EA201201275A1 - Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5) - Google Patents

Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5)

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Publication number
EA201201275A1
EA201201275A1 EA201201275A EA201201275A EA201201275A1 EA 201201275 A1 EA201201275 A1 EA 201201275A1 EA 201201275 A EA201201275 A EA 201201275A EA 201201275 A EA201201275 A EA 201201275A EA 201201275 A1 EA201201275 A1 EA 201201275A1
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EA
Eurasian Patent Office
Prior art keywords
glutaminilcyclases
pyroglutamic acid
heterocyclic inhibitors
intramolecular cyclization
free state
Prior art date
Application number
EA201201275A
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English (en)
Other versions
EA022420B1 (ru
Inventor
Ульрих Хайзер
Ульф-Торстен Гертнер
Ханс-Ульрих Демут
Original Assignee
Пробиодруг Аг
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Publication date
Application filed by Пробиодруг Аг filed Critical Пробиодруг Аг
Publication of EA201201275A1 publication Critical patent/EA201201275A1/ru
Publication of EA022420B1 publication Critical patent/EA022420B1/ru

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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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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
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    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
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  • Oncology (AREA)
  • Epidemiology (AREA)
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Abstract

Изобретение относится к новым гетероциклическим производным в качестве ингибиторов глутаминилциклазы (QC, ЕС 2.3.2.5). QC катализирует внутримолекулярную циклизацию N-концевых глутаминовых остатков с образованием пироглутаминовой кислоты (5-оксопролил, pGlu*) с выделением в свободном состоянии аммиака, и внутримолекулярную циклизацию N-концевых глутаматных остатков с образованием пироглутаминовой кислоты с выделением в свободном состоянии воды.
EA201201275A 2010-03-10 2011-03-10 Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5) EA022420B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31233910P 2010-03-10 2010-03-10
PCT/EP2011/053576 WO2011110613A1 (en) 2010-03-10 2011-03-10 Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)

Publications (2)

Publication Number Publication Date
EA201201275A1 true EA201201275A1 (ru) 2013-04-30
EA022420B1 EA022420B1 (ru) 2015-12-30

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EA201201275A EA022420B1 (ru) 2010-03-10 2011-03-10 Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5)

Country Status (17)

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US (2) US8269019B2 (ru)
EP (1) EP2545047B9 (ru)
JP (1) JP5688745B2 (ru)
KR (1) KR101790806B1 (ru)
CN (1) CN102791704B (ru)
AU (1) AU2011226074B2 (ru)
BR (1) BR112012022478B1 (ru)
CA (1) CA2789440C (ru)
DK (1) DK2545047T3 (ru)
EA (1) EA022420B1 (ru)
ES (1) ES2481823T3 (ru)
HK (1) HK1178528A1 (ru)
IL (1) IL221243A (ru)
MX (1) MX2012010470A (ru)
NZ (1) NZ602312A (ru)
SG (1) SG183229A1 (ru)
WO (1) WO2011110613A1 (ru)

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EP2545047B9 (en) * 2010-03-10 2015-06-10 Probiodrug AG Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
JP2014515364A (ja) * 2011-05-27 2014-06-30 プロビオドルグ エージー 放射能標識グルタミニルシクラーゼ阻害剤
GB201308217D0 (en) 2013-05-08 2013-06-12 Ucl Business Plc Compounds and their use in therapy
WO2016097305A1 (en) 2014-12-19 2016-06-23 Probiodrug Ag Novel method for the detection of pglu-abeta peptides
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US10381473B2 (en) 2016-12-02 2019-08-13 Vishay-Siliconix High-electron-mobility transistor with buried interconnect
RU2662559C1 (ru) * 2017-10-27 2018-07-26 Общество С Ограниченной Ответственностью "Фарминтерпрайсез" Новый ингибитор глутаминилциклаз и его применение для лечения заболеваний легких и дыхательных путей
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
CN111757883B (zh) * 2018-02-23 2024-02-13 弗劳恩霍夫应用研究促进协会 用于治疗牙周疾病和相关疾病的细菌谷氨酰胺酰环化酶的新抑制剂
EP3543231A1 (en) * 2018-03-19 2019-09-25 ETH Zurich Compounds for treating cns- and neurodegenerative diseases
US10693288B2 (en) 2018-06-26 2020-06-23 Vishay SIliconix, LLC Protection circuits with negative gate swing capability
US10833063B2 (en) 2018-07-25 2020-11-10 Vishay SIliconix, LLC High electron mobility transistor ESD protection structures
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EP2545047B1 (en) 2014-04-23
WO2011110613A1 (en) 2011-09-15
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US8269019B2 (en) 2012-09-18
US20120283259A1 (en) 2012-11-08
AU2011226074A1 (en) 2012-10-04
CN102791704B (zh) 2015-11-25
CA2789440A1 (en) 2011-09-15
SG183229A1 (en) 2012-09-27
BR112012022478B1 (pt) 2021-09-21
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IL221243A (en) 2016-06-30
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NZ602312A (en) 2014-02-28
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IL221243A0 (en) 2012-10-31
EA022420B1 (ru) 2015-12-30
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