AR058968A1 - Antagonistas del receptor de urotensina ii - Google Patents

Antagonistas del receptor de urotensina ii

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Publication number
AR058968A1
AR058968A1 ARP070100096A ARP070100096A AR058968A1 AR 058968 A1 AR058968 A1 AR 058968A1 AR P070100096 A ARP070100096 A AR P070100096A AR P070100096 A ARP070100096 A AR P070100096A AR 058968 A1 AR058968 A1 AR 058968A1
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Argentina
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alkyl
amino
alkoxy
optionally substituted
group
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Janssen Pharmaceutica Nv
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Abstract

Reivindicacion 1: Un compuesto de Formula (1) donde: cuando A está presente, entonces G se selecciona entre hidrogeno, alquilo C1-8, alquenilo C2-8, cicloalquilo C3-14 o una porcion -C[(R1)(R11)]-L-D: como se muestra en la formula (2), donde alquilo C1-8 está opcionalmente sustituido con uno, dos o tres sustituyentes fluor, y donde cicloalquilo C3-14 está opcionalmente sustituido con uno, dos o tres sustituyentes alquilo C1-3 ; o, cuando A está ausente y R2 no es benciloximetilo, entonces G es alcoxi C1-8 o heterocicliloxi, donde alcoxi C1-8 está sustituido con uno de amino, (alquil C1-4)amino, di(alquil C1-8)amino, (bencil)amino o [(bencil)(alquil C1-4)]amino, y donde heterocicliloxi está opcionalmente sustituido en heterociclilo con uno, dos o tres sustituyentes aIquilo C1-3; R1 se selecciona del grupo formado por hidrogeno, alquilo C1-8 aIquenilo C2-8, y alquinilo C2-8; R11 se selecciona del grupo formado por hidrogeno, aIquilo C1-8 y ciclopropilo; L está ausente o es alquileno C1-4; D es arilo (distinto de naftalen-2-ilo), cicloalquiIo C3-14, cicloalquenilo C5-14, heterociclilo, o heteroarilo, donde arilo y heteroarilo están opcionalmente sustituidos con uno, dos, tres o cuatro sustituyentes independientemente seleccionados del grupo formado por alquilo C1-3, alcoxi C1-3, alquenilo C2-8, alqueniloxi C2-3, hidroxi, alquiltio C1-3, fluor, cloro, ciano, alquil C1-3-carbonilo, (alquil C1-3-carbonil)amino, (alquil C1-3)amino, di(alquil C1-3)amino y cicloalquiIo C3-14, donde cicloalquilo C3-14 está opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes alquilo C1-3, siempre y cuando D no sea 2-hidroxi-5-cloro-fenilo, 3-metoxi-fenilo, 4-etil-fenilo, 6,6-dimetil-biciclo[3.1.1]hept-2- en-2-il-metilo, ciclohex-3-enilo, 2,6-dicloro-fenilo y 2-cloro-4-fluoro-fenilo; A es un biradical opcionalmente presente seleccionado del grupo formado por a-1; a-2, a-3, a-4 opcionalmente insaturados, a-5 y a-6 opcionalmente insaturados, donde, la porcion inferior de A está ligada, con respecto al átomo de nitrogeno de la Formula (1), a la posicion 3 o 4 en la porcion anillo benceno de la Formula (1); donde a-1, a-2, a-3, a-4 y a-5 están opcionalmente sustituidos con uno a dos sustituyentes alquilo C1-4; siempre y cuando A no sea cis-(1,2)-ciclohexildiamino; R4 es hidrogeno o aIquilo C1-8; L2 está ausente o es -C(R2)(R5)-(CR6R7)r-, donde r es 0, 1 o 2; y donde R5, R6, y R7 son independientemente hidrogeno o alquilo C1-3; siempre y cuando L2 no sea -CH(R-carboximetil)-; R2 se selecciona del grupo formado por hidrogeno, un heteroarilo que no está fusionado a otro anillo, fenilo, y alquilo C1-6, donde fenilo está opcionalmente sustituido con (R200-alquil C1-6)amino, o [(hidroxisulfonil)(Ra)]amino, y donde alquilo C1-6 está opcionalmente sustituido con carboxi, hidroxi, R200, NRaRb, alcoxi C1-4, R200-alcoxi C1-6, R200-oxi, aminocarbonilo, carboxi-alcoxi C1-6, aminocarbonil-alcoxi C1-6, (alquil C1-6)aminocarbonilo, di(alquil C1-6)aminocarbonilo, [(R200-alquil C1-6)(Ra)]amino, (aIquil C1-6-carbonil)amino, (trihaloalquil C1-4-carbonil)amino, (R200-alquil C1-6-carbonil)amino, (alcoxi C1-6-carbonil)amino, (R200-alcoxi C1-6-carbonil)amino, (alcoxi C1-6-alquil C1-6- carbonil)amino, (R200-carbonil)amino, (amino-alquil C1-6-carbonil)amino, [(alquil C1-6)amino-alquiI C1-6-carbonil]amino, [di(alquil C1-6)amino-alquil C1-6-carbonil]amino, (alquil C1-6-carbonil-acetonitrilo-carbonil)amino, ureido, tioureido, acetamidino, guanidino, {[(R200)(Ra)]aminocarbonil-(Rc)}amino, [(R200-oxicarbonil)(Ra)]amino, [(R200)(Ra)]aminocarboniloxi, aminosulfonilo, alquil C1-6-sulfonilo, (alquil C1-6-sulfonil)amino, (R200-alquil C1-6-sulfonil)amino, (R200-alqueniI C2-6- sulfonil)amino, (alquil C16-sulfonil-alquil C1-6-sulfonil)amino, R200-sulfoniloxi, aminosulfoniloxi, (alquil C1-6)aminosulfoniloxi, di(alquil C1-6)aminosulfoniloxi, aminosulfonilamino, (alquil C1-6)aminosulfonilamino, [di(alquil C1- 6)aminosulfonil]amino, [(hidroxisulfonil)(Ra)]amino, [(R200-oxisulfonil)(Ra)]amino, [(R200-sulfonil)(Ra)]amino, [(R200)(Ra)]aminosulfoniloxi, o ({[(R200)(Ra)]aminosulfoniI}(Rc))amino; Ra y Rc se seleccionan independientemente del grupo formado por hidrogeno y alquilo C1-6; y Rb es hidrogeno, alquilo C1-6, arilo C6-10, heteroarilo, cicloaIquilo C3-8, o heterociclilo; R200 es arilo C6-10, heteroarilo, cicloalquilo C3-8, o heterociclilo, cada uno opcionalmente sustituido con uno, dos o tres sustituyentes independientemente seleccionados del grupo formado por alquilo C1-4, trihaloalquilo C1-4, alcoxi C1-4, trihaloaIcoxi C1-4, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, (alquil C1-6-carbonil)amino, alquil C1-6-sulfonilo, hidroxisulfonilo, aminosulfonilo, cloro, fluor, bromo, arilo, heteroarilo, aril-alquilo C1-6, aril-sulfonilo y heteroaril-sulfonilo, donde heterociclilo está opcionalmente sustituido con uno, dos o tres sustituyentes oxo; B es arilo C6-10, tetralinilo, indanilo, o un heteroarilo seleccionados del grupo formado por piridin-2-ilo, piridin-4-ilo, pirazol-4-ilo pirimidin-4-ilo, pirimidin-5-ilo, pirazin-2-ilo, imidazol-1-ilo, tien-2-ilo, isoquinolinilo, indolilo, quinolinilo, y tiazol-5- ilo, donde B está opcionalmente sustituido con uno, dos o tres sustituyentes Independientemente seleccionados del grupo formado por alquilo C1-4, alcoxi C1-4, alcoxi(C1-4) fluorado, halogeno, ciano, hidroxi, aminocarbonilo, alquil(C1- 4)aminocarbonilo, dialquil(C1-4)aminocarbonilo, aminosulfonilo, alquil(C1-4)aminosulfonilo, dialquil(C1-4)aminosulfonilo, hidroxisulfonilo, aminosulfonilamino, alquil(C1-4)aminosulfonilamino, dialquil(C1-4)aminosulfonilamino, aminosulfoniloxi, alquil(C1-4)aminosulfoniloxi, y dialquil(C1-4)aminosulfoniloxi, siempre que cuando B se selecciona del grupo formado por arilo C6-10, tetralinilo, indanilo, tien-2-ilo, e indolilo, entonces B esté independientemente sustituido con dos a tres sustituyentes seleccionados del grupo formado por alcoxi C1-3 e hidroxi, siempre que cuando B sea fenilo sustituido en las posiciones 3,4-, 3,5- o 4,5- con un sustituyente no ramificado alcoxi C1-3 en cada posicion, entonces fenilo pueda estar además opcionalmente sustituido en una de las restantes posiciones abiertas 3-, 4-, o 5- con un sustituyente alcoxi C1-3 o hidroxi adicional, y siempre y cuando B no sea 3-hidroxi-4-metoxi-fenilo y 3-(n-propiloxi)-4-metoxi-fenilo; E es hidrogeno, halogeno, alcoxi C1-3, alquil C2-5-RE, o -CH=CH-alquil C0-3-RE; donde RE se selecciona del grupo formado por carboxi, amino, (alquil C1-6)amino, di(alquil C1-6)amino, aminocarbonilo, (alquil C1-6)aminocarbonilo, di(alquil C1-6)aminocarbonilo, (alquil C1-6)carbonilamino, alcoxi C1-6-carbonilamino, aminocarbonilalcoxi (C1-6), ureido, tioureido, aminosulfonilo, alquil C1-6-sulfonilo, alquil C1-6-sulfonilamino, aminosulfoniloxi, (alquil C1-6)aminosulfoniloxi, di(alquil C1-6)aminosulfoniloxi, aminosulfonilamino, (alquil C1-6)aminosulfonilamino, di(aIquil C1-6)aminosulfonilamino, (R200)(Ra)aminocarbonil-(Rc)amino, R200carbonilamino, R200oxicarbonil-(Ra)amino, (R200)(Ra)aminocarboniloxi, R200oxisulfonil-(Ra)amino, R200sulfonil-(Ra)amino, (R200)(Ra)aminosulfoniloxi, y (R200)(Ra)aminosulfonil-(Rc)amino; X e Y son independientemente O o S; y enantiomeros, diastereomeros, tautomeros, solvatos, y sales farmacéuticamente aceptables del mismo.
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