AR042275A1 - Imidazo- piridinosas sustituidas, su preparacion y su empleo como medicamentos - Google Patents

Imidazo- piridinosas sustituidas, su preparacion y su empleo como medicamentos

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Publication number
AR042275A1
AR042275A1 ARP030104444A ARP030104444A AR042275A1 AR 042275 A1 AR042275 A1 AR 042275A1 AR P030104444 A ARP030104444 A AR P030104444A AR P030104444 A ARP030104444 A AR P030104444A AR 042275 A1 AR042275 A1 AR 042275A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
phenyl
substituted
atom
Prior art date
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Suspension/Interruption
Application number
ARP030104444A
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English (en)
Inventor
Hauel Norbert Dr
Himmelsbach Frank Dr
Langkopf Elke Dr
Mathias Eckhardt
Roland Maier
Michael Mark
Tadayyon Mohammad Dr
Iris Kauffmann-Hefner
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH Co KG
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Boehringer Ingelheim Pharma GmbH Co KG
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Filing date
Publication date
Priority claimed from DE2002156264 external-priority patent/DE10256264A1/de
Priority claimed from DE2003109927 external-priority patent/DE10309927A1/de
Application filed by Boehringer Ingelheim Pharma GmbH Co KG filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of AR042275A1 publication Critical patent/AR042275A1/es
Suspension/Interruption legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0031Rectum, anus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
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    • A61K9/10Dispersions; Emulsions
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    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
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    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
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    • 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
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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    • AHUMAN NECESSITIES
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    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/10Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Hematology (AREA)
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  • Rheumatology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Imidazo-piridinonas e imidazo-piridazinonas sustituidas de la fórmula general (1), en la que significa: X un átomo de nitrógeno o un grupo de la fórmula C-R5, significa R5 un átomo de hidrógeno o un grupo metilo, R1 un grupo cicloalquilenimino de 5 a 7 miembros que está sustituido en el esqueleto de carbonos con un grupo amino y que puede estar sustituido con un grupo alquilo C1-3, un grupo cicloalquilenimino de 6 a 7 miembros, en el que el grupo metileno en posición 4 está reemplaza por un grupo -NH, o un grupo amino sustituido con un grupo cicloalquilo C5-7 estando el grupo cicloalquilo C5-7 sustituido con un grupo amino, o un átomo de carbono en la posición 3 del grupo cicloalquilo C5-7 está reemplazado por un grupo -NH; R2 un grupo bencilo, en el que radical fenilo pude estar sustituido con uno o dos átomos de flúor, cloro o bromo o con un grupo ciano, un grupo alquenilo C3-8 lineal o ramificado, un grupo alquinilo C3-5, un grupo cicloalquil C3-7-metilo, un grupo cicloalquenil C5-7-metilo, o un grupo furilmetilo, tienilmetilo, pirrolilmetilo, tiazolilmetilo, imidazolilmetilo, piridinilmetilo, pirimidinilmetilo, piridazinilmetilo o pirazinilmetilo; R3 un grupo alquilo C1-6 lineal o ramificado, un grupo fenil-alquilo C1-3, o naftil-alquilo C1-3, eventualmente sustituido en la parte de arilo con un átomo de halógeno, un grupo ciano, un grupo alquilo C1-3 o un grupo metoxi, un grupo 2-fenil-2-hidroxi-etilo, un grupo fenilcarbonilmetilo, en el que el grupo fenilo puede estar sustituido con un grupo hidroxi, alquiloxi C1-3, aminocarbonil-alcoxi C1-3, (alquil(C1-3)-amino)-carbonil-alcoxi C1-3, [di-(alquil C1-3)-amino]-carbonil-alcoxi C1-3, amino, alquil(C1-3)-carbanilamino, cicloalquil(C3-6)-carbonilamino, alcoxi(C1-3)-carbonilamino, alquil(C1-3)-sulfonilamino o aminocarbonilo, un grupo (3-metil-2-oxo-2,3-dihidro-benzoxazolil)-carbonilmetilo, un grupo tienilcarbonilmetilo, un grupo heteroaril-alquilo C1-3, debiéndose entender por la expresión "grupo heteroarilo" un grupo heteroarilo monocíclico, de 5 ó 6 miembros, eventualmente sustituido con uno o dos grupos alquilo C1-3 o con un grupo morfolin-4-ilo, piridilo o fenilo, en donde el grupo heteroarilo de 6 miembros contiene uno, dos o tres átomos de nitrógeno, y el grupo heteroarilo de 5 miembros contienen un grupo imino, eventualmente sustituido con un grupo alquilo C1-3 o fenil-alquilo C1-3, un átomo de oxígeno o azufre, o un grupo imino, eventualmente sustituido con un grupo alquilo C1-3 o fenil-alquilo C1-3, o un átomo de oxígeno o azufre y, adicionalmente, un átomo de nitrógeno, o un grupo imino, eventualmente sustituido con un grupo alquilo C1-3 o fenil-alquilo C1-3, o un átomo de oxígeno o azufre y, adicionalmente, dos o tres átomos de nitrógeno, y, en donde, adicionalmente, a los grupos heteroarilo monocíclicos precedentemente mencionados puede estar condensado un anillo de fenilo a través de dos átomos de carbono contiguos, el cual puede estar eventualmente sustituido con un átomo de halógeno, con uno o dos grupos alquilo C1-3, o con un grupo trifluorometilo o metoxi, y el enlace puede realizarse a través de un átomo de la parte heterocíclica o del anillo de fenilo condensado, un grupo heteroarilmetilo bicíclico conforme a un resto de grupo de fórmula (2), o un grupo de la fórmula (3), un grupo de fórmula (4), en la que R6 significa en cada caso un átomo de hidrógeno o un grupo metilo, y R4 un átomo de hidrógeno o un grupo alquilo C1-3, pudiendo los grupos alquilo y alcoxi contenidos en las definiciones, que presentan más de dos átomos de carbono, si no se mencionó de otro modo, ser de cadena lineal o ramificados, y en donde los átomos de hidrógeno de los grupos metilo o etilo contenidos en las definiciones están reemplazados, en su totalidad o en parte, por átomos de flúor, sus tautómeros, sus enantiómeros, sus diastereoisómeros, sus mezclas y sus sales, que presentan valiosas propiedades farmacológicas, en particular un efecto inhibidor de la actividad de la enzima dipeptidilpeptidasa-IV (DDP-IV).
ARP030104444A 2002-12-03 2003-12-03 Imidazo- piridinosas sustituidas, su preparacion y su empleo como medicamentos Suspension/Interruption AR042275A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2002156264 DE10256264A1 (de) 2002-12-03 2002-12-03 Neue substituierte Imidazo-pyridinone und Imidazo-pyridazinone, ihre Herstellung und ihre Verwendung als Arzneimittel
DE2003109927 DE10309927A1 (de) 2003-03-07 2003-03-07 Neue substituierte Imidazo-pyridinone und Imidazo-pyridazinone, ihre Herstellung und ihre Verwendung als Arzneimittel

Publications (1)

Publication Number Publication Date
AR042275A1 true AR042275A1 (es) 2005-06-15

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ARP030104444A Suspension/Interruption AR042275A1 (es) 2002-12-03 2003-12-03 Imidazo- piridinosas sustituidas, su preparacion y su empleo como medicamentos

Country Status (12)

Country Link
EP (1) EP1569936B1 (es)
JP (1) JP4726493B2 (es)
AR (1) AR042275A1 (es)
AT (1) ATE425979T1 (es)
AU (1) AU2003293757A1 (es)
CA (1) CA2508233C (es)
DE (1) DE50311318D1 (es)
ES (1) ES2324294T3 (es)
PE (1) PE20040759A1 (es)
TW (1) TW200504067A (es)
UY (1) UY28103A1 (es)
WO (1) WO2004050658A1 (es)

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