AR040203A1 - COMBINATION OF A REFLUX INHIBITOR AND AN IMIDAZOPIRIDINE FOR THE TREATMENT OF GERD - Google Patents

COMBINATION OF A REFLUX INHIBITOR AND AN IMIDAZOPIRIDINE FOR THE TREATMENT OF GERD

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Publication number
AR040203A1
AR040203A1 ARP030102095A ARP030102095A AR040203A1 AR 040203 A1 AR040203 A1 AR 040203A1 AR P030102095 A ARP030102095 A AR P030102095A AR P030102095 A ARP030102095 A AR P030102095A AR 040203 A1 AR040203 A1 AR 040203A1
Authority
AR
Argentina
Prior art keywords
alkyl
represents hydrogen
heteroaryl
aryl
halogen
Prior art date
Application number
ARP030102095A
Other languages
Spanish (es)
Original Assignee
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR040203A1 publication Critical patent/AR040203A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • 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
    • A61K31/4353—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
    • 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
    • A61K31/66—Phosphorus compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C313/00—Sulfinic acids; Sulfenic acids; Halides, esters or anhydrides thereof; Amides of sulfinic or sulfenic acids, i.e. compounds having singly-bound oxygen atoms of sulfinic or sulfenic groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C313/02—Sulfinic acids; Derivatives thereof
    • C07C313/04—Sulfinic acids; Esters thereof

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

Abstract

La presente se relaciona con un medicamento que comprende, justos o por separado, (i) por lo menos un inhibidor del reflujo y (ii) por lo menos una imidazopirina. Otro aspecto de la presente se relaciona con métodos de tratamiento de la enfermedad de reflujo gastroesofágico, la regurgitación, el asma, la falta de desarrollo y la enfermedad pulmonar. Reivindicación 1: Una combinación que comprende, por separado o juntos, (i) por lo menos un inhibidor del reflujo y (ii) por lo menos una imidazopiridina de la fórmula (1) o una sal farmacéuticamente aceptable de la misma, en la cual R18 es H, CH3 o, CH2OH, R19 es CH3, CH2CH3; R20 es H, alquilo C1-6, alquilo C1-6 hidroxilado, halógeno; R21 H, alquilo C1-6, alquilo C1-6 hidroxilado o, halógeno; R22 es H, halógeno; R23 y R24 son iguales o diferentes, seleccionados entre cualquiera de: H, alquilo C1-6, alquilo C1-6 hidroxilado o, alquilo C1-6 sustituido con alcoxi C1-6; X es NH o O. Reivindicación 3: Una combinación de acuerdo con la reivindicación 1 o 2, en la cual el agente inhibidor del reflujo es un compuesto con la fórmula (2) en la cual: R1 representa hidrógeno; R2 representa hidroxi, flúor o un grupo oxo; R3 representa hidrógeno; R4 representa hidrógeno o una sal o solvato farmacéuticamente aceptable y los estereoisómeros del mismo. Reivindicación 4: Una combinación de acuerdo con la reivindicación 1 o 2, en la cual el inhibidor del reflujo es un compuesto de acuerdo con la fórmula (3) en la cual: R5 representa hidrógeno o alquilo inferior; R6 representa un grupo flúor; R7 representa hidrógeno; R8 representa hidrógeno; R9 representa metilo, fluorometilo, difluorometilo o trifluorometilo o una sal o solvato farmacéuticamente aceptable y los estereoisómeros del mismo. Reivindicación 5: Una combinación de acuerdo con la reivindicación 1 o 2, en la cual el inhibidor del reflujo es un compuesto de acuerdo con la fórmula (4) en la cual R10 representa hidrógeno, metilo, fluorometilo, difluorometilo o trifluorometilo; R11 representa hidrógeno, hidroxi, alquilo C1-7 o halógeno; R12 representa hidrógeno, alquilo C1-7 (optativamente sustituido con hidroxi, mercapto, alcoxi C1-7, tioalcoxi C1-7, arilo o heteroarilo), arilo o heteroarilo; R13 representa hidrógeno, alquilo C1-7 (optativamente sustituido con arilo o heteroarilo), arilo o heteroarilo; o una sal o solvato farmacéuticamente aceptable y los estereoisómeros del mismo. Reivindicación 6: Una combinación de acuerdo con la reivindicación 1 o 2, en la cual el inhibidor del reflujo es un compuesto de acuerdo con la fórmula (5) en la cual: R14 representa hidrógeno, hidroxi, alquilo C1-7, alcoxi C1-7 o halógeno; R15 representa hidrógeno, hidroxi, mercapto, halógeno o un grupo oxo; R16 representa hidrógeno o alquilo C1-7 (optativamente sustituido con hidroxi, mercapto, alcoxi C1-7, tioalcoxi C1-7, arilo o heteroarilo), arilo o heteroarilo; R17 representa hidrógeno, alquilo C1-7 (optativamente sustituido con arilo o heteroarilo), arilo o heteroarilo; o una sal o solvato farmacéuticamente aceptable y los estereoisómeros del mismo. Reivindicación 11: El uso de acuerdo con cualquiera de las reivindicaciones 8-10, en el cual el inhibidor del reflujo es un agonista del receptor GABAB.This is related to a medicament that comprises, just or separately, (i) at least one reflux inhibitor and (ii) at least one imidazopyrin. Another aspect of this is related to methods of treatment of gastroesophageal reflux disease, regurgitation, asthma, lack of development and lung disease. Claim 1: A combination comprising, separately or together, (i) at least one reflux inhibitor and (ii) at least one imidazopyridine of the formula (1) or a pharmaceutically acceptable salt thereof, in which R18 is H, CH3 or, CH2OH, R19 is CH3, CH2CH3; R20 is H, C1-6 alkyl, hydroxylated C1-6 alkyl, halogen; R21 H, C1-6 alkyl, hydroxylated C1-6 alkyl or, halogen; R22 is H, halogen; R23 and R24 are the same or different, selected from any of: H, C1-6 alkyl, hydroxylated C1-6 alkyl or, C1-6 alkyl substituted with C1-6 alkoxy; X is NH or O. Claim 3: A combination according to claim 1 or 2, wherein the reflux inhibitor is a compound with the formula (2) in which: R1 represents hydrogen; R2 represents hydroxy, fluorine or an oxo group; R3 represents hydrogen; R4 represents hydrogen or a pharmaceutically acceptable salt or solvate and the stereoisomers thereof. Claim 4: A combination according to claim 1 or 2, wherein the reflux inhibitor is a compound according to formula (3) in which: R5 represents hydrogen or lower alkyl; R6 represents a fluorine group; R7 represents hydrogen; R8 represents hydrogen; R9 represents methyl, fluoromethyl, difluoromethyl or trifluoromethyl or a pharmaceutically acceptable salt or solvate and the stereoisomers thereof. Claim 5: A combination according to claim 1 or 2, wherein the reflux inhibitor is a compound according to formula (4) in which R 10 represents hydrogen, methyl, fluoromethyl, difluoromethyl or trifluoromethyl; R11 represents hydrogen, hydroxy, C1-7 alkyl or halogen; R12 represents hydrogen, C1-7 alkyl (optionally substituted with hydroxy, mercapto, C1-7 alkoxy, C1-7 thioalkoxy, aryl or heteroaryl), aryl or heteroaryl; R13 represents hydrogen, C1-7 alkyl (optionally substituted with aryl or heteroaryl), aryl or heteroaryl; or a pharmaceutically acceptable salt or solvate and the stereoisomers thereof. Claim 6: A combination according to claim 1 or 2, wherein the reflux inhibitor is a compound according to formula (5) in which: R14 represents hydrogen, hydroxy, C1-7 alkyl, C1- alkoxy 7 or halogen; R15 represents hydrogen, hydroxy, mercapto, halogen or an oxo group; R16 represents hydrogen or C1-7 alkyl (optionally substituted with hydroxy, mercapto, C1-7 alkoxy, C1-7 thioalkoxy, aryl or heteroaryl), aryl or heteroaryl; R17 represents hydrogen, C1-7 alkyl (optionally substituted with aryl or heteroaryl), aryl or heteroaryl; or a pharmaceutically acceptable salt or solvate and the stereoisomers thereof. Claim 11: The use according to any of claims 8-10, wherein the reflux inhibitor is a GABAB receptor agonist.

ARP030102095A 2002-06-20 2003-06-11 COMBINATION OF A REFLUX INHIBITOR AND AN IMIDAZOPIRIDINE FOR THE TREATMENT OF GERD AR040203A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE0201940A SE0201940D0 (en) 2002-06-20 2002-06-20 New combination II

Publications (1)

Publication Number Publication Date
AR040203A1 true AR040203A1 (en) 2005-03-16

Family

ID=20288298

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030102095A AR040203A1 (en) 2002-06-20 2003-06-11 COMBINATION OF A REFLUX INHIBITOR AND AN IMIDAZOPIRIDINE FOR THE TREATMENT OF GERD

Country Status (5)

Country Link
AR (1) AR040203A1 (en)
AU (1) AU2003237739A1 (en)
SE (1) SE0201940D0 (en)
TW (1) TW200403059A (en)
WO (1) WO2004000856A1 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ547204A (en) 2000-05-26 2008-01-31 Idenix Cayman Ltd Methods and compositions for treating flaviviruses and pestiviruses
MXPA05012463A (en) * 2003-05-27 2006-01-30 Altana Pharma Ag Pharmaceutical combinations of a proton pump inhibitor and a compound which modifies gastrointestinal motility.
WO2005077345A1 (en) * 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
SE0402462D0 (en) * 2004-10-08 2004-10-08 Astrazeneca Ab New process
WO2006050471A2 (en) * 2004-11-03 2006-05-11 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use
WO2006050472A2 (en) 2004-11-03 2006-05-11 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous and -phosphinic acids
GB0525068D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
WO2008033572A1 (en) 2006-09-15 2008-03-20 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
JP2013518085A (en) 2010-02-01 2013-05-20 ノバルティス アーゲー Pyrazolo [5,1b] oxazole derivatives as CRF-1 receptor antagonists
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
ES2527849T3 (en) 2010-02-02 2015-01-30 Novartis Ag Cyclohexylamide derivatives as CRF receptor antagonists
AR086554A1 (en) 2011-05-27 2014-01-08 Novartis Ag DERIVATIVES OF PIPERIDINE 3-ESPIROCICLICA AS AGRONISTS OF GHRELINE RECEPTORS
EP2852591A1 (en) 2012-05-03 2015-04-01 Novartis AG L-malate salt of 2, 7 - diaza - spiro [4.5]dec- 7 - yle derivatives and crystalline forms thereof as ghrelin receptor agonists

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9603408D0 (en) * 1996-09-18 1996-09-18 Astra Ab Medical use
SE9801526D0 (en) * 1998-04-29 1998-04-29 Astra Ab New compounds
SE9904507D0 (en) * 1999-12-09 1999-12-09 Astra Ab New compounds
SE9904508D0 (en) * 1999-12-09 1999-12-09 Astra Ab New compounds

Also Published As

Publication number Publication date
TW200403059A (en) 2004-03-01
SE0201940D0 (en) 2002-06-20
AU2003237739A1 (en) 2004-01-06
WO2004000856A1 (en) 2003-12-31

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