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AR073631A1 - Antagonistas del receptor transitorio potencial de vanilloides 1 ( trpv1) utiles para tratar inflamacion y dolor - Google Patents

Antagonistas del receptor transitorio potencial de vanilloides 1 ( trpv1) utiles para tratar inflamacion y dolor

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Publication number
AR073631A1
AR073631A1 ARP090103975A ARP090103975A AR073631A1 AR 073631 A1 AR073631 A1 AR 073631A1 AR P090103975 A ARP090103975 A AR P090103975A AR P090103975 A ARP090103975 A AR P090103975A AR 073631 A1 AR073631 A1 AR 073631A1
Authority
AR
Argentina
Prior art keywords
dihydro
urea
indazol
chromen
benzopyran
Prior art date
Application number
ARP090103975A
Other languages
English (en)
Inventor
Robert G Schimidt
Arthur R Gomtsyan
Eric A Voight
Michael E Kort
Philip R Kym
Heath A Mcdonald
Erol K Bayburt
Jun Chen
Jerome F Daanen
Jr Stanley Didomenico
Richard J Perner
Original Assignee
Abbott Lab
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Publication date
Application filed by Abbott Lab filed Critical Abbott Lab
Publication of AR073631A1 publication Critical patent/AR073631A1/es

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    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links

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Abstract

Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) o una sal solvato, prodroga, sal de una prodroga aceptables para uso farmacéutico, o una combinacion de los mismos, donde R1 representa un grupo de formula (a), (b), (c) o (d); Rx, en cada caso, representa sustituyente(s) opcional(es) sobre cualquier posicion sustituible del anillo bicíclico seleccionados entre el grupo que consiste de alquilo, halogeno, haloalquilo, OH, O(alquilo), O(haloalquilo), NH2, N(H)(alquilo), y N(alquilo)2; Ra es hidrogeno o metilo; R2 y R3 son iguales o diferentes, y son cada uno en forma independiente hidrogeno, alquilo C1-5, o haloalquilo; o R2 y R3, junto con el átomo de carbono al cual se encuentran unidos, forman un anillo cicloalquilo monocíclico de 3 a 6 átomos de carbono, opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados entre el grupo que consiste de alquilo y halogeno; R4 en cada caso, representa sustituyente(s) opcional(es) sobre cualquier posicion sustituible del anillo bicíclico seleccionados entre el grupo que consiste de alquilo, halogeno, haloalquilo, O(alquilo), O(haloalquilo), y SCF3; y m y n son cada uno en forma independiente 0, 1, 2 o 3; con la condicion de que el compuesto no es N-(7-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-isoquinolin-5-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-1H-indazol-4-il-N'-(6-metil-3,4-dihidro-2H-cromen-4-il)urea; N-isoquinolin-5-il-N'-(6-metil-3,4-dihidro-2H-cromen-4-il)urea; N-(6-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(6-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-isoquinolin-5-ilurea; N-(6-cloro-7-metil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(6-cloro-7-metil-3,4-dihidro-2H-cromen-4-il)-N'-isoquinolin-5-ilurea; N-3,4-dihidro-2H-cromen-4-il-N'-1H-indazol-4-ilurea; N-(7-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-(3metilisoquinolin-5-il)urea; N-(6-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-(3-metilisoquinolin-5-il)urea; N-(6-metil-3,4-dihidro-2H-cromen-4-il)-N'-(3-metilisoquinolin-5-il)urea; N-isoquinolin-5-il-N'-(8-piperidin-1-il-3,4-dihidro-2H-cromen-4-il)urea; N-3,4-dihidro-2H-cromen-4-il-N'-isoquinolin-5-ilurea; (+)-N-isoquinolin-5-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; (-)-N-isoquinolin-5-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-1H-indazol-4-il-N'-[8-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; (-)-N-1H-indazol-4-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; (+)-N-1H-indazol-4-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-1H-indazol-4-il-N'-(8-piperidin-1-il-3,4-dihidro-2H-cromen-4-il)urea; N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-[8-cloro-7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]-N'-1H-indazol-4-ilurea; (+)-N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; (-)-N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-[8-(trifluorometoxi)-3,4-dihidro-2H-cromen-4-il]urea; N-[8-fluoro-7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-[7-(trifluorometoxi)-3,4-dihidro-2H-cromen-4-il]urea; N-(6-fluoro-2-metil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-(7-metoxi-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)urea; N-1H-indazol-4-il-N'-(7-metoxi-2,2,8-trimetil-3,4-dihidro-2H-cromen-4-il)urea; N-1H-indazol-4-il-N'-(2,2,8-trimetil-3,4-dihidro-2H-cromen-4-il)urea; N-1H-indazol-4-il-N'-(7-metoxi-2,2-dimetil-8-propil-3,4-dihidro-2H-cromen-4-il)urea; N-(2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-fluoro-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-fluoro-2,2-dietil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7,8-difluoro-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-(3,3-dimetilbutil)-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-tert-butil-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2,2-dietil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-(1-metil-1H-indazol-4-il)urea; N-(7,8-difluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-fluoro-2,2-dipropil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2,2-dibutil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2-tert-butil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2-tert-butil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-(1-metil-1H-indazol-4-il)urea; N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)urea; N-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)-N'-(6-metil-3,4-dihidro-2H-cromen-4-il)urea; N-[(4R)-3,4-dihidro-2H-cromen-4-il]-N'-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)urea; N-[(4S)-3,4-dihidro-2H-cromen-4-il]-N'-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)urea; 1-(1H-indazol-4-il)-3-(espiro[croman-2,1'-ciclohexan]-4-il)urea; 1-(7-fluoroespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-fluoroespiro[croman-2,1'-cicIobutan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-fluoroespiro[croman-2,1'-ciclobutan]-4-il)-3-(1-metil-1H-indazol-4-il)urea; 1-(6,7-dimetilespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6,8-dicloroespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6-cloroespiro[croman-2,1l-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-tertbutilespiro[croman-2,1'-ciclobutan]-4-il)-3-(1H-indazol-4-il)urea, 1-(6,8-difluoroespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6-etoxiespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(1H-indazol-4-il)-3-(6-metilespiro[croman-2,1'-ciclopentan]-4-il)urea; 1-(7-etoxiespiro[croman-2,1'-ciclopentan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6,7-dimetilespiro[croman-2,1'-ciclopentan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-fluoroespiro[croman-2,1l-ciclopentan]-4-il)-3-(1H-indazol-4-il)urea; 1-(1-metil-1H-indazol-4-il)-3-(espiro[croman-2,1'-ciclohexan]-4-il)urea; 1-(1H-indazol-4-il)-3-(7-metoxiespiro[croman-2,1'-ciclohexan]-4-il)urea; (+- )1-(3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-cloro-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-metoxi-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-metoxi-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-metil-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-metoxi-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinoIin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(6-metil-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+)1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(8-cloroisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(3-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-6-metil-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-7-metil-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-6-fluoro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+)1-(3,4-dihidro-6-fluoro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(3,4-dihidro-6-fluoro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-7-metoxi-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; 1-(6,8-difluoro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(8-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-6-metoxi-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; clorhidrato de (+- )1-(7-difluorometoxi-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-difluorometoxi-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(3-metilisoquinolin-5-il)urea; (+- )1-(7-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(3-metilisoquinolin-5-il)urea; (+)1-(6,8-difluoro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(6,8-difluoro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-8-difluorometoxi-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(6-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6,8-dicloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-7-metilespiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6,7-dicloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-cloro-3,4-dihidro-7-metilespiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(8-cloroisoquinolin-5-il)urea; (+- )1-(6-fluoro-3
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