AR079061A1 - Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep - Google Patents

Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep

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Publication number
AR079061A1
AR079061A1 ARP100104253A ARP100104253A AR079061A1 AR 079061 A1 AR079061 A1 AR 079061A1 AR P100104253 A ARP100104253 A AR P100104253A AR P100104253 A ARP100104253 A AR P100104253A AR 079061 A1 AR079061 A1 AR 079061A1
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AR
Argentina
Prior art keywords
alkyl
alkoxy
halogen
hydroxyl
independently
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ARP100104253A
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English (en)
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Novartis Ag
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Publication of AR079061A1 publication Critical patent/AR079061A1/es

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract

La presente proporciona además una combinacion de agentes farmacologicamente activos y una composicion farmacéutica. Reivindicacion 1: La presente, por consiguiente, proporciona un compuesto de la formula (1), en donde: X1 es OH, -O-alquilo C1-7, NRaRb, -NHS(O)2-alquilo C1-7 o -NHS(O)2-bencilo, en donde Ra y Rb, por cada presentacion, son independientemente H o alquilo C1-7; R1 es H, alquilo C1-6, o arilo C6-10-alquilo C1-6, en donde el alquilo está opcionalmente sustituido con benciloxilo, hidroxilo o alcoxilo C1-6; por cada presentacion, R2 es independientemente alcoxilo C1-6, hidroxilo, halogeno, alquilo C1-6, ciano o trifluorometilo; A2 es O o NR5; R4 y R5 son independientemente H o alquilo C1-6; A1 es un enlace o una cadena de alquileno C1-3; R3 es un heteroarilo de 5 o 6 miembros, arilo C6-10 o cicloalquilo C3-7, en donde cada heteroarilo, arilo o cicloalquilo está opcionalmente sustituido con uno o más grupos independientemente seleccionados a partir del grupo que consiste en alquilo C1-6, halogeno, halo-alquilo C1-6, alcoxilo C1-6, hidroxilo, CO2H y CO2-alquilo C1-6; R6, por cada presentacion, es independientemente halogeno, hidroxilo, alcoxilo C1-7, halogeno, alquilo C1-7, o halo-alquilo C1-7; o R4, A1-R3, junto con el átomo de nitrogeno con el que R4 y A1-R3 están unidos, forman un heterociclilo de 4 a 7 miembros o un heteroarilo de 5 a 6 miembros, cada uno de los cuales está opcionalmente sustituido con uno o más grupos independientemente seleccionados a partir del grupo que consiste en alquilo C1-6, halogeno, halo-alquilo C1-6, alcoxilo C1-6, hidroxilo, CO2H y CO2-alquilo C1-6; y m es 0 o un entero de 1 a 5; s es 0 o un entero de 1 a 4; o una sal farmacéuticamente aceptable del mismo.
ARP100104253A 2009-11-20 2010-11-18 Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep AR079061A1 (es)

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US26313709P 2009-11-20 2009-11-20
US35991410P 2010-06-30 2010-06-30

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AR079061A1 true AR079061A1 (es) 2011-12-21

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EP (2) EP2501683B1 (es)
JP (2) JP5543609B2 (es)
KR (1) KR101460421B1 (es)
CN (1) CN102666493B (es)
AR (1) AR079061A1 (es)
AU (1) AU2010320930B2 (es)
BR (1) BR112012011977A2 (es)
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EP2594556B1 (en) 2009-05-28 2016-08-10 Novartis AG Substituted aminopropionic derivatives as neprilysin inhibitors
JO2967B1 (en) * 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
US8993631B2 (en) * 2010-11-16 2015-03-31 Novartis Ag Method of treating contrast-induced nephropathy
AR084290A1 (es) 2010-12-15 2013-05-08 Theravance Inc Inhibidores de neprilisina, metodos para su preparacion e intermediarios utilizados en los mismos, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para tratar enfermedades mediadas por la inhibicion de nep
CA2817368C (en) 2010-12-15 2019-12-31 Theravance, Inc. Neprilysin inhibitors
MX342212B (es) 2011-02-17 2016-09-20 Theravance Inc Inhibidores de neprilisina.
WO2012154249A1 (en) 2011-02-17 2012-11-15 Theravance, Inc. Substituted aminobutyric derivatives as neprilysin inhibitors
EP2714662B1 (en) 2011-05-31 2017-10-11 Theravance Biopharma R&D IP, LLC Neprilysin inhibitors
ES2699773T3 (es) 2011-05-31 2019-02-12 Theravance Biopharma R&D Ip Llc Inhibidores de neprilisina
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