014-05-13
US61/992,717 2014-05-13
PCT/EP2015/060447 WO2015173225A1 (en) 2014-05-13 2015-05-12 Deuterated heterocyclic compounds and their use as imaging agents

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KR1020237006997A Division KR102618139B1 (ko) 2014-05-13 2015-05-12 중수소화된 헤테로사이클릭 화합물 및 이의 조영제로서의 용도

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KR102530129B1 true KR102530129B1 (ko) 2023-05-10

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KR1020237006997A Active KR102618139B1 (ko) 2014-05-13 2015-05-12 중수소화된 헤테로사이클릭 화합물 및 이의 조영제로서의 용도

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US (4) US10076581B2 (https=)
EP (2) EP3901145A1 (https=)
JP (2) JP6529986B2 (https=)
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US11623927B2 (en) 2018-03-02 2023-04-11 The Trustees Of The University Of Pennsylvania Substituted [1,2,4]triazolo[1,5-a]pyrimidines for stabilizing microtubules
JP7449242B2 (ja) 2018-05-17 2024-03-13 フォーマ セラピューティクス，インコーポレイテッド ユビキチン特異的ペプチダーゼ３０（ｕｓｐ３０）阻害剤として有用な縮合二環化合物
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CR20210175A (es) 2018-09-18 2021-06-01 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2)
JP7530889B2 (ja) 2018-10-05 2024-08-08 フォーマ セラピューティクス，インコーポレイテッド ユビキチン特異的プロテアーゼ３０（ｕｓｐ３０）阻害剤として作用する縮合ピロリン
MX2021003904A (es) 2018-10-05 2021-10-26 Annapurna Bio Inc Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor apj.
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
MX2021013574A (es) * 2019-05-09 2021-12-10 Hoffmann La Roche Sintesis de imidazo[1,2-a]pirimidinas etiquetadas.
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
JP2024534151A (ja) 2021-08-27 2024-09-18 ジェネンテック， インコーポレイテッド タウ病態の治療方法
CN120187452A (zh) 2022-06-13 2025-06-20 基因泰克公司 使用克瑞尼珠单抗延迟或预防阿尔茨海默病的发作的方法
WO2025155625A1 (en) * 2024-01-16 2025-07-24 Eli Lilly And Company Novel compounds for tau imaging
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US20100144657A1 (en) 2008-12-09 2010-06-10 Auspex Pharmaceuticals, Inc. PHENYLPIPERIDINE MODULATORS OF mu-OPIOID RECEPTORS
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US12214058B2 (en) 2025-02-04
RU2016147742A (ru) 2018-06-18
LT3143011T (lt) 2021-05-10
JP6681498B2 (ja) 2020-04-15
AU2015261008B2 (en) 2019-02-14
HUE053939T2 (hu) 2021-08-30
CN106459059B (zh) 2019-09-24
CN110483522B (zh) 2022-05-03
DK3143011T3 (da) 2021-05-03
PT3143011T (pt) 2021-04-26
US20190201561A1 (en) 2019-07-04
SI3143011T1 (sl) 2021-08-31
IL280791B1 (en) 2023-11-01
IL248692B (en) 2020-01-30
CN106459059A (zh) 2017-02-22
MX376163B (es) 2025-03-07
US10076581B2 (en) 2018-09-18
US20160250358A1 (en) 2016-09-01
HRP20210641T1 (hr) 2021-05-28
RU2696492C2 (ru) 2019-08-02
SG10201805628TA (en) 2018-08-30
KR102618139B1 (ko) 2023-12-27
MX2020010847A (es) 2021-07-16
IL271631B (en) 2021-05-31
BR112016026443A2 (pt) 2017-08-15
US10675367B2 (en) 2020-06-09
IL280791B2 (en) 2024-03-01
IL280791A (en) 2021-04-29
CA2948721C (en) 2023-03-28
BR112016026443A8 (pt) 2021-07-06
KR20170002639A (ko) 2017-01-06
SG11201609281UA (en) 2016-12-29
NZ726208A (en) 2023-11-24
EP3143011B1 (en) 2021-03-03
NZ764181A (en) 2023-11-24
WO2015173225A1 (en) 2015-11-19
JP6529986B2 (ja) 2019-06-12
CN110483522A (zh) 2019-11-22
IL271631A (en) 2020-02-27
AU2015261008A1 (en) 2016-11-17
US20200297875A1 (en) 2020-09-24
MX384604B (es) 2025-03-14
AU2019203369B2 (en) 2020-06-04
IL248692A0 (en) 2017-01-31
JP2019147825A (ja) 2019-09-05
MX2016014615A (es) 2017-03-06
EP3143011A1 (en) 2017-03-22
US11504440B2 (en) 2022-11-22
CA2948721A1 (en) 2015-11-19
US20230218782A1 (en) 2023-07-13
JP2017515856A (ja) 2017-06-15
AU2019203369A1 (en) 2019-06-06
EP3901145A1 (en) 2021-10-27
KR20230035445A (ko) 2023-03-13
RS61810B1 (sr) 2021-06-30
ES2867814T3 (es) 2021-10-20
RU2016147742A3 (https=) 2018-10-08
PL3143011T3 (pl) 2021-07-19

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