AR014903A1 - Compuestos del tipo 4-amino-fenilalanina inhibidores de la adhesion de leucocitos intermediada por vla-4, compuesto que son droga de dichos compuestos,composiciones farmaceuticas, metodo para adherir vla-4 en una muestra biologica, metodo para tratar una condicion inflamatoria - Google Patents

Compuestos del tipo 4-amino-fenilalanina inhibidores de la adhesion de leucocitos intermediada por vla-4, compuesto que son droga de dichos compuestos,composiciones farmaceuticas, metodo para adherir vla-4 en una muestra biologica, metodo para tratar una condicion inflamatoria

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Publication number
AR014903A1
AR014903A1 ARP980103777A ARP980103777A AR014903A1 AR 014903 A1 AR014903 A1 AR 014903A1 AR P980103777 A ARP980103777 A AR P980103777A AR P980103777 A ARP980103777 A AR P980103777A AR 014903 A1 AR014903 A1 AR 014903A1
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AR
Argentina
Prior art keywords
substituted
heterocyclic
compounds
group
aryl
Prior art date
Application number
ARP980103777A
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English (en)
Original Assignee
Athena Neurosciences Inc
American Home Prod
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.)
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Application filed by Athena Neurosciences Inc, American Home Prod filed Critical Athena Neurosciences Inc
Publication of AR014903A1 publication Critical patent/AR014903A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
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  • Emergency Medicine (AREA)
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Abstract

Se describen compuestos que adhieren VLA-4. Algunos de estos compuestos inhiben también la adhesion de leucocitos y en particular la adhesion de leucocitosintermediada por VLA-4. Dichos compuestos son utiles para el tratamiento de enfermedades inflamatorias en un paciente mamífero, por ejemplo en el ser humano,tales como asma, enfermedad de Alzheimer, arterosclerosis, demencia por SIDA, diabetes, enfermedad inflamatoria del intestino, artritis reumatoidea,transplantes de tejidos, metástasis de tumores e isquemia de miocardio. Los compuestos pueden ser administrados también para el tratamiento de enfermedadescerebrales inflamatorias tales como esclerosis multiples. Los compuestos son de formula I donde: R1 está seleccionado del grupo que consiste en alquilo,alquilo substituido, arilo, arilo substituido, cicloalquilo, cicloalquilo substituido, heterocíclico, heterocíclico substituido, heteroarilo y heteroarilosubstituido; R2 está seleccionado del grupo que consiste en hidrogeno, alquilo,alquilo substituido, cicloalquilo, cicloalquilo substituido, cicloalquenilo,cicloalquenilo substituido, heterocíclico, heterocíclico substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, y R1 y R2 conjuntamentecon el átomo denitrogeno unido a R2 y el grupo SO2 unido a R1 pueden formar un grupo heterocíclico o heterocíclico substituido; R3 está seleccionado del grupoque consiste en alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido,heterocíclico, heterocíclico substituido, y cuando R2 no forma un grupo heterocíclico con R1 y R2 y R3 conjuntamente con el átomo de nitrogeno adherido a R2 yel átomo de carbono adherido a R3, pueden formar un grupo heterocíclico o heterocíclico substituido; R5 es -(CH2)x-AR-R5 donde R5 esta seleccionado del grupoque consiste en -NR12C(Z)NR8R8 y -NR12C(Z)R13 donde R12 está seleccionado del grupo que consiste en hidrogeno, alquilo y arilo, R8 y R8 estánindependientemente seleccionados del grupo que consiste en hidrogeno, alquilo, alquilo substituido, arilo, arilo substituido, cicloalquilo, cicloalquilo
ARP980103777A 1997-07-31 1998-07-30 Compuestos del tipo 4-amino-fenilalanina inhibidores de la adhesion de leucocitos intermediada por vla-4, compuesto que son droga de dichos compuestos,composiciones farmaceuticas, metodo para adherir vla-4 en una muestra biologica, metodo para tratar una condicion inflamatoria AR014903A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US92035397A 1997-07-31 1997-07-31

Publications (1)

Publication Number Publication Date
AR014903A1 true AR014903A1 (es) 2001-04-11

Family

ID=25443597

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Application Number Title Priority Date Filing Date
ARP980103777A AR014903A1 (es) 1997-07-31 1998-07-30 Compuestos del tipo 4-amino-fenilalanina inhibidores de la adhesion de leucocitos intermediada por vla-4, compuesto que son droga de dichos compuestos,composiciones farmaceuticas, metodo para adherir vla-4 en una muestra biologica, metodo para tratar una condicion inflamatoria

Country Status (17)

Country Link
EP (1) EP1001974B1 (es)
JP (1) JP2003517424A (es)
KR (1) KR20010022414A (es)
CN (1) CN1265674A (es)
AR (1) AR014903A1 (es)
AT (1) ATE327245T1 (es)
AU (1) AU8584698A (es)
BR (1) BR9812118A (es)
CA (1) CA2290750A1 (es)
DE (1) DE69834642T2 (es)
HU (1) HUP0004531A3 (es)
IL (1) IL133638A0 (es)
NO (1) NO20000411L (es)
NZ (1) NZ502580A (es)
PL (1) PL338413A1 (es)
WO (1) WO1999006434A1 (es)
ZA (1) ZA986837B (es)

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NO20000411L (no) 2000-03-28
HUP0004531A3 (en) 2001-12-28
ATE327245T1 (de) 2006-06-15
WO1999006434A1 (en) 1999-02-11
CN1265674A (zh) 2000-09-06
IL133638A0 (en) 2001-04-30
HUP0004531A2 (hu) 2001-04-28
NO20000411D0 (no) 2000-01-27
DE69834642D1 (de) 2006-06-29
AU8584698A (en) 1999-02-22
JP2003517424A (ja) 2003-05-27
KR20010022414A (ko) 2001-03-15
DE69834642T2 (de) 2007-05-03
PL338413A1 (en) 2000-11-06
EP1001974A1 (en) 2000-05-24
BR9812118A (pt) 2000-07-18
NZ502580A (en) 2001-06-29
ZA986837B (en) 2000-05-02
CA2290750A1 (en) 1999-02-11
EP1001974B1 (en) 2006-05-24

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