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 nepInfo
- 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
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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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- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D261/14—Nitrogen atoms
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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.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US26313709P | 2009-11-20 | 2009-11-20 | |
US35991410P | 2010-06-30 | 2010-06-30 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR079061A1 true AR079061A1 (es) | 2011-12-21 |
Family
ID=43431937
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100104253A AR079061A1 (es) | 2009-11-20 | 2010-11-18 | Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep |
Country Status (37)
Country | Link |
---|---|
US (4) | US8222286B2 (es) |
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) |
CA (1) | CA2780150C (es) |
CL (1) | CL2012001298A1 (es) |
CO (1) | CO6540001A2 (es) |
CR (1) | CR20120237A (es) |
DK (1) | DK2501683T3 (es) |
EA (1) | EA021479B1 (es) |
EC (1) | ECSP12011978A (es) |
ES (2) | ES2598961T3 (es) |
GT (1) | GT201200153A (es) |
HK (1) | HK1170475A1 (es) |
HN (1) | HN2012001037A (es) |
HR (1) | HRP20140691T1 (es) |
IL (1) | IL219314A0 (es) |
IN (1) | IN2012DN02465A (es) |
JO (1) | JO2967B1 (es) |
MA (1) | MA33886B1 (es) |
MX (1) | MX2012005813A (es) |
MY (1) | MY158299A (es) |
NZ (1) | NZ599136A (es) |
PE (1) | PE20121311A1 (es) |
PL (1) | PL2501683T3 (es) |
PT (1) | PT2501683E (es) |
RS (1) | RS53422B (es) |
SI (1) | SI2501683T1 (es) |
TN (1) | TN2012000125A1 (es) |
TW (1) | TWI481598B (es) |
UY (1) | UY33044A (es) |
WO (1) | WO2011061271A1 (es) |
ZA (1) | ZA201202018B (es) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2763565A1 (en) | 2009-05-28 | 2010-12-02 | Novartis Ag | Substituted aminobutyric derivatives as neprilysin inhibitors |
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 |
EP2714648B1 (en) | 2011-05-31 | 2017-08-16 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
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KR101589317B1 (ko) | 2007-11-06 | 2016-01-28 | 노파르티스 아게 | 안지오텐신 수용체 길항제/차단제 (arb) 및 중성 엔도펩티다제 (nep) 억제제의 초구조에 기초한 이중-작용 제약 조성물 |
JP2011506459A (ja) | 2007-12-11 | 2011-03-03 | セラヴァンス, インコーポレーテッド | 抗高血圧剤としての二重作用性ベンゾイミダゾール誘導体およびその使用 |
EP2070928A1 (en) | 2007-12-12 | 2009-06-17 | NERVIANO MEDICAL SCIENCES S.r.l. | 7-azaindol-3-ylacrylamides active as kinase inhibitors |
AR070176A1 (es) | 2008-01-17 | 2010-03-17 | Novartis Ag | Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis |
WO2010011821A2 (en) | 2008-07-24 | 2010-01-28 | Theravance, Inc. | Dual-acting antihypertensive agents |
EP2594556B1 (en) | 2009-05-28 | 2016-08-10 | Novartis AG | Substituted aminopropionic derivatives as neprilysin inhibitors |
CA2763565A1 (en) | 2009-05-28 | 2010-12-02 | Novartis Ag | Substituted aminobutyric derivatives as neprilysin inhibitors |
EP2480523B1 (en) | 2009-09-23 | 2017-03-01 | Zhejiang Jiuzhou Pharmaceutical Co., Ltd. | Process for manufacture of n-acylbphenyl alanine |
JO2967B1 (en) * | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
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