[go: up one dir, main page]

ES2500068T3 - Inhibidores heterocíclicos de MEK y métodos de uso de los mismos - Google Patents

Inhibidores heterocíclicos de MEK y métodos de uso de los mismos Download PDF

Info

Publication number
ES2500068T3
ES2500068T3 ES11003826.2T ES11003826T ES2500068T3 ES 2500068 T3 ES2500068 T3 ES 2500068T3 ES 11003826 T ES11003826 T ES 11003826T ES 2500068 T3 ES2500068 T3 ES 2500068T3
Authority
ES
Spain
Prior art keywords
mek
methods
hoch2ch20
cyclopropyl
ethyl
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
ES11003826.2T
Other languages
English (en)
Inventor
Richard Anthony Storey
Rebecca Jane Booth
John David Pittam
Allison L. Marlow
Eli Wallace
Jeongbeob Seo
Joseph P. Lyssikatos
Hong Woon Yang
Jim Blake
John Leonard
Mark Richard Fielding
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.)
AstraZeneca AB
Array Biopharma Inc
Original Assignee
AstraZeneca AB
Array Biopharma Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37943261&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2500068(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by AstraZeneca AB, Array Biopharma Inc filed Critical AstraZeneca AB
Application granted granted Critical
Publication of ES2500068T3 publication Critical patent/ES2500068T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

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

Abstract

Composicion farmaceutica que comprende un compuesto que tiene la formula IV:**Fórmula** o una sal farmaceuticamente aceptable del mismo, en la que: R1 es Cl o F; R3 es H, Me, Et, OH, Me0-, Et0-, HOCH2CH20-, HOCH2C(Me)20-, (S)-MeCH(OH)CH20-, (R)- HOCH2CH(OH)CH20-, ciclopropil-CH20-, HOCH2CH2-, R7 es metilo o etilo, en el que dicho nnetilo y etilo estan opcionalmente sustituidos con uno o mas F; R8 es Br, I o SMe; y R9 es H, alquilo C1-C4, Cl o CN, en el que dicho alquilo esta opcionalmente sustituido con uno o mas grupos seleccionados independientemente de F o CN, siempre que cuando a) R1 es F, R8 es Br, R9 es H y R7 es o bien Me o bien Et, entonces R3 no puede ser HOCH2CH20; b) R1 es F, R8 es I, R9 es H y R3 es Me0, entonces R7 no puede ser Me; y c) R1 es F, R8 es Me, R9 es H y R3 es ciclopropil-CH20, entonces R7 no puede ser Me; en combinación con un agente antitumoral o un inhibidor de la transducción de senates

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
imagen15
imagen16
imagen17
imagen18
imagen19
imagen20
imagen21
imagen22
imagen23
imagen24
imagen25
imagen26
imagen27
imagen28
imagen29
imagen30
imagen31
imagen32
imagen33
imagen34
imagen35
imagen36
imagen37
imagen38
imagen39
imagen40
imagen41
imagen42
imagen43
imagen44
imagen45
imagen46
imagen47
imagen48
imagen49
imagen50
imagen51
imagen52
imagen53
imagen54
imagen55
imagen56
imagen57
imagen58
imagen59
imagen60
imagen61
imagen62
imagen63
imagen64
imagen65
imagen66
imagen67
imagen68
imagen69
imagen70
imagen71
imagen72
imagen73
imagen74
imagen75
imagen76
imagen77
imagen78
imagen79
imagen80
imagen81
imagen82
imagen83
imagen84
imagen85
imagen86
imagen87
imagen88
imagen89
imagen90
imagen91
imagen92

Claims (1)

  1. imagen1
    imagen2
    imagen3
ES11003826.2T 2005-05-18 2006-05-17 Inhibidores heterocíclicos de MEK y métodos de uso de los mismos Active ES2500068T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US68233505P 2005-05-18 2005-05-18
US682335P 2005-05-18

Publications (1)

Publication Number Publication Date
ES2500068T3 true ES2500068T3 (es) 2014-09-30

Family

ID=37943261

Family Applications (4)

Application Number Title Priority Date Filing Date
ES08004958T Active ES2333182T3 (es) 2005-05-18 2006-05-17 Derivados de 4-(fenilamino)-6-oxo-1,6-dihidropiridazina-3-carboxamida como inhibidores de mek para el tratamiento de enfermedades hiperproliferativas.
ES11003826.2T Active ES2500068T3 (es) 2005-05-18 2006-05-17 Inhibidores heterocíclicos de MEK y métodos de uso de los mismos
ES11003827T Active ES2405785T3 (es) 2005-05-18 2006-05-17 Inhibidores heterocíclicos de MEK y métodos de uso de los mismos
ES06836069T Active ES2378760T3 (es) 2005-05-18 2006-05-17 Inhibidores heterocíclicos de MEK y métodos de uso de los mismos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES08004958T Active ES2333182T3 (es) 2005-05-18 2006-05-17 Derivados de 4-(fenilamino)-6-oxo-1,6-dihidropiridazina-3-carboxamida como inhibidores de mek para el tratamiento de enfermedades hiperproliferativas.

Family Applications After (2)

Application Number Title Priority Date Filing Date
ES11003827T Active ES2405785T3 (es) 2005-05-18 2006-05-17 Inhibidores heterocíclicos de MEK y métodos de uso de los mismos
ES06836069T Active ES2378760T3 (es) 2005-05-18 2006-05-17 Inhibidores heterocíclicos de MEK y métodos de uso de los mismos

Country Status (32)

Country Link
US (1) US8299076B2 (es)
EP (4) EP1967516B1 (es)
JP (3) JP5270336B2 (es)
KR (3) KR20110074772A (es)
CN (5) CN102321030A (es)
AR (3) AR055057A1 (es)
AT (2) ATE539064T1 (es)
AU (1) AU2006299902B2 (es)
BR (1) BRPI0610139A2 (es)
CA (1) CA2608201C (es)
CL (2) CL2008003486A1 (es)
CY (1) CY1112297T1 (es)
DE (1) DE602006010243D1 (es)
DK (1) DK1922307T3 (es)
EC (1) ECSP078013A (es)
ES (4) ES2333182T3 (es)
HR (1) HRP20120154T1 (es)
IL (3) IL187353A (es)
MY (2) MY149960A (es)
NO (1) NO20076412L (es)
NZ (3) NZ587189A (es)
PL (3) PL1922307T3 (es)
PT (2) PT1922307E (es)
RS (1) RS52243B (es)
RU (4) RU2500673C2 (es)
SA (1) SA06270141B1 (es)
SG (2) SG177981A1 (es)
SI (1) SI1922307T1 (es)
TW (3) TW201238952A (es)
UA (2) UA93678C2 (es)
WO (1) WO2007044084A2 (es)
ZA (2) ZA200710318B (es)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7517994B2 (en) * 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
JP4869075B2 (ja) * 2003-11-19 2012-02-01 アレイ バイオファーマ、インコーポレイテッド Ｍｅｋの複素環阻害剤及びその使用方法
US7732616B2 (en) 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
RU2500673C2 (ru) 2005-05-18 2013-12-10 Астразенека Аб Гетероциклические ингибиторы мек и способы их применения
KR20090071666A (ko) 2006-10-23 2009-07-01 다케다 야쿠힌 고교 가부시키가이샤 Ｍａｐｋ／ｅｒｋ 키나아제 억제제
GB0625691D0 (en) * 2006-12-22 2007-01-31 Astrazeneca Ab Combination product
WO2008120004A1 (en) * 2007-04-02 2008-10-09 Astrazeneca Ab Combination of a mek- inhibitor and a b-raf inhibitor for the treatment of cancer
CN101678001A (zh) * 2007-04-13 2010-03-24 阿斯利康(瑞典)有限公司 包含azd2171和azd6244或mek-抑制剂ⅱ的组合治疗
BRPI0818426A2 (pt) * 2007-10-15 2017-06-13 Astrazeneca Ab produto de combinação, uso de um produto de combinação, e, método para tratar câncer
WO2009064675A1 (en) 2007-11-12 2009-05-22 Takeda Pharmaceutical Company Limited Mapk/erk kinase inhibitors
US20100004247A1 (en) * 2007-12-12 2010-01-07 Astrazeneca Ab Combination comprising a mek inhibitor and an aurora kinase inhibitor 188
KR20110028651A (ko) 2008-07-11 2011-03-21 노파르티스 아게 (ａ) 포스포이노시타이드 3-키나제 억제제 및 (ｂ) ｒａｓ/ｒａｆ/ｍｅｋ 경로의 조절제의 조합물
WO2010068738A1 (en) 2008-12-10 2010-06-17 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
CN106478496A (zh) * 2009-03-27 2017-03-08 阿迪生物科学公司 作为mek抑制剂的二氢吡啶磺酰胺和二氢吡啶硫酰胺
CN102020851B (zh) 2009-09-16 2013-10-16 大连路明发光科技股份有限公司 一种光转换柔性高分子材料及其用途
WO2011106298A1 (en) 2010-02-25 2011-09-01 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
AU2011224410B2 (en) 2010-03-09 2015-05-28 Dana-Farber Cancer Institute, Inc. Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy
EP3045450B1 (en) 2010-09-08 2018-02-07 Sumitomo Chemical Co., Ltd. Intermediate compounds in processes for producing pyridazinone compounds
CN102020651B (zh) 2010-11-02 2012-07-18 北京赛林泰医药技术有限公司 6-芳基氨基吡啶酮甲酰胺mek抑制剂
CN106893692B (zh) 2010-12-22 2021-11-26 菲特治疗公司 用于单细胞分选与增强ipsc重新编程的细胞培养平台
FI20115234A0 (fi) 2011-03-08 2011-03-08 Biotie Therapies Corp Uusia pyridatsinoni- ja pyridoniyhdisteitä
WO2012145503A1 (en) 2011-04-21 2012-10-26 Novartis Ag Pharmaceutical combinations
CN102358730A (zh) * 2011-08-24 2012-02-22 济南赛文医药技术有限公司 一种小分子mek蛋白激酶抑制剂
WO2013066483A1 (en) 2011-08-31 2013-05-10 Novartis Ag Synergistic combinations of pi3k- and mek-inhibitors
WO2013109142A1 (en) 2012-01-16 2013-07-25 Stichting Het Nederlands Kanker Instituut Combined pdk and mapk/erk pathway inhibition in neoplasia
CN103204827B (zh) 2012-01-17 2014-12-03 上海科州药物研发有限公司 作为蛋白激酶抑制剂的苯并噻二唑化合物及其制备方法和用途
GB201201332D0 (en) 2012-01-26 2012-03-14 Imp Innovations Ltd Method
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
PL2925366T3 (pl) 2012-11-29 2018-08-31 Novartis Ag Kombinacje farmaceutyczne
TW201441193A (zh) 2012-12-06 2014-11-01 Kyowa Hakko Kirin Co Ltd 吡啶酮化合物
AU2014230552B2 (en) * 2013-03-13 2017-11-16 Chugai Seiyaku Kabushiki Kaisha Dihydropyridazine-3,5-dione derivative
WO2014204263A1 (en) 2013-06-20 2014-12-24 The Asan Foundation Substituted pyridinone compounds as mek inhibitors
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
EP3046557A1 (en) 2013-09-20 2016-07-27 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
WO2015058589A1 (zh) * 2013-10-25 2015-04-30 上海恒瑞医药有限公司 吡啶酮类衍生物、其制备方法及其在医药上的应用
EP3094736A4 (en) 2014-01-14 2017-10-25 Dana-Farber Cancer Institute, Inc. Compositions and methods for identification, assessment, prevention, and treatment of melanoma using pd-l1 isoforms
ES2921874T3 (es) * 2014-02-28 2022-09-01 Nimbus Lakshmi Inc Inhibidores de TYK2 y usos de los mismos
SG10201807292YA (en) 2014-03-04 2018-09-27 Fate Therapeutics Inc Improved reprogramming methods and cell culture platforms
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
US10023879B2 (en) 2014-06-04 2018-07-17 Fate Therapeutics, Inc. Minimal volume reprogramming of mononuclear cells
AU2015328411C1 (en) 2014-10-06 2022-03-03 Dana-Farber Cancer Institute, Inc. Angiopoietin-2 biomarkers predictive of anti-immune checkpoint response
US10626372B1 (en) 2015-01-26 2020-04-21 Fate Therapeutics, Inc. Methods and compositions for inducing hematopoietic cell differentiation
MA41866A (fr) 2015-03-31 2018-02-06 Massachusetts Gen Hospital Molécules à auto-assemblage pour l'administration ciblée de médicaments
AU2016314082B2 (en) 2015-08-28 2019-07-25 Novartis Ag Mdm2 inhibitors and combinations thereof
AU2016338680B2 (en) 2015-10-16 2022-11-17 Fate Therapeutics, Inc. Platform for the induction and maintenance of ground state pluripotency
CN108473961B (zh) 2015-11-04 2022-11-29 菲特治疗公司 用于诱导造血细胞分化的方法和组合物
KR20250141836A (ko) 2015-11-04 2025-09-29 페이트 세러퓨틱스, 인코포레이티드 만능 세포의 유전자 조작
AU2016358147A1 (en) * 2015-11-18 2018-05-31 Fmc Corporation Process for the synthesis of intermediates useful for preparing 1,3,4-triazine derivatives
CA3010236A1 (en) 2016-01-20 2017-07-27 Fate Therapeutics, Inc. Compositions and methods for immune cell modulation in adoptive immunotherapies
WO2017127755A1 (en) 2016-01-20 2017-07-27 Fate Therapeutics, Inc. Compositions and methods for immune cell modulation in adoptive immunotherapies
WO2017154001A1 (en) * 2016-03-10 2017-09-14 Lutris Pharma Ltd. Use of braf inhibitors for treating cutaneous reactions
WO2018092064A1 (en) 2016-11-18 2018-05-24 Novartis Ag Combinations of mdm2 inhibitors and bcl-xl inhibitors
JP7098615B2 (ja) 2016-12-05 2022-07-11 フェイト セラピューティクス，インコーポレイテッド 養子免疫療法における免疫細胞調節のための組成物および方法
KR102435424B1 (ko) * 2017-09-13 2022-08-23 엘지디스플레이 주식회사 듀티 구동 기능을 갖는 표시장치 및 이의 구동방법
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
TWI817018B (zh) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療ｂｒａｆ相關的疾病和失調症之化合物
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
AR121078A1 (es) 2020-01-22 2022-04-13 Chugai Pharmaceutical Co Ltd Derivados de arilamida con actividad antitumoral
US12303509B2 (en) 2020-06-09 2025-05-20 Pfizer Inc. Compounds for the treatment of BRAF-associated diseases and disorders
TWI825637B (zh) 2021-03-31 2023-12-11 美商輝瑞股份有限公司 啶－１，６（２ｈ，７ｈ）－二酮
WO2022251193A1 (en) 2021-05-27 2022-12-01 Mirati Therapeutics, Inc. Combination therapies
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
WO2025073765A1 (en) 2023-10-03 2025-04-10 Institut National de la Santé et de la Recherche Médicale Methods of prognosis and treatment of patients suffering from melanoma

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3682932A (en) 1970-11-23 1972-08-08 Hoffmann La Roche 2-chloro-6-hydroxynicotinic acid
DE2150772A1 (de) 1971-10-12 1973-04-19 Cassella Farbwerke Mainkur Ag Verfahren zur herstellung von 6-hydroxy-2-pyridon-3-carbonsaeureamidverbindungen
DE2307169A1 (de) 1973-02-14 1974-09-26 Bayer Ag Azofarbstoffe
AT392789B (de) * 1985-01-23 1991-06-10 Toyama Chemical Co Ltd Verfahren zur herstellung von 1-substituierten aryl-1,4-dihydro-4-oxonaphthyridinderivaten
US4851535A (en) * 1985-01-23 1989-07-25 Toyama Chemical Co., Ltd. Nicotinic acid derivatives
GB8607683D0 (en) 1986-03-27 1986-04-30 Ici Plc Anti-tumor agents
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
FR2687676B1 (fr) * 1992-02-24 1994-07-08 Union Pharma Scient Appl Nouveaux derives de polyazaindenes antagonistes des recepteurs a l'angiotensine ii; leurs procedes de preparation, compositions pharmaceutiques les contenant.
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5750545A (en) * 1993-07-23 1998-05-12 The Green Cross Corporation Triazole derivative and pharmaceutical use thereof
DK0672041T3 (da) * 1993-10-01 2002-02-25 Novartis Ag Farmakologisk aktive pyridinderivater og fremgangsmåder til fremstilling deraf
US5525625A (en) 1995-01-24 1996-06-11 Warner-Lambert Company 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
CA2218503C (en) 1995-04-20 2001-07-24 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
EP0780386B1 (en) 1995-12-20 2002-10-02 F. Hoffmann-La Roche Ag Matrix metalloprotease inhibitors
WO1997030035A1 (en) 1996-02-13 1997-08-21 Zeneca Limited Quinazoline derivatives as vegf inhibitors
PT885198E (pt) 1996-03-05 2002-06-28 Astrazeneca Ab Derivados de 4-anilinoquinazolina
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
KR20000067904A (ko) 1996-07-18 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 매트릭스 메탈로프로테아제의 포스피네이트계 억제제
BR9711223A (pt) 1996-08-23 1999-08-17 Pfizer Derivados de cido arilsulfonilamino-hidrox mico
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
EP0950059B1 (en) 1997-01-06 2004-08-04 Pfizer Inc. Cyclic sulfone derivatives
IL131042A0 (en) 1997-02-03 2001-01-28 Pfizer Prod Inc Arylsulfonylamino hydroxamic acid derivatives
BR9807824A (pt) 1997-02-07 2000-03-08 Pfizer Derivados de n-hidróxi-beta-sulfonil-propionamida e seu uso como inibidores de metaloproteinases de matriz
KR20000070923A (ko) 1997-02-11 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 아릴설포닐 하이드록삼산 유도체
DE69837529T2 (de) 1997-02-12 2007-07-26 Electrophoretics Ltd., Cobham Proteinmarker für lungenkrebs und deren verwendung
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6821963B2 (en) * 1997-07-01 2004-11-23 Warner-Lambert Company 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
US6310060B1 (en) * 1998-06-24 2001-10-30 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
JP2002509536A (ja) 1997-07-01 2002-03-26 ワーナー−ランバート・カンパニー ２−（４−ブロモ又は４−ヨードフェニルアミノ）安息香酸誘導体及びｍｅｋ阻害物質としてのそれらの使用
US6506798B1 (en) * 1997-07-01 2003-01-14 Warner-Lambert Company 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
JP2002511092A (ja) 1997-07-01 2002-04-09 ワーナー−ランバート・コンパニー ４−ブロモまたは４−ヨードフェニルアミノベンズヒドロキサム酸誘導体およびそのｍｅｋ阻害剤としての使用
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
DE69822839T2 (de) 1997-08-08 2004-08-19 Pfizer Products Inc., Groton Derivate von aryloxyarylsulfonylamino hydroxyaminsäuren
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
JP4462654B2 (ja) 1998-03-26 2010-05-12 ソニー株式会社 映像素材選択装置及び映像素材選択方法
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
AUPP466598A0 (en) 1998-07-14 1998-08-06 University Of Newcastle Research Associates Limited, The Product and process
ES2213985T3 (es) 1998-11-05 2004-09-01 Pfizer Products Inc. Derivados de hidroxiamida de acido 5-oxo-pirrolidin-2-carboxilico.
EP1140067A1 (en) 1999-01-07 2001-10-10 Warner-Lambert Company Antiviral method using mek inhibitors
CA2350234A1 (en) * 1999-01-07 2000-07-13 Alexander James Bridges Treatment of asthma with mek inhibitors
ATE311363T1 (de) * 1999-01-13 2005-12-15 Warner Lambert Co Sulfohydroxamsäure and sulfohydroxamate und ihre verwendung als mek-inhibitoren
IL144214A0 (en) * 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
EP1144371B1 (en) 1999-01-13 2005-11-09 Warner-Lambert Company Llc Benzenesulphonamide derivatives and their use as mek inhibitors
AP2001002225A0 (en) * 1999-01-13 2001-09-30 Warner Lambert Co 1-heterocycle substituted diarylamines.
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
BR9916857A (pt) 1999-01-13 2001-12-04 Warner Lambert Co 4 heteroaril diarilaminas
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
BRPI0017548B8 (pt) 1999-02-10 2023-05-02 Astrazeneca Ab Composto
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
CN1358094A (zh) 1999-07-16 2002-07-10 沃尼尔·朗伯公司 用mek抑制剂治疗慢性疼痛的方法
JP2003504401A (ja) 1999-07-16 2003-02-04 ワーナー−ランバート・カンパニー Ｍｅｋ阻害剤を用いる慢性疼痛の治療方法
HUP0202381A3 (en) 1999-07-16 2004-12-28 Warner Lambert Co Method for treating chronic pain using mek inhibitors
US7030119B1 (en) * 1999-07-16 2006-04-18 Warner-Lambert Company Method for treating chronic pain using MEK inhibitors
AU5786000A (en) 1999-07-16 2001-02-05 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
EE05330B1 (et) 1999-11-05 2010-08-16 Astrazeneca Ab Kinasoliini derivaadid kui VEGF-i inhibiitorid
US6573293B2 (en) 2000-02-15 2003-06-03 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
BR0109188A (pt) 2000-03-15 2003-03-18 Warner Lambert Co Diarilaminas 5-amida substituìdas como inibidores de mex
US7001905B2 (en) * 2000-03-15 2006-02-21 Warner-Lambert Company Substituted diarylamines as MEK inhibitors
AU2001258628A1 (en) 2000-05-31 2001-12-11 Astrazeneca Ab Indole derivatives with vascular damaging activity
MXPA02012905A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como agentes de dano vascular..
BR0112225A (pt) 2000-07-07 2003-05-06 Angiogene Pharm Ltd Composto, composição farmacêutica, uso de um composto, e, processo papa preparar um composto
IL153817A0 (en) 2000-07-19 2003-07-31 Warner Lambert Co Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids
RU2167659C1 (ru) * 2000-08-02 2001-05-27 Закрытое акционерное общество "Центр современной медицины "Медикор" Способ коррекции иммунной системы живого организма
MXPA03001654A (es) 2000-08-25 2004-09-10 Warner Lambert Co Proceso para la elaboracion del acido n-aril-antranilico y sus derivados.
AU2002210714A1 (en) * 2000-11-02 2002-06-11 Astrazeneca Ab Substituted quinolines as antitumor agents
US6642215B2 (en) * 2001-05-24 2003-11-04 Leo Pharma A/S Method of modulating NF-kB activity
US20040039208A1 (en) * 2001-07-20 2004-02-26 Chen Michael Huai Gu Process for making n-aryl-anthranilic acids and their derivatives
US20030187026A1 (en) * 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
CA2478534A1 (en) 2002-03-13 2003-09-25 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as mek inhibitors
CA2478374C (en) * 2002-03-13 2009-01-06 Eli M. Wallace N3 alkylated benzimidazole derivatives as mek inhibitors
WO2003076405A1 (en) 2002-03-14 2003-09-18 Bayer Healthcare Ag Monocyclic aroylpyridinones as antiinflammatory agents
AU2003250844A1 (en) 2002-06-24 2004-01-06 Fagerdala Deutschland Gmbh Method for producing parts from high-grade lignocellulose fiber-filled thermoplastics
WO2005000818A1 (en) * 2003-06-27 2005-01-06 Warner-Lambert Company Llc 5-substituted-4-`(substituted phenyl)!amino!-2-pyridone deviatives for use as mek inhibitors
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
US7144907B2 (en) * 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
JP4869075B2 (ja) * 2003-11-19 2012-02-01 アレイ バイオファーマ、インコーポレイテッド Ｍｅｋの複素環阻害剤及びその使用方法
US7732616B2 (en) * 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
US7517994B2 (en) * 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
ES2251866B1 (es) 2004-06-18 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
RU2500673C2 (ru) 2005-05-18 2013-12-10 Астразенека Аб Гетероциклические ингибиторы мек и способы их применения

Also Published As

Publication number Publication date
US8299076B2 (en) 2012-10-30
CN102304086A (zh) 2012-01-04
ES2405785T3 (es) 2013-06-03
TW201302708A (zh) 2013-01-16
RU2010128512A (ru) 2012-01-20
JP2008545654A (ja) 2008-12-18
IL212398A (en) 2014-09-30
IL212398A0 (en) 2011-06-30
UA93678C2 (ru) 2011-03-10
ES2333182T3 (es) 2010-02-17
CN102304086B (zh) 2013-12-04
PL1922307T3 (pl) 2012-07-31
TW201238952A (en) 2012-10-01
RU2500673C2 (ru) 2013-12-10
CN102898364A (zh) 2013-01-30
SA06270141B1 (ar) 2009-11-15
PT2361905E (pt) 2013-03-18
AR082826A2 (es) 2013-01-09
CA2608201C (en) 2013-12-31
EP1922307B1 (en) 2011-12-28
NZ587190A (en) 2011-11-25
EP1922307A2 (en) 2008-05-21
HK1161250A1 (en) 2012-08-24
JP5576919B2 (ja) 2014-08-20
KR20080019236A (ko) 2008-03-03
PT1922307E (pt) 2012-01-25
PL2364973T3 (pl) 2014-12-31
RS52243B (sr) 2012-10-31
PL2361905T3 (pl) 2013-07-31
CL2009001993A1 (es) 2010-06-11
TWI441637B (zh) 2014-06-21
NZ563707A (en) 2011-01-28
ES2378760T3 (es) 2012-04-17
NO20076412L (no) 2008-01-14
ATE539064T1 (de) 2012-01-15
EP2364973A1 (en) 2011-09-14
RU2414455C2 (ru) 2011-03-20
SG161318A1 (en) 2010-05-27
CN102942522A (zh) 2013-02-27
RU2007146115A (ru) 2009-06-27
TW200714590A (en) 2007-04-16
AU2006299902A1 (en) 2007-04-19
RU2009118281A (ru) 2010-11-20
IL212396A0 (en) 2011-06-30
CN102321030A (zh) 2012-01-18
EP1967516B1 (en) 2009-11-04
AR055057A1 (es) 2007-08-01
EP2361905A1 (en) 2011-08-31
CL2008003486A1 (es) 2009-03-20
CN101626767A (zh) 2010-01-13
HRP20120154T1 (hr) 2012-03-31
US20080280957A1 (en) 2008-11-13
AR082825A2 (es) 2013-01-09
HK1121140A1 (en) 2009-04-17
EP1922307A4 (en) 2009-12-30
CA2608201A1 (en) 2007-04-19
SG177981A1 (en) 2012-02-28
HK1124048A1 (en) 2009-07-03
SI1922307T1 (es) 2012-04-30
DK1922307T3 (da) 2012-04-02
JP5270336B2 (ja) 2013-08-21
EP1967516A1 (en) 2008-09-10
RU2010144823A (ru) 2012-05-10
NZ587189A (en) 2011-11-25
IL212396A (en) 2015-09-24
JP2009215312A (ja) 2009-09-24
JP5089649B2 (ja) 2012-12-05
IL187353A0 (en) 2008-04-13
ZA200710318B (en) 2012-09-26
WO2007044084A2 (en) 2007-04-19
BRPI0610139A2 (pt) 2010-06-01
MY149960A (en) 2013-11-15
HK1162028A1 (en) 2012-08-17
KR20110074772A (ko) 2011-07-01
ATE447559T1 (de) 2009-11-15
AU2006299902B2 (en) 2012-11-01
UA100007C2 (ru) 2012-11-12
EP2361905B1 (en) 2013-03-06
TWI506020B (zh) 2015-11-01
CY1112297T1 (el) 2015-12-09
KR20110074908A (ko) 2011-07-04
ZA201203844B (en) 2014-02-26
ECSP078013A (es) 2008-04-28
DE602006010243D1 (de) 2009-12-17
WO2007044084A3 (en) 2009-04-16
MY149957A (en) 2013-11-15
IL187353A (en) 2013-02-28
EP2364973B1 (en) 2014-07-09
JP2013028637A (ja) 2013-02-07

Similar Documents

Publication Publication Date Title
ES2500068T3 (es) Inhibidores heterocíclicos de MEK y métodos de uso de los mismos
ES2509820T3 (es) Derivados de indazol como inhibidores de la cinasa para el tratamiento del cáncer
ES2524966T3 (es) Derivados de tieno[3,2-c]piridina como inhibidores de quinasas para uso en el tratamiento del cáncer
ES2526338T3 (es) Inhibidor de DPP-IV que incluye grupo beta-amino, método de preparación del mismo y composición farmacéutica que contiene el mismo para prevernir y tratar diabetes u obesidad
AR063015A1 (es) Derivados de quinazolinona 5-sustituida y composiciones que los comprenden y metodos para utilizarlos en el tratamiento del cancer
CO5271665A1 (es) (compuestos de pirrolo [2,3-d] pirimidina
AR061134A1 (es) Derivados de tioxantina
CO6321254A2 (es) Pirimidin -5-carboxamidas sustituidas 281
ECSP10010693A (es) Compuestos pirazólicos 436
CL2012000999A1 (es) Compuestos derivados de pirazoloespirocetona sustituida, inhibidores de acetil-coa carboxilasa; composicion farmaceutica que los comprende; uso para tratar o retrasar la progresion o el inicio de diabetes tipo 2, higado graso no alcoholico (hgna) o la resistencia hepatica a la insulina.
NO20044995L (no) Heterosykliske forbindelser
AR034282A1 (es) Derivados de difenilazetidinona, medicamentos que contienen estos compuestos, procedimiento para su preparacion, y su utilizacion para la preparacion de medicamentos
UY30314A1 (es) Derivados de benzonitrilo sustituidos con glucopiranosilo, composiciones farmacéuticas que contienen compuestos de este tipo, su uso y procedimiento para su fabricacion
UY26727A1 (es) Derivados de tropano útiles en terapia
CO6190521A2 (es) Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta -9 desaturasa
CO6150149A2 (es) Compuestos azabiciclicos como inhibidfores de la recaptacion de monoaminas
AR049578A1 (es) Derivados de hidantoina, procesos de obtencion y composiciones farmaceuticas
ATE477256T1 (de) Thienylverbindungen
PE20090357A1 (es) Compuestos heterociclicos con actividad sobre los receptores muscarinicos m3
MX2010007502A (es) Compuestos de tienopiridazina, sus preparaciones, composiciones farmaceuticas y sus usos.
UY29169A1 (es) Derivados de 2-amido-4 feniltiazol, su preparacion y su aplicacion en terapeutica
AR049274A1 (es) Acido2-{[2-(2-metilaminopirimidin-4-il)-1h-indol-5-carbonil]amino}-3-(fenilpiridin-2-ilamino)propionico sustancialmente puro como inhibidor selectivo de la quinasa ikk-2
AR065468A1 (es) Derivados de nevirapina inhibidores de la transcriptasa reversa
CO2024010726A2 (es) Compuestos heterocíclicos y métodos de uso
AR045376A1 (es) Uso de alcoxilatos de alcohol como adyuvantes para derivados de benzamidoxima fungicidas, agentes y kits correspondientes