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AR047050A1 - Derivados de 1,3 diazol como inhibidores de aspartilproteasa. composiciones farmacéuticas - Google Patents

Derivados de 1,3 diazol como inhibidores de aspartilproteasa. composiciones farmacéuticas

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Publication number
AR047050A1
AR047050A1 ARP040104647A ARP040104647A AR047050A1 AR 047050 A1 AR047050 A1 AR 047050A1 AR P040104647 A ARP040104647 A AR P040104647A AR P040104647 A ARP040104647 A AR P040104647A AR 047050 A1 AR047050 A1 AR 047050A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
arylalkyl
group
heteroaryl
Prior art date
Application number
ARP040104647A
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English (en)
Original Assignee
Schering Corp
Pharmacopeia Drug Discovery
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Publication date
Application filed by Schering Corp, Pharmacopeia Drug Discovery filed Critical Schering Corp
Publication of AR047050A1 publication Critical patent/AR047050A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/66—Heterocyclic 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
    • C07D233/88—Nitrogen atoms, e.g. allantoin
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P33/06—Antimalarials
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
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Abstract

Derivados de 1,3-diazol como inhibidores de aspartilproteasa y composiciones farmacéuticas. Reivindicacion 1: Un compuesto que tiene la formula estructural (1) o un estereoisomero, tautomero, o sal o solvato del mismo farmacéuticamente aceptable, donde W es un enlace, -C(=S)-, -S(O)-, -S(O)2-, -C(=O)-, -O-, -C(R6)(R7)-, -N(R5)- o -C(=N(R5))-; X es -O-, -N(R5)- o -C(R6)(R7)-; con la condicion de que cuando X es -O-, U no sea -O-, -S(O)-, -S(O)2-, -C(=O)- o -C(=NR5)-, U es un enlace, -S(O)-, - S(O)2-, -C(O)-, -O-, -P(O)(OR15)-, -C(=NR5)-, -(C(R6)(R7))b- o -N(R5)-; donde b es 1 o 2; con la condicion de que cuando W es -S(O)-, -S(O)2-, -O-, o -N(R5)-, U no sea -S(O)-, -S(O)2-, -O-, o -N(R5)-; con la condicion de que cuando X es -N(R5)- y W es -S(O)-, -S(O)2-, -O- o -N(R5)-, entonces U no sea un enlace; R1, R2 y R5 están independientemente seleccionados del grupo que consiste en H, alquilo, alquenilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, -OR15, -CN, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -NO2, -N=C(R8)2 y -N(R8)2, con la condicion de que R1 y R5 no estén ambos seleccionados de NO2, -N=C(R8)2 y -N(R8)2; R3, R4, R6 y R7 están independientemente seleccionados del grupo que consiste en H, alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halo, -CH2-O-Si(R9)(R10)(R19), -SH, -CN, -OR9, -C(O)R8, -C(O)OR9, -C(O)N(R11)(R12), -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)C(O)N(R12)(R13), -N(R11)C(O)OR9 y - C(=NOH)R8, con la condicion de que cuando U es -O- o -N(R5)-, entonces R6 y R7 no sean halo, -SH, -OR9, -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)C(O)N(R12)(R13) o -N(R11)C(O)OR9; con la condicion de que cuando W es -O- o -N(R5), entonces R3 y R4 no sean halo, -SH, -OR9, -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)C(O)N(R12)(R13) o -N(R11)C(O)OR9; y con la condicion de que X es - N(R5)-, W es -C(O)- y U es un enlace, R3, R4, R6 y R7 no sean halo, -CN, -SH, -OR9, -SR19, -S(O)N(R11)(R12), o -S(O)2N(R11)(R12), o R3, R4, R6 y R7, conjuntamente con el C al cual están unidos, forman un grupo cicloalquilo de 3-7 miembros opcionalmente sustituido con R14 o un éter cicloalquílico de 3-7 miembros opcionalmente sustituido con R14; o R3 y R4 o R6 y R7 conjuntamente con el C al cual están unidos se combinan para formar grupos multicíclicos seleccionados del grupo de formulas (2), donde M es -CH2-, S, -N(R19)- u O, A y B son independientemente arilo o heteroarilo y q es 0, 1 o 2 con la condicion de que q es 2, una M debe ser un átomo de C y cuando q es 2, M es opcionalmente un doble enlace; y con la condicion de que cuando R3, R4, R6 y R7 forman dichos grupos multicíclicos del grupo de formulas (2), entonces los grupos R3 y R4 o R6 y R7 adyacentes no pueden estar combinados para formar dichos grupos multicíclicos; R8 está independientemente seleccionado del grupo que consiste en H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, -OR15, -N(R15)(R16), -N(R15)C(O)R16, - N(R15)S(O)R16, -N(R15)S(O)2R16, -N(R15)S(O)2(R16)(R17), -N(R15)S(O)N(R16)(R17), -N(R15)C(O)N(R16)(R17) y -N(R15)C(O)OR16; R9 está independientemente seleccionado del grupo que consiste en H, alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo y heteroarilalquilo; R10 está independientemente seleccionado del grupo que consiste en H, alquilo, alquenilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo y -N(R15)(R16); R11, R12 y R13 están independientemente seleccionados del grupo que consiste en H, alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R15)(R16), -S(O)N(R15)(R16), -S(O)2N(R15)(R16) y -CN; R14 representa 1-5 sustituyentes independientemente seleccionados del grupo que consiste en alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halo, -CN, - OR15, -C(O)R15, -C(O)OR15, -C(O)N(R15)(R16), -SR15, S(O)N(R15)(R16), -S(O)2N(R15)(R16), -C(=NOR15)R16, -P(O)(OR15)(OR16), -N(R15)(R16), -N(R15)C(O)R16, -N(R15)S(O)R16, -N(R15)S(O)2(R16), -N(R15)S(O)2N(R16)(R17), -N(R15)S(O)N(R16)(R17), - N(R15)C(O)N(R16)(R17) y -N(R15)C(O)OR16; R15, R16 y R17 están independientemente seleccionados del grupo que consiste en H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, arilheterocicloalquilo, R18-alquilo, R18-cicloalquilo, R18-cicloalquilalquilo, R18-heterocicloalquilo, R18-heterocicloalquilalquilo, R18-arilo, R18-arilalquilo, R18-heteroarilo y R18- heteroarilalquilo; o R15, R16 y R17 son compuestos seleccionados del grupo de formulas (3), donde R23 es 0 a 5 sustituyentes, m es 0 a 6 y n es 1 a 5; R18 representa 1-5 sustituyentes independientemente seleccionados del grupo que consiste en alquilo, alquenilo, arilo, arilalquilo, arilalquenilo, arilalquinilo, -NO2, halo, heteroarilo, HO-alcoxialquilo, -CF3, -CN, alquilo-CN, -C(O)R19, -C(O)OH, -C(O)OR19, -C(O)NHR20, -C(O)NH2, -C(O)NH2-C(O)N(alquilo)2, -C(O)N(alquilo)(arilo), - C(O)N(alquilo)(heteroarilo), -SR19, -S(O)2R20, -S(O)NH2, -S(O)NH(alquilo), S(O)N(alquilo)(alquilo), -S(O)NH(arilo), -S(O)2NH2, -S(O)2NHR19, -S(O)2NH(heterocicloalquilo), -S(O)2N(alquilo)2, -S(O)2N(alquilo)(arilo), -OCF3, -OH, -OR20, -O- heterocicloalquilo, -O-cicloalquilalquilo, -O-heterocicloalquilalquilo, -NH2, -NHR20, -N(alquilo)2, -N(arilalquilo)2, -N(arilalquilo)-(heteroarilalquilo), -NHC(O)R20, -NHC(O)NH2, -NHC(O)NH(alquilo), -NHC(O)N(alquilo)(alquilo), - N(alquilo)C(O)NH(alquilo), -N(alquilo)C(O)N(alquilo)(alquilo), -NHS(O)2R20, -NHS(O)2NH(alquilo), -NHS(O)2N(alquilo)(alquilo), -N(alquilo)S(O)2NH(alquilo) y -N(alquilo)S(O)2N(alquilo)(alquilo); o dos porciones R18 en C adyacentes pueden estar ligadas conjuntamente para formar los restos del grupo de formulas (4); R19 es alquilo, cicloalquilo, arilo, arilalquilo o heteroarilalquilo; R20 es alquilo, cicloalquilo, arilo, arilo sustituido con halo, arilalquilo, heteroarilo, o heteroarilalquilo; y donde cada uno de los grupos alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, alquenilo y alquinilo en R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 y R14 están independientemente no sustituidos o están sustituidos con 1 a 5 grupos R21 independientemente seleccionados del grupo que consiste en alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halo, -CN, -OR15, -C(O)R15, -C(O)OR15, -C(O)N(R15)(R16), -SR15, S(O)N(R15)(R16), -CH(R15)(R16), -S(O)2N(R15)(R16), -C(=NOR15)R16, -P(O)(OR15)(OR16), -N(R15)(R16), -alquilo- N(R15)(R16), -N(R15)C(O)R16, -CH2-N(R15)C(O)R16, -CH2-N(R15)C(O)N(R16)(R17), -CH2-R15, -CH2N(R15)(R16), -N(R15)S(O)R16, -N(R15)S(O)2R16, -CH2-N(R15)S(O)2R16, -N(R15)S(O)2N(R16)(R17), -N(R15)S(O)N(R16)(R17), -N(R15)C(O)N(R16)(R17), -CH2- N(R15)C(O)N(R16)(R17), -N(R15)C(O)OR16, -CH2-N(R15)C(O)OR16, -S(O)R15, =NOR15, -N3, -NO2 y -S(O)2R15; y cada uno de los grupos alquilo, cicloalquenilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, alquenilo y alquinilo en R21 están independientemente no sustituidos o sustituidos con 1 a 5 grupos R22 independientemente seleccionados del grupo que consiste en alquilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, arilo, heteroarilo, halo, -CF3, -CN, -OR15, -C(O)R15, -C(O)OR15, -alquilo-C(O)OR15, -C(O)N(R15)(R16), -SR15, S(O)N(R15)(R16), -S(O)2N(R15)(R16), -C(=NOR15)R16, -P(O)(OR15)(OR16), -N(R15)(R16), -alquilo-N(R15)(R16), - N(R15)C(O)R16, -CH2-N(R15)C(O)R16, -N(R15)S(O)R16, -N(R15)S(O)2R16, -CH2-N(R15)S(O)2R16, -N(R15)S(O)2N(R16)(R17), -N(R15)S(O)N(R16)(R17), -N(R15)C(O)N(R16)(R17), -CH2-N(R15)C(O)N(R16)(R17), -N(R15)C(O)OR16, -CH2-N(R15)C(O)OR16, -N3, =NOR15, -NO2, - S(O)R15 y -S(O)2R15; o dos porciones R21 o dos porciones R22 en C adyacentes pueden estar ligadas conjuntamente para formar los restos del grupo de formulas (4); y cuando R21 o R22 están seleccionados del grupo que consiste en -C(=NOR15)R16, - N(R15)C(O)R16, -CH2-N(R15)C(O)R16, -N(R15)S(O)R16, -N(R15)S(O)2R16, -CH2-N(R15)S(O)2R16, -N(R15)S(O)2N(R16)(R17), -N(R15)S(O)N(R16)(R17), -N(R15)C(O)N(R16)(R17), -CH2-N(R15)C(O)N(R16)(R17), -N(R15)C(O)OR16, y -CH2-N(R15)C(O)OR16, R15 y R16 conjuntamente pueden ser una cadena C2 a C4 en la cual opcionalmente, uno, dos, o tres C del anillo pueden ser reemplazados con -C(O)- o -N(H)- y R15 y R16, conjuntamente con los átomos a los cuales están unidos, forman un anillo de 5 a 7 miembros, opcionalmente sustituido con R23; R23 representa 1 a 5 grupos independientemente seleccionados del grupo que consiste en alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halo, -CN, -OR24, -C(O)R24, -C(O)OR24, -C(O)N(R24)(R25), -SR24, S(O)N(R24)(R25), -S(O)2N(R24)(R25), -C(=NOR24)R25, -P(O)(OR24)(OR25), -N(R24)(R25), -alquilo-N(R24)(R25), -N(R24)C(O)R25, -CH2- N(R24)C(O)
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