BR112012022478A2 - inibidores heterocíclicos de glutaminil ciclase (qc, ec 2.3.2.5) - Google Patents

inibidores heterocíclicos de glutaminil ciclase (qc, ec 2.3.2.5)

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Publication number
BR112012022478A2
BR112012022478A2 BR112012022478A BR112012022478A BR112012022478A2 BR 112012022478 A2 BR112012022478 A2 BR 112012022478A2 BR 112012022478 A BR112012022478 A BR 112012022478A BR 112012022478 A BR112012022478 A BR 112012022478A BR 112012022478 A2 BR112012022478 A2 BR 112012022478A2
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BR
Brazil
Prior art keywords
heterocyclic
glutaminyl cyclase
cyclase inhibitors
pyroglutamic acid
intramolecular cyclization
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BR112012022478A
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English (en)
Other versions
BR112012022478B1 (pt
Inventor
Demuth Hans-Ulrich
Gaertner Ulf-Torsten
Heiser Ulrich
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Probiodrug Ag
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Publication date
Application filed by Probiodrug Ag filed Critical Probiodrug Ag
Publication of BR112012022478A2 publication Critical patent/BR112012022478A2/pt
Publication of BR112012022478B1 publication Critical patent/BR112012022478B1/pt

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    • 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
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    • 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
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    • 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
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    • 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
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    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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Abstract

inibidores heterocíclicos de glutaminil ciclase (qc, ec 2.3.5). a presente invenção refere-se a novos derivados heterocíclicos como inibidores de glutaminil ciclase (qc, ec 2.3.2.5). qc catalisa a ciclização intramolecular de resíduos glutamina n-terminais em ácido piroglutâmico (5-oxo-proplil, pglu*) sob liberação de amônia e a ciclização intramolecular de resíduos glutamato n-terminais em ácido piroglutâmico sob liberação de água.
BR112012022478-6A 2010-03-10 2011-03-10 Inibidores heterocíclicos de glutaminil ciclase (qc, ec 2.3.2.5), seu processo de preparação, e composição farmacêutica BR112012022478B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31233910P 2010-03-10 2010-03-10
US61/312,339 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
BR112012022478A2 true BR112012022478A2 (pt) 2017-02-14
BR112012022478B1 BR112012022478B1 (pt) 2021-09-21

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BR112012022478-6A BR112012022478B1 (pt) 2010-03-10 2011-03-10 Inibidores heterocíclicos de glutaminil ciclase (qc, ec 2.3.2.5), seu processo de preparação, e composição farmacêutica

Country Status (17)

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

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ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
US8945510B2 (en) * 2011-05-27 2015-02-03 Probiodrug Ag Radiolabeled glutaminyl cyclase (QC) inhibitors and uses of same
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WO2016097305A1 (en) 2014-12-19 2016-06-23 Probiodrug Ag Novel method for the detection of pglu-abeta peptides
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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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IL221243A (en) 2016-06-30
NZ602312A (en) 2014-02-28
US8269019B2 (en) 2012-09-18
EA022420B1 (ru) 2015-12-30
EA201201275A1 (ru) 2013-04-30
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AU2011226074A1 (en) 2012-10-04
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CA2789440C (en) 2020-03-24
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WO2011110613A1 (en) 2011-09-15
CN102791704B (zh) 2015-11-25
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US8420828B2 (en) 2013-04-16
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