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AR041186A1 - Moduladores del receptor de glucocorticoides - Google Patents

Moduladores del receptor de glucocorticoides

Info

Publication number
AR041186A1
AR041186A1 ARP030102442A ARP030102442A AR041186A1 AR 041186 A1 AR041186 A1 AR 041186A1 AR P030102442 A ARP030102442 A AR P030102442A AR P030102442 A ARP030102442 A AR P030102442A AR 041186 A1 AR041186 A1 AR 041186A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroaryl
aryl
heterocyclyl
hydrogen
Prior art date
Application number
ARP030102442A
Other languages
English (en)
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 AR041186A1 publication Critical patent/AR041186A1/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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    • 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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  • 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

Estos compuestos son moduladores de los receptores de glucocorticoides y que por lo tanto son útiles para el tratamiento de animales que requieren una terapia con agonistas de los receptores de glucocorticoides. Los moduladores del receptor de glucocorticoides son útiles en el tratamiento de ciertas afecciones inflamatorias. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque A es una de las fórmulas del grupo (2); cada uno de X e Y es independientemente hidrógeno, fluoro, cloro, bromo, o alquilo C1-6; R1 es alquilo C2-6, alquenilo C3-6, o bencilo opcionalmente substituido; donde dicho bencilo puede estar opcionalmente substituido con uno a tres substituyentes seleccionados independientemente entre HO-, alquil C1-6-O-, halo y amino; R2 es alquilo C1-6, alquenilo C2-6, alquinilo C3-6, cicloalquilo C3-10, arilo C6-10, heterociclilo C1-9, heteroarilo C1-9, aril C6-10 alquilo C1-4, heterociclil C1-9-alquilo C1-4, heteroaril C1-9-alquilo C1-4, o cicloalquil C3-10-alquilo C1-4; donde cada uno de los grupos mencionados anteriormente puede estar opcionalmente substituido con uno a tres substituyentes seleccionados independientemente entre halo, alquilo C1-6, alcoxi C1-6, o -CF3; R3 es hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterociclilo C1-9, heteroarilo C1-9, o arilo C6-10; donde cada uno de los grupos mencionados anteriormente puede estar opcionalmente substituido con uno a tres substituyentes seleccionados independientemente entre HO-, alquil C1-6-O-, halo y amino; R4 es HO- o R14R15N-; R5 es un radical seleccionado entre el grupo compuesto por hidrógeno, halo, alquilo C1-6, alquenilo C2-6, alquinilo C3-6, cicloalquilo C3-10, arilo C6-10, heteroarilo C1-9, heterociclilo C1-9, -OH, alquil C1-6-O-, cicloalquil C3-10-O-, aril C6-10-O-, heteroaril C1-9-O-, heterociclil C1-9-O-, cicloalquil C3-10-alquil C1-6-O-, aril C6-10-alquil C1-6-O-, heteroaril C1-9-alquil C1-6-O-, heterociclil C1-9-alquil C1-6-O-, R16R17N-(C=O)-, R16-(C=O)-(R25-N)-, R16R7-N-SO2-, R18-SO2-, R18-SO2-(NR19)-, R18-SO3-, -C:::N, R18-(C-O)-O-, R18-(C-O)-, R16R17N-(C-O)-O-, R16R17N-(C=O)-(R25-N)-, R19-O-(C=O)-(R25-N)-, y R19-O-(C-O)-; donde cada uno de dichos restos alquilo C1-6, cicloalquilo C3-10, arilo C6-10, heteroarilo C1-9, heterociclilo C1-9 de dichos radicales alquilo C1-6, arilo C6-10, heteroarilo C1-9, heterociclilo C1-9, alquil C1-6-O-, cicloalquil C3-10-O-, aril C6-10-O-, heteroaril C1-9-O-, heterociclil C1-9-O-, cicloalquil C3-10-alquil C1-6-O-, aril C6-10-alquil C1-6-O-, heteroaril C1-9-alquil C1-6-O- y heterociclil C1-9-alquil C1-6-O- , puede estar opcionalmente substituido con uno a tres substituyentes seleccionados independientemente entre el grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-10, heteroaril C1-9 (CH2)n-, heterociclilo C1-9, halo, HO-, HO-(C=O)-, R20-O-(C-O)-, R21-(C-O)-, R22-CO2-, NC-, R23R24N-, R23R24N-alquil-, R23R24N-(C=O)-, R23R24-N-SO2-, R21-SO2-, R21-SO2-(NR21)-, R21-SO3-, R21(C=O)-NH-, R21(C=O)-[N-alquil C1-6]-; R21(C=O)-NH-alquil C1-6-; y R21(C=O)-[N-alquil C1-6]-alquil C1-6-; donde dichos substituyentes cicloalquilo C3-10, arilo C6-10, heteroaril C1-9 (CH2)n-, heterociclo C1-9 pueden estar opcionalmente substituidos sobre un carbono o nitrógeno del anillo con uno a tres miembros por anillo seleccionados independientemente entre halo, alquilo C1-6, y alcoxi C1-6; n es un número entero de cero a cuatro; cada uno de R6, R7, R8 y R9 se selecciona independientemente entre el grupo compuesto por hidrógeno, alquilo C1-6, fluoro y -OH; cada uno de R10 y R11 se selecciona independientemente entre el grupo compuesto por hidrógeno y alquilo C1-6; cada uno de R12 y R13 se selecciona entre el grupo compuesto por hidrógeno, fluoro y alquilo C1-6; cada uno de R14 y R15 se selecciona independientemente entre hidrógeno o alquilo C1-4; opcionalmente substituido de R16 y R17 se selecciona independientemente entre hidrógeno, alquilo C1-6, arilo C6-10, heteroarilo C1-9, heterociclilo C1-9, heteroaril C1-9 alquilo C1-6, aril C6-10 alquilo C1-6, heterociclil C1-9 alquilo C1-6, HO-alquilo C1-6, amino-alquilo C1-6, alquilamino C1-6-alquilo C1-6, y [alquil C1-6]2amino-alquilo C1-6; donde cada uno de dichos restos de arilo C6-10, heteroarilo C1-9, y heterociclilo C1-9 de dichos aril C6-10-, heteroaril C1-9-, heterociclo C1-9-, aril C6-10-alquilo C1-6, heteroaril C1-9-alquilo C1-6 y heterociclo C1-9-alquilo C1-6, puede estar opcionalmente substituido con uno a tres substituyentes seleccionados independientemente entre el grupo compuesto por halo, alquilo C1-6 o alcoxi C1-6, o R16 y R17 se toman conjuntamente para formar un anillo de azetidinilo, pirrolidinilo, piperidinilo, piperazinilo, alquil C1-6-piperazinilo, o morfolinilo; R18 es hidrógeno, alquilo C1-6, arilo C6-10 o heteroarilo C1-9; donde dicho alquilo C1-6 puede estar opcionalmente substituido con un substituyente seleccionado entre el grupo compuesto por HO-, amino, alquilamino C1-6, [alquil C1-6]2amino, arilo C6-10, heteroarilo C1-9, heterociclo C1-9, alcoxi C1-6, HO-(C=O)-, alquil C1-6-O-(C=O)-, alquil C1-6-(C-O)-, NC-, [alquil C1-6]2N-(C=O)- y alquil C1-6 (C=O)-NH-; R19 es hidrógeno o alquilo C1-6; R20 es hidrógeno o alquilo C1-6; R21 es hidrógeno o alquilo C1-6; R22 es hidrógeno o alquilo C1-6; cada uno de R23 y R24 se seleccionan independientemente entre hidrógeno, alquilo C1-6, arilo C6-10, heteroarilo C1-9, heterociclilo C1-9, heteroaril C1-9 alquilo C1-6, aril C6-10 alquilo C1-6, heterociclil C1-9 alquilo C1-8, HO-alquilo C1-6, NC-alquilo C1-6, amino-alquilo C1-6, alquilamino C1-6-alquilo C1-6, y [alquil C1-6]2amino-alquilo C1-6; donde cada uno de los restos arilo C6-10, heteroarilo C1-9, y heterociclilo C1-9 de dichos aril C1-6-, heteroaril C1-9-, heterociclil C1-9-, aril C6-10-alquilo C1-6, heteroaril C1-9-alquilo C1-6 y heterociclil C1-9-alquilo C1-6, puede estar opcionalmente substituido con uno a tres substituyentes seleccionados independientemente entre el grupo compuesto por halo, alquilo C1-6 o alcoxi C1-6, o R23 y R24 se toman conjuntamente para formar un anillo de azetidinilo, pirrolidinilo, piperidinilo, piperazinilo, alquil C1-6-piperazinilo, o morfolinilo; R25 es hidrógeno o alquilo C1-6; o una sal farmacéuticamente aceptable del mismo.
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