EA201991755A1 - Бициклические бисгетероарильные производные в качестве модуляторов агрегации белков - Google Patents

Бициклические бисгетероарильные производные в качестве модуляторов агрегации белков

Info

Publication number
EA201991755A1
EA201991755A1 EA201991755A EA201991755A EA201991755A1 EA 201991755 A1 EA201991755 A1 EA 201991755A1 EA 201991755 A EA201991755 A EA 201991755A EA 201991755 A EA201991755 A EA 201991755A EA 201991755 A1 EA201991755 A1 EA 201991755A1
Authority
EA
Eurasian Patent Office
Prior art keywords
disease
protein aggregation
bisheteroaryl
bicyclic
methods
Prior art date
Application number
EA201991755A
Other languages
English (en)
Inventor
Адриан Халл
Лоран Провен
Малькольм Маккосс
Original Assignee
Юсб Байофарма Спрл
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 Юсб Байофарма Спрл filed Critical Юсб Байофарма Спрл
Publication of EA201991755A1 publication Critical patent/EA201991755A1/ru

Links

Classifications

    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61P25/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

В заявке описаны некоторые бициклические бисгетероарильные соединения, содержащие их фармацевтические композиции и способы их применения, включая способы предупреждения, обращения, замедления или подавления агрегации белков, и способы лечения заболеваний, которые связаны с агрегацией белков, включая нейродегенеративные заболевания, такие как болезнь Паркинсона, болезнь Альцгеймера, болезнь телец Леви, болезнь Паркинсона со слабоумием, лобно-височное слабоумие, болезнь Гентингтона, боковой амиотрофический склероз и мультисистемную атрофию, и рак, включая меланому.
EA201991755A 2017-01-26 2018-01-23 Бициклические бисгетероарильные производные в качестве модуляторов агрегации белков EA201991755A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17153217 2017-01-26
PCT/EP2018/051584 WO2018138088A1 (en) 2017-01-26 2018-01-23 Bicyclic bis-heteroaryl derivatives as modulators of protein aggregation

Publications (1)

Publication Number Publication Date
EA201991755A1 true EA201991755A1 (ru) 2020-01-22

Family

ID=57906529

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201991755A EA201991755A1 (ru) 2017-01-26 2018-01-23 Бициклические бисгетероарильные производные в качестве модуляторов агрегации белков

Country Status (16)

Country Link
US (1) US10889584B2 (ru)
EP (1) EP3573986B1 (ru)
JP (1) JP7073385B2 (ru)
KR (1) KR20190112022A (ru)
CN (1) CN110167937B (ru)
AU (1) AU2018212438C1 (ru)
BR (1) BR112019011924A2 (ru)
CA (1) CA3045221A1 (ru)
CL (1) CL2019001891A1 (ru)
CO (1) CO2019007830A2 (ru)
EA (1) EA201991755A1 (ru)
ES (1) ES2884145T3 (ru)
IL (1) IL267993A (ru)
MX (1) MX2019008256A (ru)
RU (1) RU2019126167A (ru)
WO (1) WO2018138088A1 (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111039939B (zh) 2014-01-29 2023-09-19 优时比生物医药有限公司 用作蛋白质聚集抑制剂的杂芳基酰胺
ES2885049T3 (es) 2015-07-29 2021-12-13 UCB Biopharma SRL Derivados de bis-heteroarilo como moduladores de la agregación de proteínas
BR112019011924A2 (pt) * 2017-01-26 2019-10-29 Ucb Biopharma Sprl derivados de bis-heteroarila bicíclicos como moduladores de agregação de proteína
ES2918048T3 (es) 2017-01-26 2022-07-13 UCB Biopharma SRL Derivados de alcoxi bis-heteroarilo como moduladores de la agregación de proteínas
WO2018138086A1 (en) * 2017-01-26 2018-08-02 Ucb Biopharma Sprl Bis-heteroaryl derivatives as modulators of protein aggregation
JP7297053B2 (ja) 2018-08-20 2023-06-23 アルビナス・オペレーションズ・インコーポレイテッド 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解
KR20230057381A (ko) * 2020-08-25 2023-04-28 내셔널 인스티튜츠 포 퀀텀 사이언스 앤드 테크놀로지 신규 화합물, α-시누클레인 응집체 결합제 및 그 이용
WO2023125376A1 (zh) * 2021-12-27 2023-07-06 上海京新生物医药有限公司 作为蛋白质聚集抑制剂的稠合双环杂芳基酰胺化合物
GB202213796D0 (en) * 2022-09-21 2022-11-02 Wista Lab Ltd Tau aggregation inhibitors

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
JP5922031B2 (ja) 2009-12-16 2016-05-24 ニューロポア セラピーズ，インコーポレイティド 化合物
GB201021103D0 (en) 2010-12-13 2011-01-26 Univ Leuven Kath New compounds for the treatment of neurodegenerative diseases
WO2013134371A1 (en) 2012-03-06 2013-09-12 Neuropore Therapies, Inc. Methods and compounds to be used in the treatment of neurodegenerative diseases
EP2830608B8 (en) 2012-03-28 2020-01-15 UCB Biopharma SRL Phenyl-urea and phenyl-carbamate derivatives as inhibitors of protein aggregation
US9284309B2 (en) 2012-07-16 2016-03-15 Neuropore Therapies, Inc. Di- and tri-heteroaryl derivatives as inhibitors of protein aggregation
CN111039939B (zh) * 2014-01-29 2023-09-19 优时比生物医药有限公司 用作蛋白质聚集抑制剂的杂芳基酰胺
ES2885049T3 (es) * 2015-07-29 2021-12-13 UCB Biopharma SRL Derivados de bis-heteroarilo como moduladores de la agregación de proteínas
BR112019011924A2 (pt) * 2017-01-26 2019-10-29 Ucb Biopharma Sprl derivados de bis-heteroarila bicíclicos como moduladores de agregação de proteína
WO2018138086A1 (en) 2017-01-26 2018-08-02 Ucb Biopharma Sprl Bis-heteroaryl derivatives as modulators of protein aggregation

Also Published As

Publication number Publication date
CA3045221A1 (en) 2018-08-02
ES2884145T3 (es) 2021-12-10
CO2019007830A2 (es) 2019-07-31
MX2019008256A (es) 2019-09-09
IL267993A (en) 2019-09-26
CN110167937B (zh) 2022-03-29
WO2018138088A1 (en) 2018-08-02
JP7073385B2 (ja) 2022-05-23
EP3573986B1 (en) 2021-05-26
BR112019011924A2 (pt) 2019-10-29
EP3573986A1 (en) 2019-12-04
CL2019001891A1 (es) 2019-11-22
CN110167937A (zh) 2019-08-23
KR20190112022A (ko) 2019-10-02
JP2020505369A (ja) 2020-02-20
AU2018212438A1 (en) 2019-07-25
AU2018212438B2 (en) 2020-12-17
AU2018212438C1 (en) 2021-05-06
RU2019126167A (ru) 2021-02-26
US20190367513A1 (en) 2019-12-05
US10889584B2 (en) 2021-01-12

Similar Documents

Publication Publication Date Title
EA201991755A1 (ru) Бициклические бисгетероарильные производные в качестве модуляторов агрегации белков
EA201991756A1 (ru) Бисгетероарильные производные в качестве модуляторов агрегации белков
PH12016501493B1 (en) Heteroaryl amides as inhibitors of protein aggregation
MX2019007480A (es) Anticuerpos monoclonales anti-alfa-sinucleina para prevenir la agregacion de tau.
EA201790992A1 (ru) Иммунорегуляторные агенты
MX2016010053A (es) Composiciones de compuestos y usos de los mismos.
MX2019004859A (es) Tratamientos de combinacion que comprenden la administracion de imidazopirazinonas.
MX2019003805A (es) Activadores de flujo autofágico y fosfolipasa d y depuración de acumulaciones de proteína que incluyen tau y tratamiento de proteinopatías.
EA201990400A1 (ru) Соединения и композиции и их применение
MX2015000618A (es) Derivados de di- y tri-heteroarilo como inhibidores de la agregacion de proteinas.
EP3773547A4 (en) IDENTIFICATION OF GRANINES AS A PATHOGENIC FACTOR OF ALZHEIMER'S MORBUS AND COMPOSITIONS AND METHODS FOR INHIBITING GRANINE AGGREGATION AND TREATMENT OF ALZHEIMER'S MORBUS
EA201991753A1 (ru) Алкоксибисгетероарильные производные в качестве модуляторов агрегации белков
MX2019001634A (es) Compuestos amidas, composiciones farmacéuticas de estos y métodos para utilizarlos.
PH12019502850A1 (en) AMIDE DERIVATIVES AS Nav1.7 AND Nav1.8 BLOCKERS
EP4219507A3 (en) Thienopyrimidinone nmda receptor modulators and uses thereof
MX2018001592A (es) Composiciones y metodos para el tratamiento y la prevencion de trastornos neurodegenerativos.
UA120083C2 (uk) АНТИМЕТАСТАТИЧНІ 2H-СЕЛЕНОФЕНО[3,2-h]ХРОМЕНИ, ЇХ СИНТЕЗ ТА СПОСОБИ ЗАСТОСУВАННЯ ЦИХ АГЕНТІВ
EP3610879A4 (en) COMPOSITION OF TREATMENT AND / OR PREVENTION OF ALZHEIMER'S DISEASE
MX2019008920A (es) Moduladores de rorgamma y usos de los mismos.
MX2019008603A (es) Una composicion farmaceutica que comprende un derivado de oxazina y su uso en el tratamiento o la prevencion de la enfermedad de alzheimer.
MA39227B1 (fr) Amides hétéroaryles comme inhibiteurs de l'agrégation protéique
AU2017902307A0 (en) Treatment of alzheimer's disease
AU2017902309A0 (en) Treatment of alzheimer's disease
HUP1600098A2 (en) Cosmetic composition for the prevention and treatment of peridontal diseases
PL409386A1 (pl) Preparaty peptydowe do zastosowania jako środek farmaceutyczny lub dodatek do żywności w zapobieganiu i leczeniu chorób neurodegeneracyjnych