[go: up one dir, main page]

MX2016016384A - Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares. - Google Patents

Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares.

Info

Publication number
MX2016016384A
MX2016016384A MX2016016384A MX2016016384A MX2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A MX 2016016384 A MX2016016384 A MX 2016016384A
Authority
MX
Mexico
Prior art keywords
aggregates
tau
alzheimer
relates
agents
Prior art date
Application number
MX2016016384A
Other languages
English (en)
Other versions
MX375282B (es
Inventor
James Mulhearn
Yaode Wang
M Walji Abbas
Hostetler Eric
GRESHOCK Thomas
Li Jing
P Moore Keith
Bennacef Idriss
Selnick Harold
Yang Kun
Fu Jianmin
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of MX2016016384A publication Critical patent/MX2016016384A/es
Publication of MX375282B publication Critical patent/MX375282B/es

Links

Classifications

    • 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
    • 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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Psychiatry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)

Abstract

La presente invención se refiere a compuestos de pirrolopiridina de fórmula (I) (ver Fórmula) o sus sales farmacéuticamente aceptables, que pueden ser adecuadas para la obtención de imágenes de agregados de tau, agregados de hojas b, agregados de beta-amiloide o agregados de alfa-sinucleína y, por tanto, son útiles en la unión y formación de imágenes de agregados de tau en pacientes de Alzheimer; más específicamente, esta invención se refiere a un método de utilización de los compuestos de esta invención como trazadores en las imágenes de tomografía por emisión de positrones (PET) para estudiar los depósitos de tau en el cerebro in vivo para permitir el diagnóstico de la enfermedad de Alzheimer y otras enfermedades neurodegenerativas caracterizadas por patología tau; la invención se refiere además a un método para medir la eficacia clínica de agentes terapéuticos para la enfermedad de Alzheimer y otras enfermedades neurodegenerativas caracterizadas por patología tau.
MX2016016384A 2014-06-13 2015-06-09 Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares. MX375282B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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
MX2016016384A true MX2016016384A (es) 2017-05-01
MX375282B MX375282B (es) 2025-03-06

Family

ID=54832744

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016016384A MX375282B (es) 2014-06-13 2015-06-09 Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares.

Country Status (15)

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

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2894994C (en) 2012-12-21 2019-11-12 National Institute Of Radiological Sciences Compounds for imaging tau proteins that accumulate in brain
JP7197476B2 (ja) 2016-07-22 2022-12-27 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
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
EP3636262A4 (en) 2017-06-02 2020-06-10 FUJIFILM Toyama Chemical Co., Ltd. AGENT FOR PREVENTING OR TREATING ALZHEIMER-LIKE DEMENTIA
US11951092B2 (en) 2017-06-02 2024-04-09 Fujifilm Toyama Chemical Co., Ltd. Agent for preventing or treating brain atrophy
US20200155505A1 (en) * 2017-06-02 2020-05-21 Fujifilm Toyama Chemical Co., Ltd. Agent for preventing or treating tauopathy
AU2018277983B2 (en) 2017-06-02 2021-04-08 Fujifilm Toyama Chemical Co., Ltd. Amyloid-β protein level decreasing agent
BR112019024881A2 (pt) 2017-06-02 2020-06-16 Fujifilm Toyama Chemical Co., Ltd. Agente para evitar ou tratar ataxia espinocerebelar
EP3705121B1 (en) 2017-10-30 2023-08-30 FUJIFILM Toyama Chemical Co., Ltd. Emopamil binding protein binding agent and use thereof
EP3743423A1 (en) 2018-01-24 2020-12-02 AC Immune SA Gamma-carboline compounds for the detection of tau aggregates
WO2019145292A1 (en) 2018-01-24 2019-08-01 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
US12116364B2 (en) * 2018-05-09 2024-10-15 Aprinoia Therapeutics Inc. Heteroaryl compounds and uses thereof
CN112839648B (zh) 2018-06-07 2025-04-04 达萨玛治疗公司 Sarm1抑制剂
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
EP3897670A4 (en) 2018-12-19 2022-09-07 Disarm Therapeutics, Inc. MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS
KR20220100921A (ko) 2019-11-13 2022-07-18 아프리노이아 테라퓨틱스 리미티드 타우 단백질 응집체를 분해하기 위한 화합물 및 이의 용도
US20220008563A1 (en) * 2020-07-10 2022-01-13 The Regents Of The University Of California Radiolabelled and nonradiolabelled pegylated compounds and uses thereof
WO2022031946A1 (en) * 2020-08-06 2022-02-10 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

Family Cites Families (16)

* 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
CA2583572C (en) * 2004-10-07 2016-07-12 Merck & Co., Inc. Thiazolyl mglur5 antagonists and methods for their use
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
CA2760791C (en) 2009-05-07 2017-06-20 Intellikine, Inc. Heterocyclic compounds and uses thereof
GB201004311D0 (en) * 2010-03-15 2010-04-28 Proximagen Ltd New enzyme inhibitor compounds
CN103298474B (zh) 2010-11-10 2016-06-29 无限药品股份有限公司 杂环化合物及其用途
CA2825599C (en) 2011-02-01 2021-07-13 The Board Of Trustees Of The University Of Illinois 4-methyl-n-hydroxybenzamide compounds as histone deacetylase (hdac) inhibitors
US8684313B2 (en) 2011-02-02 2014-04-01 Ocean Rodeo Sports Inc. Inflatable kite with leading edge swept forwards at wingtip
US20140348748A1 (en) * 2011-09-16 2014-11-27 Lisheng Cai Beta-amyloid imaging agents, methods of manufacture, and methods of use thereof
US20150336948A1 (en) * 2012-05-29 2015-11-26 Merck Sharp & Dohme Corp. Isotopically Labeled Biaryl Urea Compounds
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

Also Published As

Publication number Publication date
PL3154970T3 (pl) 2020-04-30
US9808542B2 (en) 2017-11-07
RU2016150404A (ru) 2018-07-18
DK3154970T3 (da) 2020-01-20
RU2695373C2 (ru) 2019-07-23
BR112016028345B1 (pt) 2022-11-29
JP2017521387A (ja) 2017-08-03
WO2015191506A2 (en) 2015-12-17
AU2015274843B2 (en) 2018-11-22
KR20170016481A (ko) 2017-02-13
US20170119912A1 (en) 2017-05-04
WO2015188368A1 (en) 2015-12-17
HUE048395T2 (hu) 2020-08-28
JP6513107B2 (ja) 2019-05-15
KR102478430B1 (ko) 2022-12-15
BR112016028345A8 (pt) 2021-06-29
US20180071412A1 (en) 2018-03-15
US10022461B2 (en) 2018-07-17
RU2019115483A (ru) 2019-06-13
WO2015191506A3 (en) 2016-02-04
EP3154970A2 (en) 2017-04-19
BR112016028345A2 (pt) 2017-08-22
CA2948528A1 (en) 2015-12-17
RU2016150404A3 (es) 2018-11-30
EP3154970B1 (en) 2019-11-06
EP3154970A4 (en) 2017-11-15
MX375282B (es) 2025-03-06
ES2763095T3 (es) 2020-05-27
CN106661018A (zh) 2017-05-10
CA2948528C (en) 2022-05-31
CN106661018B (zh) 2019-07-19
AU2015274843A1 (en) 2016-11-10

Similar Documents

Publication Publication Date Title
MX2016016384A (es) Pirrolo[2,3-c]piridinas como agentes de formacion de imagenes para ovillos neurofibrilares.
ECSP088645A (es) Nuevos benzotiazoles sustituidos con heteroaril
IL290693A (en) Neuromelanin-sensitive mri for assessing parkinson's disease
MX385045B (es) Anticuerpo monoclonal recombinante para usarse en el tratamiento de la enfermedad de alzheimer.
ECSP13012609A (es) Composición farmacéutica
CL2020001097A1 (es) Derivados de piridincarbonilo y usos terapéuticos de los mismos como inhibidores de trpc6.
MX2014003357A (es) Terapia basada en proteina y diagnostico de patalogia mediada por tau en la enfermedad de alzheimer.
MX375424B (es) Derivados de 1,1,1-trifluoro-3-hidroxipropan-2-il carbamato y derivados de 1,1,1-trifluoro-4- hidroxibutan-2-il carbamato como inhibidores de magl
CO7131359A2 (es) Agentes de imagen para detectar disfunción neurológica
UY33863A (es) Metodos y medicamentos para el tratamiento de la enfermedad de alzheimer
BR112014012822A2 (pt) radioligantes rotulados com flúor-18 e carbono-11 para imagiologia por tomografia por emissão de pósitrons (pet) para lrrk2
MX379043B (es) Uso de sobetirome en el tratamiento de enfermedades de mielinización.
AR092779A1 (es) Composicon farmaceutica que comprende anticuerpos que se unen a conformeros de proteinas tau
UY35273A (es) Tiadiazol, análogos del mismo, y métodos para el tratamiento de condiciones relacionadas con defici encia de smn
MX2016008624A (es) Inhibidores de serina/treonina cinasa.
AR114029A2 (es) Compuestos adecuados como precursores de compuestos que son útiles para obtener imágenes de depósitos amiloides, usos y procesos
HUE063369T2 (hu) Vegyületek Alzheimer-kór kezelésében történõ alkalmazásra APOE4+/+ betegekben
MX392523B (es) Compuestos, composiciones farmaceuticas y metodos de uso de agonistas de ppar
ECSP19043790A (es) Pirazolo[3,4-b]piridinas e imidazo[1,5-b]piridazinas como inhibidores de PDE1
CO6592030A2 (es) Uso de la tasa de dilatación ventricular en el tratamiento de la enfermedad de alzheimer con inmunoglobulina intravenosa
ECSP099641A (es) Nuevos benzotiofenos y benzofuranos sustituidos en la posición 2 con heteroarilo 709
BR112015027015A2 (pt) derivados de 2-fenil ou 2-hetaril imidazol[1,2-a]piridina
MX386900B (es) Compuestos para formacion de imagenes de agregados de proteinas tau.
WO2010051196A8 (en) Novel substituted azabenzoxazoles
MX2013015001A (es) Formas solidas y sales de derivados de tetrahidro-pirido-pirimidin a.

Legal Events

Date Code Title Description
FG Grant or registration