AR084290A1 - 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 - Google Patents

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

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Publication number
AR084290A1
AR084290A1 ARP110104683A AR084290A1 AR 084290 A1 AR084290 A1 AR 084290A1 AR P110104683 A ARP110104683 A AR P110104683A AR 084290 A1 AR084290 A1 AR 084290A1
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AR
Argentina
Prior art keywords
alkyl
phenyl
benzyl
cycloalkyl
halo
Prior art date
Application number
Other languages
English (en)
Inventor
Ryan Hudson
Cameron Smith
Melissa Fleury
Roland Gendron
Adam Hughes
Original Assignee
Theravance Inc
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Publication date
Application filed by Theravance Inc filed Critical Theravance Inc
Publication of AR084290A1 publication Critical patent/AR084290A1/es

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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/41Heterocyclic 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

Estos compuestos tienen actividad de inhibición de neprilisina. Composiciones farmacéuticas que comprenden dichos compuestos; métodos para usar dichos compuestos; y proceso e intermediarios para preparar dichos compuestos.Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), donde: R1 se selecciona entre -OR7 y -NR8R9; R2 es H o -P(O)(OH)2 o R2 se toma junto con R7 para formar -CR18R19- o se toma junto con R8 para formar -C(O)-; X es un -heteroarilo C1-9; R3 se encuentra ausente o se selecciona entre H; halo; -alquilen C0-5-OH; -NH2; -alquilo C1-6; -CF3; -cicloalquilo C3-7; -alquilen C0-2-O-alquilo C1-6; -C(O)R20; -alquilen C0-1-COOR21; -C(O)NR22R23; -NHC(O)R24; =O; -NO2; -C(CH3)=N(OH); fenilo opcionalmente sustituido con uno o dos grupos seleccionados en forma independiente entre halo, -OH, -CF3, -OCH3, -NHC(O)CH3, y fenilo; naftalenilo; piridinilo; pirazinilo; pirazol opcionalmente sustituido con metilo; tiofenilo opcionalmente sustituido con metilo o halo; furanilo; y -CH2-morfolinilo; y R3, cuando está presente, se une a un átomo de carbono; R4 se encuentra ausente o se selecciona entre H; -OH; -alquilo C1-6; -alquilen C1-2-COOR35; -CH2OC(O)CH(R36)NH2; -OCH2OC(O)CH(R36)NH2; -OCH2OC(O)CH3; -CH2OP(O)(OH)2; -CH2CHOHCH2OH; -CH[CH(CH3)2]-NHC(O)O-alquilo C1-6; piridinilo; y fenilo o bencilo opcionalmente sustituido con uno o más grupos seleccionados entre halo, -COOR35, -OCH3, -OCF3, y -SCF3; y R4, cuando está presente, se une a un átomo de carbono o nitrógeno; o R3 y R4 se toman juntos para formar -fenilen-O-(CH2)1-3- o -fenilen-O-CH2-CHOH-CH2-; a es 0 ó 1; R5 se selecciona entre halo, -CH3, -CF3, y -CN; b es 0 o un entero entre 1 y 3; cada R6 se selecciona en forma independiente entre halo, -OH, -CH3, -OCH3, y -CF3; R7 se selecciona entre H, -alquilo C1-8, -alquilen C1-3-arilo C6-10, -alquilen C1-3-heteroarilo C1-9, -cicloalquilo C3-7, -[(CH2)2O]1-3CH3, -alquilen C1-6-OC(O)R10, -alquilen C1-6-NR12R13, -alquilen C1-6-C(O)R31, -alquilen C0-6morfolinilo; -alquilen C1-6-SO2-alquilo C1-6; o un resto del grupo de fórmulas (2); R10 se selecciona entre -alquilo C1-6, -O-alquilo C1-6, -cicloalquilo C3-7, -O-cicloalquilo C3-7, fenilo, -O-fenilo, -NR12R13, -CH[CH(CH3)2]-NH2, -CH[CH(CH3)2]-NHC(O)O-alquilo C1-6, y -CH(NH2)CH2COOCH3; y R12 y R13 se seleccionan en forma independiente entre H, -alquilo C1-6, y bencilo; o R12 y R13 se toman juntos como -(CH2)3-6-, -C(O)-(CH2)3-, o -(CH2)2O(CH2)2-; y R31 se selecciona entre -O-alquilo C1-6, -O-bencilo, y -NR12R13; R32 es -alquilo C1-6 o -alquilen C0-6-arilo C6-10; R8 se selecciona entre H, -OH, -OC(O)R14, -CH2COOH, -O-bencilo, piridilo, y -OC(S)NR15R16; R14 se selecciona entre H, -alquilo C1-6, -arilo C6-10, -OCH2-arilo C6-10, -CH2O-arilo C6-10, y -NR15R16; y R15 y R16 se seleccionan en forma independiente entre H y -alquilo C1-4; R9 se selecciona entre H, -alquilo C1-6, y -C(O)R17; y R17 se selecciona entre H, -alquilo C1-6, -cicloalquilo C3-7, -arilo C6-10, y -heteroarilo C1-9; R18 y R19 se seleccionan en forma independiente entre H, -alquilo C1-6, y -O-cicloalquilo C3-7, o R18 y R19 se toman juntos para formar =O; R20 se selecciona entre H y -alquilo C1-6; R21 y R35 se seleccionan en forma independiente entre H, -alquilo C1-6, -alquilen C1-3-arilo C6-10, -alquilen C1-3-heteroarilo C1-9, -cicloalquilo C3-7, -[(CH2)2O]1-3CH3, -alquilen C1-6-OC(O)R25; -alquilen C1-6-NR27R28, -alquilen C1-6-C(O)R33, -alquilen C0-6morfolinilo, -alquilen C1-6-SO2-alquilo C1-6, o un resto del grupo de fórmulas (3); R25 se selecciona entre -alquilo C1-6, -O-alquilo C1-6, -cicloalquilo C3-7, -O-cicloalquilo C3-7, fenilo, -O-fenilo, -NR27R28, -CH[CH(CH3)2]-NH2, -CH[CH(CH3)2]-NHC(O)O-alquilo C1-6, y -CH(NH2)CH2COOCH3; R27 y R28 se seleccionan en forma independiente entre H, -alquilo C1-6, y bencilo; o R27 y R28 se toman juntos como -(CH2)3-6-, -C(O)-(CH2)3-, o -(CH2)2O(CH2)2-; R33 se selecciona entre -O-alquilo C1-6, -O-bencilo, y -NR27R28; y R34 es -alquilo C1-6 o -alquilen C0-6-arilo C6-10; R22 y R23 se seleccionan en forma independiente entre H, -alquilo C1-6, -CH2COOH, -(CH2)2OH; -(CH2)2OCH3, -(CH2)2SO2NH2, -(CH2)2N(CH3)2, -alquilen C0-1-cicloalquilo C3-7, y -(CH2)2-imidazolilo; o R22 y R23 se toman juntos para formar un -heterociclo C3-5 saturado o parcialmente insaturado opcionalmente sustituido con halo, -OH, -COOH, o -CONH2; y que contiene opcionalmente un átomo de oxígeno en el anillo; R24 se selecciona entre -alquilo C1-6; -alquilen C0-1-O-alquilo C1-6; fenilo opcionalmente sustituido con halo o -OCH3 y -heteroarilo C1-9; y R36 se selecciona entre H, -CH(CH3)2, fenilo, y bencilo; donde cada grupo alquilo en R1, R3, y R4 está opcionalmente sustituido con entre 1 y 8 átomos de flúor; y; donde el ligando metileno en el bifenilo está opcionalmente sustituido con uno o dos grupos -alquilo C1-6 o ciclopropilo; o una sal farmacéuticamente aceptable de los mismos. Reivindicación 19: Un intermediario útil en la síntesis de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 17, caracterizado porque es de fórmula (4) donde P1 es H o un grupo protector de amino seleccionado entre t-butoxicarbonilo, tritilo, benciloxicarbonilo, 9-fluorenilmetoxicarbonilo, formilo, trimetilsililo, y t-butildimetilsililo; o una sal del mismo. Reivindicación 21: Un intermediario útil en la síntesis de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 17, caracterizado porque se selecciona entre los compuestos de fórmula (5), (6), (7) u (8), o una sal del mismo; donde R1P se selecciona entre -O-P3, -NHP2, y -NH(O-P4); R3P se selecciona entre -alquilen C0-5-O-P4, -alquilen C0-1-COO-P3, y fenilo sustituido con -O-P4; R4P se selecciona entre -O-P4; -alquilen C1-2-COO-P3; y fenilo o bencilo sustituido con -COO-P3; P2 es un grupo protector de amino seleccionado entre t-butoxicarbonilo, tritilo, benciloxicarbonilo, 9-fluorenilmetoxicarbonilo, formilo, trimetilsililo, y t-butildimetilsililo; P3 es un grupo protector de carboxi seleccionado entre metilo, etilo, t-butilo, bencilo, p-metoxibencilo, 9-fluorenilmetilo, trimetilsililo, t-butildimetilsililo, y difenilmetilo; y P4 es un grupo protector de hidroxilo seleccionado entre -alquilo C1-6, trialquilsililo C1-6, -alcanoilo C1-6, benzoilo, bencilo, p-metoxibencilo, 9-fluorenilmetilo, y difenilmetilo.
ARP110104683 2010-12-15 2011-12-14 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 AR084290A1 (es)

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Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100518998C (zh) * 2005-09-29 2009-07-29 宝山钢铁股份有限公司 薄带连铸结晶辊加热方法和装置
ME02295B (me) 2010-12-15 2016-02-20 Theravance Biopharma R&D Ip Llc Inhibitori neprilizina
NZ611528A (en) 2010-12-15 2015-06-26 Theravance Biopharma R & D Ip Llc Neprilysin inhibitors
ES2564275T3 (es) 2011-02-17 2016-03-21 Theravance Biopharma R&D Ip, Llc Derivados aminobutíricos sustituidos como inhibidores de neprilisina
CA2825737C (en) 2011-02-17 2018-11-13 Theravance, Inc. Substituted aminobutyric derivatives as 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
ES2653215T3 (es) 2011-05-31 2018-02-06 Theravance Biopharma R&D Ip, Llc Inhibidores de neprilisina
TWI560172B (en) 2011-11-02 2016-12-01 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
WO2013148768A1 (en) 2012-03-28 2013-10-03 Theravance, Inc. Crystalline forms of (r)-3-[n-(3'-chlorobiphenyl-4-ylmethyl)-n'-(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester
CA2871292A1 (en) * 2012-05-31 2013-12-05 Theravance Biopharma R&D Ip, Llc Nitric oxide donor neprilysin inhibitors
RS55967B1 (sr) 2012-06-08 2017-09-29 Theravance Biopharma R&D Ip Llc Inhibitori neprilizina
EP2858650B1 (en) * 2012-06-08 2018-11-14 Theravance Biopharma R&D IP, LLC Neprilysin inhibitors
BR112015002821B1 (pt) 2012-08-08 2022-10-18 Theravance Biopharma R&D Ip, Llc Compostos inibidores de neprilisina e composição farmacêutica
RS56300B1 (sr) 2013-03-05 2017-12-29 Theravance Biopharma R&D Ip Llc Inhibitori neprilizina
SG11201606057PA (en) 2014-01-30 2016-08-30 Theravance Biopharma R&D Ip Llc 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors
ES2718239T3 (es) 2014-01-30 2019-06-28 Theravance Biopharma R&D Ip Llc Inhibidores de neprilisina
ES2923002T3 (es) 2015-02-11 2022-09-22 Theravance Biopharma R&D Ip Llc Acido (2S,4R)-5-(5'-cloro-2'-fluorobifenil-4-il)-4-(etoxioxailamino)-2-hidroximetil-2-metilpentanoico como inhibidor de la neprilisina
RS61325B1 (sr) 2015-02-19 2021-02-26 Theravance Biopharma R&D Ip Llc (2r,4r)-5-(5'-hloro-2'-fluorobifenil-4-il)-2-hidroksi-4-[(5-metiloksazol-2-karbonil)amino]pentanska kiselina
HUE055546T2 (hu) 2016-03-08 2021-12-28 Theravance Biopharma R&D Ip Llc Kristályos (2S,4R)-5-(5'-klór-2-fluor-[1,1'-bifenil]-4-il)-2-(etoximetil)-4-(3-hidroxi izoxazol-5-karboxamido)-2-metilpentánsav és alkalmazásaik
US11993590B2 (en) 2016-12-04 2024-05-28 712 North Inc. Pyranone compounds useful to modulate OMA1 protease
CN110049769A (zh) 2016-12-04 2019-07-23 阿拉维·霍拉萨尼·默哈达姆·马塞尔·维克托 治疗与线粒体应激相关的疾病的方法
EP3735398B1 (en) 2018-01-03 2022-02-16 Ecolab Usa Inc. Benzotriazole derivatives as corrosion inhibitors
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4189604A (en) 1975-07-22 1980-02-19 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Bestatin
US4206232A (en) 1976-05-10 1980-06-03 E. R. Squibb & Sons, Inc. Relieving hypertension with carboxyalkylacylamino acids
IL58849A (en) 1978-12-11 1983-03-31 Merck & Co Inc Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them
FR2480747A1 (fr) 1980-04-17 1981-10-23 Roques Bernard Derives d'acides amines et leur application therapeutique
US4906615A (en) 1980-12-18 1990-03-06 Schering Corporation Substituted dipeptides as inhibitors of enkephalinases
US4722810A (en) 1984-08-16 1988-02-02 E. R. Squibb & Sons, Inc. Enkephalinase inhibitors
US4939261A (en) 1984-06-08 1990-07-03 Ciba-Geigy Corporation N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase
EP0225292A3 (en) 1985-12-06 1988-11-30 Ciba-Geigy Ag Certain n-substituted butyramide derivatives
US4929641B1 (en) 1988-05-11 1994-08-30 Schering Corp Mercapto-acylamino acid antihypertensives
KR880007441A (ko) 1986-12-11 1988-08-27 알렌 제이.스피겔 스피로-치환된 글루타르아미드 이뇨제
FR2623498B1 (fr) 1987-11-24 1990-04-06 Bioprojet Soc Civ Nouveaux composes enantiomeres derives d'amino-acides, leur procede de preparation et leurs applications therapeutiques
GB8820844D0 (en) 1988-09-05 1988-10-05 Pfizer Ltd Therapeutic agents
US5599951A (en) 1989-09-15 1997-02-04 Societe Civile Bioprojet Amino acid derivatives, the process for their preparation and their applications to therapy
US5155100A (en) 1991-05-01 1992-10-13 Ciba-Geigy Corporation Phosphono/biaryl substituted dipeptide derivatives
US5294632A (en) 1991-05-01 1994-03-15 Ciba-Geigy Corporation Phosphono/biaryl substituted dipetide derivatives
US5217996A (en) 1992-01-22 1993-06-08 Ciba-Geigy Corporation Biaryl substituted 4-amino-butyric acid amides
US5508272A (en) 1993-06-15 1996-04-16 Bristol-Myers Squibb Company Compounds containing a fused bicycle ring and processes therefor
DE19510566A1 (de) 1995-03-23 1996-09-26 Kali Chemie Pharma Gmbh Benzazepin-, Benzoxazepin- und Benzothiazepin-N-essigsäurederivate sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
WO1996033170A1 (en) 1995-04-21 1996-10-24 Novarits Ag N-aroylamino acid amides as endothelin inhibitors
US6660756B2 (en) 2001-03-28 2003-12-09 Pfizer Inc. N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
GB0119305D0 (en) 2001-04-12 2001-10-03 Aventis Pharma Gmbh Mercaptoacetylamide derivatives,a process for their preparation and their use
EP2385037A1 (en) * 2003-06-24 2011-11-09 Chemtura Corporation Fungicidal phenoxyphenylhydrazine derivatives
WO2006027680A1 (en) 2004-09-10 2006-03-16 Pfizer Limited 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme
BRPI0607230A2 (pt) * 2005-02-10 2009-08-25 Medivir Ab inibidores de protease hiv
AR057882A1 (es) 2005-11-09 2007-12-26 Novartis Ag Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra
WO2007106708A2 (en) 2006-03-10 2007-09-20 Novartis Ag Combinations of the angiotensin ii antagonist valsartan and the nep inhibitor daglutril
MY151993A (en) 2007-01-12 2014-07-31 Novartis Ag Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid
TWI448284B (zh) 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
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
MA33364B1 (fr) 2009-05-28 2012-06-01 Novartis Ag Dérivés aminobutyriques substitués en tant qu'inhibiteurs de néprilysine
ES2602826T3 (es) * 2009-05-28 2017-02-22 Novartis Ag Derivados aminobutíricos sustituidos como inhibidores de neprilisina
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
EP2526088B1 (en) 2010-01-22 2015-08-05 Novartis AG Intermediates of neutral endopeptidase inhibitors and preparation method thereof
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
US8993631B2 (en) 2010-11-16 2015-03-31 Novartis Ag Method of treating contrast-induced nephropathy
NZ611528A (en) 2010-12-15 2015-06-26 Theravance Biopharma R & D Ip Llc Neprilysin inhibitors
ME02295B (me) 2010-12-15 2016-02-20 Theravance Biopharma R&D Ip Llc Inhibitori neprilizina
CA2825737C (en) * 2011-02-17 2018-11-13 Theravance, Inc. Substituted aminobutyric derivatives as neprilysin inhibitors
ES2564275T3 (es) * 2011-02-17 2016-03-21 Theravance Biopharma R&D Ip, Llc Derivados aminobutíricos sustituidos como inhibidores de neprilisina
ES2653215T3 (es) 2011-05-31 2018-02-06 Theravance Biopharma R&D Ip, Llc Inhibidores de neprilisina
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
CA2835281A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
TWI560172B (en) 2011-11-02 2016-12-01 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
WO2013148768A1 (en) 2012-03-28 2013-10-03 Theravance, Inc. Crystalline forms of (r)-3-[n-(3'-chlorobiphenyl-4-ylmethyl)-n'-(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester
CA2871292A1 (en) 2012-05-31 2013-12-05 Theravance Biopharma R&D Ip, Llc Nitric oxide donor neprilysin inhibitors
EP2858650B1 (en) 2012-06-08 2018-11-14 Theravance Biopharma R&D IP, LLC Neprilysin inhibitors
RS55967B1 (sr) 2012-06-08 2017-09-29 Theravance Biopharma R&D Ip Llc Inhibitori neprilizina
BR112015002821B1 (pt) 2012-08-08 2022-10-18 Theravance Biopharma R&D Ip, Llc Compostos inibidores de neprilisina e composição farmacêutica

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