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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
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
halogen
hydroxyl
independently
Prior art date
Application number
ARP100104253A
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English (en)
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
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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    • 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
    • A61K31/42—Oxazoles
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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)

Applications Claiming Priority (2)

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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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US (4) US8222286B2 (es)
EP (2) EP2735561B1 (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)
CA (1) CA2780150C (es)
CL (1) CL2012001298A1 (es)
CO (1) CO6540001A2 (es)
CR (1) CR20120237A (es)
DK (1) DK2501683T3 (es)
EA (1) EA021479B1 (es)
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PT (1) PT2501683E (es)
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SI (1) SI2501683T1 (es)
TN (1) TN2012000125A1 (es)
TW (1) TWI481598B (es)
UY (1) UY33044A (es)
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ZA (1) ZA201202018B (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201101672A1 (ru) * 2009-05-28 2012-06-29 Новартис Аг Замещенные производные аминомасляной кислоты в качестве ингибиторов неприлизина
SI2435409T1 (sl) 2009-05-28 2014-12-31 Novartis Ag Substituirani aminopropionski derivati kot inhibitorji neprilizina
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
SG191175A1 (en) 2010-12-15 2013-07-31 Theravance Inc Neprilysin inhibitors
WO2012082853A1 (en) 2010-12-15 2012-06-21 Theravance, Inc. Neprilysin inhibitors
CN103380119B (zh) 2011-02-17 2016-02-17 施万生物制药研发Ip有限责任公司 作为脑啡肽酶抑制剂的经取代的氨基丁酸衍生物
US8449890B2 (en) 2011-02-17 2013-05-28 Theravance, Inc. Neprilysin inhibitors
WO2012166389A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
CN103582630B (zh) 2011-05-31 2016-08-17 施万生物制药研发Ip有限责任公司 脑啡肽酶抑制剂
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