AR082665A1 - Derivados heteroarilicos inhibidores de quinasas pi3k, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos proliferativos, inflamatorios y/o cardiovasculares - Google Patents

Derivados heteroarilicos inhibidores de quinasas pi3k, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos proliferativos, inflamatorios y/o cardiovasculares

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Publication number
AR082665A1
AR082665A1 ARP110102929A ARP110102929A AR082665A1 AR 082665 A1 AR082665 A1 AR 082665A1 AR P110102929 A ARP110102929 A AR P110102929A AR P110102929 A ARP110102929 A AR P110102929A AR 082665 A1 AR082665 A1 AR 082665A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
membered
nitrogen
sulfur
oxygen
Prior art date
Application number
ARP110102929A
Other languages
English (en)
Inventor
Zhan Shi
Masaaki Hirose
Hong Myung Lee
Todd B Sells
Yongbo Hu
Stepan Vyskocil
Zhigen Hu
Tianlin Xu
Brian S Freeze
Original Assignee
Millennium Pharm 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45567940&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR082665(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of AR082665A1 publication Critical patent/AR082665A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto de formula (1) ó (2), o una sal aceptable para uso farmacéutico del mismo, donde: Z es S o Se; R1 es CY, -C(O)N(R3)2, -C(O)OR3, -C(O)(NH)OH, -C(=NH)NHOH, -C(O)NR3N(R3)2, -C(=N-NH2)NH2, -C(=N)N(R3)2, donde CY es un resto de fórmula (3); donde: G2 es -N=, =N-, o -N(R3’)-, donde cada aparición de R3 y R3’ es independientemente hidrógeno o un alifático C1-6 opcionalmente sustituido, donde X1, X2, y X3, son cada uno de ellos independientemente N, NR3’, O, S, o CR4, siempre que sólo uno de X1, X2, o X3 pueda ser O, S, o NR3’; cada aparición de R4 es independientemente hidrógeno, -CN, halógeno, -Z3-R6, o un grupo opcionalmente sustituido seleccionado de alifático C1-6, o cicloalifático de 3 a 10 miembros, donde: Z3 se selecciona de una cadena de alquileno C1-3 opcionalmente sustituido, -O-, -N(R4a)-, -S-, -S(O)-, -S(O)2, -C(O)-, -CO2-, -C(O)NR4a-, -N(R4a)C(O)-, -N(R4a)CO2-, -S(O)2NR4a-, -N(R4a)S(O)2-, -OC(O)N(R4a)-, -N(R4a)C(O)NR4a-, -N(R4a)S(O)2N(R4a)-, o -OC(O)-; R4a es hidrógeno o un alifático C1-4 opcionalmente sustituido, y R6 es hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C1-6, cicloalifático de 3 a 10 miembros, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; o donde dos apariciones adyacentes de R3’ o R4, tomados juntos con el átomo al cual están unidos, forman un grupo fusionado opcionalmente sustituido seleccionado de arilo de 5 a 6 miembros, o heteroarilo de 5 a 6 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno o azufre; el anillo A es un grupo seleccionado de cicloalifático de 3 a 10 miembros, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos seleccionados de nitrógeno, oxígeno, o azufre; cada aparición de R2 es independientemente -R12a, -T2-R12d, -V2-T2-R12d, y: cada aparición de R12a es independientemente halógeno, -CN, -NO2, -R12c, -N(R12b)2, -OR12b, -SR12c, -S(O)2R12c, -C(O)R12b, -C(O)OR12b, -C(O)N(R12b)2, -S(O)2N(R12b)2, -OC(O)N(R12b)2, -N(R12e)C(O)R12b, -N(R12e)SO2R12c, -N(R12e)C(O)OR12b, -N(R12e)C(O)N(R12b)2, o -N(R12e)SO2N(R12b)2, o dos apariciones de R12b, tomadas juntas con un átomo de nitrógeno al cual están unidas, forman un anillo heterociclilo de 4 a 7 miembros opcionalmente sustituido que tiene 0 a 1 heteroátomo adicional seleccionado de nitrógeno, oxigeno, o azufre; cada aparición de R12b es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C1-6, cicloalifático de 3 a 10 miembros, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; cada aparición de R12c es independientemente un grupo opcionalmente sustituido seleccionado de alifático C1-6, cicloalifático de 3 a 10 miembros, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; cada aparición de R12d es independientemente hidrógeno o un cicloalifático de 3 a 10 miembros opcionalmente sustituido, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; cada aparición de R12e es independientemente hidrógeno o un grupo alifático C1-6 opcionalmente sustituido; cada aparición de V2 es independientemente -N(R12e)-, -O-, -S-, -S(O)-, -S(O)2-, -C(O)-, -C(O)O-, -C(O)N(R12e)-, -S(O)2N(R12e)-, -OC(O)N(R12e)-, -N(R12e)C(O)-, -N(R12e)SO2-, -N(R12e)C(O)O-, -N(R12e)C(O)N(R12e)-, -N(R12e)SO2N(R12e)-, -OC(O)-, o -C(O)N(R12e)-O-; y T2 es una cadena de alquileno C1-6 opcionalmente sustituido donde la cadena alquileno opcionalmente está interrumpida por -N(R13)-, -O-, -S-, -S(O)-, -S(O)2, -C(O)-, -C (O)O-, -C(O)N(R13)-, -S(O)2N(R13)-, -OC(O)N(R13)-, -N(R13)C(O)-, -N(R13)SO2-, -N(R13)C(O)O-, -N(R13)C(O)N(R13)-, -N(R13)S(O)2N(R13)-, -OC(O)-, o -C(O)N(R13)-O- o donde T2 o una porción del mismo opcionalmente forma parte de un cicloalifático de 3 a 7 miembros opcionalmente sustituido o un anillo heterociclilo donde R13 es hidrogeno o un grupo alifático C1-4 opcionalmente sustituido; n es 0 a 4; W selecciona de -C(R7)2-, -C(=C(R7)2)-, -C(R7)2O-, -C(R7)2NR7a-, -O-, -N(R7b)-, -S-, -S(O)-, -S(O)2, -C(O)-, -C(O)NR7a- o -N(R7a)C(O)-, donde: cada aparición de R7 es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C1-6, arilo de 6 a 10 miembros, heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, -N(R7b)2, -OR7a, -SR7a, halo, o -CN; cada aparición de R7a es independientemente hidrógeno o alifático C1-6 opcionalmente sustituido; cada aparición de R7b es independientemente hidrógeno, alifático C1-6 opcionalmente sustituido, -C(O)R7a, o -S(O)2R7a; o donde cualquiera de dos apariciones de R7, R7a, o R7b tomadas juntas con el átomo al cual están unidas, forman un grupo opcionalmente sustituido seleccionado del anillo cicloalifático de 3 a 6 miembros, arilo de 6 a 10 miembros, heterociclilo de 3 a 6 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, o donde cualquiera de dos apariciones de R7a y R2 o R7b y R2 tomadas juntas con el átomo de nitrógeno al cual están unidas, forman un grupo opcionalmente sustituido seleccionado del anillo cicloalifático de 3 a 6 miembros, arilo de 6 a 10 miembros, heterociclilo de 3 a 6 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; G1 es N o -CR8, donde R8 es H, -CN, halógeno, -Z-R9, alifático C1-6, o cicloalifático de 3 a 10 miembros, donde: Z se selecciona de una cadena de alquileno C1-3 opcionalmente sustituido -O-, N(R8a)-, -S-, -S(O)-, S(O)2-, -C(O)-, -CO2-, -C(O)NR8a-, -N(R8a)C(O)-, -N(R8a)CO2-, -S(O)2NR8a-, -N(R8a)S(O)2-, -OC(O)N(R8a)-, -N(R8a)C(O)NR8a-, -N(R8a)S(O)2N(R8a)-, o -OC(O)-; R8a es hidrógeno o un alifático C1-4 opcionalmente sustituido, y R9 es hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C1-6, cicloalifático de 3 a 10 miembros, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; y HY es un grupo opcionalmente sustituido seleccionado de los restos de fórmulas (4) a (9); donde cada aparición de X4, X5, X6, y X7, es independientemente -CR10 o N, siempre que no más de dos apariciones de X4, X5, X6, y X7, sean N; cada aparición de Q1 y Q2 es independientemente S, O ó -NR5; cada aparición de Y1, Y2, Y3, Y4, Y5, Y6, Y7, Y8, e Y9 es independientemente -CR10 o N, siempre que no más de dos apariciones de Y6, Y7, Y8, e Y9 sean N; o donde dos apariciones adyacentes de X4 y X5, X6 y X7, Y1 y Q1, Y3 y Q2, o Y4 y Y5 tomados juntos con el átomo al cual están unidos, forman un grupo fusionado opcionalmente sustituido seleccionado de arilo de 5 a 6 miembros, o heteroarilo de 5 a 6 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno o azufre; donde R10 es -R10b, -V1-R10c, -T1-R10b, o -V1-T1-R10b donde: V1 es -NR11-, -NR11-C(O)-, -NR11-C(S)-, -NR11-C(NR11)-, -NR11C(O)OR10a-, -NR11C(O)NR11-, -NR11C(O)SR10a-, -NR11C(S)OR10a-, -NR11C(S)NR11-, -NR11C(S)SR10a-, -NR11C(NR11)OR10a-, -NR11C(NR11)NR11-, -NR11S(O)2-, -NR11S(O)2NR11, -C(O)-, -CO2-, -C(O)NR11-, -C(O)NR11O-, -SO2-, o -SO2NR11-; cada aparición de R10a es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C1-6, cicloalifático de 3 a 10 miembros, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxigeno, o azufre; T1 es una cadena de alquileno C1-6 opcionalmente sustituido donde la cadena alquileno opcionalmente está interrumpida por S(O)2N(R11)-, -OC(O)N(R11)-, -N(R11)C(O)-, -N(R11)SO2-, -N(R11a)C(O)O-, -NR10a-C(O)N(R10a)-, -N(R10a)S(O)2N(R10a-, -OC(O)-, o -C(O)N(R11)-O- o donde T1 forma parte de un cicloalifático de 3 a 7 miembros opcionalmente sustituido o un anillo heterociclilo; cada aparición de R10b es independientemente hidrógeno, halógeno, CN, -NO2, -N(R11)2, -OR10a, -SR10a, -S(O)2R10a, -C(O)R10a, -C(O)OR10a, -C(O)N(R11)2, -S(O)2N(R11)2, -OC(O)N(R11)2, -N(R11)C(O)R10a, -N(R11)SO2R10a, -N(R11)C(O)OR10a, -N(R11)C(O)N(R11)2, o -N(R11)SO2N(R11)2, o un grupo opcionalmente sustituido seleccionado de alifático C1-6, cicloalifático de 3 a 10 miembros, heterociclilo de 4 a 10 miembros que tiene 1 a 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo de 6 a 10 miembros, o heteroarilo de 5 a 10 miembros que tiene 1 a 5
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