AR089189A1 - Inhibidores de quinasa - Google Patents

Inhibidores de quinasa

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Publication number
AR089189A1
AR089189A1 ARP120104598A ARP120104598A AR089189A1 AR 089189 A1 AR089189 A1 AR 089189A1 AR P120104598 A ARP120104598 A AR P120104598A AR P120104598 A ARP120104598 A AR P120104598A AR 089189 A1 AR089189 A1 AR 089189A1
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Argentina
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nrarb
cycloalkylene
alkylene
ord
alkyl
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ARP120104598A
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English (en)
Inventor
Charles Ray Nicholas
Alcaraz Lilian
Aaron Panchal Terry
Stephen Robert Jennings Andrew
Armani Elisabetta
Peter Cridland Andrew
Hurley Christopher
Bodil Van Niel Monique
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Chiesi Farma Spa
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47471708&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR089189(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chiesi Farma Spa filed Critical Chiesi Farma Spa
Publication of AR089189A1 publication Critical patent/AR089189A1/es

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/02—Formic acid
    • C07C53/06—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Útiles como agentes antiinflamatorios en el tratamiento de enfermedades del tracto respiratorio, entre otras. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o una sal farmacéuticamente aceptable del mismo, donde: W es un heteroátomo seleccionado entre N ó O, donde N está sustituido con hidrógeno, alquilo C₁₋₆ o cicloalquilo C₃₋₅; Y se selecciona entre el grupo que consiste en: un grupo -S(O)ₚ- donde p es 0, 1 ó 2; un grupo -O(CR³R⁴)ₙ-; un grupo -(CR⁵R⁶)ₙ-; un grupo -NR⁷-; un grupo -OC(O)-; un grupo -OC(O)NH-; y un grupo -OC(O)O-; R³, R⁴, R⁵ y R⁶ son en forma independiente entre sí hidrógeno, flúor o alquilo C₁₋₆, o, respectivamente, R³ y R⁴, o R⁵ y R⁶ pueden formar junto con el átomo de carbono al cual se encuentran unidos un anillo carbocíclico monocíclico saturado de 3 - 6 miembros opcionalmente sustituido con un grupo alquilo C₁₋₆, hidroxilo o halo; n es 0, 1, 2 ó 3; R⁷ es hidrógeno, alquilo C₁₋₆, o cicloalquilo C₃₋₇, donde dichos alquilo C₁₋₆ o cicloalquilo C₃₋₇ están opcionalmente sustituidos con un grupo alquilo C₁₋₃, cicloalquilo C₃₋₆, hidroxilo, ciano o halo; R¹ es un grupo seleccionado entre los compuestos de fórmulas (2) - (4); R⁸ y R⁹ son en forma independiente entre sí hidrógeno o alquilo C₁₋₆, o R⁸ y R⁹ pueden formar junto con el átomo de nitrógeno al cual están unidos un sistema de anillos monocíclico o bicíclico fusionado o espiro saturado de 5 - 11 miembros que contiene opcionalmente un heteroátomo adicional que es oxígeno o nitrógeno, donde dicho átomo de nitrógeno está opcionalmente sustituido con alquilo C₁₋₆; donde dichos grupos alquilo C₁₋₆ pueden estar opcionalmente sustituidos con un grupo alquilo C₁₋₆, cicloalquilo C₃₋₆, hidroxilo o halo; X¹, X², X³, X⁴ y X⁵ son en forma independiente entre sí un átomo de carbono, un átomo de nitrógeno, un grupo -(CH)- o un grupo -NH-; de manera que cada combinación de los mismos forma un sistema de anillos aromático; R¹⁰ se selecciona entre un grupo que consiste en: hidrógeno, -CN, NRARB, -N(RC)(alquilen C₂₋₆)-NRARB, -N(RC)(cicloalquilen C₃₋₇)-NRARB, (alquilen C₁₋₆)-NRARB, (cicloalquilen C₃₋₇)-NRARB, -O-(alquilen C₂₋₆)-NRARB, -O-(cicloalquilen C₃₋₇)-NRARB, S-(alquilen C₂₋₆)-NRARB, -S-(cicloalquilen C₃₋₇)-NRARB, -N(RC)C(O)-(alquilen C₁₋₆)-NRARB, -N(RC)C(O)-(cicloalquilen C₃₋₇)-NRARB, -C(O)N(RC)-(alquilen C₂₋₆)-NRARB, -C(O)N(RC)-(cicloalquilen C₃₋₇)-NRARB, -C(O)N(RC)-(alquilen C₂₋₆)-ORD, -C(O)N(RC)-(cicloalquilen C₃₋₇)-ORD, -N(RC)C(O)NRARB, -C(O)NRARB, -N(RC)C(O)N(RC)-(alquilen C₂₋₆)-NRARB,-N(RC)C(O)N(RC)-(cicloalquilen C₃₋₇)-NRARB, -(alquilen C₂₋₆)-ORD, -(cicloalquilen C₃₋₇)-ORD, -O-(alquilen C₂₋₆)-ORD, -O-(cicloalquilen C₃₋₇)-ORD, -S-(alquilen C₂₋₆)-ORD, -S-(cicloalquilen C₃₋₇)-ORD, -N(RC)S(O)₂-(alquilen C₁₋₆)-NRARB, -N(RC)S(O)₂-(cicloalquilen C₃₋₇)-NRARB, -S(O)₂N(RC)-(alquilen C₂₋₆)-NRARB, -S(O)₂N(RC)-(cicloalquilen C₃₋₇)-NRARB, -S(O)₂N(RC)-(alquilen C₂₋₆)-ORD, -S(O)₂N(RC)-(cicloalquilen C₃₋₇)-ORD, N(RC)S(O)₂-(alquilen C₂₋₆)-ORD, -N(RC)S(O)₂-(cicloalquilen C₃₋₇)-ORD, -S(O)₂N(RARB), -N(RC)S(O)₂RD, -N(RC)C(O)RC, -ORC, -SRC, -(heterocicloalquilo C₃₋₇), (heterocicloalquil C₅₋₇)-(alquilo C₁₋₆), (heterocicloalquil C₅₋₇)(cicloalquilo C₃₋₆)-, y heterocicloalquil C₃₋₇carbonilo; donde cualquiera de dichos alquilo C₁₋₆, cicloalquilo C₃₋₆, -(alquilen C₁₋₆)-, -(alquileno C₂₋₆)-, -(cicloalquileno C₃₋₇)-, -(heterocicloalquilo C₃₋₇), (heterocicloalquil C₅₋₇)-(alquilo C₁₋₆), (heterocicloalquil C₅₋₇)-(cicloalquilo C₃₋₆) y (heterocicloalquil C₃₋₇)carbonilo de los grupos que se han enumerado puede estar opcionalmente sustituido con un grupo alquilo C₁₋₆, cicloalquilo C₃₋₇, hidroxilo o halo; R¹¹ está unido a X⁴ y se selecciona entre un grupo que consiste en: hidrógeno; -CN; alquilo C₁₋₆, el cual está sustituido con un grupo seleccionado entre -CN, -ORC, -SRC, halo; cicloalquilo C₃₋₆, el cual está sustituido con un grupo seleccionado entre alquilo C₁₋₄, -CN, -ORC, -SRD, halo; -NRARB, -N(RC)(alquilen C₂₋₆)-NRARB, -N(RC)(cicloalquilen C₃₋₇)-NRARB, -(alquilen C₁₋₆)-NRARB, -(cicloalquilen C₃₋₇)-NRARB, -O-(alquilen C₂₋₆)-NRARB, -O-(cicloalquilen C₃₋₇)-NRARB, -S-(alquilen C₂₋₆)-NRARB, -S-(cicloalquilen C₃₋₇)-NRARB, -N(RC)C(O)-(alquilen C₁₋₆)-NRARB, -N(RC)C(O)-(cicloalquilen C₃₋₇)-NRARB, -C(O)N(RC)-(alquilen C₂₋₆)-NRARB, -C(O)N(RC)-(cicloalquilen C₃₋₇)-NRARB, -C(O)N(RC)-(alquilen C₂₋₆)-ORD, -C(O)N(RC)-(cicloalquilen C₃₋₇)-ORD, -N(RC)C(O)N(RARB), -C(O)N(RARB), -N(RC)C(O)N(RC)-(alquilen C₂₋₆)-NRARB, -N(RC)C(O)N(RC)-(cicloalquilen C₃₋₇)-NRARB, -O-(alquilen C₂₋₆)-ORD, -O-(cicloalquilen C₃₋₇)-ORD, -S-(alquilen C₂₋₆)-ORD, -S-(cicloalquilen C₃₋₇)-ORD, -N(RC)S(O)₂-(alquilen C₁₋₆)-NRARB, -N(RC)S(O)₂-(cicloalquilen C₃₋₇)-NRARB, -S(O)₂N(RC)-(alquilen C₂₋₆)-NRARB, -S(O)₂N(RC)-(cicloalquilen C₃₋₇)-NRARB, -S(O)₂N(RC)-(alquilen C₂₋₆)-ORD, -S(O)₂N(RC)-(cicloalquilen C₃₋₇)-ORD, -N(RC)S(O)₂-(alquilen C₂₋₆)-ORD, -N(RC)S(O)₂-(cicloalquilen C₃₋₇)-ORD, -S(O)₂N(RARB), -N(RC)S(O)₂RD, -N(RC)C(O)RC, ORC, SRC, -(heterocicloalquilo C₃₋₇), (heterocicloalquil C₅₋₇)-(alquilo C₁₋₆), (heterocicloalquil C₅₋₇)(cicloalquilo C₃₋₆) y (heterocicloalquil C₃₋₇)carbonilo, donde cualquiera de dichos alquilo C₁₋₆, cicloalquilo C₃₋₆, -(alquilen C₁₋₆)-, -(alquileno C₂₋₆)-, -(cicloalquileno C₃₋₇)-, -(heterocicloalquilo C₃₋₇), (heterocicloalquil C₅₋₇)-(alquilo C₁₋₆), (heterocicloalquil C₅₋₇)-(cicloalquilo C₃₋₆) y (heterocicloalquil C₃₋₇)carbonilo de los grupos que se han enumerado puede estar opcionalmente sustituido con uno, dos o tres grupos R²⁵ que se seleccionan en forma independiente de la lista que consiste en: alquilo C₁₋₆, haloalquilo C₁₋₃, hidroxialquilo C₁₋₄, cicloalquilo C₃₋₇, hidroxilo y halo; o R¹¹ está unido a X⁴ y es fenilo o heteroarilo monocíclico de 5 ó 6 miembros, donde dichos fenilo o heteroarilo monocíclico de 5 ó 6 miembros están sustituidos con un grupo seleccionado de la lista que consiste en: alquilo C₁₋₆, el cual está sustituido con un grupo -CN; cicloalquilo C₃₋₆, el cual está sustituido con un grupo seleccionado entre: -CN, -ORC, -SRC o halo; -N(RC)-(alquilen C₂₋₆)-NRARB, -N(RC)-(cicloalquilen C₃₋₇)-NRARB, -(alquilen C₁₋₆)-NRARB, -(cicloalquilen C₃₋₇)-NRARB, -O-(cicloalquilen C₃₋₇)-NRARB, -S-(alquilen C₂₋₆)-NRARB, -S-(cicloalquilen C₃₋₇)-NRARB, -N(RC)C(O)-(alquilen C₁₋₆)-NRARB, -N(RC)C(O)-(cicloalquilen C₃₋₇)-NRARB, -C(O)N(RC)-(alquilen C₂₋₆)-NRARB, -C(O)N(RC)-(cicloalquilen C₃₋₇)-NRARB, -C(O)N(RC)-(alquilen C₂₋₆)-ORD, -C(O)N(RC)-(cicloalquilen C₃₋₇)-ORD, -N(RC)C(O)N(RC)-(alquilen C₂₋₆)-NRARB, -N(RC)C(O)N(RC)-(cicloalquilen C₃₋₇)-NRARB, -O-(cicloalquilen C₃₋₇)-ORD, -S-(cicloalquilen C₃₋₇)-ORD, -N(RC)S(O)₂-(alquilen C₁₋₆)-NRARB, -N(RC)S(O)₂-(cicloalquilen C₃₋₇)-NRARB, -S(O)₂N(RC)-(alquilen C₂₋₆)-NRARB, -S(O)₂N(RC)-(cicloalquilen C₃₋₇)-NRARB, -S(O)₂N(RC)-(alquilen C₂&#x208
ARP120104598A 2011-12-09 2012-12-07 Inhibidores de quinasa AR089189A1 (es)

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EP11192871 2011-12-09
EP12187931 2012-10-10

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AR089189A1 true AR089189A1 (es) 2014-08-06

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KR20140103925A (ko) * 2011-12-09 2014-08-27 키에시 파르마슈티시 엣스. 피. 에이. 4-히드록시-1,2,3,4-테트라히드로나프탈렌-1-일 우레아 및 호흡기 질환의 치료에서의 이들의 용도
SG11201402986RA (en) * 2011-12-09 2014-12-30 Chiesi Farma Spa Kinase inhibitors
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