CN106661018B - 用作神经原纤维缠结显像剂的吡咯并[2,3-c]吡啶 - Google Patents

用作神经原纤维缠结显像剂的吡咯并[2,3-c]吡啶 Download PDF

Info

Publication number
CN106661018B
CN106661018B CN201580031335.2A CN201580031335A CN106661018B CN 106661018 B CN106661018 B CN 106661018B CN 201580031335 A CN201580031335 A CN 201580031335A CN 106661018 B CN106661018 B CN 106661018B
Authority
CN
China
Prior art keywords
mmol
pyrrolo
pyridin
compound
synthesis
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
CN201580031335.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN106661018A (zh
Inventor
A·M·瓦尔基
E·霍斯泰特勒
T·格雷斯霍克
J·李
K·P·摩尔
I·本纳斯夫
J·马尔赫恩
H·塞尔尼克
Y·王
K·杨
J·付
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.)
Merck Sharp and Dohme BV
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of CN106661018A publication Critical patent/CN106661018A/zh
Application granted granted Critical
Publication of CN106661018B publication Critical patent/CN106661018B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K51/0455Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Hospice & Palliative Care (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
CN201580031335.2A 2014-06-13 2015-06-09 用作神经原纤维缠结显像剂的吡咯并[2,3-c]吡啶 Active CN106661018B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2014/079834 2014-06-13
PCT/CN2014/079834 WO2015188368A1 (en) 2014-06-13 2014-06-13 Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles
PCT/US2015/034794 WO2015191506A2 (en) 2014-06-13 2015-06-09 Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles

Publications (2)

Publication Number Publication Date
CN106661018A CN106661018A (zh) 2017-05-10
CN106661018B true CN106661018B (zh) 2019-07-19

Family

ID=54832744

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580031335.2A Active CN106661018B (zh) 2014-06-13 2015-06-09 用作神经原纤维缠结显像剂的吡咯并[2,3-c]吡啶

Country Status (15)

Country Link
US (2) US9808542B2 (enExample)
EP (1) EP3154970B1 (enExample)
JP (1) JP6513107B2 (enExample)
KR (1) KR102478430B1 (enExample)
CN (1) CN106661018B (enExample)
AU (1) AU2015274843B2 (enExample)
BR (1) BR112016028345B1 (enExample)
CA (1) CA2948528C (enExample)
DK (1) DK3154970T3 (enExample)
ES (1) ES2763095T3 (enExample)
HU (1) HUE048395T2 (enExample)
MX (1) MX375282B (enExample)
PL (1) PL3154970T3 (enExample)
RU (1) RU2695373C2 (enExample)
WO (2) WO2015188368A1 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014097474A1 (ja) 2012-12-21 2014-06-26 独立行政法人放射線医学総合研究所 脳内に蓄積したタウタンパク質をイメージングするための新規化合物
SG11201811311VA (en) 2016-07-22 2019-01-30 Ac Immune Sa Compounds for imaging tau protein aggregates
JP7059270B2 (ja) * 2016-07-22 2022-04-25 エーシー・イミューン・エス・アー タウタンパク質凝集体を画像化するための化合物
CN116473962A (zh) 2017-06-02 2023-07-25 富士胶片富山化学株式会社 脑萎缩预防或治疗剂
JPWO2018221728A1 (ja) 2017-06-02 2020-04-02 富士フイルム富山化学株式会社 アルツハイマー型認知症予防または治療剤
JP7133547B2 (ja) 2017-06-02 2022-09-08 富士フイルム富山化学株式会社 脊髄小脳変性症予防または治療剤
CN110691595A (zh) 2017-06-02 2020-01-14 富士胶片富山化学株式会社 β-淀粉样蛋白量减少剂
JP7370859B2 (ja) * 2017-06-02 2023-10-30 富士フイルム富山化学株式会社 タウオパチー予防または治療剤
WO2019088083A1 (ja) 2017-10-30 2019-05-09 富士フイルム富山化学株式会社 エモパミル結合タンパク質結合剤およびその利用
US11306089B2 (en) 2018-01-24 2022-04-19 Life Molecular Imaging Limited Gamma-carboline compounds for the detection of Tau aggregates
US20210041447A1 (en) 2018-01-24 2021-02-11 Ac Immune Sa Azacarboline compounds for the detection of tau aggregates
WO2019192533A1 (zh) * 2018-04-04 2019-10-10 深圳福沃药业有限公司 用于治疗乳腺癌的雌激素受体降解剂
KR102017324B1 (ko) 2018-04-30 2019-09-02 경북대학교 산학협력단 신규한 asm 활성 직접 억제 화합물 2-아미노-2-(1,2,3-트리아졸-4-일)프로판-1,3-디올 유도체 및 이의 용도
JP7293343B2 (ja) * 2018-05-09 2023-06-19 アプリノイア セラピューティクス リミテッド ヘテロアリール化合物及びその使用
WO2019236884A1 (en) 2018-06-07 2019-12-12 Disarm Therapeutics, Inc. Inhibitors of sarm1
CN108676007B (zh) * 2018-06-22 2020-06-26 厦门大学 放射性核素标记的苯并蝶啶类衍生物及其制备方法和应用
CA3123215C (en) 2018-12-19 2024-04-02 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
WO2021097243A1 (en) 2019-11-13 2021-05-20 Aprinoia Therapeutics Inc. Compounds for degrading tau protein aggregates and uses thereof
US20220008563A1 (en) * 2020-07-10 2022-01-13 The Regents Of The University Of California Radiolabelled and nonradiolabelled pegylated compounds and uses thereof
US12036292B2 (en) * 2020-08-06 2024-07-16 Chdi Foundation, Inc. Heterobiaryl compounds and imaging agents for imaging huntingtin protein
CN112939753B (zh) * 2020-09-15 2022-04-05 浙江大学 一种1-茚酮类化合物的合成方法
KR102240400B1 (ko) 2020-11-19 2021-04-15 한국원자력연구원 베타-아밀로이드 검출용 수용성 화합물
CN112745299B (zh) * 2021-01-07 2022-01-25 温州大学 4-氰基-7,8-二氢异喹啉衍生物及其制备方法和应用
TWI782769B (zh) * 2021-10-28 2022-11-01 行政院原子能委員會核能研究所 一種新穎神經纖維糾結微管相關蛋白質Tau造影化合物、其製備方法及用途
CN114149425A (zh) * 2021-11-16 2022-03-08 上海应用技术大学 5-氟甲基吡啶衍生物和18-f同位素标记的5-氟甲基吡啶衍生物及其制备与应用
CN114276259B (zh) * 2022-01-04 2022-12-06 济川(上海)医学科技有限公司 一种马来酸二甲茚定关键中间体的制备方法
CN115417816B (zh) * 2022-09-05 2024-01-26 江苏南大光电材料股份有限公司 一种3,6-二溴-1-氯-异喹啉的制备方法
WO2025230262A1 (ko) * 2024-04-29 2025-11-06 심플렉스 주식회사 신규한 헤테로아릴 유도체 및 이의 aak1 억제 용도

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013181075A1 (en) * 2012-05-29 2013-12-05 Merck Sharp & Dohme Corp. Isotopically labeled biaryl urea compounds

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5451566A (en) 1993-11-17 1995-09-19 Zeneca Limited Herbicidal pyrrolopyridine compounds
JP5635727B2 (ja) 2004-10-07 2014-12-03 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. チアゾリルmglur5アンタゴニスト及びそれらの使用のための方法
US20080027044A1 (en) 2006-06-13 2008-01-31 Kim Lewis Prodrug antibiotic screens
WO2008103615A1 (en) 2007-02-21 2008-08-28 Kalypsys, Inc. Isoquinolines useful as inducible nitric oxide synthase inhibitors
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
AU2009260526A1 (en) 2008-05-30 2009-12-23 Merck Sharp & Dohme Corp. Novel substituted indoles
WO2010129816A2 (en) 2009-05-07 2010-11-11 Intellikine, Inc. Heterocyclic compounds and uses thereof
GB201004311D0 (en) 2010-03-15 2010-04-28 Proximagen Ltd New enzyme inhibitor compounds
US8901133B2 (en) 2010-11-10 2014-12-02 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AU2012212323A1 (en) 2011-02-01 2013-09-12 The Board Of Trustees Of The University Of Illinois HDAC inhibitors and therapeutic methods using the same
US8684313B2 (en) 2011-02-02 2014-04-01 Ocean Rodeo Sports Inc. Inflatable kite with leading edge swept forwards at wingtip
WO2013040183A1 (en) * 2011-09-16 2013-03-21 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Beta-amyloid imaging agents, methods of manufacture, and methods of use thereof
CN103450152B (zh) * 2012-06-04 2015-11-18 济南海乐医药技术开发有限公司 基于吲唑、吲哚或氮杂吲唑、氮杂吲哚的双芳基脲类结构抗肿瘤药物
GB201304526D0 (en) 2013-03-13 2013-04-24 Proximagen Ltd New compounds
GB201404498D0 (en) * 2014-03-13 2014-04-30 Proximagen Ltd New compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013181075A1 (en) * 2012-05-29 2013-12-05 Merck Sharp & Dohme Corp. Isotopically labeled biaryl urea compounds

Also Published As

Publication number Publication date
DK3154970T3 (da) 2020-01-20
AU2015274843A1 (en) 2016-11-10
RU2016150404A3 (enExample) 2018-11-30
MX2016016384A (es) 2017-05-01
MX375282B (es) 2025-03-06
EP3154970A4 (en) 2017-11-15
US10022461B2 (en) 2018-07-17
AU2015274843B2 (en) 2018-11-22
EP3154970B1 (en) 2019-11-06
PL3154970T3 (pl) 2020-04-30
ES2763095T3 (es) 2020-05-27
CN106661018A (zh) 2017-05-10
US9808542B2 (en) 2017-11-07
RU2016150404A (ru) 2018-07-18
CA2948528C (en) 2022-05-31
US20170119912A1 (en) 2017-05-04
KR102478430B1 (ko) 2022-12-15
WO2015188368A1 (en) 2015-12-17
RU2695373C2 (ru) 2019-07-23
WO2015191506A3 (en) 2016-02-04
US20180071412A1 (en) 2018-03-15
WO2015191506A2 (en) 2015-12-17
BR112016028345B1 (pt) 2022-11-29
JP6513107B2 (ja) 2019-05-15
RU2019115483A (ru) 2019-06-13
BR112016028345A2 (pt) 2017-08-22
CA2948528A1 (en) 2015-12-17
EP3154970A2 (en) 2017-04-19
BR112016028345A8 (pt) 2021-06-29
JP2017521387A (ja) 2017-08-03
HUE048395T2 (hu) 2020-08-28
KR20170016481A (ko) 2017-02-13

Similar Documents

Publication Publication Date Title
CN106661018B (zh) 用作神经原纤维缠结显像剂的吡咯并[2,3-c]吡啶
CN110088099B (zh) 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法
JP2016500073A (ja) 寄生虫病の処置のための化合物および組成物
CN102256493A (zh) 表现出抗癌活性和抗增殖活性的环丙烷酰胺及其类似物
KR20230107800A (ko) Hsd17b13 억제제 및 이의 용도
CN105358558A (zh) 作为tau-pet-配体的二氮杂咔唑衍生物
KR102798858B1 (ko) 추가로 치환된 트리아졸로 퀴녹살린 유도체
KR20180128937A (ko) 질환을 치료하는데 유용한 fimh의 만노스-유래 길항제
JP6392352B2 (ja) リーシュマニア症などの寄生虫病を処置するための原生動物のプロテアソーム阻害剤としての[1,2,4]トリアゾロ[1,5−a]ピリミジン誘導体
CN112292183A (zh) 作为RORγt的调节剂的6-氨基吡啶-3-基吡唑
WO2024240231A1 (zh) Fgfr2/3选择性抑制剂、药物组合物及其应用
TW201605858A (zh) 縮合吡唑衍生物
WO2020135195A1 (zh) 氨基吡啶类化合物及其制备方法和用途
TW202440574A (zh) 作為pkmyt1抑制劑的雜芳基化合物
TW201422610A (zh) 作爲pde10抑制劑之經二級醇取代之三唑
RU2788916C2 (ru) Пирроло[2,3-с]пиридины в качестве визуализирующих агентов для нейрофибриллярных клубков
CN104619694A (zh) 适用作pde10抑制剂的氮杂环丁烷和哌啶化合物
TW202413367A (zh) Tam受體抑制劑
TW202517629A (zh) 蛋白質精胺酸酶甲基轉移酶-5抑制劑及其醫藥用途
HK40113493A (zh) 甲硫氨酸腺苷转移酶2a(mat2a)抑制剂及其用途
HK40117292A (zh) Parp1抑制剂及其用途
HK40114168A (zh) Parp1抑制剂及其用途
WO2025007777A1 (zh) 嘧啶类化合物、其制备方法及其医药用途
HK40046165B (zh) 吡啶基及吡嗪基-(氮杂)吲哚磺酰胺
HK1164060A (en) Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
TR01 Transfer of patent right

Effective date of registration: 20221123

Address after: new jersey

Patentee after: MERCK SHARP & DOHME B.V.

Address before: new jersey

Patentee before: MERCK SHARP & DOHME Corp.

TR01 Transfer of patent right