AR016133A1 - Compuesto de carbamiloxi que inhiben la adhesion de leucocitos mediada por vla-4, compuestos que son prodrogas de dichos compuestos, composicionfarmaceutica, metodo para fijar vla-4 a una muestra biologica, metodo para el tratamiento de una condicion inflamatoria - Google Patents

Compuesto de carbamiloxi que inhiben la adhesion de leucocitos mediada por vla-4, compuestos que son prodrogas de dichos compuestos, composicionfarmaceutica, metodo para fijar vla-4 a una muestra biologica, metodo para el tratamiento de una condicion inflamatoria

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Publication number
AR016133A1
AR016133A1 ARP980103779A ARP980103779A AR016133A1 AR 016133 A1 AR016133 A1 AR 016133A1 AR P980103779 A ARP980103779 A AR P980103779A AR P980103779 A ARP980103779 A AR P980103779A AR 016133 A1 AR016133 A1 AR 016133A1
Authority
AR
Argentina
Prior art keywords
substituted
compounds
heterocycle
group
cycloalkyl
Prior art date
Application number
ARP980103779A
Other languages
English (en)
Original Assignee
Wyeth Corp
Athena Neurosciences Inc
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 Wyeth Corp, Athena Neurosciences Inc filed Critical Wyeth Corp
Publication of AR016133A1 publication Critical patent/AR016133A1/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
    • C07K5/06008—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
    • 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
    • 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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0215—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing natural amino acids, forming a peptide bond via their side chain functional group, e.g. epsilon-Lys, gamma-Glu
    • 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
    • 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

Abstract

Se describe compuestos que fijan VLA-4. Ciertos de estos compuestos inhiben también la adhesion de leucocitos y, en particular, la adhesion de leucocitosmedida por VLA-4. Tales compuestos son utiles en el tratamiento de enfermedades inflamatorias enun paciente mamífero, por ejemplo un ser humano, tal como asmaenfermedad de Alzheimer, aterosclerosis, demencia por SIDA, diabetes, enfermedad inflamatoria del intestino, artritis reumatoide, transplante de tejido,metástasis tumoral e isquemia en elmiocardio. Los compuestos pueden ser administrados también para el tratamiento de enfermedades inflamatorias del cerebrotal como esclerosis multiple. Los compuestos descriptos pueden ser de la formula (I) en la cual: R1 está seleccionado del grupo que consiste de alquilo,alquilo sustituido, arilo, arilo sustituido, cicloalquilo, cicloalquilo sustituido, heterociclo, hetereociclo sustituido, heteroarilo y heteroarilo sustituido;R2 está seleccionado del grupo que consiste de hidrogeno, alquilo, cicloalquilo, cicloalquilo sustituido, cicloalquenilo, cicloalquenilo sustituido,heterociclo, heterociclo sustituido, alquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido y R1 y R2 junto con el átomo de nitrogenounido a R2 yel grupo S0(2), unido a R1 pueden formar un grupo heterociclico o un grupo heterocíclico sustituido; R3 está seleccionado del grupo que consistede hidrogeno, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclo sustituidoy cuando R2 no forma un grupo heterocíclico con R1, R2 y R3 junto con el átomo de nitrogeno unido a R2 y el átomo carbono unido a R3 pueden formar unheterocíclico o un grupo heterocíclico sustituido; R5 es -(CH2)x-Ar-R5 en la cual R5 está seleccionado del grupo que consiste de -O-Z-NR8R8 y -O-Z-R12 en lacual R8 y R8 están seleccionados independientmente del grupo que consiste de hidrogeno, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido,heterociclo, heterociclo sustituido y en la cual R8 y R8están unidos para formar un heterociclo o un heterociclo sustituido, R12 está seleccionado del grupo
ARP980103779A 1997-07-31 1998-07-30 Compuesto de carbamiloxi que inhiben la adhesion de leucocitos mediada por vla-4, compuestos que son prodrogas de dichos compuestos, composicionfarmaceutica, metodo para fijar vla-4 a una muestra biologica, metodo para el tratamiento de una condicion inflamatoria AR016133A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US90442497A 1997-07-31 1997-07-31
US5445397P 1997-08-01 1997-08-01

Publications (1)

Publication Number Publication Date
AR016133A1 true AR016133A1 (es) 2001-06-20

Family

ID=26733051

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980103779A AR016133A1 (es) 1997-07-31 1998-07-30 Compuesto de carbamiloxi que inhiben la adhesion de leucocitos mediada por vla-4, compuestos que son prodrogas de dichos compuestos, composicionfarmaceutica, metodo para fijar vla-4 a una muestra biologica, metodo para el tratamiento de una condicion inflamatoria

Country Status (18)

Country Link
EP (3) EP1452532A1 (es)
JP (3) JP4431717B2 (es)
KR (1) KR100639055B1 (es)
CN (1) CN1119340C (es)
AR (1) AR016133A1 (es)
AT (2) ATE236146T1 (es)
AU (2) AU740681B2 (es)
BR (1) BR9811598A (es)
CA (2) CA2290745C (es)
DE (2) DE69812890T2 (es)
ES (1) ES2221183T3 (es)
IL (1) IL133636A0 (es)
NO (1) NO20000413L (es)
NZ (1) NZ502578A (es)
PL (1) PL338521A1 (es)
RU (1) RU2220964C2 (es)
TW (1) TW533211B (es)
WO (2) WO1999006390A1 (es)

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EP0954519A1 (en) 1999-11-10
EP1000051A1 (en) 2000-05-17
PL338521A1 (en) 2000-11-06
DE69824007T2 (de) 2005-05-25
BR9811598A (pt) 2000-10-03
AU8584998A (en) 1999-02-22
EP0954519B1 (en) 2003-04-02
CN1119340C (zh) 2003-08-27
AU8605098A (en) 1999-02-22
JP2009269924A (ja) 2009-11-19
CA2290745A1 (en) 1999-02-11
DE69812890T2 (de) 2003-12-18
ATE236146T1 (de) 2003-04-15
KR20010022373A (ko) 2001-03-15
NO20000413L (no) 2000-03-28
WO1999006391A1 (en) 1999-02-11
EP1452532A1 (en) 2004-09-01
AU740681B2 (en) 2001-11-08
CA2267175C (en) 2009-12-15
JP4431717B2 (ja) 2010-03-17
TW533211B (en) 2003-05-21
CA2290745C (en) 2009-09-08
DE69812890D1 (de) 2003-05-08
WO1999006390A1 (en) 1999-02-11
NZ502578A (en) 2001-08-31
EP1000051B1 (en) 2004-05-19
DE69824007D1 (de) 2004-06-24
ES2221183T3 (es) 2004-12-16
ATE267188T1 (de) 2004-06-15
CN1265657A (zh) 2000-09-06
KR100639055B1 (ko) 2006-10-27
CA2267175A1 (en) 1999-02-11
JP2001512114A (ja) 2001-08-21
JP2001502361A (ja) 2001-02-20
IL133636A0 (en) 2001-04-30
RU2220964C2 (ru) 2004-01-10
NO20000413D0 (no) 2000-01-27

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