AR043063A1 - Bencimidazoles 6-sustituidos y su uso como inhibidores de secreciones gastricas - Google Patents

Bencimidazoles 6-sustituidos y su uso como inhibidores de secreciones gastricas

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Publication number
AR043063A1
AR043063A1 ARP030104544A ARP030104544A AR043063A1 AR 043063 A1 AR043063 A1 AR 043063A1 AR P030104544 A ARP030104544 A AR P030104544A AR P030104544 A ARP030104544 A AR P030104544A AR 043063 A1 AR043063 A1 AR 043063A1
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AR
Argentina
Prior art keywords
alkoxy
alkyl
hydroxy
hydrogen
alkoxycarbonyl
Prior art date
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ARP030104544A
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English (en)
Inventor
Zimmermann Peter Jan Dr
Buhr Wilm Dr
Chiesa M Vittoria Dr
Palmer Andreas Dr
Brehm Christof Dr
Grundler Gerhard Dr
Senn-Bilfinger Joerg Dr
Simon Wolfgang-Alexander Dr
Postius Stefan Dr
Dr Kromer Wolfgang Prof
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Altana Pharma Ag
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Application filed by Altana Pharma Ag filed Critical Altana Pharma Ag
Publication of AR043063A1 publication Critical patent/AR043063A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado por la fórmula (1) donde R1 es hidrógeno, alquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, alcoxi C1-4, alcoxi C1-4-alquilo C1-4, alcoxicarbonilo C1-4, alquenilo C2-4, alquinilo C2-4, fluoro-alquilo C1-4, hidroxi-alquilo C1-4, mono- o di-alquilamino C1-4 o alquilcarboniloxi C1-4-alquilo C1-4, R2 es hidrógeno, alquilo C1-4, arilo, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, alcoxicarbonilo C1-4, mono- o di-alquilamino C1-4 alquilcarbonilo C1-4, hidroxi-alquilo C1-4, fluoro-alquilo C2-4, aril-alcoxi C1-4-alquilo C1-4, hidroxi o alcoxi C1-4, R3 es hidrógeno, halógeno, fluoro-alquilo C1-4, carboxilo,-CO-alcoxi C1-4, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4,alcoxi C1-4-alcoxi C1-4-alquilo C1-4, fluoro-alcoxi C1-4-alquilo C1-4, ciano, el grupo -CO-NR31R32, el grupo SO2-NR31R32 o el grupo Het, donde R31 es hidrógeno, hidroxilo, alquilo C1-7, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4 o cicloalquilo C3-7, amino y R32 es hidrógeno, alquilo C1-7, hidroxi-alquilo C1-4 o alcoxi C1-4-alquilo C1-4, o donde R31 y R32 tomados conjuntamente, incluyendo el átomo de nitrógeno al cual están ligados, son un grupo pirrolidino, piperidino, piperazino, N-alquil C1-4piperazino, morfolino, aziridino o azetidino y Het es un residuo heterocíclico, substituido por R33, R34 y R35, seleccionado del grupo formado por oxadiazol, dihidro-oxazol, dihidroimidazol, oxazol, imidazol, isoxazol, dihidroisoxazol, pirazol y tetrazol; donde R33 es hidrógeno, alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4, alqueniloxi C2-4, alquilcarbonilo C1-4, carboxi, alcoxicarbonilo C1-4, carboxi-alquilo C1-4, alcoxicarbonil C1-4-alquilo C1-4, halógeno, hidroxi, arilo, aril-alquilo C1-4, ariloxi, aril-alcoxi C1-4, trifluorometilo, nitro, amino, mono- o di-alquil C1-4amino, alquil C1-4carbonilamino, alcoxi C1-4carbonilamino, alcoxi C1-4-alcoxi C1-4carbonilamino o sulfonilo, R34 es hidrógeno, alquilo C1-4, alcoxi C1-4, alcoxicarbonilo C1-4, halógeno, trifluorometilo o hidroxi, R35 es hidrógeno, alquilo C1-4, alcoxi C1-4, alcoxicarbonilo C1-4, halógeno, trifluorometilo o hidroxi, X es O (oxígeno) o NH e Y tiene el significado -CH2-Ar donde Ar es un residuo aromático mono- o bicíclico, substituido por R4, R5, R6 y R7, que es seleccionado del grupo formado por fenilo, naftilo, pirrolilo, pirazolilo, imidazolilo, 1,2,3-triazolilo, indolilo, benzimidazolilo, furilo, benzofurilo, tienilo, benzotienilo, tiazolilo, isoxazolilo, piridinilo, pirimidinilo, quinolinilo y isoquinolinilo, o Y significa el radical (2) donde Z tiene el significado -CHR8- o -CHR8-CHR9- donde en Ar y/o en el radical (2) R4 es hidrógeno, alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4, alqueniloxi C2-4, alquilcarbonilo C1-4, carboxi, alcoxicarbonilo C1-4,carboxi-alquilo C1-4, alcoxicarbonil C1-4-alquilo C1-4, halógeno, hidroxi, arilo, aril-alquilo C1-4, ariloxi, aril-alcoxi C1-4, trifluorometilo, nitro, amino, mono- o di-alquil C1-4amino, alquil C1-4carbonilamino, alcoxi C1-4carbonilamino, alcoxi C1-4-alcoxi C1-4carbonilamino o sulfonilo, R5 es hidrógeno, alquilo C1-4, alcoxi C1-4, alcoxicarbonilo C1-4, halógeno, trifluorometilo o hidroxi, R6 es hidrógeno, alquilo C1-4 o halógeno y R7 es hidrógeno, alquilo C1-4 o halógeno, R8 es hidrógeno, alquilo C1-4, alquenilo C2-7, hidroxilo, alcoxi C1-4, alcoxi C1-4 oxo-substituido, cicloalcoxi C3-7, cicloalquil C3-7-alcoxi C1-4, hidroxi-alcoxi C1-4, alcoxi C1-4-alcoxi C1-4, alcoxi C1-4-alcoxi C1-4-alcoxi C1-4, cicloalcoxi C3-7-alcoxi C1-4, cicloalquil C3-7-alcoxi C1-4-alcoxi C1-4, alquilcarboniloxi C1-4, halo-alcoxi C1-4, amino, mono- o di-alquilamino C1-4, alquilcarbonilamino C1-4, alcoxi C1-4carbonilamino, mono- o di-alquil C1-4amino-alquil C1-4carboniloxi, alcoxi C1-4-alcoxi C1-4carbonilamino o alcoxi C1-4-alquil C1-4carboniloxi, R9 es hidrógeno, alquilo C1-7, alquenilo C2-7, hidroxilo, alcoxi C1-4, alcoxi C1-4 oxo-substituido, cicloalcoxi C3-7, cicloalquil C3-7-alcoxi C1-4, hidroxi-alcoxi C1-4, alcoxi C1-4-alcoxi C1-4, alcoxi C1-4-alcoxi C1-4-alcoxi C1-4, cicloalcoxi C3-7-alcoxi C1-4, cicloalquil C3-7-alcoxi C1-4-alcoxi C1-4, alquilcarboniloxi C1-4, halo-alcoxi C1-4, amino, mono- o di-alquilamino C1-4, alquilcarbonilamino C1-4, alcoxicarbonilamino C1-4, mono- o di-alquilamino C1-4-alquilcarboniloxi C1-4, alcoxi C1-4-alcoxicarbonilamino C1-4 o alcoxi C1-4-alquilcarboniloxi C1-4, y donde arilo es fenilo o fenilo substituido por uno, dos o tres substituyentes iguales o diferentes del grupo formado por alquilo C1-4, alcoxi C1-4, carboxi, alcoxicarbonilo C1-4, halógeno, trifluorometilo, nitro, trifluorometoxi, hidroxi y ciano, con la condición de que R3 no tiene el significado de hidrógeno o halógeno cuando Y significa -CH2-Ar y R2 significa hidrógeno, alquilo o cicloalquil-alquilo, o una sal del mismo.
ARP030104544A 2002-12-13 2003-12-10 Bencimidazoles 6-sustituidos y su uso como inhibidores de secreciones gastricas AR043063A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02027874 2002-12-13
EP03021348 2003-09-20

Publications (1)

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AR043063A1 true AR043063A1 (es) 2005-07-13

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US (1) US20060194969A1 (es)
EP (1) EP1575924A1 (es)
JP (1) JP2006511600A (es)
KR (1) KR20050084170A (es)
AR (1) AR043063A1 (es)
AU (1) AU2003294831A1 (es)
BR (1) BR0317041A (es)
CA (1) CA2508838A1 (es)
CO (1) CO5580786A2 (es)
EA (1) EA008779B1 (es)
HR (1) HRP20050612A2 (es)
IS (1) IS7926A (es)
MX (1) MXPA05006052A (es)
NO (1) NO20053242L (es)
NZ (1) NZ540862A (es)
PL (1) PL375820A1 (es)
RS (1) RS20050435A (es)
TW (1) TW200504031A (es)
WO (1) WO2004054984A1 (es)

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BR112015031073B1 (pt) 2013-06-21 2022-11-29 Zenith Epigenetics Ltd Compostos inibidores bicíclicos de bromodomínio e composição farmacêutica contendo os referidos compostos
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
KR101472686B1 (ko) 2013-07-09 2014-12-16 씨제이헬스케어 주식회사 벤즈이미다졸 유도체의 제조방법
KR20160038008A (ko) 2013-07-31 2016-04-06 제니쓰 에피제네틱스 코포레이션 브로모도메인 억제제로서 신규 퀴나졸리논
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NZ540862A (en) 2008-07-31
PL375820A1 (en) 2005-12-12
TW200504031A (en) 2005-02-01
NO20053242D0 (no) 2005-07-01
RS20050435A (en) 2007-08-03
KR20050084170A (ko) 2005-08-26
BR0317041A (pt) 2005-10-25
HRP20050612A2 (en) 2006-08-31
AU2003294831A1 (en) 2004-07-09
JP2006511600A (ja) 2006-04-06
EA008779B1 (ru) 2007-08-31
WO2004054984A1 (en) 2004-07-01
EA200500895A1 (ru) 2005-12-29
MXPA05006052A (es) 2005-08-18
NO20053242L (no) 2005-07-01
IS7926A (is) 2005-07-01
US20060194969A1 (en) 2006-08-31
CA2508838A1 (en) 2004-07-01
CO5580786A2 (es) 2005-11-30
EP1575924A1 (en) 2005-09-21

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