EA201400245A1 - Ингибиторы dyrk1 и их применение - Google Patents

Ингибиторы dyrk1 и их применение

Info

Publication number
EA201400245A1
EA201400245A1 EA201400245A EA201400245A EA201400245A1 EA 201400245 A1 EA201400245 A1 EA 201400245A1 EA 201400245 A EA201400245 A EA 201400245A EA 201400245 A EA201400245 A EA 201400245A EA 201400245 A1 EA201400245 A1 EA 201400245A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
dyrk1
application
alleviating
treating
Prior art date
Application number
EA201400245A
Other languages
English (en)
Other versions
EA026377B1 (ru
Inventor
Бертран Леблон
Анн-Софи Касагранде
Лоран Дезир
Алисия Фукур
Тьери Бессон
Original Assignee
Диаксонхит
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 Диаксонхит filed Critical Диаксонхит
Publication of EA201400245A1 publication Critical patent/EA201400245A1/ru
Publication of EA026377B1 publication Critical patent/EA026377B1/ru

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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
    • A61K31/495—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2

Landscapes

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

Abstract

Изобретение касается новых соединений тиазоло[5,4-f]хиназолинов и способов, применимых для облегчения, лечения или контролирования синдрома Дауна или ранней стадии болезни Альцгеймера либо для облегчения, лечения или контролирования раковых заболеваний, в особенности солидных опухолей. Более конкретно, изобретение касается ингибиторов DYRK1A и/или DYRK1B и способов получения таких соединений.
EA201400245A 2011-08-19 2012-08-17 Ингибиторы dyrk1 и их применение EA026377B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11178190 2011-08-19
PCT/EP2012/066151 WO2013026806A1 (en) 2011-08-19 2012-08-17 Dyrk1 inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
EA201400245A1 true EA201400245A1 (ru) 2014-07-30
EA026377B1 EA026377B1 (ru) 2017-04-28

Family

ID=46704656

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201400245A EA026377B1 (ru) 2011-08-19 2012-08-17 Ингибиторы dyrk1 и их применение

Country Status (15)

Country Link
US (1) US9446044B2 (ru)
EP (1) EP2744797B1 (ru)
JP (1) JP6017559B2 (ru)
KR (1) KR102006749B1 (ru)
CN (1) CN103797002B (ru)
AU (1) AU2012298510B2 (ru)
BR (1) BR112014003774B1 (ru)
CA (1) CA2848896C (ru)
DK (1) DK2744797T3 (ru)
EA (1) EA026377B1 (ru)
ES (1) ES2551268T3 (ru)
IL (1) IL230917A (ru)
PL (1) PL2744797T3 (ru)
PT (1) PT2744797E (ru)
WO (1) WO2013026806A1 (ru)

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JP3374198B2 (ja) 1993-02-23 2003-02-04 株式会社バルダン 縫製方法
JP3374197B2 (ja) 1993-02-24 2003-02-04 株式会社バルダン 縫製方法
JP2015534584A (ja) * 2012-10-10 2015-12-03 フェリシテックス・セラピューティクス，インコーポレイテッド 静止癌細胞の標的化による癌の治療
FR3002044A1 (fr) * 2013-02-08 2014-08-15 Centre Nat Rech Scient Marqueur dyrk1a pour la maladie d'alzheimer
CA2854542A1 (en) 2013-06-18 2014-12-18 4Sc Discovery Gmbh Method of inhibiting dyrk1b
JP2015107945A (ja) * 2013-12-05 2015-06-11 国立大学法人京都大学 神経新生に関する化合物及び医薬組成物
US10730842B2 (en) 2015-09-03 2020-08-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK1A and uses thereof
CA3021021A1 (en) * 2016-04-15 2017-10-19 Felicitex Therapeutics, Inc. Combinations for the treatment of neoplasms using quiescent cell targeting and egfr inhibitors
EP3443351A4 (en) * 2016-04-15 2019-12-18 Felicitex Therapeutics, Inc. COMBINATIONS FOR THE TREATMENT OF NEOPLASIA BY TARGETING RESTING CELLS AND INHIBITORS OF MITOSIS
PL3558321T3 (pl) 2016-12-23 2023-10-23 Felicitex Therapeutics, Inc. Pochodne chinolin jako inhibitory kinaz dyrk1a i/lub dyrk1b
WO2019100062A1 (en) 2017-11-20 2019-05-23 Ichan School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
WO2019136320A1 (en) 2018-01-05 2019-07-11 Icahn School Of Medicine At Mount Sinai Method of increasing proliferation of pancreatic beta cells, treatment method, and composition
US12528810B2 (en) 2018-03-01 2026-01-20 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK/CLK and uses thereof
CN112135613A (zh) 2018-03-20 2020-12-25 西奈山伊坎医学院 激酶抑制剂化合物和组合物及使用方法
CA3118093A1 (en) 2018-09-28 2020-04-02 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of dyrk1/clk and uses thereof
JP2022515650A (ja) * 2018-12-31 2022-02-21 アイカーン スクール オブ メディシン アット マウント サイナイ キナーゼ阻害剤化合物及び組成物ならびに使用方法
US20230138851A1 (en) * 2020-01-30 2023-05-04 Carna Biosciences, Inc. Novel alkyne derivatives
WO2022059778A1 (ja) * 2020-09-18 2022-03-24 カルナバイオサイエンス株式会社 環状ウレア誘導体
EP4215534A4 (en) * 2020-09-18 2024-10-02 Carna Biosciences, Inc. AMINE DERIVATIVE
WO2023008470A1 (ja) * 2021-07-28 2023-02-02 住友ファーマ株式会社 縮環アミン誘導体
JPWO2023008472A1 (ru) * 2021-07-28 2023-02-02
WO2023140846A1 (en) * 2022-01-20 2023-07-27 Felicitex Therapeutics, Inc. Combination cancer therapy with dyrk1 inhibitors and inhibitors of the ras-raf-mek-erk (mapk) pathway
WO2024249488A2 (en) * 2023-05-30 2024-12-05 Beth Israel Deaconess Medical Center, Inc. Inhibitors of dyrk1a
WO2025069008A1 (en) 2023-09-28 2025-04-03 Graviton Bioscience Bv Therapy for treating type 1 diabetes using rock2 and dyrk1 inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL112249A (en) * 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) * 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
GB0705566D0 (en) * 2007-03-23 2007-05-02 Univ Dundee Method of treating learning impairment in down's syndrome subjects
FR2943057B1 (fr) * 2009-03-12 2011-06-03 Centre Nat Rech Scient DERIVES DE 10-AMINO-1,2,3,4-TETRAHYDROPYRIDO°2,1-a!ISOINDOL-6(10bH)- ONES, LEUR PROCEDE DE PREPARATION ET LEURS UTILISATIONS THERAPEUTIQUES
WO2011041655A1 (en) * 2009-10-01 2011-04-07 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Quinazolin-4-amine derivatives; and methods of use

Also Published As

Publication number Publication date
PL2744797T3 (pl) 2016-01-29
KR102006749B1 (ko) 2019-08-02
US20140275064A1 (en) 2014-09-18
CN103797002A (zh) 2014-05-14
BR112014003774A2 (pt) 2017-03-07
AU2012298510A1 (en) 2014-04-10
PT2744797E (pt) 2015-11-16
JP2014525928A (ja) 2014-10-02
JP6017559B2 (ja) 2016-11-02
CA2848896A1 (en) 2013-02-28
EP2744797A1 (en) 2014-06-25
ES2551268T3 (es) 2015-11-17
EP2744797B1 (en) 2015-09-09
HK1198827A1 (en) 2015-06-12
EA026377B1 (ru) 2017-04-28
CN103797002B (zh) 2017-02-22
BR112014003774B1 (pt) 2021-12-14
WO2013026806A1 (en) 2013-02-28
CA2848896C (en) 2019-10-29
US9446044B2 (en) 2016-09-20
IL230917A0 (en) 2014-03-31
KR20140057614A (ko) 2014-05-13
DK2744797T3 (en) 2015-10-19
AU2012298510B2 (en) 2016-10-27
IL230917A (en) 2017-02-28

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KG TJ TM