AR038259A1 - Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p - Google Patents

Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p

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Publication number
AR038259A1
AR038259A1 ARP020104440A ARP020104440A AR038259A1 AR 038259 A1 AR038259 A1 AR 038259A1 AR P020104440 A ARP020104440 A AR P020104440A AR P020104440 A ARP020104440 A AR P020104440A AR 038259 A1 AR038259 A1 AR 038259A1
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AR
Argentina
Prior art keywords
heterocycloalkyl
substituted
heteroaryl
pyrazine
aryl
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ARP020104440A
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English (en)
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Upjohn Co
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Publication date
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Publication of AR038259A1 publication Critical patent/AR038259A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/18—Oxygen or sulfur atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/575—Hormones
    • G01N2333/5751—Corticotropin releasing factor [CRF] (Urotensin)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/02—Screening involving studying the effect of compounds C on the interaction between interacting molecules A and B (e.g. A = enzyme and B = substrate for A, or A = receptor and B = ligand for the receptor)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S206/00—Special receptacle or package
    • Y10S206/828—Medicinal content

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto que comprende un derivado sustituido de aril-1,4-pirazina de fórmula (1) o un estereoisómero de dicha fórmula, una sal farmacéuticamente aceptable de dicha fórmula, ó un profármaco de dicha fórmula, en donde en la fórmula (1): X se selecciona entre NR3R4, -OR3, -CR3R5R5, -C(O)R3,-S(O)mR3, -NR3C(O)R4, -NR3S(O)mR4, m es 0, 1 ó 2; Ar se selecciona entre arilo, arilo sustituido, heteroarilo, heteroarilo sustituido; R1, R2 y R5 se seleccionan independientemente entre halógeno, -NO2, -CN, -Ra, -ORa, -S(O)mRa, -NRaRa, -C(O)NRaRa, -C(S)NRaRa-S(O)mNRaRa,-NRaS(O)mRa, -NRaC(O)ORa, -OC(O)NRaRa, -NRaC(O)NRaRa, -NRaC(S)NRaRa, -C(O)ORa, -C(S)ORa, y -OC(O)ORa; R3 y R4 se seleccionan independientemente entre Ra, heterocicloalquilo, heterocicloalquilo sustituido, heteroarilo sustituido, arilo sustituido, aril-cicloalquilo, aril-cicloalquilo sustituido, heteroaril-cicloalquilo, heteroaril-cicloalquilo sustituido, aril-heterocicloalquilo, aril-heterocicloalquilo sustituido, heteroaril-heterocicloalquilo, ó heteroaril-heterocicloalquilo sustituido siempre que por lo menos uno entre R3 ó R4 sea heteroarilo, heteroarilo sustituido, aril-cicloalquilo, aril-cicloalquilo sustituido, heteroaril-cicloalquilo, heteroaril-cicloalquilo sustituido, aril-heterocicloalquilo, aril-heterocicloalquilo sustituido, heteroaril-heterocicloalquilo, heteroaril-heterocicloalquilo sustituido, heterocicloalquilo ó heterocicloalquilo sustituido; cada Ra se selecciona entre H, alquilo, cicloalquilo, haloalquilo, arilo, heteroarilo, ó heterocicloalquilo opcionalmente sustituido con 1 a 5 de Rt, -ORt, -S(O)mRt, NRtRt, oxo(=O), tiona (=S), fenilo, heteroarilo, ó heterocicloalquilo en donde fenilo, heteroarilo, y heterocicloalquilo están opcionalmente sustituidos con 1 a 5 grupos seleccionados independientemente entre Rt; y cada Rt se selecciona entre H, halógeno, -NO2, -NH2, -OH, -SH, -CN, -C(O)NH2, -C(O)-NH alquilo, -C(O)N alquilalquilo, -O alquilo, NH alquilo, Nalquilalquilo, -S(O)malquilo, SO2NH2, SO2NHalquilo y SO2N alquilalquilo, alquilo, cicloalquilo, haloalquilo, fenilo, bencilo, heteroarilo, ó heterocicloalquilo en donde fenilo, bencil-heteroarilo y heterocicloalquilo pueden estar opcionalmente sustituidos con alquilo o halógeno, siempre que el compuesto no sea: 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-metilpiperidin-4-il)oxi]pirazina; 2,5-dimetil-3-(2,4-diclorofenil)-6-(tetrahidrofuran-3-il)oxi]pirazina; 2,5-dimetil-3-(2,4-diclorofenil)-6-(tetrahidro-2H-piran-4-iloxi)pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-metilpiperidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[1-etilpiperdin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-(1-piperidin-4-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-piperidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-etilpirrolidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-metilpirrolidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(pirrolidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(piridin-4-il)oxi]pirazina. También se dan a conocer composiciones farmacéuticas que los contienen, su uso para la elaboración de medicamentos, artículo de fabricación que los comprende, método para inhibir la unión del CRF al receptor CRF1, método para clasificar ligandos de receptores del CRF y método para detectar receptores del CRF en tejidos. Estos compuestos son útiles para la elaboración de medicamentos útiles para el tratamiento de trastornos de ansiedad, depresión y trastornos relacionados con el estrés.
ARP020104440A 2001-11-21 2002-11-19 Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p AR038259A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US33205201P 2001-11-21 2001-11-21
US35854602P 2002-02-21 2002-02-21
US38828502P 2002-06-13 2002-06-13
US41037802P 2002-09-13 2002-09-13

Publications (1)

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AR038259A1 true AR038259A1 (es) 2005-01-12

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ARP020104440A AR038259A1 (es) 2001-11-21 2002-11-19 Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p

Country Status (4)

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US (2) US6992087B2 (es)
AR (1) AR038259A1 (es)
MY (1) MY130489A (es)
TW (1) TWI292758B (es)

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