HUP0104390A2 - Alfa-2B vagy alfa-2B/2C adrenerg receptorokra nézve szelektív agonista aktivitással rendelkező imidazolszármazékok és alkalmazásuk - Google Patents

Alfa-2B vagy alfa-2B/2C adrenerg receptorokra nézve szelektív agonista aktivitással rendelkező imidazolszármazékok és alkalmazásuk

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Publication number
HUP0104390A2
HUP0104390A2 HU0104390A HUP0104390A HUP0104390A2 HU P0104390 A2 HUP0104390 A2 HU P0104390A2 HU 0104390 A HU0104390 A HU 0104390A HU P0104390 A HUP0104390 A HU P0104390A HU P0104390 A2 HUP0104390 A2 HU P0104390A2
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Hungary
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group
alpha
formula
atom
alkyl
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HU0104390A
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Inventor
James A. Burke
Ken Chow
Michael E. Garst
Daniel W. Gil
Dale A. Harcourt
Stephen A. Munk
Larry A. Wheeler
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Allergan Sales, Inc.
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Publication of HUP0104390A2 publication Critical patent/HUP0104390A2/hu
Publication of HUP0104390A3 publication Critical patent/HUP0104390A3/hu

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • 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
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/06Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
    • C07D233/08Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms
    • C07D233/10Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/84Sulfur atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/28Nitrogen atoms not forming part of a nitro radical
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • C07D405/00Heterocyclic 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
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    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • 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
    • C07D413/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A tal lm ny (I) ltal nos képletű vegyületekre vonatkozik. A képletben- adott esetben jelenlevő kettősk"tést képvisel, R jelentésehidrogénatom vagy alkilcsoport, X jelentése kénatom vagy C(H)R1 ltalnos képletű csoport, ahol R1 jelentése hidrogénatom vagy alkilcsoport,Y jelentése oxigén-, nitrogén- vagy kénatom, (CR12)y ltal nos képletűcsoport, ahol y értéke 1-3, -CH=CH- vagy -Y1CH2- ltal nos képletűcsoport, ahol Y1 jelentése oxigén-, nitrogén- vagy kénatom, x értéke 1vagy 2, bizonyos megk"tésekkel R2 jelentése hidrogén- vagyhalogénatom, hidroxil-, alkil-, alkoxi-, alkenil-, acil-,alkinilcsoport vagy amennyiben egy telített szénatomhoz kapcsolódik,akkor oxocsoport, R3 és R4 jelentése hidrogén- vagy halogénatom,alkil-, alkenil-, acil-, alkinilcsoport, adott esetben helyettesítettarilcsoport, heteroarilcsoport, vagy pedig együttesen[C(R2)x]z-; -Y1[C(R2)x]z'-; -Y1[C(R2)x]yY1-; -[C(R2)x]-Y1[C(R2)x]-; -[C(R2)x]-Y1-[C(R2)x]-vagy -Y1-[C(R2)x]-Y1-[C(R2)x]- ltal nos képletű csoportotképviselnek, tov bb az említett kétértékű csoportok b rmelyik végekapcsolódhat R3 vagy R4 szubsztituens b rmelyikéhez, és így egykondenz lt gyűrűrendszert alkothat. A vegyületek szelektív agonistaaktivit ssal rendelkeznek "nmag ban az alfa-2B adrenerg receptoraltípusokra, vagy pedig az alfa-2B és alfa-2C adrenerg receptoraltípusokra nézve, így olyan gyógyszerkészítmények hatóanyagakéntalkalmazhatók, amelyek glaukoma, szemen belüli nyom s cs"kkentése,krónikus f jdalom, hasmenés és orrvérzés, tov bb izomg"rcs"k, megvonsi tünetek, f jdalmak, neuro- degeneratív betegségek, félelmet,depressziót, magas vérnyom s, vértolul sos szívelégtelenség ésszíviszkémia kezelésére és megelőzésére alkalmazhatók, anélkül, hogyszedatív vagy kardiovaszkul ris mellékhat sokat okozn nak. Ó
HU0104390A 1999-06-10 2000-06-08 Imidazole derivatives as selective agonists at alpha 2b or 2b/2c adrenergic receptors HUP0104390A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32975299A 1999-06-10 1999-06-10
PCT/US2000/015795 WO2001000586A1 (en) 1999-06-10 2000-06-08 Compounds as selective agonists at alpha 2b or 2b/2c adrenergic receptors

Publications (2)

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HUP0104390A2 true HUP0104390A2 (hu) 2002-04-29
HUP0104390A3 HUP0104390A3 (en) 2002-05-28

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HU0104390A HUP0104390A3 (en) 1999-06-10 2000-06-08 Imidazole derivatives as selective agonists at alpha 2b or 2b/2c adrenergic receptors

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EP (1) EP1104407B1 (hu)
AT (1) ATE283843T1 (hu)
AU (1) AU773668B2 (hu)
CZ (1) CZ2001864A3 (hu)
DE (1) DE60016359T2 (hu)
ES (1) ES2228544T3 (hu)
HK (1) HK1035724A1 (hu)
HU (1) HUP0104390A3 (hu)
RU (1) RU2232154C2 (hu)
TW (1) TWI283669B (hu)
WO (1) WO2001000586A1 (hu)

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HK1035724A1 (en) 2001-12-07
HUP0104390A3 (en) 2002-05-28
AU5474900A (en) 2001-01-31
ES2228544T3 (es) 2005-04-16
EP1104407B1 (en) 2004-12-01
ATE283843T1 (de) 2004-12-15
RU2232154C2 (ru) 2004-07-10
EP1104407A1 (en) 2001-06-06
CZ2001864A3 (cs) 2001-09-12
TWI283669B (en) 2007-07-11
DE60016359T2 (de) 2005-12-01
WO2001000586A1 (en) 2001-01-04
DE60016359D1 (de) 2005-01-05
AU773668B2 (en) 2004-06-03

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