MA38330B1 - Dérivés d'acide phosphonique butanoïque de bisphénol substitués en qualité d'inhibiteurs de nep (endopeptidase neutre) - Google Patents

Dérivés d'acide phosphonique butanoïque de bisphénol substitués en qualité d'inhibiteurs de nep (endopeptidase neutre)

Info

Publication number
MA38330B1
MA38330B1 MA38330A MA38330A MA38330B1 MA 38330 B1 MA38330 B1 MA 38330B1 MA 38330 A MA38330 A MA 38330A MA 38330 A MA38330 A MA 38330A MA 38330 B1 MA38330 B1 MA 38330B1
Authority
MA
Morocco
Prior art keywords
butanoic
acid derivatives
phosphonic acid
neutral endopeptidase
nep inhibitors
Prior art date
Application number
MA38330A
Other languages
English (en)
Other versions
MA38330A1 (fr
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 MA38330A1 publication Critical patent/MA38330A1/fr
Publication of MA38330B1 publication Critical patent/MA38330B1/fr

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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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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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    • 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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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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
    • C07F9/547—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
    • 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
    • C07F9/547—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
    • C—CHEMISTRY; METALLURGY
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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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne un procédé selon la formule (i), ou un sel pharmaceutiquement acceptable de celui-ci, dans lequel r1, r2 et r3 sont tels que définis présentement. L'invention concerne également un procédé de production des composés de la présente invention, ainsi que ses utilisations thérapeutiques. L'invention concerne également une composition pharmaceutique des composés de l'invention, et une combinaison d'agents pharmacologiquement actifs et d'un composé de l'invention.
MA38330A 2013-02-14 2014-02-12 Dérivés d'acide phosphonique butanoïque de bisphénol substitués en qualité d'inhibiteurs de nep (endopeptidase neutre) MA38330B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361764679P 2013-02-14 2013-02-14
PCT/US2014/015980 WO2014126979A1 (fr) 2013-02-14 2014-02-12 Dérivés d'acide phosphonique butanoïque de bisphénol substitués en qualité d'inhibiteurs de nep (endopeptidase neutre)

Publications (2)

Publication Number Publication Date
MA38330A1 MA38330A1 (fr) 2016-02-29
MA38330B1 true MA38330B1 (fr) 2016-09-30

Family

ID=50193599

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38330A MA38330B1 (fr) 2013-02-14 2014-02-12 Dérivés d'acide phosphonique butanoïque de bisphénol substitués en qualité d'inhibiteurs de nep (endopeptidase neutre)

Country Status (36)

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

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NZ710574A (en) 2013-02-14 2017-11-24 Novartis Ag Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors
EP2990800A1 (fr) * 2014-08-29 2016-03-02 Fundació Institut d'Investigació en Ciències de la Salut Germans Trias i Pujol Neprilysin comme marqueur pronostique pour l'insuffisance cardiaque
CN106397249A (zh) * 2015-08-03 2017-02-15 深圳信立泰药业股份有限公司 一种高稳定性lcz696结晶粉末及其制备方法
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
CN113166101A (zh) 2018-11-27 2021-07-23 诺华股份有限公司 作为治疗代谢障碍的蛋白质原转换酶枯草杆菌蛋白酶/kexin 9型（PCSK9）抑制剂的环状五聚体化合物
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
JP7657151B2 (ja) 2018-11-27 2025-04-04 ノバルティス アーゲー 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド
CA3192236A1 (fr) 2020-09-10 2022-03-17 Tony Lahoutte Fragment d'anticorps contre fap
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 (fr) 2022-04-22 2023-10-26 Precirix N.V. Anticorps radiomarqué amélioré
AU2023264245A1 (en) 2022-05-02 2024-12-19 Precirix N.V. Pre-targeting

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