ES2333802T3 - Inhibidores no nucleicos de transcriptasa inversa. - Google Patents

Inhibidores no nucleicos de transcriptasa inversa. Download PDF

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Publication number
ES2333802T3
ES2333802T3 ES05742851T ES05742851T ES2333802T3 ES 2333802 T3 ES2333802 T3 ES 2333802T3 ES 05742851 T ES05742851 T ES 05742851T ES 05742851 T ES05742851 T ES 05742851T ES 2333802 T3 ES2333802 T3 ES 2333802T3
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alkyl
group
optionally substituted
alkoxy
halogen
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James Patrick Dunn
Donald Roy Hirschfeld
Tania Silva
Harit Vora
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F Hoffmann La Roche AG
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    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
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    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • C07C233/07—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
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    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/46—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms
    • C07C323/49—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to sulfur atoms
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    • C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
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    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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  • Plural Heterocyclic Compounds (AREA)

Abstract

Uso de compuestos de la fórmula I **(Ver fórmula)** en la que X1 se elige entre el grupo formado por -O-, -S-, -CH2- y -C(O)-; R1 y R2 con independencia entre sí se eligen entre el grupo formado por hidrógeno, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, alquiltio C1-6, alquilsulfinilo C1-6, sulfonilo C1-6, haloalcoxi C1-6, haloalquiltio C1-6, halógeno, amino, alquilamino, dialquilamino, acilamino, nitro y ciano; o R1 y R2, juntos, son -OCH= CH- u -O-CH2CH2-; R3 y R4 con independencia entre sí se eligen entre el grupo formado por hidrógeno, alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquiltio C1-6, haloalquiltio C1-6, halógeno, amino, nitro y ciano; R5 se elige entre el grupo formado por alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, arilo o heteroarilo elegido entre el grupo formado por piridinilo, N-hidroxipiridina, pirimidinilo, indol, pirazinilo y pirrolilo; en el que, dicho arilo y dicho heteroarilo están opcionalmente sustituidos de una a tres veces por sustituyentes elegidos con independencia entre sí entre el grupo formado por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, alquiltio C1-6, alquilsulfinilo C1-6, sulfonilo C1-6, haloalcoxi C1-6, haloalquiltio C1-6, hidroxi, halógeno, amino, alquilamino C1-6, di(alquil C1-6)amino, acilamino, acilo, (alcoxi C1-6)-carbonilo, carbamoílo, N-(alquil C1-6)-carbamoílo, N,N-di(alquil C1-6)-carbamoílo, alquinol, -CCCH2OH, -CCCH2N(CH3)2, nitro y ciano, dicho alquilo y dicho cicloalquilo están opcionalmente sustituidos por uno o dos sustituyentes elegidos con independencia entre sí entre el grupo formado por alquilo, hidroxi, alcoxi, tiol, alquiltio, halógeno, amino, alquilamino, dialquilamino, aminoalquilo, alquilaminoalquilo y dialquilamino; Ar es fenilo opcionalmente sustituido por 1-3 sustituyentes elegidos con independencia entre sí en cada caso entre el grupo formado por alquilo C1-6, cicloalquilo C3-8, haloalquilo C1-3, alcoxi C1-6, haloalcoxi C1-6, halógeno, ciano, alquiltio C1-6, alquilsulfinilo C1-6, sulfonilo C1-6, aminoalquilsulfonilo C1-6, haloalcoxi C1-6, haloalquiltio C1-6, acilo C1-6, nitro, heteroalquilo C1-6, heteroalcoxi C1-6, hidroxilo, -X2(CH2)p S(O)nNR8R9; -(CH2)pCOOR11, -X2(CH2)pNHC(O)NHR8R9, X2(CH2)pCONR8R9, -SO2R13, -NR8aR9a, X2 (CH2)pNR11S(O)2NR8R9, -X2(CH2)pNHCOOR10, -X6(CH2)pCOOR10, -X2(CH2)pCN, -OR15 y C(=O)CH2 N[(CH2)2]2X4; o, un anillo heteroarilo seleccionado del grupo constituido por piridinilo, N-óxido de piridina, piridacinilo, pirimidilo, piracilo, triacinilo, pirrolilo, pirazolilo, imidazolilo, (1,2,3)- y (1,2,4-triazolilo, piracinilo, pirimidinilo, tetrazolilo, furilo, tienilo, isoxazolilo, tiazolilo, tienilo, isoxazolilo, indol, N-óxido de indol, quinolina, N-óxido de quinolina y oxazolilo estando dicho anillo de heteroarilo opcionalmente sustituido con uno a tres sustituyentes seleccionados del grupo constituido por alquilo C1-6, alcoxi C1-6, alquiltio C1-6, halógeno, aminoacilo C1-6, ciano y NR8bR9b; R8 y R9 tomados con independencia entre sí, uno de R8 y R9 es hidrógeno o alquilo C1-6 y el otro de R8 y R9 y se elige entre el grupo formado por hidrógeno, -C(=O)R14, -C(=O)CHR12NH2, -(CH2)2N[(CH2)2]2O, COCO2Me, cicloalquilo C3-8, dicho cicloalquilo está opcionalmente sustituido por uno o dos sustituyentes hidroxilo, piranilo, alquilo C1-6 o arilo, dichos grupos alquilo y dichos grupos arilo están opcionalmente sustituidos por uno o dos sustituyentes elegidos con independencia entre sí entre el grupo formado por hidroxi, alcoxi C1-6, tiol, alquiltio C1-6, alquilsulfinilo C1-6, sulfonilo C1-6 y halógeno; o, (ii) R8 y R9, juntos, son (CH2)2-X5- (CH2)2 o -(CH2)o- opcionalmente sustituido por uno o dos sustituyentes elegidos entre el grupo formado por halógeno, hidroxilo y NR11aR11b; R8a y R9a con independencia entre sí se eligen entre el grupo formado por hidrógeno, alquilo C1-6, C(=O)CO2R11 y SO2R10 o (ii), juntos, son (CH2)rSO2 o (CH2)2S(O)p(CH2)2; R10 es alquilo C1-6; R11 es hidrógeno o alquilo C1-6; R11a, R11b y R11c con independencia entre sí son R11; R12 es la cadena lateral de un -aminoácido de origen natural; R13 es alquilo C1-6; -(CH2)sCO2R11, -(CH2)2CN, -(CH2)2NH2 o -(CH2)uOH; R14 es alquilo C1-6, -(CH2)sNHR11aR11b, (CH2)sOR11, -CH2CH(OH)CH3, CH2N[(CH2)2]2O, -(CH2)2CO2R11, fenilo o piridinilo opcionalmente sustituidos; R15 es alquilo C1-6 opcionalmente sustituido de una a tres veces por grupos hidroxilo; X2 es -O- o un enlace; X4 es -O- o -NMe-; X5 es -O-, -S(O)n- o NR11; X6 es O- o -S(O)n-; n es un número entero de 0 a 2; o es un número entero de 4 a 6; p es un número entero de 0 a 6; r es un número entero de 3 a 4; s es un número entero de 1 a 2; u es un número entero de 2 a 3; y, y de los hidratos, solvatos y sales de los mismos; para la fabricación de un medicamento destinado a tratar una infección de VIH o a prevenir una infección de VIH o a tratar el SIDA o el ARC.
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