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PE20040650A1 - Moduladores del receptor de glucocorticoides - Google Patents

Moduladores del receptor de glucocorticoides

Info

Publication number
PE20040650A1
PE20040650A1 PE2003000681A PE2003000681A PE20040650A1 PE 20040650 A1 PE20040650 A1 PE 20040650A1 PE 2003000681 A PE2003000681 A PE 2003000681A PE 2003000681 A PE2003000681 A PE 2003000681A PE 20040650 A1 PE20040650 A1 PE 20040650A1
Authority
PE
Peru
Prior art keywords
alkyl
ethyl
receptor modulators
glucocorticoid receptor
inyl
Prior art date
Application number
PE2003000681A
Other languages
English (en)
Inventor
Yves Andre Chantigny
Edward Fox Kleinman
Ralph P Robinson
Original Assignee
Pfizer Prod 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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of PE20040650A1 publication Critical patent/PE20040650A1/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
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    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61P35/00—Antineoplastic agents
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    • C07C255/13—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound oxygen atoms bound to the same saturated acyclic carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
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    • C07C255/29—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton containing cyano groups and acylated amino groups bound to the carbon skeleton
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    • C07C271/52—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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    • C07C35/42—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system with a hydroxy group on a condensed system having three rings derived from the phenanthrene skeleton
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  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE A ES -CR6R7-CR8R9-, -C=O-CR10R11-, ENTRE OTROS; X E Y SON CADA UNO H, F, ALQUILO C1-C6, ENTRE OTROS; R1 ES ALQUILO C2-C6, ALQUENILO C3-C6, BENCILO; R2 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C3-C6, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R4 ES HO-, R14R15N-; R5 ES H, HALO, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R6, R7, R8 Y R9 SON CADA UNO H, ALQUILO C1-C6, -F, -OH; R10 Y R11 SON CADA UNO H O ALQUILO C1-C6; R14 Y R15 SON CADA UNO H, ALQUILO C1-C4. SON COMPUESTOS PREFERIDOS: (2R,3S,4aR,10aR)-4a-ETIL-2-PROP-1-INIL-1,2,3,4,4a,9,10,10a-OCTAHIDROFENANTRENO-2,3,7-TRIOL; (2R,3S,4aR,10aR)-4a-ETIL-7-(2-METILPIRIDIN-3-ILMETOXI)-2-PROP-1-INIL-1,2,3,4,4a,9,10,10a-OCTAHIDROFENANTRENO-2,3-DIOL Y (2R,3R,4aR,10aR)-4a-ETIL-3-METIL-2-PROPENIL-1,2,3,4,4a,9,10,10a-OCTAHIDROFENANTRENO-2,3,7-TRIOL. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LOS RECEPTORES DE GLUCOCORTICOIDES UTILES EN EL TRATAMIENTO DE TRASTORNOS INFLAMATORIOS,ENDOCRINOS, ENTRE OTRAS
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