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AR039823A1 - Moduladores ureicos derivados de la amino-tetralina del receptor vr1 de vanilloides - Google Patents

Moduladores ureicos derivados de la amino-tetralina del receptor vr1 de vanilloides

Info

Publication number
AR039823A1
AR039823A1 ARP030101730A ARP030101730A AR039823A1 AR 039823 A1 AR039823 A1 AR 039823A1 AR P030101730 A ARP030101730 A AR P030101730A AR P030101730 A ARP030101730 A AR P030101730A AR 039823 A1 AR039823 A1 AR 039823A1
Authority
AR
Argentina
Prior art keywords
alkanyl
group
independently selected
halogen
optionally substituted
Prior art date
Application number
ARP030101730A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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=29550146&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR039823(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR039823A1 publication Critical patent/AR039823A1/es

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    • 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
    • C07D213/40—Acylated substituent nitrogen atom
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/26—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
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    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
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    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/32—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04—Derivatives of thiourea
    • C07C335/14—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of rings other than six-membered aromatic rings
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    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
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    • C07D217/08—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

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  • Chemical & Material Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

Son potentes antagonistas o agonistas de VR1 que son útiles para el tratamiento y prevención de trastornos inflamatorios y de otros trastornos dolorosos en mamíferos. Reivindicación 1: Una composición que comprende un compuesto de fórmula (1) en donde: R1 es un sustituyente independientemente seleccionado a partir del grupo que consiste de hidrógeno; hidroxi; halógeno; alcanilo C1-8 opcionalmente sustituido con uno o más sustituyentes independientemente seleccionados a partir del grupo que consiste de halógeno, alcanilo fluorado y alcaniloxi C1-8; alcaniloxi C1-8 opcionalmente sustituido con uno o más sustituyentes independientemente seleccionados a partir del grupo formado por halógeno, alcanilo fluorado y alcaniloxi C1-8, alcaniloxi fluorado, alcanilo fluorado, alcaniltio C1-8 opcionalmente sustituido con uno o más sustituyentes independientemente seleccionados a partir del grupo formado por halógeno, alcanilo fluorado y alcaniloxi C1-8; cicloalcanilo C3-8; cicloalcaniloxi C3-8; nitro; amino; alcanilamino C1-8; dialcanilamino C1-8; cicloalcanilamino C3-8; ciano; carboxi; alcaniloxicarbonilo C1-7; alcanilcarboniloxi C1-7; formilo; fenilo opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por halógeno, hidroxilo, nitro, amino y ciano; aroilo; carbamoilo; amidino; (alcanilamino C1-8)carbonilo; (arilamino)carbonilo y aril(alcanilC1-8)carbonilo; n es un número entero entre 1 a 3; m es un número entero entre 0 a 3; R2 es independientemente seleccionado a partir del grupo formado por hidrógeno; hidroxi; alcanilo C1-8; alquenilo C2-8; alquilidenilo C1-8; alquilidinilo C1-8; flúor; cloro; cicloalcanilo C3-8; fenilo opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por halógeno, hidroxi, alcanilo C1-8, alcaniloxi C1-8, fenilalcaniloxi C1-8, alcanilo fluorado, ciano, nitro, amino, alcanilamino C1-8 y dialcanilamino C1-8; naftilo opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por halógeno, hidroxi, alcanilo C1-8, alcaniloxi C1-8, fenilalcaniloxi C1-8, alcanilo fluorado, ciano, nitro, amino, alcanilamino C1-8 y dialcanilamino C1-8; fenoxi opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por halógeno, hidroxi, alcanilo C1-8, alcaniloxi C1-8, alcanilo fluorado, ciano y nitro; y heteroarilo opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por alcanilo C1-8 y halógeno donde dicho heteroarilo es piridilo, pirimidilo, furilo, tienilo o imidazolilo; pirrolidino; y piperidino; L es un enlace directo, alcandiilo C1-8, alquendiilo C2-8, alquindiilo C2-8, ó cicloalcandiilo C3-8; R3 está seleccionado a partir del grupo formado por fenilo opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por alcanilo C1-8, halógeno, alcaniloxi C1-8, hidroxi, alcanilo fluorado, nitro, amino, dialcanilamino C1-8, alcanilamino C1-8 y ciano; naftilo opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por alcanilo C1-8, halógeno, alcaniloxi C1-8, hidroxi, alcanilo fluorado, nitro, amino, dialcanilamino C1-8, alcanilamino C1-8 y ciano; y heteroarilo opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados a partir del grupo formado por alcanilo C1-8, halógeno, nitro, amino y ciano en donde dicho heteroarilo es quinolinilo, quinolinil-N-óxido, isoquinolinilo, isoquinolinil-N-oxido, piridilo, piridil-N-óxido, pirimidilo, furilo, tienilo o imidazolilo; R4 está seleccionado a partir del grupo formado por hidrógeno y alcanilo C1-8; R5 está seleccionado a partir del grupo formado por hidrógeno y alcanilo C1-8; X está seleccionado a partir del grupo formado por O y S; y enantiómeros, diastereómeros, tautómeros, solvatos y sales farmacéuticamente aceptables de los mismos.
ARP030101730A 2002-05-17 2003-05-16 Moduladores ureicos derivados de la amino-tetralina del receptor vr1 de vanilloides AR039823A1 (es)

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