AR076706A1 - Derivados aminobutiricos sustituidos como inhibidores de neprilisina - Google Patents

Derivados aminobutiricos sustituidos como inhibidores de neprilisina

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Publication number
AR076706A1
AR076706A1 ARP100101808A ARP100101808A AR076706A1 AR 076706 A1 AR076706 A1 AR 076706A1 AR P100101808 A ARP100101808 A AR P100101808A AR P100101808 A ARP100101808 A AR P100101808A AR 076706 A1 AR076706 A1 AR 076706A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroaryl
halogen
heterocyclyl
independently selected
Prior art date
Application number
ARP100101808A
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English (en)
Original Assignee
Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR076706A1 publication Critical patent/AR076706A1/es

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Abstract

Se proporciona además una combinacion de agentes farmacologicamente activos y una composicion farmacéutica. Reivindicacion 1: Un compuesto de la formula (1) o una sal farmacéuticamente aceptable del mismo, en donde; R1 es alquilo C1-7; por cada presentacion, R2 es independientemente alquilo C1-7, NO2, CN, halogeno, cicloalquilo C3-7, hidroxilo, alcoxilo C1-7, halo-alquilo C1-7, NRbRc, arilo C6-10, heteroarilo, o heterociclilo; en donde Rb y Rc por cada presentacion, son independientemente H o alquilo C1-7; R3 es A1C(O)X1 o A2-R4; R4 es arilo C6-10, o un heteroarilo, el cual puede ser monocíclico o bicíclico, y el cual puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente a partir de hidroxilo, hidroxialquilo C1-7, NRbRc, nitro, alcoxilo C1-7, halogeno, alquilo C1-7, halo-alquilo C1-7, alquenilo C2-7, arilo C6-10, heteroarilo, -C(O)-alquilo C1-7, -NHS(O)2-alquilo C1-7, -SO2-alquilo C1-7, y bencilo; R5 es H, halogeno, hidroxilo, alcoxilo C1-7, halogeno, alquilo C1-7, o halo-alquilo C1-7; y X y X1 son independientemente OH, -O-alquilo C1-7, NRbRc, -NHS(O)2-alquilo C1-7, -NHS(O)2-bencilo u -O-arilo C6-10; en donde alquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente a partir del grupo que consiste en arilo, heteroarilo, heterociclilo, -C(O)NH2, -C(O)NHalquilo C1-6, y -C(O)N(alquilo C1-6)2; A1 es un enlace o un alquileno lineal C1-4 sustituido con uno o más sustituyentes seleccionados independientemente a partir del grupo que consiste en halogeno, O-acetato, alquilo C1-7 y cicloalquilo C3-7; en donde dos grupos alquilo geminales pueden combinarse opcionalmente para formar un cicloalquilo C3-7; o A1 es un alquenileno C2-6 lineal o ramificado; o A1 es un alquileno lineal C1-4 en donde uno o más átomos de carbono son reemplazados con un heteroátomo seleccionado a partir de O, NRa; y A1 está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente a partir del grupo que consiste en halogeno y alquilo C1-7; en donde Ra por cada presentacion, es independientemente H, alquilo C1-7, o CH2C(O)OH; o A1 es un cicloalquilo C3-7, heterociclilo, fenilo o un heteroarilo, en donde fenilo y heteroarilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente a partir del grupo que consiste en alquilo C1-7, cicloalquilo C3-7, halo-alquilo C1-7, hidroxilo, alcoxilo C1-7, halogeno, NRbRc, OCH2CO2H, y OCH2C(O)NH2; o A1 es -alquileno C1-4-arilo C6-10-, -alquileno C1-4-heteroaril- o -alquileno C1-4-heterociclil-, en donde A1 puede estar en cualquier direccion; y A2 es un enlace o un alquileno lineal o ramificado C1-7 que está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente a partir del grupo que consiste en halogeno, alcoxilo C1-7, hidroxilo, O-acetato, y cicloalquilo C3-7; n es 0, 1, 2, 3, 4 o 5; en donde cada heteroarilo es un anillo aromático monocíclico o bicíclico que comprende de 5 a 10 átomos del anillo seleccionados a partir de átomos de carbono, y de 1 a 5 heteroátomos, y cada heterociclilo es una fraccion monocíclica saturada parcialmente saturada, pero no aromática, la cual comprende de 4 a 7 átomos del anillo seleccionados a partir de átomos de carbono, y de 1 a 5 heteroátomos, en donde cada heteroátomo de un heteroarilo o de un heterociclilo se selecciona independientemente a partir de O, N y S.
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KR20120041702A (ko) 2012-05-02
WO2010136474A2 (en) 2010-12-02
EA201101672A1 (ru) 2012-06-29
US20150174089A1 (en) 2015-06-25
US20120252830A1 (en) 2012-10-04
US20100305145A1 (en) 2010-12-02
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