AR055751A1 - Derivados de tiofeno y composiciones farmaceuticas - Google Patents

Derivados de tiofeno y composiciones farmaceuticas

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Publication number
AR055751A1
AR055751A1 ARP060101135A ARP060101135A AR055751A1 AR 055751 A1 AR055751 A1 AR 055751A1 AR P060101135 A ARP060101135 A AR P060101135A AR P060101135 A ARP060101135 A AR P060101135A AR 055751 A1 AR055751 A1 AR 055751A1
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AR
Argentina
Prior art keywords
pyrrolidin
carboxylic acid
propoxy
hydroxy
alkyl
Prior art date
Application number
ARP060101135A
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English (en)
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Actelion Pharmaceuticals Ltd
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Publication date
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Publication of AR055751A1 publication Critical patent/AR055751A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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

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

Abstract

Composiciones farmacéuticas y su uso como inmunosupresores. Reivindicacion 1: Un compuesto seleccionado del grupo formado por tiofenos de la formula (1), en los que: el anillo A representa un grupo de formulas (2) o (3); R1 representa hidrogeno, alquilo C1-5, alcoxi C1-5, o halogeno; R2 representa hidrogeno, alquilo C1-5, alcoxi C1-5, trifluorometilo, trifluorometoxi, o halogeno; R3 representa hidrogeno, hidroxi-alquiloC1-5, 2,3-dihidroxipropilo, di-(hidroxi-alquiloC1-5)-alquilo C1-5, -CH2- (CH2)k-NR31R32, (ácido de azetidin-3-carboxílico)-1-il-metilo, (alquilC1-5 éster del ácido azetidin-3-carboxílico)-1-il-metilo, 2 [(ácido azetidin-3-carboxílico)-1-il]-etilo, 2-[(alquil C1-5 éster del ácido azetidin-3-carboxílico)-1-il]-etilo, 3- [(ácido azetidin-3-carboxílico)-1-il]-propilo, 3-[(alquilC1-5 éster del ácido azetidin-3-carboxílico)-1-il]-propilo, (ácido de pirrolidin-3-carboxílico)-1-il-metilo, (alquil C1-5 éster del ácido pirrolidin-3-carboxílico)-1-il-metilo, (ácido pirrolidin-2-carboxílico)-1-il-metilo, (alquil C1-5 éster del ácido pirrolidin-2-carboxílico)-1-il-metilo, 2-[(ácido pirrolidin-3-carboxílico)-1-il]-etilo, 2-[(alquil C1-5 éster del ácido pirrolidin-3-carboxílico)-1-il]-etilo, 2-[(ácido pirrolidin-2- carboxílico)-1-il]-etilo, 2-[(alquil C1-5 éster del ácido pirrolidin-2-carboxílico)-1-il]-etilo, 3-[(ácido pirrolidin-3-carboxílico)-1-il]-propilo, 3-[(alquil C1-5 éster del ácido pirrolidin-3-carboxílico)-1-il]-propilo, 3-[(ácido pirrolidin-2- carboxílico)-1-il]-propilo, 3-[(alquil C1-5 éster del ácido pirrolidin-2-carboxílico)-1-il]-propilo, --CH2-(CH2)n-COOH, -CH2- (CH2)n-CONR31R32, -CO-NHR31, -(CH2)nCH(OH)-CH2-NR31R32, hidroxi, alcoxi C1-5, fluoro-alcoxiC1-5, hidroxi-alcoxiC2-5, di- (hidroxi-alquiloC1-5)-alcoxiC1-5, 1-glicerilo, 2-glicerilo, 2-hidroxi-3-metoxi-propoxi, -OCH2-(CH2)m-R31R32, 2-pirrolidin-1-il-etoxi, 3-pirrolidin-1-il-propoxi, 2-piperazin-1-il-etoxi, 2-[4-(alquiloC1-5)-piperazin-1-il]-etoxi, 2-[4-(2-hidroxi-etil)- piperazin-1-il]-etoxi, 3-piperazin-1-il-propoxi, 3-[4-(alquiloC1-5)-piperazin-1-il]-propoxi, 3-[4-(2-hidroxi-etil)-piperazin-1-il]-propoxi, 2-morfolin-4-il-etoxi, 3-morfolin-4-il-propoxi, 2-[(ácido azetidin-3-carboxílico)-1-il]-etoxi, 2-[(alquil C1- 5 éster del ácido azetidin-3-carboxílico)-1-il]-etoxi, 2-[(ácido pirrolidin-3-carboxílico)-1-il]-etoxi, 2-[(alquil C1-5 éster del ácido pirrolidin-3-carboxílico)-1-il]-etoxi, 2-[(ácido pirrolidin-2-carboxílico)-1-il]-etoxi, 2-[(alquil C1-5 éster del ácido pirrolidin-2-carboxílico)-1-il]-etoxi, 2-[(2-hidroxi-pirrolidin)-1-il]-etoxi, 2-[(3-hidroxi-pirrolidin)-1-il]-etoxi, 3-[(ácido azetidin-2-carboxílico)-1-il]-propoxi, 3-[(alquil C1-5 éster del ácido azetidin-3-carboxílico)-1-il]-propoxi, 3- [(ácido pirrolidin-3-carboxílico)-1-il]-propoxi, 3-[(alquil C1-5 éster del ácido pirrolidin-3-carboxílico)-1-il]-propoxi, 3-[(ácido pirrolidin-2-carboxílico)-1-il]-propoxi, 3-[(alquil C1-5 éster del ácido pirrolidin-2-carboxílico)-1-il]-propoxi, 3- [(2-hidroxi-pirrolidin)-1-il]-propoxi, 3-[(3-hidroxi-pirrolidin)-1-il]-propoxi, 2-amino-3-hidroxi-2-hidroximetil-propoxi, -O-CH2-CONR31R32, 3-carbamoil-propoxi, 3-(alquiloC1-5-carbamoil)propoxi, 3-(2-hidroxietilcarbamoil)propoxi, -OCH2-CH(OH)-CH2- NR31R32, 3-[(ácido azetidin-3-carboxílico)-1-il]-2-hidroxipropoxi, 3-[(alquilC1-5 éster del ácido azetidin-3-carboxílico)-1-il]-2-hidroxipropoxi, 2-hidroxi-3-[(ácido pirrolidin-3-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(alquilC1-5 éster del ácido pirrolidin-3-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(ácido pirrolidin-2-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(alquil C1-5 éster del ácido pirrolidin-2-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(2-hidroxi-pirrolidin)-1-il]-propoxi, 2-hidroxi-3- [(3-hidroxi-pirrolidin)-1-il]-propoxi, 2-hidroxi-3-pirrolidin-1-il-propoxi, 2-hidroxi-3-piperazin-1-il-propoxi, 2-hidroxi-3-[4-(alquil C1-5)-piperazin-1-il]-propoxi, 2-hidroxi-3-[4-(2-hidroxi-etil)-piperazin-1-il]-propoxi, 2-hidroxi-3-morfolin-4-il- propoxi, -NR31R32, -NHCO-R31, -CH2-(CH2)k-NHSO2R33, -(CH2)nCH(OH)-CH2-NHSO2R33, -OCH2-(CH2)m-NHSO2R33, -OCH2-CH(OH)-CH2-NHSO2R33, -CH2-(CH2)k-NHCOR34, -(CH2)nCH(OH)-CH2-NHCOR34, -OCH2-(CH2)m-NHCOR34, o -OCH2-CH(OH)-CH2-NHCOR34; R31 representa hidrogeno, metilo, etilo, 1-propilo, 2-propilo, 2-hidroxietilo, 2-hidroxi-1-hidroximetil-etilo, 2-alcoxietiloC1-5, 3-hidroxipropilo, 3-alcoxipropiloC1-5, 2-aminoetilo, 2-(alquilaminoC1-5)etilo, 2-(di-(alquiloC1-5)amino)etilo, carboximetilo, alquiloC1-5-carboximetilo, 2-carboxietilo, o 2-(alquiloC1-5-carboxi)etilo; R32 representa hidrogeno, metilo, o etilo; R33 representa metilo, etilo, propilo, isopropilo, butilo, 2-hidroxietilo, 2-metoxietilo, metilamino, etilamino, propilamino, isopropilamino, n-butilamino, o dimetilamino; R34 representa hidroximetilo, hidroxietilo, aminometilo, metilaminometilo, dimetilaminometilo, aminoetilo, 2-metilamino-etilo, o 2-dimetilamino-etilo; k representa el numero entero 1, 2, o 3; m representa el numero entero 1 o 2; n representa 0, 1, o 2; y R4 representa hidrogeno, alquilo C1-5, o halogeno; y los isomeros de configuracion tales como enantiomeros opticamente puros, mezclas de enantiomeros tales como racematos, diastereomeros, mezclas de diastereomeros, racematos diastereoméricos, y mezclas de racematos diastereoméricos, como también sales y complejos de solventes de dichos compuestos, y formas morfologicas.
ARP060101135A 2005-03-23 2006-03-22 Derivados de tiofeno y composiciones farmaceuticas AR055751A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP2005003070 2005-03-23

Publications (1)

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AR055751A1 true AR055751A1 (es) 2007-09-05

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ARP060101135A AR055751A1 (es) 2005-03-23 2006-03-22 Derivados de tiofeno y composiciones farmaceuticas

Country Status (25)

Country Link
US (1) US7605269B2 (es)
EP (1) EP1863474B1 (es)
JP (1) JP5072825B2 (es)
KR (1) KR20070116645A (es)
CN (1) CN101146529B (es)
AR (1) AR055751A1 (es)
AT (1) ATE413874T1 (es)
AU (1) AU2006226020A1 (es)
BR (1) BRPI0609668A2 (es)
CA (1) CA2602475C (es)
CY (1) CY1108750T1 (es)
DE (1) DE602006003642D1 (es)
DK (1) DK1863474T3 (es)
ES (1) ES2316062T3 (es)
IL (1) IL186150A0 (es)
MX (1) MX2007011672A (es)
NO (1) NO20075298L (es)
NZ (1) NZ562561A (es)
PL (1) PL1863474T3 (es)
PT (1) PT1863474E (es)
RU (1) RU2404178C2 (es)
SI (1) SI1863474T1 (es)
TW (1) TW200700406A (es)
WO (1) WO2006100633A1 (es)
ZA (1) ZA200709087B (es)

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