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AR049324A1 - Derivados de hidroxi-6-fenilfenantridinas amido sustituidas. composiciones farmacéuticas. - Google Patents

Derivados de hidroxi-6-fenilfenantridinas amido sustituidas. composiciones farmacéuticas.

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Publication number
AR049324A1
AR049324A1 ARP050100931A ARP050100931A AR049324A1 AR 049324 A1 AR049324 A1 AR 049324A1 AR P050100931 A ARP050100931 A AR P050100931A AR P050100931 A ARP050100931 A AR P050100931A AR 049324 A1 AR049324 A1 AR 049324A1
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AR
Argentina
Prior art keywords
alkyl
hydrogen
nitrogen
heterocyclic ring
alkoxy
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Application number
ARP050100931A
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English (en)
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Altana Pharma Ag
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Publication date
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Publication of AR049324A1 publication Critical patent/AR049324A1/es

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    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes
    • C07D221/12—Phenanthridines
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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Abstract

Composiciones farmacéuticas que los componen. Reivindicacion 1: Compuestos de formula (1), caracterizados porque: R1 es hidroxilo, alcoxi C1-4, cicloalcoxi C3-7, cicloalquilmetoxi C3-7, 2,2-difluoroetoxi, o alcoxi C1-4 completamente o predominantemente sustituido por fluor; R2 es hidroxilo, alcoxi C1-4, cicloalcoxi C3-7, cicloalquilmetoxi C3-7, 2,2-difluoroetoxi, o alcoxi C1-4 completamente o predominantemente sustituido por fluor, o en donde, R1 y R2 juntos son un grupo alquilendioxi C1-2; R3 es hidrogeno o alquilo C1-4; R31 es hidrogeno o alquilo C1-4; o, en una primera realizacion (realizacion a) de acuerdo con la presente; R4 es -O-R41, en donde R41 es hidrogeno, alquilo C1-4, alcoxi C1-4alquiloC1-4, hidroxialquilo C2-4, alquilcarbonilo C1-7, o alquilo C1-4 completamente o predominantemente sustituido por fluor; y R5 es hidrogeno o alquilo C1-4; o, en una segunda realizacion (realizacion b) de acuerdo con la presente; R4 es hidrogeno o alquilo C1-4; y R5 es -O-R51, en donde, R51 es hidrogeno, alquilo C1-4, alcoxiC1-4alquiloC1-4, hidroxialquilo C2-4, alquilcarbonilo C1-7, o alquilo C1-4 completamente o predominantemente sustituido por fluor; R6 es hidrogeno, halogeno, alquilo C1-4 o alcoxi C1-4, ya sea, en un primer aspecto (aspecto 1) de acuerdo con la presente; R7 es -N(R8)R9, en donde R8 es hidrogeno, alquilo C1-4 o alcoxiC1-4alquiloC2-4; R9 es hidrogeno, alquilo C1-4, mono- o dialcoxiC1-4alquiloC2-4; hidroxialquilo C2-4, mono- o dialcoxicarboniloC1-4-alquiloC1-4, Har1, piridinilo-alquiloC1-4, cicloalquilo C3-7, o alquilo C2-4 sustituido por -N(R39)R94, en donde, Har1 está opcionalmente sustituido por R91 y/o R92, y es un radical heteroarilo insaturado monocíclico o bicíclico fusionado de 5 a 10 miembros que comprende 1 a 4 heteroátomos seleccionados independientemente del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde, R91 es alquilo C1-4 o alcoxi C1-4; R92 es alquilo C1-4 o alcoxi C1-4; R93 es hidrogeno o alquilo C1-4; R94 es hidrogeno o alquilo C1-4; o R93 y R94 en forma conjunta y con conclusion del átomo de nitrogeno al cual están unidos, forman un anillo heterocíclico Het1, en donde, Het1 está opcionalmente sustituido por R931, y es un radical de anillo heterocíclico monocíclico saturado de 3 a 7 miembros que comprende el átomo de nitrogeno al cual R93 y R94 están enlazados, y opcionalmente otro heteroátomo seleccionado del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde R931 es alquilo C1-4, o R8 y R9 juntos o con conclusion del átomo de nitrogeno al cual están unidos, forman un anillo heterocíclico Het2, en donde, Het2 está opcionalmente sustituido por R10, y es un radical de anillo heterocíclico monocíclico saturado de 3 a 7 miembros que comprende el átomo de nitrogeno al cual R8 y R9 están enlazados, y opcionalmente otro heteroátomo seleccionado del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde R10 es alquilo C1-4, -C(O)R11, piridilo, alquilo C2-4 sustituido por -N(R14)R15, o alquilo C1-4 sustituido por -C(O)N(R16)R17, en donde R11 es alquilo C1-4 sustituido por -N(R12)R13, en donde, R12 es hidrogeno o alquilo C1-4; R13 es hidrogeno o alquilo C1-4; o R12 y R13 juntos o con inclusion del átomo de nitrogeno al cual están unidos, forman un anillo heterocíclico Het3, en donde Het3 está opcionalmente sustituido por R121, y es un radical de anillo heterocíclico monocíclico saturado de 3 a 7 miembros que comprende el átomo de nitrogeno al cual R12 y R13 están enlazados, y opcionalmente otro heteroátomo seleccionado del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde R121 es alquilo C1-4; R14 es hidrogeno o alquilo C1-4; R15 es hidrogeno o alquilo C1-4; o R14 y R15 juntos o con inclusion del átomo de nitrogeno al cual están unidos, forman un anillo heterocíclico Het4, en donde Het4 está opcionalmente sustituido por R141, y es un radical de anillo heterocíclico monocíclico saturado de 3 a 7 miembros que comprende el átomo de nitrogeno al cual R14 y R15 están enlazados, y opcionalmente otro heteroátomo seleccionado del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde R141 es alquilo C1-4; R16 es hidrogeno, alquilo C1-4 o piridilo; R17 es hidrogeno o alquilo C1-4; o R16 y R17 juntos o con inclusion del átomo de nitrogeno al cual están unidos, forman un anillo heterocíclico Het5, en donde, Het5 está opcionalmente sustituido por R161, y es un radical de anillo heterocíclico monocíclico saturado de 3 a 7 miembros que comprende el átomo de nitrogeno al cual R16 y R17 están enlazados, y opcionalmente otro heteroátomo seleccionado del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde R141 es alquilo C1-4, o en un segundo aspecto (aspecto 2) de acuerdo con la presente R7 es -NH-N(R18)R19, en donde R18 es hidrogeno; R19 es -C(O)R20, o fenilo sustituido por R21, en donde R20 es Har2, Het6, o arilalquilo C1-4, en donde Har2 está opcionalmente sustituido por R201 y/o R202, y es un radical heteroarilo insaturado monocíclico o bicíclico fusionado de 5 a 10 miembros que comprende 1 a 4 heteroátomos seleccionados independientemente del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde, R201 es alquilo C1-4 o alcoxi C1-4; R202 es alquilo C1-4 o alcoxi C1-4; Het6 está opcionalmente sustituido por R203 y/o R204, y es un radical de anillo heterocíclico saturado monocíclico de 3 a 7 miembros que comprende uno a tres heteroátomos, cada uno de los cuales se selecciona del grupo que consiste en nitrogeno, oxígeno y sulfuro, en donde, R203 es alquilo C1-4; R204 es alquilo C1-4; Arilo es fenilo sustituido por R205 y/o R206; R205 es alcoxi C1-4; R206 es alcoxi C1-4; R21 es aminosulfonilo; o R18 y R19 juntos o con inclusion del átomo de nitrogeno al cual están unidos, forman un anillo heterocíclico Het7, en donde, Het7 está opcionalmente sustituido por R181, y es un radical de anillo heterocíclico monocíclico saturado de 3 a 7 miembros que comprende el átomo de nitrogeno al cual R18 y R19 están enlazados, y opcionalmente otro heteroátomo seleccionado del grupo que consiste en oxígeno, nitrogeno y sulfuro, en donde, R181 es alquilo C1-4; y las sales, los N-oxidos y las sales de los N-oxidos de estos compuestos.
ARP050100931A 2004-03-10 2005-03-11 Derivados de hidroxi-6-fenilfenantridinas amido sustituidas. composiciones farmacéuticas. AR049324A1 (es)

Applications Claiming Priority (2)

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EP04100990 2004-03-10
EP04106677 2004-12-17

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AR049324A1 true AR049324A1 (es) 2006-07-19

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ARP050100931A AR049324A1 (es) 2004-03-10 2005-03-11 Derivados de hidroxi-6-fenilfenantridinas amido sustituidas. composiciones farmacéuticas.

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US (1) US20070185149A1 (es)
EP (1) EP1725534A1 (es)
JP (1) JP2007527901A (es)
KR (1) KR20060130697A (es)
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EP1725534A1 (en) 2006-11-29
BRPI0508481A (pt) 2007-07-31
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WO2005087745A1 (en) 2005-09-22
US20070185149A1 (en) 2007-08-09
CA2558391A1 (en) 2005-09-22
IL177496A0 (en) 2006-12-10
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CN1926113A (zh) 2007-03-07

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