ES2526352T3 - Derivados de piridazinona - Google Patents

Derivados de piridazinona Download PDF

Info

Publication number
ES2526352T3
ES2526352T3 ES08758359T ES08758359T ES2526352T3 ES 2526352 T3 ES2526352 T3 ES 2526352T3 ES 08758359 T ES08758359 T ES 08758359T ES 08758359 T ES08758359 T ES 08758359T ES 2526352 T3 ES2526352 T3 ES 2526352T3
Authority
ES
Spain
Prior art keywords
nhet
conr3
nhconh
atoms
nhet1
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES08758359T
Other languages
English (en)
Inventor
Dieter Dorsch
Frank Stieber
Oliver Schadt
Andree Blaukat
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Application granted granted Critical
Publication of ES2526352T3 publication Critical patent/ES2526352T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D403/10Heterocyclic 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 aromatic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • 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
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • 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
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/02Suppositories; Bougies; Bases therefor; Ovules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • 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
    • A61K9/2004Excipients; 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • 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
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/282Organic compounds, e.g. fats
    • A61K9/2826Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)

Abstract

Compuestos de la fórmula I**Fórmula** en donde R1 representa Ar o Het, R2 representa un heterociclo insaturado, saturado o aromático de 6 miembros con 1 a 4 átomos de N-, O- y/o S, que es mono-, di- o tri- sustituido por N>=CR3N(R3)2, SR3, NO2, CN, COOR3; CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, [C(R3)2]nN(R3)2, [C(R3)2]nHet, O[C(R3)2]pOR3, O[C(R3)2]nN(R3)2, O[C(R3)2]nC>=C[C(R3)2]nN(R3)2, O[C(R3)2]nN+O-(R3)2, O[C(R3)2]nHet, S[C(R3)2]nN(R3)2, S[C(R3)2]nHet, NR3[C(R3)2]nN(R3)2, NR3[C(R3)2]nHet, NHCON(R3)2, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet, [C(R3)2]nNHCO[C(R3)2]nN(R3)2, [C(R3)2]nNHCO[C(R3)2]nHet, CON(R3)2, CONR3[C(R3)2]nN(R3)2, CONR3[C(R3)2]nNR3COOA, CONR3[C(R3) 2]nOR3, CONR3[C(R3)2]nHet, COHet, COA, CH>=CH-COOR3 y/o CH>=CH-N(R3)2, R3 representa H o A, R4, R4, respectivamente de forma independiente el uno del otro, representan H, Hal, A, OR3, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2 ó S(O)mA, Ar representa fenilo, naftilo o bifenilo no sustituido o mono-, di- o tri- sustituido por Hal, A, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het, Het, O[C(R3)2]nN(R3)2. O[C(R3)2]nHet, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet, NHCONH[C(R3)2]nN(R3)2, NHCONH[ C(R3)2]nHet, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet, CONR3[C(R3)2]nN(R3)2, CONR3[C(R320 )2]nHet y/o COA, Het representa un heterociclo saturado, insaturado o aromático mononuclear, binuclear o trinuclear con 1 a 4 átomos de N, O y/o S, que puede ser no sustituido o mono- di-, tri-, tetra- o penta- sustituido por Hal, A, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het1, [C(R3)2]nHet1, O[C(R3)2]n(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1, CO-Het1, CHO, COA, >=S, >=NH, >=NA y/o >=O (oxígeno de carbonilo), y donde un nitrógeno anular puede ser oxidado, Het1 representa un heterociclo saturado mononuclear con 1 a 2 átomos de N y/o de O que puede ser mono- o disustituido por A, OA, OH, Hal y/o >=O (oxígeno de carbonilo), A representa alquilo no ramificado o ramificado con 1-10 átomos de C, en donde 1-7 átomos de H pueden ser reemplazados por F, y/o en donde uno o dos grupos CH2 no contiguos pueden ser reemplazados por O, NH, S, SO, SO2 y/o por grupos CH>=CH, o alquilo cíclico con 3-7 átomos de C, Hal representa F, Cl, Br o I, m representa 0, 1 ó 2, n representa 0, 1, 2, 3 ó 4, p representa 1, 2, 3 ó 4.
ES08758359T 2007-07-12 2008-04-29 Derivados de piridazinona Active ES2526352T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102007032507A DE102007032507A1 (de) 2007-07-12 2007-07-12 Pyridazinonderivate
DE102007032507 2007-07-12
PCT/EP2008/003473 WO2009006959A1 (de) 2007-07-12 2008-04-29 Pyridazinonderivate

Publications (1)

Publication Number Publication Date
ES2526352T3 true ES2526352T3 (es) 2015-01-09

Family

ID=39638671

Family Applications (3)

Application Number Title Priority Date Filing Date
ES14001269T Active ES2614283T3 (es) 2007-07-12 2008-04-29 Derivados de piridazinona
ES08758359T Active ES2526352T3 (es) 2007-07-12 2008-04-29 Derivados de piridazinona
ES08773881T Active ES2388883T3 (es) 2007-07-12 2008-07-04 Derivados de pirimidinil-piridazinona

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES14001269T Active ES2614283T3 (es) 2007-07-12 2008-04-29 Derivados de piridazinona

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES08773881T Active ES2388883T3 (es) 2007-07-12 2008-07-04 Derivados de pirimidinil-piridazinona

Country Status (36)

Country Link
US (8) US8580781B2 (es)
EP (3) EP2754660B1 (es)
JP (2) JP5426543B2 (es)
KR (2) KR101553418B1 (es)
CN (2) CN101743241B (es)
AR (2) AR066543A1 (es)
AU (2) AU2008274670B2 (es)
BR (2) BRPI0814616B1 (es)
CA (2) CA2693600C (es)
CL (1) CL2008001392A1 (es)
CO (2) CO6170360A2 (es)
CY (4) CY1113137T1 (es)
DE (1) DE102007032507A1 (es)
DK (3) DK2754660T3 (es)
EA (2) EA016782B1 (es)
EC (2) ECSP109953A (es)
ES (3) ES2614283T3 (es)
FR (1) FR22C1024I2 (es)
HK (2) HK1142891A1 (es)
HR (3) HRP20120661T1 (es)
HU (2) HUE030519T2 (es)
IL (2) IL203091A (es)
LT (2) LT2754660T (es)
MY (2) MY153727A (es)
NL (1) NL301176I2 (es)
NO (1) NO2022015I1 (es)
NZ (1) NZ583187A (es)
PE (1) PE20090287A1 (es)
PL (3) PL2164843T3 (es)
PT (3) PT2164843E (es)
SG (1) SG183739A1 (es)
SI (3) SI2164843T1 (es)
TW (1) TWI501768B (es)
UA (2) UA99621C2 (es)
WO (2) WO2009006959A1 (es)
ZA (1) ZA201001023B (es)

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007038957A1 (de) * 2007-08-17 2009-02-19 Merck Patent Gmbh 6-Thioxo-pyridazinderivate
DE102007041115A1 (de) * 2007-08-30 2009-03-05 Merck Patent Gmbh Thiadiazinonderivate
DE102007061963A1 (de) * 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
DE102008019907A1 (de) 2008-04-21 2009-10-22 Merck Patent Gmbh Pyridazinonderivate
DE102008028905A1 (de) 2008-06-18 2009-12-24 Merck Patent Gmbh 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate
DE102008037790A1 (de) * 2008-08-14 2010-02-18 Merck Patent Gmbh Bicyclische Triazolderivate
PE20120016A1 (es) * 2008-12-22 2012-01-24 Merck Patent Gmbh Nuevas formas polimorficas de dihidrogeno-fosfato de 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2h-piridazin-3-ona y procesos para su preparacion
DE102008062826A1 (de) * 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
DE102009003954A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Pyridazinonderivate
CA2749012C (en) 2009-01-08 2017-01-31 Merck Patent Gmbh Polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof
EP2221053A1 (de) * 2009-02-20 2010-08-25 Albert-Ludwigs-Universität Freiburg Pharmazeutische Zusammensetzung enthaltend Hemmstoffe der Proteinmethyltransferase I und deren Verwendung zur Behandlung von Tumorerkrankungen
WO2012003338A1 (en) 2010-07-01 2012-01-05 Takeda Pharmaceutical Company Limited COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET
DE102011101482B4 (de) 2011-05-13 2017-05-11 Thyssenkrupp Presta Aktiengesellschaft Sensoranordnung für eine drehbare Welle
EP2827872A1 (en) * 2012-03-19 2015-01-28 Merck Patent GmbH Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with other anti-tumor compounds
KR101842645B1 (ko) * 2012-04-12 2018-03-29 한국화학연구원 신규한 히드라진온이 치환된 피리미딘 유도체 및 그의 용도
WO2014056566A1 (en) * 2012-10-11 2014-04-17 Merck Patent Gmbh Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with a mek inhibitor
EP2914264B1 (en) * 2012-11-02 2017-08-09 Merck Patent GmbH A 6-oxo-1,6-dihydro-pyridazine derivative for the use for the treatment of hepatocellular carcinoma (hcc)
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
EP2935253B1 (en) 2012-12-21 2018-08-01 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
ES2634627T3 (es) * 2013-02-07 2017-09-28 Merck Patent Gmbh Derivados de amidas piridazinona
JP6599852B2 (ja) 2013-06-21 2019-10-30 ゼニス・エピジェネティクス・リミテッド ブロモドメイン阻害剤としての新規の置換された二環式化合物
ES2806135T3 (es) 2013-06-21 2021-02-16 Zenith Epigenetics Ltd Nuevos inhibidores de bromodominios bicíclicos
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
ES2930305T3 (es) 2013-10-18 2022-12-09 Celgene Quanticel Res Inc Inhibidores del bromodominio
CN105848718B (zh) * 2013-12-04 2019-07-30 盖尔梅德研究与发展有限公司 Aramchol盐
US20160331748A1 (en) * 2014-01-07 2016-11-17 Merck Patent Gmbh A 6-oxo-1,6-dihydro-pyridazine derivative for the use for the treatment of renal cell carcinoma (RCC)
WO2015104043A1 (en) * 2014-01-07 2015-07-16 Merck Patent Gmbh Combination of a 6-oxo- 1,6-dihydro-pyridazine derivate having anti-cancer activity with gefitinib
US9919034B2 (en) 2014-03-28 2018-03-20 Tamir Biotechnology, Inc. Methods of treating and prophylactically protecting mammalian patients infected by viruses classified in Baltimore group V
PT3125894T (pt) * 2014-04-01 2020-11-05 Merck Sharp & Dohme Profármacos de inibidores da transcriptase reversa do vih
US10835598B2 (en) 2014-08-18 2020-11-17 Orgenesis Inc. Prophylactic protection against viral infections, particularly HIV
US9642794B2 (en) * 2014-08-18 2017-05-09 Tamir Biotechnology, Inc. Antiviral pharmaceutical for topical administration
CA2966298A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
TWI695837B (zh) 2014-12-04 2020-06-11 比利時商健生藥品公司 作為激酶調節劑之三唑並嗒
WO2016091891A1 (en) 2014-12-09 2016-06-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Human monoclonal antibodies against axl
KR20170090498A (ko) * 2014-12-11 2017-08-07 메르크 파텐트 게엠베하 항암 활성을 갖는 6-옥소-1,6-디히드로-피리다진 유도체와 퀴나졸린 유도체의 조합
JP2017537946A (ja) 2014-12-11 2017-12-21 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての置換複素環
WO2016091346A1 (en) * 2014-12-12 2016-06-16 Merck Patent Gmbh Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with an egfr inhibitor
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains
WO2016135041A1 (en) 2015-02-26 2016-09-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Fusion proteins and antibodies comprising thereof for promoting apoptosis
WO2016192831A1 (en) 2015-05-29 2016-12-08 Merck Patent Gmbh Compositions of anions and cations with pharmacological activity
US10293032B2 (en) 2015-06-15 2019-05-21 Tamir Biotechnology, Inc. Methods and pharmaceuticals for treatment of viral infections of the eye
HUE051734T2 (hu) * 2016-10-27 2021-03-29 Fujian Cosunter Pharmaceutical Co Ltd Piridon-vegyület, mint C-Met inhibitor
MA46856A (fr) 2016-11-18 2019-09-25 Merck Sharp & Dohme Dérivés d'indazole utiles en tant qu'inhibiteurs de la diacylglycéride o-acyltransférase 2
WO2019028440A1 (en) 2017-08-04 2019-02-07 Skyhawk Therapeutics, Inc. METHODS AND COMPOSITIONS FOR MODULATING SPLICING
JP7274473B2 (ja) 2017-10-17 2023-05-16 パラウ ファルマ,エス.エル.ユー. 4-アミノピリミジン化合物の合成
WO2019101178A1 (zh) 2017-11-24 2019-05-31 南京明德新药研发股份有限公司 作为c-MET/AXL抑制剂的尿嘧啶类化合物
TWI768205B (zh) 2018-04-26 2022-06-21 大陸商福建廣生堂藥業股份有限公司 一種c-MET抑制劑的晶型及其鹽型和製備方法
CN108752322A (zh) * 2018-09-12 2018-11-06 广州新民培林医药科技有限公司 一种新型Tepotinib衍生物和制备方法及其在抗肿瘤药物中的应用
JP2022506686A (ja) 2018-11-06 2022-01-17 エッジワイズ セラピューティクス, インコーポレイテッド ピリダジノン化合物およびその使用
EA202191084A1 (ru) 2018-11-06 2021-10-19 Эджвайз Терапьютикс, Инк. Соединения пиридазинонов и их применения
PL3877052T3 (pl) 2018-11-06 2024-02-05 Edgewise Therapeutics, Inc. Pochodne pirydazynonu i ich zastosowania
WO2020130125A1 (ja) 2018-12-21 2020-06-25 第一三共株式会社 抗体-薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
CN113365997B (zh) * 2019-02-01 2022-06-07 南京明德新药研发有限公司 作为c-Met抑制剂的含嘧啶基团的三并环类化合物
JP2022521467A (ja) 2019-02-05 2022-04-08 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングを調節するための方法および組成物
JP2022519323A (ja) 2019-02-06 2022-03-22 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングを調節するための方法および組成物
EP3941475A4 (en) * 2019-03-20 2023-01-25 Goldfinch Bio, Inc. PYRIDAZINONES AND THEIR METHODS OF USE
RS64906B1 (sr) 2019-07-10 2023-12-29 Merck Patent Gmbh Farmaceutski preparat
CN114174298B (zh) * 2019-08-14 2023-08-01 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
WO2022063869A2 (en) 2020-09-24 2022-03-31 Merck Patent Gmbh Compounds for the treatment of viral infections
WO2022250350A1 (ko) * 2021-05-26 2022-12-01 주식회사 이노큐어테라퓨틱스 피페리딘디온 유도체
KR102489160B1 (ko) * 2021-05-26 2023-01-18 주식회사 이노큐어테라퓨틱스 피페리딘디온 유도체
EP4346829A1 (en) 2021-06-04 2024-04-10 Merck Patent GmbH Compounds for the treatment of glioblastoma
EP4433473A1 (en) * 2021-11-17 2024-09-25 Edgewise Therapeutics, Inc. Pyridazinone compounds and uses thereof
CN114394957B (zh) * 2021-12-24 2023-05-09 武汉九州钰民医药科技有限公司 Met抑制剂盐酸特泊替尼的制备方法
TW202421146A (zh) 2022-07-08 2024-06-01 瑞典商阿斯特捷利康公司 用於治療癌症的上皮生長因子受體酪胺酸激酶抑制劑與hgf受體抑制劑的組合
CN116496253B (zh) * 2022-08-19 2024-10-11 中国人民解放军军事科学院军事医学研究院 c-MET蛋白靶向降解剂及其医药应用
CN115583939A (zh) * 2022-11-04 2023-01-10 苏州莱安医药化学技术有限公司 一种特泊替尼中间体的合成方法
KR20240075764A (ko) * 2022-11-22 2024-05-29 주식회사 이노큐어테라퓨틱스 cMET 단백질을 분해하는 디그레이더 및 이를 포함하는 약학 조성물
KR20240076745A (ko) * 2022-11-22 2024-05-30 주식회사 이노큐어테라퓨틱스 신규한 c-MET 단백질 리간드를 포함하는 디그레이더 및 이를 포함하는 약학 조성물
CN116082309B (zh) * 2023-01-04 2023-10-24 广东莱恩医药研究院有限公司 嘧啶衍生物1d228盐酸盐晶型及其制备方法和应用
CN116768868B (zh) * 2023-08-15 2023-12-08 云南省药物研究所 一种哒嗪酮硫代衍生物及其制备方法和应用
CN118084871B (zh) * 2024-04-29 2024-07-09 中国药科大学 一种靶向降解c-Met蛋白的化合物及其制法和应用

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3853946A (en) 1971-11-11 1974-12-10 Hoffmann La Roche Process for the preparation of aminomethylene malononitrile
JPS5795964A (en) 1980-12-04 1982-06-15 Morishita Seiyaku Kk Preparation of 2-substituted-3(2h)-pyridazinone derivative
US4397854A (en) 1981-05-14 1983-08-09 Warner-Lambert Company Substituted 6-phenyl-3(2H)-pyridazinones useful as cardiotonic agents
IL115889A0 (en) 1994-11-14 1996-01-31 Rohm & Haas Pyridazinones and their use as fungicides
US5635494A (en) 1995-04-21 1997-06-03 Rohm And Haas Company Dihydropyridazinones and pyridazinones and their use as fungicides and insecticides
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE19604388A1 (de) 1996-02-07 1997-08-14 Merck Patent Gmbh Arylalkyl-diazinone
EP0880508B1 (en) 1996-02-13 2003-04-16 AstraZeneca AB Quinazoline derivatives as vegf inhibitors
IL125954A (en) 1996-03-05 2003-06-24 Zeneca Ltd Quinazoline derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the manufacture of medicaments having an antiangiogenic and/or vascular permeability reducing effect
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
JPH10259176A (ja) 1997-03-17 1998-09-29 Japan Tobacco Inc 血管新生阻害作用を有する新規アミド誘導体及びその用途
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
MXPA00004955A (es) 1997-11-19 2002-10-17 Kowa Co Derivados novedosos de piridazina y medicinas que los contienen como ingredientes activos.
TWI241295B (en) 1998-03-02 2005-10-11 Kowa Co Pyridazine derivative and medicine containing the same as effect component
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
AUPQ462299A0 (en) 1999-12-13 2000-01-13 Fujisawa Pharmaceutical Co., Ltd. Pyrazolopyridine compound and pharmaceutical use thereof
US6242461B1 (en) 2000-01-25 2001-06-05 Pfizer Inc. Use of aryl substituted azabenzimidazoles in the treatment of HIV and AIDS related diseases
DE10010422A1 (de) 2000-03-03 2001-09-06 Bayer Ag 6-Carboxyphenylpyridazinon-Derivate und ihre Verwendung
JP2003535078A (ja) 2000-05-31 2003-11-25 アストラゼネカ アクチボラグ 血管損傷活性のあるインドール誘導体
BR0112224A (pt) 2000-07-07 2003-06-10 Angiogene Pharm Ltd Composto, composição farmacêutica, uso de um composto ou de um sal, solvato ou pró-droga farmaceuticamente aceitável do mesmo, e, processo para preparar um composto
WO2002008213A1 (en) 2000-07-07 2002-01-31 Angiogene Pharmaceuticals Limited Colchinol derivatives as angiogenesis inhibitors
EP1463509A1 (en) 2001-10-31 2004-10-06 MERCK PATENT GmbH Type 4 phosphodiesterase inhibitors and uses thereof
EP1470112A1 (en) * 2002-01-18 2004-10-27 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
UA77526C2 (en) 2002-06-07 2006-12-15 Sanofi Aventis Substituted derivatives of 1-piperazineacylpiperidine, a method for the preparation thereof and their use in therapy
EP1572682A4 (en) 2002-12-20 2008-01-23 Pharmacia Corp ACYCLIC PYRAZOLE COMPOUNDS
BRPI0412003A (pt) 2003-07-02 2006-08-15 Sugen Inc arilmetil triazol e imidazopirazinas como inibidores de c-met
US7959919B2 (en) * 2003-11-19 2011-06-14 Novelmed Therapeutics, Inc. Method of inhibiting factor B-mediated complement activation
US20070043057A1 (en) 2005-02-09 2007-02-22 Threshold Pharmaceuticals, Inc. Lonidamine analogs
US20070015771A1 (en) 2004-07-29 2007-01-18 Threshold Pharmaceuticals, Inc. Lonidamine analogs
TW200612918A (en) 2004-07-29 2006-05-01 Threshold Pharmaceuticals Inc Lonidamine analogs
WO2007044796A2 (en) 2005-10-11 2007-04-19 Nps Pharmaceuticals, Inc. Pyridazinone compounds as calcilytics
DE102005055355A1 (de) 2005-11-21 2007-10-31 Merck Patent Gmbh 3,6-Dihydro-2-oxo-6H-[1,3,4]thiadiazinderivate
DE102005055354A1 (de) 2005-11-21 2007-10-31 Merck Patent Gmbh Substituierte 5-Phenyl-3,6-dihydro-2-oxo-6H-[1,3,4]thiadiazine
AU2006320580B2 (en) 2005-11-30 2011-06-23 Vertex Pharmaceuticals Incorporated Inhibitors of c-Met and uses thereof
DE102005057924A1 (de) 2005-12-05 2007-06-06 Merck Patent Gmbh Pyridazinonderivate
ME02736B (me) 2005-12-21 2017-10-20 Janssen Pharmaceutica Nv Triazolopiridazini kao modulatori tirozin kinaze
WO2007130383A2 (en) 2006-04-28 2007-11-15 Northwestern University Compositions and treatments using pyridazine compounds and secretases
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
PE20091079A1 (es) 2007-10-16 2009-08-24 Novartis Ag Compuestos heterociclicos como moduladores npy y2
EP2215085B1 (en) 2007-10-25 2011-09-07 AstraZeneca AB Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders
EP2203429A1 (en) 2007-10-31 2010-07-07 Nissan Chemical Industries, Ltd. Pyridazinone derivatives and use thereof as p2x7 receptor inhibitors
JP5769970B2 (ja) 2007-11-16 2015-08-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ベンゾモルファン及び関連骨格のアリール−及びヘテロアリールカルボニル誘導体、かかる化合物を含有する医薬及びこれらの使用
CN101903382B (zh) 2007-12-21 2012-11-28 弗·哈夫曼-拉罗切有限公司 杂环抗病毒化合物
DE102007061963A1 (de) 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
WO2009080364A1 (en) 2007-12-21 2009-07-02 Synthon B.V. Raloxifene composition
GB0725059D0 (en) 2007-12-21 2008-01-30 Syngenta Participations Ag Novel pyridazine derivatives
US7816540B2 (en) 2007-12-21 2010-10-19 Hoffmann-La Roche Inc. Carboxyl- or hydroxyl-substituted benzimidazole derivatives
EP2235010A1 (en) 2007-12-21 2010-10-06 AstraZeneca AB Bicyclic derivatives for use in the treatment of androgen receptor associated conditions
EP2072506A1 (de) 2007-12-21 2009-06-24 Bayer CropScience AG Thiazolyloxyphenylamidine oder Thiadiazolyloxyphenylamidine und deren Verwendung als Fungizide
AU2008340421B2 (en) 2007-12-21 2013-12-19 F. Hoffmann-La Roche Ag Heteroaryl derivatives as orexin receptor antagonists
US8202996B2 (en) 2007-12-21 2012-06-19 Bristol-Myers Squibb Company Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide
PE20091669A1 (es) 2007-12-21 2009-12-06 Exelixis Inc Benzofuropirimidinonas
CL2008003785A1 (es) 2007-12-21 2009-10-09 Du Pont Compuestos derivados de piridazina; composiciones herbicidas que comprenden a dichos compuestos; y método para controlar el crecimiento de la vegetación indeseada.
PE20091339A1 (es) 2007-12-21 2009-09-26 Glaxo Group Ltd Derivados de oxadiazol con actividad sobre receptores s1p1
KR101639819B1 (ko) 2007-12-21 2016-07-14 팔라우 파르마 에스에이 히스타민 h4 수용체 길항제로서 4-아미노피리미딘 유도체
CN101537006B (zh) * 2008-03-18 2012-06-06 中国科学院上海药物研究所 哒嗪酮类化合物在制备抗肿瘤药物中的用途
DE102008019907A1 (de) 2008-04-21 2009-10-22 Merck Patent Gmbh Pyridazinonderivate
WO2009142732A2 (en) * 2008-05-20 2009-11-26 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
DE102008028905A1 (de) 2008-06-18 2009-12-24 Merck Patent Gmbh 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate
JP5390610B2 (ja) * 2008-07-25 2014-01-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 11β−ヒドロキシステロイドデヒドロゲナーゼ1型の阻害剤の合成
BRPI1013159A2 (pt) * 2009-03-30 2015-09-15 Sumitomo Chemical Co Uso de composto de piridazinona para controle de peste artrópode
AR082590A1 (es) * 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton

Also Published As

Publication number Publication date
HRP20150031T1 (en) 2015-03-13
FR22C1024I1 (fr) 2022-07-22
JP2010532768A (ja) 2010-10-14
US20130184261A1 (en) 2013-07-18
TW200906409A (en) 2009-02-16
CN101743241B (zh) 2013-12-25
CA2692867C (en) 2016-05-24
AR067505A1 (es) 2009-10-14
NZ583187A (en) 2011-10-28
US20140128396A1 (en) 2014-05-08
US20150011534A1 (en) 2015-01-08
US9403799B2 (en) 2016-08-02
HUE030519T2 (en) 2017-05-29
ES2614283T3 (es) 2017-05-30
CY1118498T1 (el) 2017-07-12
UA99621C2 (en) 2012-09-10
SI2754660T1 (sl) 2017-03-31
PL2164843T3 (pl) 2015-03-31
DK2164844T3 (da) 2012-08-20
US20100234354A1 (en) 2010-09-16
HUS2200024I1 (hu) 2022-06-28
NL301176I2 (nl) 2022-11-03
SG183739A1 (en) 2012-09-27
SI2164843T1 (sl) 2015-02-27
KR101553418B1 (ko) 2015-09-15
EA016782B1 (ru) 2012-07-30
HK1145265A1 (en) 2011-04-08
IL203091A (en) 2013-10-31
EP2164843A1 (de) 2010-03-24
CN101743241A (zh) 2010-06-16
EA017281B1 (ru) 2012-11-30
KR20100031771A (ko) 2010-03-24
EP2754660B1 (de) 2016-11-02
HRP20170100T1 (hr) 2017-03-24
NO2022015I1 (no) 2022-05-13
PL2754660T3 (pl) 2017-05-31
AU2008274534B2 (en) 2013-05-30
CA2692867A1 (en) 2009-01-15
CN101687857B (zh) 2013-07-17
CA2693600A1 (en) 2009-01-15
US20120295908A1 (en) 2012-11-22
JP2010532774A (ja) 2010-10-14
DE102007032507A1 (de) 2009-04-02
JP5426543B2 (ja) 2014-02-26
CL2008001392A1 (es) 2009-01-23
UA99833C2 (en) 2012-10-10
ECSP109953A (es) 2010-03-31
SI2164844T1 (sl) 2012-10-30
US8921357B2 (en) 2014-12-30
US9284300B2 (en) 2016-03-15
EA201000094A1 (ru) 2010-06-30
HRP20120661T1 (hr) 2012-09-30
BRPI0814616A2 (pt) 2015-01-27
AU2008274534A1 (en) 2009-01-15
EP2164843B1 (de) 2014-10-29
US9062029B2 (en) 2015-06-23
AR066543A1 (es) 2009-08-26
ES2388883T3 (es) 2012-10-19
CA2693600C (en) 2015-10-06
US8658643B2 (en) 2014-02-25
NL301176I1 (es) 2022-06-01
CN101687857A (zh) 2010-03-31
WO2009007074A1 (de) 2009-01-15
DK2164843T3 (en) 2014-12-01
HK1142891A1 (en) 2010-12-17
KR20100050504A (ko) 2010-05-13
US20130184260A1 (en) 2013-07-18
US20150133452A1 (en) 2015-05-14
EP2164844B1 (de) 2012-06-27
ECSP109957A (es) 2010-03-31
US8329692B2 (en) 2012-12-11
US8580781B2 (en) 2013-11-12
FR22C1024I2 (fr) 2023-03-24
CO6170360A2 (es) 2010-06-18
CY1115925T1 (el) 2017-01-25
ZA201001023B (en) 2010-11-24
AU2008274670A1 (en) 2009-01-15
AU2008274670B2 (en) 2013-03-14
CY1113137T1 (el) 2016-04-13
TWI501768B (zh) 2015-10-01
BRPI0813707A2 (pt) 2014-12-30
KR101544624B1 (ko) 2015-08-17
MY163477A (en) 2017-09-15
EP2164844A1 (de) 2010-03-24
CY2022017I1 (el) 2023-01-05
PL2164844T3 (pl) 2012-10-31
WO2009006959A1 (de) 2009-01-15
LT2754660T (lt) 2016-12-12
PE20090287A1 (es) 2009-03-19
BRPI0813707B1 (pt) 2022-02-22
EP2754660A1 (de) 2014-07-16
CY2022017I2 (el) 2023-01-05
US20100197690A1 (en) 2010-08-05
LTPA2022009I1 (es) 2022-06-10
PT2754660T (pt) 2017-02-10
CO6270257A2 (es) 2011-04-20
DK2754660T3 (en) 2017-02-13
PT2164843E (pt) 2014-12-23
US8927540B2 (en) 2015-01-06
PT2164844E (pt) 2012-08-31
JP5426544B2 (ja) 2014-02-26
BRPI0814616B1 (pt) 2022-04-19
IL203094A (en) 2013-08-29
MY153727A (en) 2015-03-13
EA201000093A1 (ru) 2010-06-30

Similar Documents

Publication Publication Date Title
ES2526352T3 (es) Derivados de piridazinona
AR057214A1 (es) Derivados de piridazinona como inhibidores, reguladores o moduladores de quinasas.
AR071208A1 (es) Derivados de piridazinona
AR068659A1 (es) Derivados de imidazol inhibidores de autotaxina
AR066770A1 (es) Derivados de piridazinona
AR068658A1 (es) Derivados de tiazol
AR090867A1 (es) Compuestos y composiciones plaguicidas y procesos relacionados
AR068748A1 (es) Derivados de piridina activadores de glucoquinasa
AR066769A1 (es) Derivados de arileter-piridazinona
AR077567A1 (es) Derivados de aminopiridina
CO6241076A2 (es) Compuestos de benzamida y aplicaciones de los mismos
AR092211A1 (es) Derivados de hidropirrolopirrol
AR076006A1 (es) Compuestos heterociclicos inhibidores de autotaxina utiles para el tratamiento de tumores, proceso para prepararlos y medicamentos que los contienen.
NI200900037A (es) Derivados de 2-aril-6-fenil-imidazo[1,2-alfa] piridinas, su preparación y su aplicación en terapéutica.
AR073369A1 (es) Derivados de 2-carboxamida-cicloamino-urea como inhibidores de pi-3
AR069843A1 (es) Derivados de piridazinona, procedimiento para preparar dichos compuestos, composiciones farmaceuticas y usos de los mismos para preparar un medicamento
CO6331462A2 (es) Compuesto de fenil pirrol o una sal farmaceuticamente aceptable del mismo con actividad activadora de la glucoquinasa
AR067081A1 (es) Derivados de pirrolo[2,3-b]piridin-pirimidina,proceso de preparacion, medicamentos que los contienen y usos de los mismos para el tratamiento de tumores cancerigenos y metastasis tumorales.
CO6321166A2 (es) Compuestos de pirrol
AR067691A1 (es) Derivados heterociclicos de sulfonimidoil, composiciones plaguicidas que los contienen y usos de los mismos para el control de plagas.
BRPI0821653B8 (pt) composto de piridina substituída com anel heterocíclico e grupo fosfonoximetila ou um sal do mesmo, composição farmacêutica compreendendo-os e uso dos mesmos para tratar uma doença fungíca
AR072192A1 (es) Derivados de tiazolil-piperidina
AR095422A1 (es) Compuestos de piperidina sustituidos y su uso como moduladores de receptores de orexina
AR113842A1 (es) Derivados de tiazol microbiocidas
TR201907373T4 (tr) Tetrazolinon bileşiği ve bunun kullanımı.