EA201891948A1 - Отрицательные аллостерические модуляторы метаботропного глутаматного рецептора 5 для применения в лечении зрелых повреждений головного мозга - Google Patents

Отрицательные аллостерические модуляторы метаботропного глутаматного рецептора 5 для применения в лечении зрелых повреждений головного мозга

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Publication number
EA201891948A1
EA201891948A1 EA201891948A EA201891948A EA201891948A1 EA 201891948 A1 EA201891948 A1 EA 201891948A1 EA 201891948 A EA201891948 A EA 201891948A EA 201891948 A EA201891948 A EA 201891948A EA 201891948 A1 EA201891948 A1 EA 201891948A1
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EA
Eurasian Patent Office
Prior art keywords
treatment
metabotropic
receptor
glutamatny
head
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EA201891948A
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English (en)
Inventor
Тадеуш Вилох
Карин Сьёлунд
Керстин Бейруп
Карстен Рушер
Роджер Олссон
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Синнтаксис Аб
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Publication of EA201891948A1 publication Critical patent/EA201891948A1/ru

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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
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    • 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
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    • 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
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    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • 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
    • A61K31/4965—Non-condensed pyrazines
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    • 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
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
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Abstract

Настоящее изобретение относится к применению отрицательных аллостерических модуляторов (negative allosteric modulators, NAM) метаботропного глутаматного рецептора 5 (mGluR5) в лечении зрелого повреждения головного мозга, такого как повреждение после инсульта.
EA201891948A 2016-03-30 2016-03-30 Отрицательные аллостерические модуляторы метаботропного глутаматного рецептора 5 для применения в лечении зрелых повреждений головного мозга EA201891948A1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/SE2016/050264 WO2017171594A1 (en) 2016-03-30 2016-03-30 Negative allosteric modulators of mglur5 for use in the treatment of mature brain damages.

Publications (1)

Publication Number Publication Date
EA201891948A1 true EA201891948A1 (ru) 2019-04-30

Family

ID=59964972

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891948A EA201891948A1 (ru) 2016-03-30 2016-03-30 Отрицательные аллостерические модуляторы метаботропного глутаматного рецептора 5 для применения в лечении зрелых повреждений головного мозга

Country Status (12)

Country Link
US (1) US11033545B2 (ru)
EP (1) EP3436009B1 (ru)
JP (2) JP2019515892A (ru)
KR (1) KR102648875B1 (ru)
CN (1) CN108883104A (ru)
AU (1) AU2016400019A1 (ru)
BR (1) BR112018069868A2 (ru)
CA (1) CA3018375A1 (ru)
EA (1) EA201891948A1 (ru)
MX (1) MX2018011765A (ru)
PL (1) PL3436009T3 (ru)
WO (1) WO2017171594A1 (ru)

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA75871C2 (en) * 1999-08-19 2006-06-15 Nps Pharma Inc 1,2,4-oxadiazole derivatives and use thereof as antagonists at metabotropic glutamate receptors
JP4519404B2 (ja) * 2001-02-21 2010-08-04 アストラゼネカ アクチボラグ ヘテロ多環式化合物およびその代謝型グルタミン酸受容体アンタゴニストとしての使用
UA80888C2 (en) * 2003-06-05 2007-11-12 Hoffmann La Roche Imidazole derivatives as glutmate receptor antagonists
DK1756086T3 (da) * 2004-06-01 2008-08-04 Hoffmann La Roche Pyridin-4-yl-ethynyl-imidazoler og pyrazoler som mglu5-receptorantagonister
EP2235161A1 (en) * 2007-12-11 2010-10-06 Research Development Foundation Small molecules for neuronal differentiation of embryonic stem cells
PE20150733A1 (es) 2012-10-18 2015-05-17 Hoffmann La Roche Derivados de etinilo como moduladores de la actividad del receptor mglur5
KR101439203B1 (ko) * 2013-03-29 2014-09-12 한림대학교 산학협력단 Ｆｋ506 결합단백질 융합단백질과 피노밤을 포함하는 뇌 허혈손상 치료용 약제학적 조성물
CA2950988C (en) * 2014-06-18 2024-02-06 Csl Behring Gmbh Therapy using a factor xii inhibitor in a neurotraumatic disorder
KR101785155B1 (ko) * 2015-09-22 2017-10-16 국립암센터 Ｔｉｍ－３을 표적으로 하는 뇌손상 질환 치료용 조성물 및 이의 스크리닝 방법
CA3075759A1 (en) * 2017-09-15 2019-03-21 Azevan Pharmaceuticals, Inc. Compositions and methods for treating brain injury

Also Published As

Publication number Publication date
JP2019515892A (ja) 2019-06-13
EP3436009C0 (en) 2024-03-06
US20190365753A1 (en) 2019-12-05
JP7267326B2 (ja) 2023-05-01
CA3018375A1 (en) 2017-10-05
JP2021098701A (ja) 2021-07-01
AU2016400019A1 (en) 2018-10-04
PL3436009T3 (pl) 2024-05-06
EP3436009B1 (en) 2024-03-06
KR102648875B1 (ko) 2024-03-15
KR20180123565A (ko) 2018-11-16
BR112018069868A2 (pt) 2019-01-29
EP3436009A4 (en) 2019-11-27
WO2017171594A1 (en) 2017-10-05
EP3436009A1 (en) 2019-02-06
MX2018011765A (es) 2019-05-20
CN108883104A (zh) 2018-11-23
US11033545B2 (en) 2021-06-15

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