AR033542A1 - Esteres oxigenados de acidos 4-yodo fenilamino benzhidroxamicos - Google Patents

Esteres oxigenados de acidos 4-yodo fenilamino benzhidroxamicos

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Publication number
AR033542A1
AR033542A1 ARP010103402A ARP010103402A AR033542A1 AR 033542 A1 AR033542 A1 AR 033542A1 AR P010103402 A ARP010103402 A AR P010103402A AR P010103402 A ARP010103402 A AR P010103402A AR 033542 A1 AR033542 A1 AR 033542A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
alkoxy
compound
phenyl
Prior art date
Application number
ARP010103402A
Other languages
English (en)
Inventor
Stephen Douglas Barrett
Cathlin Biwersi
Michael Kaufman
Haile Tecle
Joseph Scott Warmus
Gu Chen Michael Huai
Original Assignee
Warner Lambert Co
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 Warner Lambert Co filed Critical Warner Lambert Co
Publication of AR033542A1 publication Critical patent/AR033542A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/52—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C229/54—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C229/56—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho-position
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/10—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/18—Radicals substituted by singly bound oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
    • C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

Se refiere a ésteres oxigenados de derivados del ácido 4-iodofenilamino benzhidroxámico, composiciones farmacéuticas y métodos de uso de aquéllos y también con formas cristalinas de ésteres oxigenados de derivados del ácido 4-iodofenilamino benzhidroxámico, composiciones farmacéuticas y métodos de uso de los mismos. Los compuestos de la presente son inhibidores de MEK y son utiles en el tratamiento de una variedad de estados de enfermedades proliferativas, tales como las condiciones relacionadas con la hiperactividad de MEK, así como enfermedades moduladas por la cascada de MEK. Un compuesto que tiene la formula (1), en donde:R1 es hidrogeno, halogeno, o nitro; R2 es hidrogeno o fluor; R3 es hidrogeno o fluor; R4 es hidrogeno, yodo, bromo, cloro, o fluor; R5 es hidrogeno, halogeno, hidroxi, alquilo C1-8, alcoxi C1-8, trifluorometilo, o ciano; n es 1 a 5; R6, R7, R8, R9, y R10 son independientemente hidrogeno, alquilo C1-8, cicloalquilo C3-8, hidroxi, alcoxi C1-8, perhaloalquilo C1-3, hidroxialquilo C1-8, alcoxi C1-5, alquilo C1-5, [alquilo C1-4]2 aminometilo, heterociclo C2-7, alquilo C1-5, o ariloxialquilo C1-5, o puede ser unido independientemente para completar un anillo cíclico de 3-10 miembros que contiene optativamente heteroátomos adicionales seleccionados del grupo formado por O, S, NH, y N-alquilo, en donde R7 y R8 se seleccionan independientemente para n > 1; Ra y Rb son independientemente hidrogeno o alquilo C1-4; W es O o NRa; R11 es hidrogeno, alquilo C1-8, alquenilo C2-6, cicloalquilo C3-8, hidroxialquilo C1-8, alcoxi C1-5 alquilo C1-5, fenilo, heteroarilo C2-7, alquilcarbonilo C1-8, (fenil) carbonilo, (fenil) (alquilo C1-3) carbonilo, o trifluoroalquilo C1-6; en donde los grupos alquilo, alcoxi, cicloalquilo, heteroarilo y fenilo se pueden sustituir optativamente con entre 1 y 5 sustituyentes seleccionados independientemente del grupo formado por hidroxi, amino, monoalquilamino, dialquilamino, halogeno, ciano, alcoxi C1-3, COOR, OCORa, CONRb, NRaCORb, SO, SO2, SO4 y SO2NRaRb; y sales farmacéuticamente aceptables; siempre que cuando R11 es fenilo y n es 1, W no puede ser O; además siempre que el compuesto no sea 5-bromo-N-(2-dietilamino-etoxi)-3,4-difluoro-(4-yodo-2-metil-fenilamino)-benzamida; 5-bromo-N-(2-dimetilamino-propoxi)-3,4-difluoro-2-(4-yodo-2-metil-fenilamino)-benzamida; o 5-bromo-2-(2-cloro-4-yodo-fenilamino)-N-(2-dimetilamino-etoxi)-3,4-difluoro-benzamida. Una composicion farmacéutica que comprende dicho compuesto y un portador farmacéuticamente aceptable. Dicha composicion es de aplicacion en un método de tratamiento de una enfermedad proliferativa en un paciente que lo necesita, que comprende administrar una cantidad terapéuticamente efectiva de dicho compuesto. Dicho método donde la enfermedad proliferativa se selecciona del grupo formado por cáncer, restenosis, soriasis y aterosclerosis. La composicion también es de utilidad en un método de tratamiento de la psoriasis, cáncer, osteoartritis, artritis reumatoidea, insuficiencia cardíaca, dolor cronico, dolor neuropático, en un paciente que lo necesita, que comprende administrar una cantidad terapéuticamente efectiva de dicho compuesto.
ARP010103402A 2000-07-19 2001-07-17 Esteres oxigenados de acidos 4-yodo fenilamino benzhidroxamicos AR033542A1 (es)

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US21937200P 2000-07-19 2000-07-19

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AR033542A1 true AR033542A1 (es) 2003-12-26

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ID=22819013

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Application Number Title Priority Date Filing Date
ARP010103402A AR033542A1 (es) 2000-07-19 2001-07-17 Esteres oxigenados de acidos 4-yodo fenilamino benzhidroxamicos
ARP140103181A AR097445A2 (es) 2000-07-19 2014-08-25 Ésteres oxigenados de ácidos 4-yodo fenilamino benzhidroxámicos

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ARP140103181A AR097445A2 (es) 2000-07-19 2014-08-25 Ésteres oxigenados de ácidos 4-yodo fenilamino benzhidroxámicos

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US (2) US6960614B2 (es)
EP (1) EP1301472B1 (es)
JP (1) JP3811775B2 (es)
KR (1) KR100773621B1 (es)
CN (1) CN1219753C (es)
AP (2) AP2003002742A0 (es)
AR (2) AR033542A1 (es)
AU (2) AU2001273498B2 (es)
BG (1) BG66386B1 (es)
BR (1) BRPI0112584B8 (es)
CA (1) CA2416685C (es)
CZ (1) CZ303815B6 (es)
DK (1) DK1301472T3 (es)
DZ (1) DZ3401A1 (es)
EA (1) EA005818B1 (es)
EC (1) ECSP034430A (es)
EE (1) EE05450B1 (es)
ES (1) ES2461854T3 (es)
GE (1) GEP20053496B (es)
GT (1) GT200100141A (es)
HK (1) HK1055943A1 (es)
HR (1) HRP20030083A2 (es)
HU (1) HU230251B1 (es)
IL (1) IL153817A0 (es)
IS (1) IS6666A (es)
MA (1) MA26930A1 (es)
MY (1) MY151458A (es)
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OA (1) OA12333A (es)
PA (1) PA8522601A1 (es)
PE (1) PE20020664A1 (es)
PL (1) PL203387B1 (es)
PT (1) PT1301472E (es)
SI (1) SI1301472T1 (es)
SK (1) SK288317B6 (es)
SV (1) SV2002000563A (es)
TN (1) TNSN01108A1 (es)
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UA (1) UA76425C2 (es)
WO (1) WO2002006213A2 (es)
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