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AR058338A1 - Derivados de pirrol fusionado, composiciones farmaceuticas que los contienen y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la quinasa. - Google Patents

Derivados de pirrol fusionado, composiciones farmaceuticas que los contienen y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la quinasa.

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Publication number
AR058338A1
AR058338A1 ARP060105492A ARP060105492A AR058338A1 AR 058338 A1 AR058338 A1 AR 058338A1 AR P060105492 A ARP060105492 A AR P060105492A AR P060105492 A ARP060105492 A AR P060105492A AR 058338 A1 AR058338 A1 AR 058338A1
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AR
Argentina
Prior art keywords
alkyl
optionally substituted
ring
cycloalkyl
heteroaryl
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Application number
ARP060105492A
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English (en)
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Hoffmann La Roche
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37782002&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR058338(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR058338A1 publication Critical patent/AR058338A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P13/12—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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04—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
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/06—Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Estos compuestos inhiben la quinasa y pueden utilizarse como medicamentos. Reivindicacion 1: Compuestos de la formula (1) en la que A es un anillo bencénico o un anillo heteroarilo, que es un anillo aromático monocíclico de 5 o 6 átomos en el anillo, que tiene 1, 2 o 3 heteroátomos en el anillo elegidos entre N, O y S, los demás átomos el anillo son C; Ar es naftalenilo o heteroarilo, que es un radical aromático bicíclico de 8 a 10 átomos en el anillo, que tiene por lo menos un anillo aromático que contiene 1, 2 o 3 heteroátomos en el anillo, elegidos entre N, O y S, los demás átomos del anillo son C, dichos naftalenilo y heteroarilo están opcionalmente sustituidos con 1 a 3 sustituyentes elegidos con independencia entre sí entre el grupo formado por alquilo C1-6, cicloalquilo C3-7, (cicloalquil C3-7)-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, hidroxi, alcoxi C1-6, halogeno, heteroalquilo, heteroalcoxi, nitro, cano, amino y amino mono- o disustituido con alquilo C1-6; R1 es H, halogeno, alquilo C1-6, alcoxi C1-6, carboxilo, nitro, ciano, amino, amino mono- o disustituido con alquilo C1-6, heteroalquilo, heteroalcoxi, cicloalquilo C3-7, (cicloalquil C3-7)-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, hidroxi, alcoxi C1-6, heterociclil-alquilo C1-6 opcionalmente sustituido, heterociclilcarbonil-alquilo C1-6 opcionalmente sustituido, fenil-alquilo C1-6 opcionalmente sustituido, fenilcarbonil-alquilo C1-6 opcionalmente sustituido, heteroaril-alquilo C1-6 opcionalmente sustituido, heteroarilcarbonil-alquilo C1-6 opcionalmente sustituido o heteroalcoxi-alquilo C1-6, o R1 es N(R')(Rö), N(R')(Rö)-alquilo C1-6- o N(R')(Rö)-carbonil-alquilo C1-6-, en los que R' y Rö con independencia entre sí se eligen entre el grupo formado por H, alquilo C1-6, cicloalquilo C3-7, (cicloalquil C3-7)-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, heteroalquilo, fenil-alquilo C1-6 opcionalmente sustituido, heteroaril-alquilo C1-6 opcionalmente sustituido, heterociclil-alquilo C1-6 opcionalmente sustituido, fenilcarbonilo opcionalmente sustituido, heteroarilcarbonilo opcionalmente sustituido y heterociclilcarbonilo opcionalmente sustituido; o R1 es R'-CO-N(Rö)-alquilo C1-6-, R'-O-CO-N(Rö)-alquilo C1-6- , R'-SO2-N(Rö)-alquilo C1-6- o (R')(Rö)N-SO2-N(R'ö)-alquilo C1-6-, en los que R', Rö y R'ö con independencia entre sí se eligen entre el grupo formado por H, alquilo C1-6, cicloalquilo C3-7, (cicloalquil C3-7)-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, heteroalquilo, fenilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, fenil-alquilo C1-6 opcionalmente sustituido, heteroaril-alquilo C1-6 opcionalmente sustituido y heterociclil-alquilo C1-6 opcionalmente sustituido; R2, R2', y R2ö con independencia entre sí son H, halogeno, ciano, nitro, amino, amino mono-o disustituido con alquilo C1-6, alquilo C1-6, cicloalquilo C3-7, (cicloalquil C3-7)-alquilo C1-6, alquenilo C2-6, alquinilo C2- 6, heteroalquilo, hidroxi, alcoxi C1-6 o heteroalcoxi; n es un numero entero de 0 a 4; y los profármacos y sales farmacéuticamente aceptables de los mismos; en la que, a menos que se definan de otro modo, el término ôheteroalquiloö significa alquilo C1-6 sustituido con uno o más sustituyentes elegidos con independencia entre el grupo formado por nitro, hidroxi, halogeno, ciano, alcoxi C1-6, formilo, (alquil C1-6)-carbonilo, carboxilo, alquiltio C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, carbamoílo, amino y amino mono- o disustituido con alquilo C1-6; el término ôheteroalcoxiö significa heteroalquil-O-; el término ôheteroariloö significa un radical aromático monocíclico de 5 a 8 átomos en el anillo, que contiene 1, 2 o 3 heteroátomos en el anillo elegidos entre N, O y S, los demás átomos del anillo son C; el término ôheterocicliloö significa radicales monocíclicos no aromáticos, de 3 a 8 átomos en el anillo, en el que 1 o 2 átomos del anillo son heteroátomos elegidos entre N, O y S(O)n (en el que n es un numero entero entre 0 y 2), los demás átomos del anillo son C; los términos ôfenilo opcionalmente sustituidoö, ôheteroarilo opcionalmente sustituidoö y ôheterociclilo opcionalmente sustituidoö significan fenilo, heteroarilo y heterociclilo, respectivamente, opcionalmente sustituidos con 1 o más sustituyentes elegidos con independencia entre sí entre el grupo formado por halogeno, nitro, ciano, amino, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, hidroxi, alcoxi C1-6, amino mono- o disustituido con alquilo C1-6, heteroalquilo y heteroalcoxi; el término ôradical aromático bicíclicoö significa un radical que tiene dos anillos aromáticos, que están fusionados.
ARP060105492A 2005-12-15 2006-12-13 Derivados de pirrol fusionado, composiciones farmaceuticas que los contienen y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la quinasa. AR058338A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05112210 2005-12-15

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AR058338A1 true AR058338A1 (es) 2008-01-30

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Country Link
US (1) US7696240B2 (es)
EP (1) EP1966134B1 (es)
JP (1) JP4955012B2 (es)
KR (1) KR101355754B1 (es)
CN (1) CN101351446B (es)
AR (1) AR058338A1 (es)
AU (1) AU2006326136B2 (es)
BR (1) BRPI0619963A2 (es)
CA (1) CA2637740A1 (es)
CR (1) CR10027A (es)
EC (1) ECSP088549A (es)
IL (1) IL191768A0 (es)
MA (1) MA30162B1 (es)
MY (1) MY146491A (es)
NO (1) NO20082561L (es)
NZ (1) NZ568594A (es)
RU (1) RU2434853C2 (es)
TW (1) TWI363755B (es)
UA (1) UA95788C2 (es)
WO (1) WO2007068621A1 (es)

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