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AR075050A1 - Dicianopiridinas alquilamino-sustituidas - Google Patents

Dicianopiridinas alquilamino-sustituidas

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Publication number
AR075050A1
AR075050A1 ARP100100173A ARP100100173A AR075050A1 AR 075050 A1 AR075050 A1 AR 075050A1 AR P100100173 A ARP100100173 A AR P100100173A AR P100100173 A ARP100100173 A AR P100100173A AR 075050 A1 AR075050 A1 AR 075050A1
Authority
AR
Argentina
Prior art keywords
alkyl
represents hydrogen
group
substituted
alkoxy
Prior art date
Application number
ARP100100173A
Other languages
English (en)
Inventor
Barbara Albrecht-Kupper
Ursula Krenz
Alexandros Vakalopoulos
Daniel Meibom
Katja Zimmermann
Hans-Georg Lerchen
Joerg Keldenich
Peter Nell
Frank Suebmeier
Original Assignee
Bayer Schering Pharma 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41724154&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR075050(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR075050A1 publication Critical patent/AR075050A1/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
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    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
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    • C07K5/06086Dipeptides with the first amino acid being basic
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    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06147Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
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    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
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  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Crystallography & Structural Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
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  • Hospice & Palliative Care (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract

La presente se refiere a dicianopiridinas 6-alquilamino sustituidas, a sus profármacos de éster de aminoácido, a procedimientos para su preparacion, a su uso para el tratamiento y/o la profilaxis de enfermedades y a su uso para preparar medicamentos para el tratamiento y/o la profilaxis de enfermedades preferiblemente para el tratamiento y/o la prevencion de trastornos cardiovasculares. Reivindicacion 1: Un compuesto de formula (1) en la que R1 representa hidrogeno o alquilo C1-4, R2 representa alquilo C1-6, alquenilo C2-4, alquinilo C2-4 o cicloalquilo C3-7, donde alquilo C1-6 puede estar sustituido con 1 a 3 sustituyentes seleccionados independientemente entre sí entre el grupo constituido por fluor, cloro, trifluorometilo, trifluorometoxi, alcoxi C1-4, cicloalquilo C3-7, cicloalcoxi C3-7, alquilsulfanilo C1-4 y alquilsulfonilo C1-4, y donde alquenilo C2-4 y alquinilo C2-4 pueden estar sustituidos con 1 o 2 sustituyentes seleccionados independientemente entre si entre el grupo constituido por fluor, trifluorometilo, alquilo C1-4, trifluorometoxi y alcoxi C1-4, y donde cicloalquilo C3-7 puede estar sustituido con 1 o 2 sustituyentes seleccionados independientemente entre si entre el grupo constituido por fluor, cloro, trifluorometilo, alquilo C1-4, trifluorometoxi y alcoxi C1-4, o R1 y R2 junto con el átomo de nitrogeno al que están unidos, forman un heterociclo de 4 a 7 miembros que puede contener un heteroátomo adicional del grupo constituido por N, O y S, donde el heterociclo de 4 a 7 miembros puede estar sustituido con 1 o 2 sustituyentes seleccionados independientemente entre sí entre el grupo constituido por fluor, cloro, oxo, trifluorometilo, alquilo C1-4, trifluorometoxi y alcoxi C1-4; R3 representa hidrogeno o una estructura del grupo de formulas (2) en las que representa el punto de union al átomo de oxígeno; L1 representa alcanodiílo C2-6; L2 representa alcanodiílo C2-6; R4 representa hidrogeno o el grupo lateral de un a-aminoácido natural o sus homologos o isomeros; R5 representa hidrogeno o metilo; R6 representa hidrogeno o alquilo C1-4; R7 representa hidrogeno o alquilo C1-4; o R6 y R7 junto con al átomo de nitrogeno al que están unidos, forman un heterociclo de 5 o 6 miembros, donde el heterociclo de 5 o 6 miembros puede estar sustituido con 1 o 2 sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, amino, hidroxilo y alcoxi C1-4; o R7 junto con R4 y los átomos a los que están unidos, forma un anillo de pirrolidona o piperidina; R8 representa hidrogeno o el grupo lateral de un a-aminoácido natural o sus homologos o isomeros; R9 representa hidrogeno o metilo; R10 representa hidrogeno o metilo; R11 representa hidrogeno o el grupo lateral de un a-aminoácido natural o sus homologos o isomeros; 2 representa hidrogeno o metilo; R13 representa hidrogeno o alquilo C1-4; R14 representa hidrogeno o alquilo C1-4; o R13 y R14 junto con el átomo de nitrogeno al que están unidos, forman un heterociclo de 5 o 6 miembros, donde el heterociclo de 5 o 6 miembros puede estar sustituido con 1 o 2 sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, amino, hidroxilo y alcoxi C1-4; o R14 junto con R11 y los átomos a los que están unidos, forma un anillo de pirrolidina o piperidina; R15 representa hidrogeno o alquilo C1-4; R16 representa hidrogeno o alquilo C1-4; o R15 y R16 junto con el átomo de nitrogeno al que están unidos, forman un heterociclo de 5 o 6 miembros, donde el heterociclo de 5 o 6 miembros puede estar sustituido con 1 o 2 sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, amino, hidroxilo y alcoxi C1-4; R17 representa hidrogeno o alquilo C1-4; R18 representa hidrogeno o alquilo C1-4; o R17 y R18 junto con el átomo de nitrogeno al que están unidos forman un heterociclo de 5 o 6 miembros, donde el heterociclo de 5 o 6 miembros puede estar sustituido con 1 o 2 sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, amino, hidroxilo y alcoxi C1-4; R19 representa hidrogeno o metilo; y los N-oxidos, sales, solvatos, sales de los N-oxidos y solvatos de los N-oxidos y sales del mismo.
ARP100100173A 2009-01-29 2010-01-26 Dicianopiridinas alquilamino-sustituidas AR075050A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102009006602A DE102009006602A1 (de) 2009-01-29 2009-01-29 Alkylamino-substituierte Dicyanopyridine und deren Aminosäureester-Prodrugs

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AR075050A1 true AR075050A1 (es) 2011-03-02

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US (3) US8420825B2 (es)
EP (2) EP2743270B1 (es)
JP (2) JP5693469B2 (es)
KR (2) KR101833188B1 (es)
CN (2) CN104844687B (es)
AR (1) AR075050A1 (es)
AU (1) AU2010207786B2 (es)
BR (1) BRPI1007308A2 (es)
CA (2) CA2962039A1 (es)
CO (1) CO6400193A2 (es)
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CY (2) CY1115403T1 (es)
DE (1) DE102009006602A1 (es)
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DO (1) DOP2011000243A (es)
EA (1) EA019275B1 (es)
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