AR069146A1 - Derivados de pirimidina, composicion farmaceutica que los comprende y el uso de esta para el tratamiento de enfermedades relacionadas con la activacion del sistema inmunitario. - Google Patents

Derivados de pirimidina, composicion farmaceutica que los comprende y el uso de esta para el tratamiento de enfermedades relacionadas con la activacion del sistema inmunitario.

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Publication number
AR069146A1
AR069146A1 ARP080104783A ARP080104783A AR069146A1 AR 069146 A1 AR069146 A1 AR 069146A1 AR P080104783 A ARP080104783 A AR P080104783A AR P080104783 A ARP080104783 A AR P080104783A AR 069146 A1 AR069146 A1 AR 069146A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydroxy
carboxylic acid
pyrrolidine
carboxy
Prior art date
Application number
ARP080104783A
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English (en)
Original Assignee
Actelion Pharmaceuticals Ltd
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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Publication date
Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of AR069146A1 publication Critical patent/AR069146A1/es

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    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de pirimidina, y su uso como compuestos farmacéuticamente activos. Dichos compuestos actuan, en particular, como agentes inmunomoduladores. Reivindicacion 1: Un compuesto de la formula (1) donde A representa el grupo de formulas (2) donde los asteriscos indican el enlace que se une al grupo pirimidina de la formula (1); R1 representa alcoxi C1-4, alquilamino C1-4, N-alquilo C1-4-N-alquilamino C1-3, cicloalquilamino C3-5, cicloalquilmetilamino C3-5, pirrolidina o piperidina; R2 representa alquilo C1-2 o alquilo C3-4; R3 representa hidrogeno, alquilo C1-4, o alcoxi C1-3; R4 representa hidrogeno, alquilo C1-4, o alcoxi C1-3; R5 representa 2,3-dihidroxipropilo, di-(hidroxi-alquilo C1-4)-alquilo C1-4, -CH2-(CH2)k-NHSO2R53, (CH2)nCH(OH)-CH2-NHSO2R53, -CH2-(CH2)k-NHCOR54, -(CH2)nCH(OH)-CH2-NHCOR54, -CH2-(CH2)n-CONR51R52, 1-(3-carboxi-azetidinil)-2-acetilo, 1-(2-carboxi-pirrolidinil)-2-acetilo, 1-(3-carboxi-pirrolidinil)-2-acetilo, 1-(3-carboxi-azetidinil)-3-propionilo, 1-(2-carboxi-pirrolidinil)-3-propionilo, 1-(3-carboxi-pirrolidinil)-3-propionilo, -(CH2)nCH(OH)-CH2-NR51R52, hidroxi-alcoxi C2-5, di-(hidroxi-alquilo C1-4)-alcoxi C1-4, 2,3-dihidroxi-propoxi, 2-hidroxi-3-metoxi-propoxi, -OCH2-(CH2)m-NR51R52, 2-[(ácido azetidina-3-carboxílico)-1-il]-etoxi, 2-[(ácido azetidina-3-carboxílico alquiléster C1-5)-1-il]-etoxi, 2-[(ácido pirrolidina-3-carboxílico)-1-il]-etoxi, 2-[(ácido pirrolidina-3-carboxílico alquiléster C1-5)-1-il]-etoxi, -OCH2-CH(OH)-CH2-NR51R52, 3-[(ácido azetidina-3-carboxílico)-1-iI]-2-hidroxipropoxi, 3-[(ácido azetidina-3-carboxílico alquiléster C1-5)-1-il]-2-hidroxipropoxi, 2-hidroxi-3-[(ácido pirrolidina-3-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(ácido pirrolidina-3-carboxílico alquiléster C1-5)-1-il]-propoxi, 2-hidroxi-3-[(ácido pirrolidina-2-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(ácido pirrolidina-2-carboxílico alquiléster C1-5)-1-il]-propoxi, -OCH2-(CH2)m-NHSO2R53, -OCH2-CH(OH)-CH2-NHSO2R53, -OCH2-(CH2)m-NHCOR54, o -OCH2-CH(OH)-CH2-NHCOR54; R51 representa hidrogeno, alquilo C1-3, 2-hidroxietilo, 2-hidroxi-1- hidroximetil-etilo, 2,3-dihidroxipropilo, carboximetilo, (alquilcarboxi C1-5)metilo, 2-carboxietilo, 2-(alquilcarboxi C1-5)etilo o 2-aminoetilo; R52 representa hidrogeno, metilo, o etilo; R53 representa alquilo C1-3, metilamino, etilamino, o dimetilamino; R54 representa hidroxi-alquilo C1-2 o R55R56N-alquilo C1-2; R55 y R56, de manera independiente, representan hidrogeno o metilo; k representa el numero entero 1; 2; o 3; m representa el numero entero 1 o 2; n representa 0; 1 o 2; y R6 representa hidrogeno, alquilo C1-4 o halogeno; o una sal de dicho compuesto.
ARP080104783A 2007-11-01 2008-10-31 Derivados de pirimidina, composicion farmaceutica que los comprende y el uso de esta para el tratamiento de enfermedades relacionadas con la activacion del sistema inmunitario. AR069146A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IB2007054437 2007-11-01

Publications (1)

Publication Number Publication Date
AR069146A1 true AR069146A1 (es) 2009-12-30

Family

ID=40577704

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080104783A AR069146A1 (es) 2007-11-01 2008-10-31 Derivados de pirimidina, composicion farmaceutica que los comprende y el uso de esta para el tratamiento de enfermedades relacionadas con la activacion del sistema inmunitario.

Country Status (18)

Country Link
US (1) US8299086B2 (es)
EP (1) EP2217594B1 (es)
JP (1) JP5517944B2 (es)
KR (1) KR20100092473A (es)
CN (1) CN101970430B (es)
AR (1) AR069146A1 (es)
AU (1) AU2008320374A1 (es)
BR (1) BRPI0818804A2 (es)
CA (1) CA2700917A1 (es)
ES (1) ES2449749T3 (es)
IL (1) IL205425A0 (es)
MA (1) MA31849B1 (es)
MX (1) MX2010004576A (es)
NZ (1) NZ585775A (es)
RU (1) RU2010121969A (es)
TW (1) TW200920746A (es)
WO (1) WO2009057079A2 (es)
ZA (1) ZA201003875B (es)

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JP2011502980A (ja) 2011-01-27
TW200920746A (en) 2009-05-16
MA31849B1 (fr) 2010-11-01
EP2217594A2 (en) 2010-08-18
MX2010004576A (es) 2010-05-17
WO2009057079A2 (en) 2009-05-07
WO2009057079A3 (en) 2009-12-03
KR20100092473A (ko) 2010-08-20
CA2700917A1 (en) 2009-05-07
AU2008320374A1 (en) 2009-05-07
EP2217594B1 (en) 2014-01-08
CN101970430A (zh) 2011-02-09
IL205425A0 (en) 2010-12-30
ZA201003875B (en) 2012-08-29
JP5517944B2 (ja) 2014-06-11
NZ585775A (en) 2011-12-22
US20100234346A1 (en) 2010-09-16
US8299086B2 (en) 2012-10-30
BRPI0818804A2 (pt) 2015-04-22
ES2449749T3 (es) 2014-03-21
CN101970430B (zh) 2013-05-08
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