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AR065311A1 - Agonistas del adrenoreceptor alfa2c funcionalmente selectivos y composicion farmaceutica - Google Patents

Agonistas del adrenoreceptor alfa2c funcionalmente selectivos y composicion farmaceutica

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Publication number
AR065311A1
AR065311A1 ARP080100597A ARP080100597A AR065311A1 AR 065311 A1 AR065311 A1 AR 065311A1 AR P080100597 A ARP080100597 A AR P080100597A AR P080100597 A ARP080100597 A AR P080100597A AR 065311 A1 AR065311 A1 AR 065311A1
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Argentina
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groups
optionally substituted
group
heterocyclyl
alkyl
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ARP080100597A
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Schering Corp
Pharmacopeia Inc
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Publication of AR065311A1 publication Critical patent/AR065311A1/es

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Abstract

La presente provee una nueva clase de indolinas como inhibidores de los agonistas del receptor alfa2C adrenérgico, y composiciones farmacéuticas que contienen uno o más de dichos compuestos. Estos compuestos actuan como receptores alfa2C adrenérgicos siendo utiles en el tratamiento del dolor, la migrana, trastornos psicofísicos e isquemia. Reivindicacion 1: Un compuesto representado por la estructura (1) o una sal, éster, solvato o prodroga farmacéuticamente aceptable del mismo, en donde: A es un anillo heterocíclico de 5 miembros que contiene 1-3 heteroátomos, y está opcionalmente sustituido con al menos un grupo R5 y/o 1 o 2 grupos (=O); J1, J2, y J3 son independientemente -N-, -N(O) o -C(R2)-; J4 es C o N; J5 es -C(R6)- o -N(R6)-; ------ es un enlace simple o doble; R1 está seleccionado del grupo integrado por -[C(Ra)(Rb)]qYR7', -[C(Ra)(Rb)]qN(R7)YR7', -[C(Ra)(Rb)]qNR7R7', -[C(Ra)(Rb)]qOYR7', -[C(Ra)(Rb)]qON=CR7R7', -P(=O)(OR7)(OR7'), -P(=O)(NR7R7')2, y -P(=O)R82; Y está seleccionado del grupo integrado por un enlace, -C(=O)-, -C(=O)NR7-; -C(=O)O-, -C(=O)-[C(Ra)(Rb)]n-O-C(=O)-, -C(=O)N(Rc)-O-, -C(=NR7)-, -C(=NOR7)-, -C(=NR7)NR7-, -C(=NR7)NR7O-, -S(O)p-, SO2NR7-, y -C(=S)NR7-, en donde Ra y Rb están independientemente seleccionados del grupo integrado por H, alquilo, alcoxi, y halo, y Rc es H o alquilo; R2 está independientemente seleccionado del grupo integrado por H, -OH, halo, -CN, -NO2, S(O)pR7, -NR7R7', (CH2)qYR7', (CH2)qN(R7)YR7', (CH2)qOYR7',-(CH2)qON=CR7R7', P(=O)(OR7)(OR7'), P(=O)NR7R7', y P(=O)R82, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con al menos un R5; R3 está independientemente seleccionado del grupo integrado por H, halo y (=O), y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con al menos un R5, siempre que cuando w sea 3, no más de 2 de los grupos R3 puedan ser (=O); R4 está independientemente seleccionado del grupo integrado por H, -CN y halo, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con al menos un R5; R5 está independientemente seleccionado del grupo integrado por H, halo, -OH, -CN, -NO2, -NR7R7', y -S(O)pR7, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, -NR7R7', y -S(O)pR7 y/o 1 o 2 grupos (=O); R6 está independientemente seleccionado del grupo integrado por H y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, NR7R7', y -S(O)pR7 y/o 1 o 2 grupos (=O), y -C(=O)R7, -C(=O)OR7, C(=O)NR7R7', -SO2R7 y -SO2NR7R7'; R7 está independientemente seleccionado del grupo integrado por H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, ciclociclenilo, ciclociclenilalquilo, arilo, arilalquilo, heterociclilo, heterociclilalquilo, heterociclenilo, heterociclenilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido una o más veces con R12; R7' está independientemente seleccionado del grupo integrado por H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, ciclociclenilo, ciclociclenilalquilo, arilo, arilalquilo, heterociclilo, heterociclilalquilo, heterociclenilo, heterociclenilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido una o más veces con R12; R7 y R7' conjuntamente con el átomo de nitrogeno al cual ellos están unidos forman un anillo heterociclilo, heterociclenilo o heteroarilo de 3 a 8 miembros que tiene, además del átomo de N, 1 o 2 heteroátomos adicionales seleccionados del grupo integrado por O, N, -N(R9)- y S, en donde dichos anillos están opcionalmente sustituidos con 1 a 5 restos R5 independientemente seleccionados y/o 1 o 2 grupos (=O), R8 está independientemente seleccionado del grupo integrado por grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, alcoxi, -OH, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O); R9 está independientemente seleccionado del grupo integrado por H, -C(O)-R10, -C(O)-OR10, y -S(O)p-OR10 y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O); y R10 está seleccionado del grupo integrado por grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O); R11 es un resto independientemente seleccionado del grupo integrado por H y alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos un sustituyente independientemente seleccionado del grupo integrado por halo, -OH, -CN, -NO2, -N(R11')2, y -S(O)pR11 y/o 1 o 2 grupos (=O); R11' está independientemente seleccionado del grupo integrado por H, alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo; R12 está independientemente seleccionado del grupo integrado por H, halo, -OH, -CN, -NO2, -N(R11)2 , y -S(O)pR11 y/o 1 o 2 grupos (=O), y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalquenilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroariloxi, heteroarilalquilo, heterociclilo, heterociclenilo, heterocicleniloxi, heterociclilalquilo, heterociclenilalquilo, arilalcoxi, heteroarilalcoxi, heterociclilalcoxi, y heterociclenilalcoxi, cada uno de los cuales a su vez está opcionalmente sustituido al menos una vez con un sustituyente seleccionado del grupo integrado por H, alquilo, haloalquilo, halo, -OH, alcoxi opcionalmente sustituido, ariloxi opcionalmente sustituido, cicloalcoxi opcionalmente sustituido, heteroariloxi opcionalmente sustituido, heterocicleniloxi opcionalmente sustituido, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O), en donde dichos ariloxi, alcoxi opcionalmente sustituido, cicloalcoxi opcionalmente sustituido, heterocicleniloxi y heteroariloxi opcionalmente sustituido, cuando están sustituidos están sustituidos una o más veces con R11, m es 1-5; n es independientemente 1-3; p es independientemente 0-2; q es independientemente 0-6; y w es 1-3; con las siguientes condiciones: (a) si J1-J3 son -C(H)-, R1 es -[C(Ra)(Rb)]qYR7', q es 0, y A es imidazolilo no sustituido, entonces Y es distinto a un enlace; (b) si J1-J3 son -C(H)-, R1 es [C(Ra)(Rb)]qYR7', q es 0, y A es imidazolilo no sustituido, entonces Y es distinto a un enlace; (c) si J4 es N, entonces J5 es -C(R6)-; (d) si J4 es C, entonces J5 es -N(R6)- y (e) si A es imidazolilo no sustituido, R1 es -[C(RA)(Rb)]qYR7', q es 0, Y es -C(=O)- o -C(=O)O-, entonces R7 es distinto a H o alquilo, (f) si R1 es -[C(Ra)(Rb)]qYR7', q =0, e Y = - C(=NR7)-, -C(=NOR7)-, -C(NR7)NR7-, o C(=NR7)N(Rc)O, entonces R7 y R7' pueden no tomarse conjuntamente para formar un anillo heterociclilo, heterociclenilo o heteroarilo de 3 a 8 miembros; y (g) si R1 es -[C(Ra)(Rb)]qN(R7)YR7 o -[C(Ra)(Rb)]qNR7R7' y q = 0, entonces R7 y R7' pueden no tomarse conjuntamente para formar un anillo heterociclilo, heterociclenilo o heteroarilo de 3 a 8 miembros.
ARP080100597A 2007-02-13 2008-02-12 Agonistas del adrenoreceptor alfa2c funcionalmente selectivos y composicion farmaceutica AR065311A1 (es)

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US11/705,683 US8003624B2 (en) 2005-08-25 2007-02-13 Functionally selective ALPHA2C adrenoreceptor agonists

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EP (1) EP2125784A2 (es)
KR (1) KR20090110938A (es)
CN (1) CN101903373A (es)
AR (1) AR065311A1 (es)
AU (1) AU2008216798A1 (es)
CA (1) CA2679849A1 (es)
CL (1) CL2008000439A1 (es)
IL (1) IL200424A0 (es)
PE (1) PE20090069A1 (es)
TW (1) TW200836721A (es)
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CA2678072A1 (en) * 2007-02-13 2008-08-21 Schering Corporation Functionally selective alpha2c adrenoreceptor agonists
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WO2010017120A1 (en) * 2008-08-04 2010-02-11 Schering Corporation Cyclopropylchromene derivatives as modulators of the alpha-2c receptor
UA103195C2 (uk) 2008-08-11 2013-09-25 Глаксосмитклайн Ллк Похідні пурину для застосування у лікуванні алергій, запальних та інфекційних захворювань
US20120028940A1 (en) * 2008-09-16 2012-02-02 Merck Sharp & Dohme Corp. Functionally selective azanitrile alpha-2c adrenoreceptor agonists
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