EA201990450A1 - Ингибиторы киназы, содержащей домен с двумя лейциновыми "застежками-молниями" (dlk), для лечения заболевания - Google Patents

Ингибиторы киназы, содержащей домен с двумя лейциновыми "застежками-молниями" (dlk), для лечения заболевания

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Publication number
EA201990450A1
EA201990450A1 EA201990450A EA201990450A EA201990450A1 EA 201990450 A1 EA201990450 A1 EA 201990450A1 EA 201990450 A EA201990450 A EA 201990450A EA 201990450 A EA201990450 A EA 201990450A EA 201990450 A1 EA201990450 A1 EA 201990450A1
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Eurasian Patent Office
Prior art keywords
disease
result
dlk
domain
nervous system
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EA201990450A
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English (en)
Inventor
Майкл Дж. Сот
Филип Джоунс
Джеймс Рэй
Ган Лю
Кан Лэ
Джейсон Кросс
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Боард Оф Реджентс, Де Юниверсити Оф Техас Систем
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Publication of EA201990450A1 publication Critical patent/EA201990450A1/ru

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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/535—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
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    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • C07D498/04—Ortho-condensed systems

Abstract

В данном документе раскрыты соединения, которые подавляют киназную активность киназы, содержащей домен с двумя лейциновыми "застежками-молниями" (DLK) (MAP3K12), фармацевтические композиции и способы лечения заболеваний, опосредованных DLK, таких как неврологические заболевания, которые возникают в результате травматического повреждения нейронов центральной нервной системы и периферической нервной системы (например, инсульт, травматическое повреждение головного мозга, повреждение спинного мозга), или которые возникают в результате хронического нейродегенеративного состояния (например, болезни Альцгеймера, лобно-височной деменции, болезни Паркинсона, болезни Хантингтона, амиотрофического латерального склероза, спинально-церебеллярной атаксии, прогрессирующего надъядерного паралича, болезни телец Леви, болезни Кеннеди и других связанных с ними состояний), которые возникают в результате невропатий, возникающих в результате неврологического повреждения (периферическая невропатия, индуцированная химиотерапией, диабетическая невропатия и связанные с ними состояния), и которые возникают в результате когнитивных расстройств, обусловленных фармакологическим воздействием (например, когнитивного расстройства, индуцированного химиотериапией, также известного как "химический мозг").
EA201990450A 2016-08-29 2017-08-28 Ингибиторы киназы, содержащей домен с двумя лейциновыми "застежками-молниями" (dlk), для лечения заболевания EA201990450A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662380822P 2016-08-29 2016-08-29
PCT/US2017/048941 WO2018044808A1 (en) 2016-08-29 2017-08-28 Inhibitors of dual leucine ziper (dlk) kinase for the treatment of disease

Publications (1)

Publication Number Publication Date
EA201990450A1 true EA201990450A1 (ru) 2019-07-31

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US (1) US20180057507A1 (ru)
EP (1) EP3503889A1 (ru)
JP (1) JP2019528319A (ru)
KR (1) KR20190040068A (ru)
CN (1) CN109789132A (ru)
AU (1) AU2017321313A1 (ru)
BR (1) BR112019004243A2 (ru)
CA (1) CA3035195A1 (ru)
CL (1) CL2019000534A1 (ru)
CO (1) CO2019002839A2 (ru)
EA (1) EA201990450A1 (ru)
EC (1) ECSP19021843A (ru)
MX (1) MX2019002444A (ru)
WO (1) WO2018044808A1 (ru)

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Publication number Priority date Publication date Assignee Title
CA3045947A1 (en) * 2016-12-08 2018-06-14 Michael J. Soth Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease
US11560366B2 (en) * 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease
AU2021336300A1 (en) 2020-09-02 2023-03-16 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services LZK-targeting degraders and methods of use
CA3193415A1 (en) * 2020-10-13 2022-04-21 The Johns Hopkins University Substituted 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)thiophene-2-carboxamide derivatives and use thereof
CN114605497B (zh) * 2021-02-10 2023-04-28 北京欣安诚科技有限公司 一种dapk1磷酸化底物的人工小分子干扰肽及其制药用途
CA3229861A1 (en) 2021-09-01 2023-03-09 John F. BROGNARD Mixed lineage kinase inhibitors and methods of use
CN115770239B (zh) * 2022-12-05 2024-01-30 南京中医药大学 呋喃并色酮及药学上可接受的盐在制备治疗周围神经病变的药物中的应用

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US7332476B2 (en) * 2003-04-25 2008-02-19 Novartis Ag Pyridyl substituted ketolide antibiotics
US7163924B2 (en) * 2003-04-25 2007-01-16 Chiron Corporation Ketolide derivatives
TW200944520A (en) * 2008-01-29 2009-11-01 Glaxo Group Ltd Spiro compounds as NPY Y5 receptor antagonists
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EP2651930B1 (en) * 2010-12-16 2015-10-28 Boehringer Ingelheim International GmbH Biarylamide inhibitors of leukotriene production
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Publication number Publication date
BR112019004243A2 (pt) 2019-06-04
ECSP19021843A (es) 2019-05-31
KR20190040068A (ko) 2019-04-16
WO2018044808A1 (en) 2018-03-08
CN109789132A (zh) 2019-05-21
CL2019000534A1 (es) 2019-08-02
JP2019528319A (ja) 2019-10-10
CA3035195A1 (en) 2018-03-08
CO2019002839A2 (es) 2019-04-30
MX2019002444A (es) 2019-09-02
AU2017321313A1 (en) 2019-03-21
EP3503889A1 (en) 2019-07-03
US20180057507A1 (en) 2018-03-01

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