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PE20151666A1 - Derivados sustituidos del acido bisfenil butanoico fosfonico como inhibidores de la nep - Google Patents

Derivados sustituidos del acido bisfenil butanoico fosfonico como inhibidores de la nep

Info

Publication number
PE20151666A1
PE20151666A1 PE2015001738A PE2015001738A PE20151666A1 PE 20151666 A1 PE20151666 A1 PE 20151666A1 PE 2015001738 A PE2015001738 A PE 2015001738A PE 2015001738 A PE2015001738 A PE 2015001738A PE 20151666 A1 PE20151666 A1 PE 20151666A1
Authority
PE
Peru
Prior art keywords
acid
nep
inhibitors
compounds
oxobutan
Prior art date
Application number
PE2015001738A
Other languages
English (en)
Inventor
David Weninger Barnes
Scott Louis Cohen
Dean Franklin Rigel
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 PE20151666A1 publication Critical patent/PE20151666A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3808—Acyclic saturated acids which can have further substituents on alkyl
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
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    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring

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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
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  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
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  • Pulmonology (AREA)
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  • Hospice & Palliative Care (AREA)
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  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente invencion proporciona un compuesto de la formula l; o una sal farmaceuticamente aceptable del mismo, en donde R1, R2 y R3 se definen como R1 es H, alquilo C1-C7, etc. R2 es Cl, CH3 o F, R3 es H, Cl, etc. La invencion tambien se relaciona con un metodo para fabricar los compuestos de la invencion, y sus usos en el tratamiento de hipertension, enfermedad vascular periferica, insuficiencia cardiaca congestiva, entre otros. La presente invencion proporciona ademas la composicion farmaceutica de los compuestos de la invencion y una combinacion de agentes farmacologicamente activos y un compuesto de la invencion. Los compuestos preferidos son: Acido (3-(((R)-1-(5'-cloro-2'-fluoro-[1,1'-bifenil]-4-il)-4-((S)-1-(((ciclohexiloxi)carbonil)oxi)etoxi)-4-oxobutan-2-il)amino)-3-oxopropil)fosfonico; Acido (3-(((2R)-4-(1-(benzoyloxi)etoxi)-1-(5'-cloro-2'-fluoro-[1,1'-bifenil]-4-il)-4-oxobutan-2-il)ameno)-3-oxopropil)fosfonico, entre otros
PE2015001738A 2013-02-14 2014-02-12 Derivados sustituidos del acido bisfenil butanoico fosfonico como inhibidores de la nep PE20151666A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361764679P 2013-02-14 2013-02-14

Publications (1)

Publication Number Publication Date
PE20151666A1 true PE20151666A1 (es) 2015-11-19

Family

ID=50193599

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015001738A PE20151666A1 (es) 2013-02-14 2014-02-12 Derivados sustituidos del acido bisfenil butanoico fosfonico como inhibidores de la nep

Country Status (36)

Country Link
US (3) US9163040B2 (es)
EP (1) EP2956464B1 (es)
JP (1) JP6295277B2 (es)
KR (1) KR20150119109A (es)
CN (1) CN105073762B (es)
AP (1) AP2015008621A0 (es)
AR (1) AR094790A1 (es)
AU (1) AU2014216424B2 (es)
BR (1) BR112015019369A2 (es)
CA (1) CA2900027A1 (es)
CR (1) CR20150419A (es)
CU (1) CU24330B1 (es)
CY (1) CY1120378T1 (es)
DK (1) DK2956464T3 (es)
EA (1) EA028583B1 (es)
ES (1) ES2675216T3 (es)
HR (1) HRP20180958T1 (es)
HU (1) HUE038248T2 (es)
IL (1) IL240336A0 (es)
LT (1) LT2956464T (es)
MA (1) MA38330B1 (es)
MX (1) MX367525B (es)
NZ (1) NZ710574A (es)
PE (1) PE20151666A1 (es)
PH (1) PH12015501752B1 (es)
PL (1) PL2956464T3 (es)
PT (1) PT2956464T (es)
RS (1) RS57358B1 (es)
SG (1) SG11201506018PA (es)
SI (1) SI2956464T1 (es)
TN (1) TN2015000324A1 (es)
TR (1) TR201808541T4 (es)
TW (1) TWI636057B (es)
UY (1) UY35325A (es)
WO (1) WO2014126979A1 (es)
ZA (1) ZA201505490B (es)

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JP6295277B2 (ja) 2013-02-14 2018-03-14 ノバルティス アーゲー Ｎｅｐ（中性エンドペプチダーゼ）阻害剤としての置換ビスフェニルブタン酸ホスホン酸誘導体
EP2990800A1 (en) * 2014-08-29 2016-03-02 Fundació Institut d'Investigació en Ciències de la Salut Germans Trias i Pujol Neprilysin as heartfailure (HF) prognostic marker
WO2017020841A1 (zh) * 2015-08-03 2017-02-09 深圳信立泰药业股份有限公司 一种含有lcz696的药物组合物及其制备方法
CN105748420B (zh) * 2016-03-04 2018-11-06 山东省药学科学院 一种治疗心力衰竭的lcz696缓释骨架片的制备方法
CN107764910B (zh) * 2017-09-05 2020-02-07 华侨大学 一种沙库比曲缬沙坦三钠半五水合物胶囊有效成分的含量测定方法
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
EP3887388A1 (en) 2018-11-27 2021-10-06 Novartis AG Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders
WO2020110008A1 (en) 2018-11-27 2020-06-04 Novartis Ag Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
UY38485A (es) 2018-11-27 2020-06-30 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación
KR20230093251A (ko) 2020-09-10 2023-06-27 프리시릭스 엔.브이. Fap에 대한 항체 단편
TW202333563A (zh) 2021-11-12 2023-09-01 瑞士商諾華公司 用於治療疾病或障礙之二胺基環戊基吡啶衍生物
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
KR20250034289A (ko) 2022-05-02 2025-03-11 프리시릭스 엔.브이. 사전 표적화

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