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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Argentina
Prior art keywords
alkyl
hydrogen
nitrogen
heterocyclic ring
alkoxy
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ARP050100931A
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English (en)
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Altana Pharma Ag
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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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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    • 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)

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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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US (1) US20070185149A1 (es)
EP (1) EP1725534A1 (es)
JP (1) JP2007527901A (es)
KR (1) KR20060130697A (es)
CN (1) CN1926113B (es)
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Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE353217T1 (de) 2002-08-29 2007-02-15 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridine als pde-4 inhibitoren
EP1539164B1 (en) 2002-08-29 2006-12-20 ALTANA Pharma AG 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
GB0316915D0 (en) 2003-07-18 2003-08-20 Glaxo Group Ltd Compounds
US7585872B2 (en) 2004-02-18 2009-09-08 Nycomed Gmbh Guanidinyl-substituted hydroxy-6-phenylphenanthridines as effective phosphodiesterase (PDE) 4 inhibitors
CN104803973A (zh) 2004-03-03 2015-07-29 塔科达有限责任公司 新的羟基-6-杂芳基菲啶及其作为pde4抑制剂的用途
AR049419A1 (es) * 2004-03-03 2006-08-02 Altana Pharma Ag Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo
ATE508130T1 (de) 2004-09-08 2011-05-15 Nycomed Gmbh 3-oxa-10-aza-phenanthrene als pde4- oder pde3/4- inhibitoren
US7589205B2 (en) 2004-09-08 2009-09-15 Nycomed Gmbh 3-thia-10-aza-phenanthrene derivatives
PL1856093T3 (pl) 2005-03-02 2010-05-31 Takeda Gmbh Chlorowodorek (2R,4aR,10bR)-6-(2,6-dimetoksy-pirydyn-3-ylo)-9-etoksy-8-metoksy-1,2,3,4,4a,10b-heksahydrofenantrydyn-2-olu
GB0601951D0 (en) 2006-01-31 2006-03-15 Novartis Ag Organic compounds
RU2009120389A (ru) 2006-10-30 2010-12-10 Новартис АГ (CH) Гетероциклические соединения в качестве противовоспалительных агентов
AU2008307195B2 (en) 2007-10-04 2012-11-22 F. Hoffmann-La Roche Ag Cyclopropyl aryl amide derivatives and uses thereof
WO2009087224A1 (en) 2008-01-11 2009-07-16 Novartis Ag Pyrimidines as kinase inhibitors
EP2406210A1 (en) * 2009-03-09 2012-01-18 Basf Se Process for preparing substituted 2-nitrobiphenyls
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
MA34969B1 (fr) 2011-02-25 2014-03-01 Irm Llc Composes et compositions en tant qu inibiteurs de trk

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0916346A3 (en) * 1991-09-20 2000-12-06 Glaxo Group Limited NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis
SI0882021T1 (en) * 1996-01-31 2003-10-31 Altana Pharma Ag New phenanthridines
US6127378A (en) * 1996-03-26 2000-10-03 Byk Gulden Lomberg Chemische Fabrik Gmbh Phenanthridines substituted in the 6 position
WO1998021208A1 (en) * 1996-11-11 1998-05-22 Byk Gulden Lomberg Chemische Fabrik Gmbh Benzonaphthyridines as bronchial therapeutics
IL133825A (en) * 1997-07-25 2005-12-18 Altana Pharma Ag Substituted 6-phenylphenanthridines, medicaments containing same and use thereof in the production of medicaments
WO1999005112A1 (en) * 1997-07-25 1999-02-04 Byk Gulden Lomberg Chemische Fabrik Gmbh Substituted 6-alkylphenanthridines
ES2217575T3 (es) * 1997-07-25 2004-11-01 Altana Pharma Ag Nuevos derivados de tetrazol.
JP2002513793A (ja) * 1998-05-05 2002-05-14 ビイク グルデン ロンベルク ヒエーミツシエ フアブリーク ゲゼルシヤフト ミツト ベシユレンクテル ハフツング 新規ｎ−オキシド
BR0007527B1 (pt) * 1999-01-15 2011-12-27 fenilfenantridinas com atividade inibitària de pde-iv, seu uso, bem como medicamento compreendendo as mesmas.
PT1147087E (pt) * 1999-01-15 2005-09-30 Altana Pharma Ag Feantridina-n-oxidos com actividade de inibicao de pde-iv
US6534519B1 (en) * 1999-01-15 2003-03-18 Altana Pharma Ag Phenanthridine-N-oxides with PDE-IV inhibiting activity
PT1303506E (pt) * 2000-07-14 2005-06-30 Altana Pharma Ag 6-heteroarilfenantridinas
ATE287403T1 (de) * 2001-02-21 2005-02-15 Byk Gulden Lomberg Chem Fab 6-phenylbenzonaphthyidine
US20060116518A1 (en) * 2002-08-17 2006-06-01 Altana Pharma Ag Novel phenanthridines
ATE353217T1 (de) * 2002-08-29 2007-02-15 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridine als pde-4 inhibitoren
EP1539164B1 (en) * 2002-08-29 2006-12-20 ALTANA Pharma AG 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
WO2004031724A2 (en) * 2002-09-30 2004-04-15 Ciphergen Biosystems, Inc. Apparatus and method for expression and capture of biomolecules and complexes on adsorbent surfaces
AR049419A1 (es) * 2004-03-03 2006-08-02 Altana Pharma Ag Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo
AU2005220034A1 (en) * 2004-03-09 2005-09-15 Nycomed Gmbh Novel isoamido-substituted hydroxy-6-phenylphenanthridines and their use as PDE4 inhibitors
WO2005085203A1 (en) * 2004-03-10 2005-09-15 Altana Pharma Ag Novel difluoroethoxy-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors
WO2005087744A1 (en) * 2004-03-10 2005-09-22 Altana Pharma Ag Novel thio-containing hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors
US20080119505A1 (en) * 2005-02-01 2008-05-22 Altana Pharma Ag Novel 6-Pyridylphenanthridines
EA200701815A1 (ru) * 2005-03-02 2008-02-28 Никомед Гмбх 6-гетероарил-1,2,3,4,4а,10в-гексагидрофенантридины в качестве pde-4 ингибиторов для лечения воспалительных заболеваний
PL1856093T3 (pl) * 2005-03-02 2010-05-31 Takeda Gmbh Chlorowodorek (2R,4aR,10bR)-6-(2,6-dimetoksy-pirydyn-3-ylo)-9-etoksy-8-metoksy-1,2,3,4,4a,10b-heksahydrofenantrydyn-2-olu
AU2006221957A1 (en) * 2005-03-09 2006-09-14 Nycomed Gmbh Amido-substituted 6-phenylphenanthridines

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BRPI0508481A (pt) 2007-07-31
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