CU20150084A7 - Derivados del ácido 4-((1,1) bisfenil -4-il)-3-(3-fosfonopropanamido)butanoico,activo como inhibidores de nep(endopeptidasa neutral) - Google Patents

Derivados del ácido 4-((1,1) bisfenil -4-il)-3-(3-fosfonopropanamido)butanoico,activo como inhibidores de nep(endopeptidasa neutral)

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Publication number
CU20150084A7
CU20150084A7 CUP2015000084A CU20150084A CU20150084A7 CU 20150084 A7 CU20150084 A7 CU 20150084A7 CU P2015000084 A CUP2015000084 A CU P2015000084A CU 20150084 A CU20150084 A CU 20150084A CU 20150084 A7 CU20150084 A7 CU 20150084A7
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CU
Cuba
Prior art keywords
phosphonopropanamide
bisfenil
butanoic
active
acid derivatives
Prior art date
Application number
CUP2015000084A
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English (en)
Other versions
CU24330B1 (es
Inventor
David Weninger Barnes
Scott Louis Cohen
Dean Frankinn Rigel
Original Assignee
Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CU20150084A7 publication Critical patent/CU20150084A7/es
Publication of CU24330B1 publication Critical patent/CU24330B1/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
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    • 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
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    • A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
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    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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    • 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
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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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    • 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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  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
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  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
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  • Dermatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente invención proporciona un compuesto de la fórmula I; Espacio para la Fórmula o una sal farmacéuticamente aceptable del mismo, en donde R1, R2 y R3 se definen en la presente. La invención también se relaciona con un método para fabricar los compuestos de la invención, y sus usos terapéuticos. La presente invención proporciona además la composición farmacéutica de os compuestos de la invención y una combinación de agentes farmacéuticamente activos y un compuesto de la invención
CUP2015000084A 2013-02-14 2014-02-12 Derivados del ácido 4-((1,1) bifenil-4-il)-3-(3-fosfonopropanamido) butanoico, activos como inhibidores de nep (endopeptidasa neutral) CU24330B1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361764679P 2013-02-14 2013-02-14
PCT/US2014/015980 WO2014126979A1 (en) 2013-02-14 2014-02-12 Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors

Publications (2)

Publication Number Publication Date
CU20150084A7 true CU20150084A7 (es) 2016-01-29
CU24330B1 CU24330B1 (es) 2018-03-13

Family

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CUP2015000084A CU24330B1 (es) 2013-02-14 2014-02-12 Derivados del ácido 4-((1,1) bifenil-4-il)-3-(3-fosfonopropanamido) butanoico, activos como inhibidores de nep (endopeptidasa neutral)

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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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NZ710574A (en) 2013-02-14 2017-11-24 Novartis Ag Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors
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
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 (en) 2020-09-10 2022-03-17 Tony Lahoutte Antibody fragment against 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 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
AU2023264245A1 (en) 2022-05-02 2024-12-19 Precirix N.V. Pre-targeting

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