AR038420A1 - Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende - Google Patents

Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende

Info

Publication number
AR038420A1
AR038420A1 ARP030100474A ARP030100474A AR038420A1 AR 038420 A1 AR038420 A1 AR 038420A1 AR P030100474 A ARP030100474 A AR P030100474A AR P030100474 A ARP030100474 A AR P030100474A AR 038420 A1 AR038420 A1 AR 038420A1
Authority
AR
Argentina
Prior art keywords
methyl
pyrazol
carboxamide
phenyl
alkyl
Prior art date
Application number
ARP030100474A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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
Priority claimed from GB0203677A external-priority patent/GB0203677D0/en
Priority claimed from GB0203673A external-priority patent/GB0203673D0/en
Priority claimed from GB0203680A external-priority patent/GB0203680D0/en
Priority claimed from GB0209032A external-priority patent/GB0209032D0/en
Priority claimed from GB0209035A external-priority patent/GB0209035D0/en
Priority claimed from GB0209003A external-priority patent/GB0209003D0/en
Priority claimed from GB0221318A external-priority patent/GB0221318D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR038420A1 publication Critical patent/AR038420A1/es

Links

Classifications

    • 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
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/04—Antipruritics
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • 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
    • C07D215/38—Nitrogen 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
    • C07D409/12—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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Uso del compuesto de la fórmula (1) o una de sus sales o solvatos farmacéuticamente aceptables para la fabricación de un medicamento para el tratamiento o profilaxis de trastornos en los que es beneficioso el antagonismo del receptor vainilloide (VR1). Procedimiento para preparar tales compuestos y composición farmacéutica que los comprende. Reivindicación 1:Un compuesto de amida caracterizado porque responde a la fórmula (1) o una de sus sales o solvatos farmacéuticamente aceptables, en la que, P se selecciona entre fenilo, heteroarilo o heterociclilo; R1 y R2 se seleccionan independientemente entre halo, alquilo, alcoxi, cicloalquilo, aralquilo, aralcoxi, cicloalquilalquilo, cicloalquilalcoxi, -CN, -NO2, -OH, =O, -OCF3, -CF3, -NR4R5, S(O)mR6, -S(O)2NR4R5, -OS(O)2R6, -OS(O)2CF3, -O(CH2)nNR4R5, -C(O)CF3, -C(O)alquilo, -C(O)cicloalquilo, -C(O)aralquilo, -C(O)Ar, -C(O)(CH2)nOR6, -C(O)(CH2)nNR4R5, -C(O)alcoxi, -C(O)NR4R5, -(CH2)nC(O)alcoxi, -(CH2)nOC(O)R6, -O(CH2)nOR6, -(CH2)nOR6, -(CH2)nR4R5, -(CH2)nC(O)NR4R5, -(CH2)nN(R4)C(O)R6, -(CH2)nS(O)2NR4R5, -(CH2)nN(R4)S(O)2R6, -ZAr, -(CH2)nS(O)2R6, -(OCH2)nS(O)2R6, -N(R4)S(O)2R6, -N(R4)C(O)R6, -(CH2)nN(R4)S(O)2R6, -(CH2)nN(R4)C(O)R6 o -(CH2)nC(O)alquilo; R3 se selecciona entre alquilo, alcoxi, -CF3, halo, -O(CH2)nOR6, -O(CH2)nNR4R5, fenilo, ciclohexilo, benzo[1,3]dioxiolilo, morfolinilo, piridilo, pirimidinilo, pirazinilo, piperazinilo, piperidinilo, piridizinilo, tienilo, furilo, pirazolilo, pirrolilo, triazolilo, indanilo, imidazolilo, oxazolilo, tiazolilo, oxadiazolilo, isotiazolilo, isoxazolilo o tiadiazolilo; donde dichos grupos alquilo, alcoxi, fenilo, ciclohexilo, benzo[1,3]dioxolilo, morfolinilo, piridilo, pirimidinilo, pirazinilo, piperazinilo, piperidinilo, piridizinilo, tienilo, furilo, pirazolilo, pirrolilo, triazolilo, indanilo, imidazolilo, oxazolilo, tiazolilo, oxadiazolilo, isotiazolilo, isoxazolilo o tiadiazolilo pueden estar opcionalmente sustituidos con uno o más grupos, que pueden ser iguales o diferentes, seleccionados de R2; R4 y R5 pueden ser iguales o diferentes y representa -H o alquilo o R4 y R5 junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico; R6 es -H, alquilo o arilo; R7 es -H, alquilo o arilo; R8 se selecciona entre -H, alquilo, hidroxialquilo, cicloalquilo, aralquilo, alcoxialquilo, cicloalquilalquilo, heterociclilalquilo, -S(O)mR6, -C(O)CF3, -C(O)alquilo, -C(O)cicloalquilo, -C(O)aralquilo, -C(O)Ar, -C(O)(CH2)nOR6, -C(O)(CH2)nNR4R5, -C(O)alcoxi, -C(O)NR4R5, -(CH2)nC(O)alcoxi, -(CH2)nOC(O)R6, -O(CH2)nOR6, -(CH2)nOR6, -(CH2)nR4R5, -(CH2)nC(O)NR4R5, -(CH2)nN(R4)C(O)R6, -(CH2)nS(O)2NR4R5, -(CH2)nN(R4)S(O)2R6, -(CH2)nS(O)2R6, -(CH2)nS(O)2R6, -(CH2)nN(R4)S(O)2R6, -(CH2)nN(R4)C(O)R6 o -(CH2)nC(O)alquilo; o cuando X es NR8 e Y es C(R9)2, R8 se puede combinar con R1 para formar un grupo de benzoquinuclidina; R9 es -H o R1; Ar es arilo o heteroarilo, cada uno de los cuales puede estar opcionalmente sustituido con R2; Z es un enlace, O, S, NR7 o CH2; m es 0, 1 o 2; n es un número entero de 1 a 6; q y r se seleccionan independientemente entre 0, 1, 2 o 3; s es 0, 1, 2, o 3; y X e Y se seleccionan entre las combinaciones (Tabla 1) con la condición de que dicho compuesto de la fórmula (1) no es un compuesto seleccionado entre: N-{3-[(N,N-dimetilamino)metil]-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida; N-{3-[(N,N-dimetilamino)metil]-1-formil-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida, N-{1-acetil-3-[(N,N-dimetilamino)metil]-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida, N-{3-[(N,N-dimetilamino)metil]-1-metilsulfonil-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida; 5-amino-N-isoquinolin-5-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 5-metil-N-quinolin-8-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 5-metil-N-quinolin-7-il-1-[3-trilfuorometil)fenil]-1H-pirazol-3-carboxamida; 5-metil-N-quinolin-3-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, N-isoquinolin-5-il-5-metil-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 5-metil-N-quinolin-5-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 1-(3-clorofenil)-N-isoquinolin-5-il-5-metil-1H-pirazol-3-carboxamida, N-isoquinolin-5-il-1-(3-metoxifenil)-5-metil-1H-pirazol-3-carboxamida, 1-(3-fluorofenil)-N-isoquinolin-5-il-5-metil-1H-pirazol-3-carboxamida, 1-(2-cloro-5-trifluorometilfenil)-N-isoquinolin-5-il-5-metil-1H-pirazol-3-carboxamida, 5-metil-N-(3-metilisoquinolin-5-il)-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, y 5-metil-N-(1,2,3,4-tetrahidroisoquinolin-5-il)-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida.
ARP030100474A 2002-02-15 2003-02-13 Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende AR038420A1 (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB0203677A GB0203677D0 (en) 2002-02-15 2002-02-15 Novel compounds
GB0203673A GB0203673D0 (en) 2002-02-15 2002-02-15 Novel compounds
GB0203680A GB0203680D0 (en) 2002-02-15 2002-02-15 Novel compounds
GB0209032A GB0209032D0 (en) 2002-04-19 2002-04-19 Novel compounds
GB0209035A GB0209035D0 (en) 2002-04-19 2002-04-19 Novel compounds
GB0209003A GB0209003D0 (en) 2002-04-19 2002-04-19 Novel compounds
GB0221318A GB0221318D0 (en) 2002-09-13 2002-09-13 Novel compounds

Publications (1)

Publication Number Publication Date
AR038420A1 true AR038420A1 (es) 2005-01-12

Family

ID=27739514

Family Applications (1)

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ARP030100474A AR038420A1 (es) 2002-02-15 2003-02-13 Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende

Country Status (10)

Country Link
US (1) US7538121B2 (es)
EP (2) EP2033953A1 (es)
JP (1) JP2005526723A (es)
AR (1) AR038420A1 (es)
AT (1) ATE416168T1 (es)
AU (1) AU2003245773A1 (es)
DE (1) DE60325025D1 (es)
ES (1) ES2316777T3 (es)
TW (1) TW200403223A (es)
WO (1) WO2003068749A1 (es)

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