AR046445A1 - Derivados de piridazin-3(2h)-ona - Google Patents

Derivados de piridazin-3(2h)-ona

Info

Publication number
AR046445A1
AR046445A1 ARP040104120A ARP040104120A AR046445A1 AR 046445 A1 AR046445 A1 AR 046445A1 AR P040104120 A ARP040104120 A AR P040104120A AR P040104120 A ARP040104120 A AR P040104120A AR 046445 A1 AR046445 A1 AR 046445A1
Authority
AR
Argentina
Prior art keywords
mono
amino
alkoxy
hydroxy
group
Prior art date
Application number
ARP040104120A
Other languages
English (en)
Inventor
Piaz Vittorio Dal
Albero Maria Antonia Buil
Maria Paola Giovannoni
Rubio Yolanda Garrido
Claudia Vergelli
Amador Wenceslao Lumeras
Izquierdo Nuria Aguilar
Jordi Gracia Ferrer
Original Assignee
Almirall Prodesfarma Sa
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 Almirall Prodesfarma Sa filed Critical Almirall Prodesfarma Sa
Publication of AR046445A1 publication Critical patent/AR046445A1/es

Links

Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/22—Nitrogen and oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Manufacturing & Machinery (AREA)
  • Pulmonology (AREA)
  • Ceramic Engineering (AREA)
  • Structural Engineering (AREA)
  • Materials Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Procedimientos para su preparación y composiciones farmacéuticas que los contienen. Estos compuestos son inhibidores de potentes y selectivos de la fosfodiesterasa 4 (PDE4) y por ello son útiles en el tratamiento, prevención o supresión de estados patológicos, enfermedades y trastornos que se conocen por ser susceptibles de mejorar mediante la inhibición de la PDE4. Reivindicación 1: Un derivado de piridazinona de fórmula (1), en el que, R1 representa: un átomo de hidrógeno; un grupo seleccionado de acilo, alcoxicarbonilo, carbamoilo, monoalquilcarbamoilo o dialquilcarbamoilo; un grupo alquilo, alquenilo o alquinilo, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, alcoxi, ariloxi, alquiltio, ariltio, oxo, amino, mono- o di-alquilamino, acilamino, hidroxicarbonilo, alcoxicarbonilo, carbamoilo o mono- o di-alquilcarbamoilo; un grupo arilo o heteroarilo que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, hidroxialquilo, hidroxicarbonilo, alcoxi, alquilendioxi, alcoxicarbonilo, ariloxi, acilo, aciloxi, alquiltio, ariltio, amino, nitro, ciano, mono- o di-alquilamino, acilamino, carbamoilo o mono- o di-alquilcarbamoilo, difluorometilo, trifluorometilo, difluorometoxi o trifluorometoxi; un grupo heterocíclico saturado o insaturado que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, hidroxialquilo, hidroxicarbonilo, alcoxi, alquilendioxi, alcoxicarbonilo, ariloxi, acilo, aciloxi, alquiltio, ariltio, oxo, amino, nitro, ciano, mono- o di-alquilamino, acilamino, carbamoilo o mono- o di-alquilcarbamoilo, difluorometilo, trifluorometilo, difluorometoxi o trifluorometoxi; un grupo de fórmula: -(CH2)n-R6, donde n es un número entero de 0 a 4 y R6 representa: un grupo cicloalquilo o cicloalquenilo; un grupo arilo, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, hidroxi, alcoxi, alquilendioxi, alquiltio, amino, mono- o di-alquilamino, nitro, acilo, hidroxicarbonilo, alcoxicarbonilo, carbamoilo, mono- o di-alquilcarbamoilo, ciano, trifluorometilo, difluorometoxi o trifluorometoxi; o un anillo de 3 a 7 miembros que comprende de 1 a 4 heteroátomos seleccionados de nitrógeno, oxígeno, y azufre, cuyo anillo está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, hidroxi, alcoxi, alquilendioxi, amino, mono- o di-alquilamino, nitro, ciano o trifluorometilo; R2 representa: un átomo de hidrógeno; un grupo seleccionado de acilo, alcoxicarbonilo, carbamoilo, monoalquilcarbamoilo o dialquilcarbamoilo; un grupo alquilo, alquenilo o alquinilo, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, alcoxi, hidroxicarbonilo, alcoxicarbonilo, ariloxi, alquiltio, ariltio, oxo, amino, mono- o di-alquilamino, acilamino, carbamoilo o mono- o di-alquilcarbamoilo; un grupo arilo o heteroarilo que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, hidroxialquilo, hidroxicarbonilo, alcoxi, alquilendioxi, alcoxicarbonilo, ariloxi, acilo, aciloxi, alquiltio, ariltio, amino, nitro, ciano, mono- o di-alquilamino, acilamino, carbamoilo o mono- o di-alquilcarbamoilo, difluorometilo, trifluorometilo, difluorometoxi o trifluorometoxi; un grupo heterocíclico saturado o insaturado que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, hidroxialquilo, hidroxicarbonilo, alcoxi, alquilendioxi, alcoxicarbonilo, ariloxi, acilo, aciloxi, alquiltio, ariltio, oxo, amino, nitro, ciano, mono- o di-alquilamino, acilamino, carbamoilo o mono- o di-alquilcarbamoilo, difluorometilo, trifluorometilo, difluorometoxi o trifluorometoxi; un grupo de fórmula: -(CH2)n-R6, donde n es un número entero de 0 a 4 y R6 representa: un grupo cicloalquilo o cicloalquenilo; un grupo arilo, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, hidroxi, alcoxi, alquilendioxi, alquiltio, amino, mono- o di-alquilamino, nitro, acilo, hidroxicarbonilo, alcoxicarbonilo, carbamoilo, mono- o di-alquilcarbamoilo, ciano, trifluorometilo, difluorometoxi o trifluorometoxi; o un anillo de 3 a 7 miembros que comprende de 1 a 4 heteroátomos seleccionados de nitrógeno, oxígeno, y azufre, cuyo anillo está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, hidroxi, alcoxi, alquilendioxi, amino, mono- o di-alquilamino, nitro, ciano o trifluorometilo; R3 representa un grupo arilo o heteroarilo monocíclico o policíclico, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de: átomos de halógeno; un grupo alquilo y alquenilo, que están sustituidos opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos fenilo, hidroxi, alcoxi, ariloxi, alquiltio, ariltio, oxo, amino, mono- o di-alquilamino, acilamino, hidroxicarbonilo, alcoxicarbonilo, carbamoilo o mono- o di-alquilcarbamoilo; grupos fenilo, hidroxi, hidroxialquilo, alcoxi, cicloalcoxi, nitro, ciano, ariloxi, alquiltio, ariltio, alquilsulfinilo, alquilsulfonilo, alquilsulfamoilo, acilo, amino, mono- o di-alquilamino, acilamino, hidroxicarbonilo, alcoxicarbonilo, carbamoilo, mono- o di-alquilcarbamoilo, ureido, N'-alquilureido, N',N'-dialquilureido, alquilsulfamido, aminosulfonilo, mono- o di-alquilaminosulfonilo, difluorometoxi o trifluorometoxi; R4 representa: un átomo de hidrógeno; un grupo hidroxi, alcoxi, amino, monoalquilamino, dialquilamino o ciano; un grupo alquilo, alquenilo o alquinilo, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, aciloxi, alcoxi, ariloxi, alquiltio, ariltio, amino, mono- o di-alquilamino, acilamino, hidroxicarbonilo, alcoxicarbonilo, alcoxiimino, carbamoilo y mono- o di-alquilcarbamoilo; o un grupo de fórmula: -(CH2)n-R6, donde n es un número entero de 0 a 4 y R6 representa un grupo cicloalquilo o cicloalquenilo; un grupo arilo, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, hidroxi, alcoxi, alquilendioxi, alquiltio, amino, mono- o di-alquilamino, nitro, acilo, hidroxicarbonilo, alcoxicarbonilo, carbamoilo, mono- o di-alquilcarbamoilo, ciano, trifluorometilo, difluorometoxi o trifluorometoxi; o un anillo de 3 a 7 miembros que comprende de 1 a 4 heteroátomos seleccionados de nitrógeno, oxígeno, y azufre, cuyo anillo está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, fenilo, alcoxifenilo, halofenilo, piridilo, alcoxicarbonilo, hidroxi, alcoxi, alquilendioxi, amino, mono- o di-alquilamino, nitro, ciano o trifluorometilo; R5 representa un grupo -COOR7 o un grupo arilo o heteroarilo monocíclico o policíclico, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de: átomos de halógenos; un grupo alquilo y alquenilo, que están sustituidos opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos fenilo, hidroxi, hidroxialquilo, alcoxi, ariloxi, alquiltio, ariltio, oxo, amino, mono- o di-alquilamino, acilamino, hidroxicarbonilo, alcoxicarbonilo, carbamoilo o mono- o di-alquilcarbamoilo; y grupos fenilo, hidroxi, alquilendioxi, alcoxi, cicloalcoxi, alquiltio, alquilsulfinilo, alquilsulfonilo, alquilsulfamoilo, amino, mono- o di-alquilamino, acilamino, nitro, acilo, hidroxicarbonilo, alcoxicarbonilo, carbamoilo, mono- o di-alquilcarbamoilo, ureido, N'-alquilureido, N',N'-dialquilureido, alquilsulfamido, aminosulfonilo, mono- o di-alquilaminosulfonilo, ciano, difluorometoxi o trifluorometoxi; en el que R7 representa un alquilo que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos hidroxi, alcoxi, ariloxi, alquiltio, ariltio, oxo, amino, amino, mono- o di-alquilamino, acilamino, hidroxicarbonilo, alcoxicarbonilo, carbamoilo, mono- o di-alquilcarbamoilo o un grupo de fórmula: -(CH2)n-R6, donde n es un número entero de 0 a 4 y R6 representa un grupo cicloalquilo o cicloalquenilo; un grupo arilo, que está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, hidroxi, alcoxi, alquilendioxi, alquiltio, amino, mono- o di-alquilamino, nitro, acilo, hidroxicarbonilo, alcoxicarbonilo, carbamoilo, mono- o di-alquilcarbamoilo, ciano, trifluorometilo, difluorometoxi o trifluorometoxi; o un anillo de 3 a 7 miembros que comprende de 1 a 4 heteroátomos seleccionados de nitrógeno, oxígeno, y azufre, cuyo anillo está sustituido opcionalmente por uno o más sustituyentes seleccionados de átomos de halógenos y grupos alquilo, fenilo, alcoxifenilo, halofenilo, piridilo, alcoxicarbonilo, hidroxi, alcoxi, alquilendioxi, amino, mono- o di-alquilamino, nitro, ciano o trifluorometilo; y su sales o N-óxidos de los mismos; con la condición de que cuando R1 es metilo, R2 es H, y tanto R3 como R5 son fenilo, entonces R4 no es grupo 1-hidroxietilo.
ARP040104120A 2003-11-10 2004-11-09 Derivados de piridazin-3(2h)-ona AR046445A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES200302613A ES2232306B1 (es) 2003-11-10 2003-11-10 Nuevos derivados de piridazin-3(2h)-ona.

Publications (1)

Publication Number Publication Date
AR046445A1 true AR046445A1 (es) 2005-12-07

Family

ID=34586123

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040104120A AR046445A1 (es) 2003-11-10 2004-11-09 Derivados de piridazin-3(2h)-ona

Country Status (20)

Country Link
US (1) US7511038B2 (es)
EP (1) EP1682519A1 (es)
JP (1) JP2007510689A (es)
KR (1) KR20070001907A (es)
CN (1) CN1878759A (es)
AR (1) AR046445A1 (es)
AU (1) AU2004291282A1 (es)
BR (1) BRPI0416212A (es)
CA (1) CA2545193A1 (es)
CO (1) CO5690558A2 (es)
EC (1) ECSP066541A (es)
ES (1) ES2232306B1 (es)
IL (1) IL175278A0 (es)
NO (1) NO20062726L (es)
PE (1) PE20050490A1 (es)
RU (1) RU2006120082A (es)
TW (1) TW200526593A (es)
UA (1) UA82420C2 (es)
WO (1) WO2005049581A1 (es)
ZA (1) ZA200602415B (es)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
US7214687B2 (en) 1999-07-14 2007-05-08 Almirall Ag Quinuclidine derivatives and medicinal compositions containing the same
ES2211344B1 (es) 2002-12-26 2005-10-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
EP1604988A1 (en) * 2004-05-18 2005-12-14 Sanofi-Aventis Deutschland GmbH Pyridazinone derivatives, methods for producing them and their use as pharmaceuticals
ES2257152B1 (es) 2004-05-31 2007-07-01 Laboratorios Almirall S.A. Combinaciones que comprenden agentes antimuscarinicos y agonistas beta-adrenergicos.
ES2251866B1 (es) 2004-06-18 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2251867B1 (es) * 2004-06-21 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
CA2584261A1 (en) * 2004-10-13 2006-04-20 Kyowa Hakko Kogyo Co., Ltd. Pharmaceutical composition
US20070287689A1 (en) * 2004-10-13 2007-12-13 Kyowa Hakko Kogyo Co., Ltd. Therapeutic And/Or Preventive Agents For Chronic Skin Diseases
ES2265276B1 (es) 2005-05-20 2008-02-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
ES2298049B1 (es) 2006-07-21 2009-10-20 Laboratorios Almirall S.A. Procedimiento para fabricar bromuro de 3(r)-(2-hidroxi-2,2-ditien-2-ilacetoxi)-1-(3-fenoxipropil)-1-azoniabiciclo (2.2.2) octano.
ES2306595B1 (es) 2007-02-09 2009-09-11 Laboratorios Almirall S.A. Sal de napadisilato de 5-(2-((6-(2,2-difluoro-2-feniletoxi)hexil)amino)-1-hidroxietil)-8-hidroxiquinolin-2(1h)-ona como agonista del receptor adrenergico beta2.
ES2320955B1 (es) 2007-03-02 2010-03-16 Laboratorios Almirall S.A. Nuevos derivados de 3-((1,2,4)triazolo(4,3-a)piridin-7-il)benzamida.
ES2320954B1 (es) * 2007-03-02 2010-03-16 Laboratorio Almirall S.A. Nuevo procedimiento de preparacion de 3-metil-4-fenilisoxazolo (3,4-d)iridazin-7(6h)-ona.
ES2320961B1 (es) 2007-11-28 2010-03-17 Laboratorios Almirall, S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor adrenergico beta2.
ES2420846T3 (es) * 2008-02-05 2013-08-27 F. Hoffmann-La Roche Ag Nuevas piridinonas y piridazinonas
EP2096105A1 (en) * 2008-02-28 2009-09-02 Laboratorios Almirall, S.A. Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the b2 adrenergic receptor
EP2100599A1 (en) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
EP2100598A1 (en) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
EP2108641A1 (en) 2008-04-11 2009-10-14 Laboratorios Almirall, S.A. New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
EP2113503A1 (en) 2008-04-28 2009-11-04 Laboratorios Almirall, S.A. New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
EP2196465A1 (en) * 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
UY32297A (es) 2008-12-22 2010-05-31 Almirall Sa Sal mesilato de 5-(2-{[6-(2,2-difluoro-2-fenilitoxi) hexil]amino}-1-hidroxietil)-8-hidroxiquinolin-2( 1h)-ona como agonista del receptor b(beta)2 acrenérgico
EP2221297A1 (en) 2009-02-18 2010-08-25 Almirall, S.A. 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one and its use in the treatment of pulmonary diseases
EP2221055A1 (en) 2009-02-18 2010-08-25 Almirall, S.A. 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one for the treatment of lung function
EP2228368A1 (en) 2009-03-12 2010-09-15 Almirall, S.A. Process for manufacturing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one
EP2322176A1 (en) 2009-11-11 2011-05-18 Almirall, S.A. New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2360158A1 (en) 2010-02-18 2011-08-24 Almirall, S.A. Pyrazole derivatives as jak inhibitors
EP2386555A1 (en) 2010-05-13 2011-11-16 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities
EP2394998A1 (en) * 2010-05-31 2011-12-14 Almirall, S.A. 3-(5-Amino-6-oxo-1,6-dihydropyridazin-3-yl)-biphenyl derivatives as PDE4 inhibitors
EP2397482A1 (en) 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
EP2441755A1 (en) 2010-09-30 2012-04-18 Almirall, S.A. Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
EP2457900A1 (en) 2010-11-25 2012-05-30 Almirall, S.A. New pyrazole derivatives having CRTh2 antagonistic behaviour
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
EP2510928A1 (en) 2011-04-15 2012-10-17 Almirall, S.A. Aclidinium for use in improving the quality of sleep in respiratory patients
EP2518070A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
EP2518071A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Imidazopyridine derivatives as PI3K inhibitors
EP2526945A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. New CRTH2 Antagonists
EP2527344A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases
EP2548863A1 (en) 2011-07-18 2013-01-23 Almirall, S.A. New CRTh2 antagonists.
EP2548876A1 (en) 2011-07-18 2013-01-23 Almirall, S.A. New CRTh2 antagonists
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
EP2578570A1 (en) 2011-10-07 2013-04-10 Almirall, S.A. Novel process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(r)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one via novel intermediates of synthesis.
EP2592077A1 (en) 2011-11-11 2013-05-15 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
EP2592078A1 (en) 2011-11-11 2013-05-15 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
EP2641900A1 (en) 2012-03-20 2013-09-25 Almirall, S.A. Novel polymorphic Crystal forms of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one, heminapadisylate as agonist of the ß2 adrenergic receptor.
EP2647627A1 (en) 2012-04-02 2013-10-09 Almirall, S.A. Salts of 5-[(1r)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl] ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1h)-one.
EP2666465A1 (en) 2012-05-25 2013-11-27 Almirall, S.A. Novel dosage and formulation
EP2668941A1 (en) 2012-05-31 2013-12-04 Almirall, S.A. Novel dosage form and formulation of abediterol
MX2014015156A (es) * 2012-06-12 2015-08-06 Abbvie Inc Derivados de piridinona y piridazinona.
WO2014060431A1 (en) 2012-10-16 2014-04-24 Almirall, S.A. Pyrrolotriazinone derivatives as pi3k inhibitors
EP2738172A1 (en) 2012-11-28 2014-06-04 Almirall, S.A. New bicyclic compounds as crac channel modulators
PT2931275T (pt) 2012-12-17 2022-06-30 Almirall Sa Aclidínio para usar no aumento da atividade física na vida diária de um doente que sofre de doença pulmonar obstrutiva crónica
ES2750523T3 (es) 2012-12-18 2020-03-26 Almirall Sa Derivados de ciclohexil y quinuclidinil carbamato que tienen actividades de agonista beta2 adrenérgicos y antagonistas muscarínicos M3
UY35332A (es) 2013-02-15 2014-11-28 Almirall Sa Derivados de pirrolotriazina como inhibidores de pi3k
EP2848615A1 (en) 2013-07-03 2015-03-18 Almirall, S.A. New pyrazole derivatives as CRAC channel modulators
FR3027901B1 (fr) * 2014-10-31 2018-03-16 Universite De Reims Champagne Ardenne Nouveaux procedes appartenant a la famille des pyridazinones.
US11319318B2 (en) * 2015-03-05 2022-05-03 Boehringer Ingelheim International Gmbh Pyridinones and isoquinolinones as inhibitors of the bromodomain BRD9
CN112533601A (zh) * 2018-06-04 2021-03-19 俄亥俄州创新基金会 Eaat2活化剂及其使用方法
CN109620829B (zh) * 2018-12-29 2021-04-06 温州医科大学附属第一医院 一种治疗急性呼吸窘迫综合征的药物组合物及其制备方法
TW202321229A (zh) * 2021-08-18 2023-06-01 美商富曼西公司 殺真菌的取代的雜環化合物
WO2023204124A1 (ja) * 2022-04-20 2023-10-26 日本曹達株式会社 ピリダジノン化合物並びに農園芸用殺菌剤、殺線虫剤、および医療用・動物用抗真菌剤

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2824873A (en) * 1958-02-25 Production of pyridazone derivatives
US2786840A (en) * 1957-03-26 Aminopyridazone compounds and their
DE579391C (de) * 1932-02-07 1933-06-24 Schering Kahlbaum Ag Verfahren zur Darstellung von in 5-Stellung substituierten 1, 3-Dialkylpyridazonen
GB656228A (en) * 1948-12-30 1951-08-15 Walter Norman Haworth The manufacture of analgesics from pyridazone and pyridazine derivatives
GB788393A (en) * 1953-04-30 1958-01-02 Ciba Ltd Process for the manufacture of pyridazone compounds
DE932489C (de) * 1953-09-11 1955-09-01 Hoffmann La Roche Verfahren zur Herstellung von neuen Xanthinbasen und deren Salzen
GB794870A (en) * 1955-05-07 1958-05-14 Basf Ag A process for the production of 3-oxo-2,3-dihydropyridazine derivatives
GB788502A (en) * 1956-05-30 1958-01-02 Chimie Atomistique Pyridazine compounds and process of preparing the latter
US2834780A (en) * 1956-07-05 1958-05-13 Dow Chemical Co Phthalidyl piperazines
US3014034A (en) * 1959-01-22 1961-12-19 Ciba Pharm Prod Inc 1, 3-diaryl, 5-amino-pyridazinones
GB889317A (en) * 1959-01-22 1962-02-14 Ciba Ltd New phenyl-diazines and a process for their manufacture
SU405344A1 (ru) 1970-06-01 1975-08-25 Всесоюзный научно-исследовательский химико-фармацевтический институт им. С.Орджоникидзе Способ получени производных 3-замещенных 5-(2-оксифениламино)-пиридазона-6
JPS5312880A (en) * 1976-07-21 1978-02-04 Morishita Pharma Pyridazinone derivatives
TWI241295B (en) * 1998-03-02 2005-10-11 Kowa Co Pyridazine derivative and medicine containing the same as effect component
AU2001262332B2 (en) * 2000-06-05 2006-05-25 Altana Pharma Ag Compounds effective as beta-2-adrenoreceptor agonists as well as PDE4-inhibitors
SI1471054T1 (sl) * 2002-01-11 2009-12-31 Daiichi Sankyo Co Ltd Amino alkoholni derivati ali derivati fosfoniäśne kisline in medicinski sestavki, ki vsebujejo le-te
ES2211344B1 (es) * 2002-12-26 2005-10-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
WO2004085406A1 (en) * 2003-03-24 2004-10-07 F. Hoffmann-La Roche Ag Benzyl-pyridazinons as reverse transcriptase inhibitors

Also Published As

Publication number Publication date
KR20070001907A (ko) 2007-01-04
IL175278A0 (en) 2006-09-05
BRPI0416212A (pt) 2007-01-02
ES2232306B1 (es) 2006-08-01
US7511038B2 (en) 2009-03-31
EP1682519A1 (en) 2006-07-26
JP2007510689A (ja) 2007-04-26
RU2006120082A (ru) 2008-01-10
CO5690558A2 (es) 2006-10-31
WO2005049581A1 (en) 2005-06-02
CN1878759A (zh) 2006-12-13
ZA200602415B (en) 2007-11-28
UA82420C2 (en) 2008-04-10
AU2004291282A1 (en) 2005-06-02
WO2005049581A8 (en) 2006-05-04
ECSP066541A (es) 2006-12-20
ES2232306A1 (es) 2005-05-16
NO20062726L (no) 2006-06-12
CA2545193A1 (en) 2005-06-02
PE20050490A1 (es) 2005-08-24
US20070197536A1 (en) 2007-08-23
TW200526593A (en) 2005-08-16

Similar Documents

Publication Publication Date Title
AR046445A1 (es) Derivados de piridazin-3(2h)-ona
AR042665A1 (es) Derivados de piridazin -3 (2 h) - ona
AR040076A1 (es) Derivados de piridazin-3(2h)-ona
AR051738A1 (es) Derivados de piridazin-3(2h)-ona, composicin farmaceutica, y uso del compuesto para fabricar medicamentos
AR049402A1 (es) Derivados de piridazin-3-(2h)-ona
PE20220931A1 (es) Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina
TW200611907A (en) Fused heterocyclic compound
ES2601518T3 (es) Composiciones plaguicidas
NZ533310A (en) Benzimidazoles useful as protein kinase inhibitors
AR082888A1 (es) Compuestos de piridina para la inhibicion de nampt
AR057979A1 (es) PIRAZOLPIRIMIDINAS COMO INHIBIDORAS DE PROTEíNA QUINASA. COMPOSICIONES FARMACEUTICAS.
TW200800949A (en) Macrocylic inhibitors of hepatitis C virus
AR076798A1 (es) Pirazinilpirazoles y composiciones que comprenden dichos compuestos
PE20030062A1 (es) Derivados aralquilsulfonil-3-(pirrol-2-ilmetiliden)-2-indolinona como inhibidores de quinasas
MX2010000658A (es) Derivados de pirimidina 934.
RU2008152065A (ru) Новое производное имидазола со спироциклической структурой в боковой цепи
WO2007149448A3 (en) Pyrazinones as cellular proliferation inhibitors
AR062965A1 (es) Compuestos moduladores de receptores de glutamatometabotropicos mglur5, composiciones farmaceuticas que los contienen y usos terapeuticos en trastornos gastrointestinales, neurologicos y psiquiatricos agudos y cronicos
CY1107747T1 (el) Υποκατεστημενα τετρακυκλικα παραγωγα πυρρολοκινολονης χρησιμα ως αναστολεις της φωσφοδιεστερασης
MX2009006650A (es) Pirimidinas substituidas que contienen una porcion heteroarilamida o heteroarilfenilo.
EA200700758A1 (ru) Новые производные бис-азаиндолов, их получение и фармацевтическое применение в качестве ингибиторов киназ
CY1110145T1 (el) Αλκυλο-υποκατεστημενες ινδολοκινοξαλινες
PE20201068A1 (es) Compuestos de pirazol sustituidos con heteroarilo y uso farmaceutico de los mismos
HRP20050082A2 (en) 6-amino-1h-indazole and 4-aminobenzofuran compounds as phosphodiesterase 4 inhibitors
AR045791A1 (es) Derivados de triazol sustituidos como antagonistas de oxitocina

Legal Events

Date Code Title Description
FB Suspension of granting procedure