CO5140126A1 - 2-fenilbenzimidazoles sustituidos, su obtencion y uso - Google Patents
2-fenilbenzimidazoles sustituidos, su obtencion y usoInfo
- Publication number
- CO5140126A1 CO5140126A1 CO99069358A CO99069358A CO5140126A1 CO 5140126 A1 CO5140126 A1 CO 5140126A1 CO 99069358 A CO99069358 A CO 99069358A CO 99069358 A CO99069358 A CO 99069358A CO 5140126 A1 CO5140126 A1 CO 5140126A1
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- CO
- Colombia
- Prior art keywords
- alkyl
- phenyl
- hydrogen
- branched
- unbranched
- Prior art date
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Abstract
Compuestos de la fórmula general I o II<EMI FILE="99069358_1" ID="1" IMF=JPEG >donde, R1 significa hidrógeno, C1-C6-alquilo ramificado o sin ramificar, pudiendo un átomo de carbono del radical alquilo llevar aún OR11 o un grupo R5, significando R11 hidrógeno o C1-C4-alquilo, yR2 significa hidrógeno, cloro, bromo, yodo, fluoro, CF3, nitro, NHCOR21, NR22R23 OH, O-C1-C4-alquil-fenilo, NH2, fenilo, pudiendo los anillos fenilo estar aún sustituidos por, como máximo, los radicales R24, y significando R21 y R22 independientemente hidrógeno o C1-C4-alquilo y significando R23 hidrógeno, C1-C4-alquilo o fenilo, y significando R24 OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NH2, yX puede ser 0, 1 y 2 yR3 significa -D- (F1)p-(E)q-(F2)r-G, donde p, q y r no pueden significar a la vez 0, o -E- (D)u-(F2)s- (G)v, donde el radical E puede estar sustituido aún por uno o dos radicales A, o R3 es igual a B yR4 significa hidrógeno, cloro, fluoro, bromo, yodo, C1-C6-alquilo ramificado o sin ramificar, OH, nitro, CF3, CN, NR41R42, NH-COR43, O-C1-C4-alquilo, donde R41 y R42 significan, cada uno independientemente del otro, hidrógeno o C1-C4-alquilo yR43 significa hidrógeno, C1-C4-alquilo, C1-C4-alquil-fenilo o fenilo, yD S y OE significa fenilo, imidazol, pirrol, tiofeno, piridina, pirimidina, piperacina, piracina, furano, tiazol, isoxazol, pirrolidina, piperidina, trihidroacepina yF1 significa una cadena de 1 a 8 átomos de carbono, donde un átomo de carbono de la cadena puede llevar aún un grupo OH o O-C1-C4-alquilo yF2 significa una cadena de 1 a 8 átomos de carbono, donde un átomo de carbono de la cadena pude llevar aún OH o un grupo O-C1-C4-alquilo yP puede significar 0 y 1 yq 0, y 1, y- 2 -r puede ser 0 y 1 ys puede ser 0 y 1 yu puede ser 0 y 1 yv puede ser 0 y 1 G puede representar NR51R52<EMI FILE="99069358_2" ID="2" IMF=JPEG >yR51 significa hidrógeno y C1-C6-alquilo ramificado o sin ramificar, (CH2)t-KyR52 significa hidrógeno, C1-C6-alquilo ramificado y sin ramificar, fenilo,<EMI FILE="99069358_3" ID="3" IMF=JPEG >, -SO2R53, - (C=N)-R53, -CO-NHR53, -(C=N)-NHR53,DondeR53 significa O-C1-C6-alquilo ramificado o sin ramificar, fenilo, C1-C4-alquil-fenilo ramificado o sin ramificar,Pudiendo un hidrógeno del radical C1-C6-alquilo en R52 y R53, independientemente, estar sustituido por uno de los radicales siguientes: OH, O-C1-C4-alquilo, ciclohexilo, ciclopentilo, tetrahidronaftilo, ciclopropilo, ciclobutilo, cicloheptilo, naftilo y fenilo, donde los carbociclos de los radicales R52 y R53 llevan independientemente, uno o dos de los radicales siguientes: C1-C6-alquilo ramificado o sin ramificar, OC1-C4-alquilo ramificado o sin ramificar, OH, F, Cl, Br, J. CF3, NO2, CN, COOH, COOC1-C4-alquilo, C1-C4-alquilamino, CC13, C1-C4-dialquilamino, SO2-C1-C4-alquilo, SO2, fenilo, CONH2-C1-C4-alquilo, CONHfenilo, CONH-C1-C4-alquil-fenilo, NHSO2-C1-C4-alquilo, NHSO2fenilo, S-C1-C4-alquilo,<EMI FILE="99069358_4" ID="4" IMF=JPEG > C1-C4-alquilo, <EMI FILE="99069358_5" ID="5" IMF=JPEG > C0-C4 -alquil - fenilo,CHO, CH2-O-C1-C4-alquilo, -CH2-C1-C4-alquil-fenilo, -CH2OH, -SO-C1-C4-alquilo, -SO-C1-C4-alquil-fenilo, -SO2,NH2, -SO2NH-C1-C4-alquilo y dos radicales forman un puente de -O-(CH2)1-2-O-,B puede representar<EMI FILE="99069358_6" ID="6" IMF=JPEG >yA significa hidrógeno, cloro, bromo, yodo, fluoro, CF3, nitro, OH, O-C1-C4-alquilo, O-C1-C4-alquil-fenilo, NH2, C1-C6-alquilo ramificado o sin ramificar, CN, NH-CO-R33, donde R33 es hidrógeno, C1-C4-alquilo o fenilo, yR31 significa hidrógeno, C1-C6-alquilo, (CH2)t-K yR32 significa hidrógeno, C1-C6-alquilo, -CO-R8, -(C-N)-R8, -CO-OR8, -CO-NHR8 y -(C=N)-NHR8 yR33 significa hidrógeno y C1-C4-alquilo yt es 0, 1, 2, 3, 4 yK significa fenilo, que puede llevar aún, como máximo dos radicales R, NRk1Rk2 (teniendo Rk1 o bien Rk2 los mismos significados que R41 o bien R42), NH-C1-C4-alquil-fenilo, pirrolidina, piperidina, 1,2,5,6-tetrahidropiridinam morfolina, morfolina, trihidroacepina, piperacina, que puede estar sustituida aún por un radical alquilo, C1-C4-alquilo, y homopiperacina, que puede estar sustituida aún por un radical alquilo, C1-C6-alquilo, yR5 significa hidrógeno, C1-C6-alquilo, NR7R9 y <EMI FILE="99069358_7" ID="7" IMF=JPEG >YR7 significa hidrógeno, C1-C6-alquilo, C1-C4-alquil-fenilo, fenilo, pudiendo el anillo estar sustituido por hasta dos radicales R71 s, yR71 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NH2, y- 3 -R8 significa hidrógeno, C1-C6-alquilo, fenilo, C1-C4-alquil-fenilo, pudiendo el radical estar sustituido por hasta dos radicales R81, yR81 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NH2, yR9 significa hidrógeno, COCH3, CO-OC1-C4-alquilo, COCF3, C1-C6-alquilo ramificado o sin ramificar, donde uno o dos hidrógenos del radical C1-C6-alquilo pueden estar sustituidos cada vez por uno de los radicales siguientes: OH, OC1-C4-alquilo y fenilo y donde el anillo fenilo puede llevar aún uno o dos de los radicales siguientes: yodo, cloro, bromo, fluoro, C1-C6-alquilo ramificado y sin ramificar, nitro, amino, C1-C4-alquilamino, C1-C4-dialquilamino, OH, O-C1-C4-alquilo, CN, CF3, SO2-C1-C4-alquilo, yAsí como sus formas tautómeras, enantiómeros y diastereómeros posibles, y sus prodrogas y sales farmacológicamente toleradas.
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HUP0104129A3 (en) | 1998-11-17 | 2002-09-30 | Basf Ag | Use of 2-phenylbenzimidazoles and 2-phenylindoles for producing pharmaceutical compositions having parp enzym effect and new 2-phenylbenzimidazol derivatives |
DE19916460B4 (de) | 1999-04-12 | 2006-12-21 | Abbott Gmbh & Co. Kg | Substituierte Benzimidazole, deren Herstellung und Anwendung |
WO2000032579A1 (de) | 1998-11-27 | 2000-06-08 | Basf Aktiengesellschaft | Substituierte benzimidazole und ihre verwendung als parp inhibitoren |
DE19920936A1 (de) * | 1999-05-07 | 2000-11-09 | Basf Ag | Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung |
WO2001021615A1 (en) | 1999-09-17 | 2001-03-29 | Yamanouchi Pharmaceutical Co., Ltd. | Benzimidazole derivatives |
WO2001021634A1 (en) | 1999-09-21 | 2001-03-29 | Lion Bioscience Ag | Benzimidazole derivatives and combinatorial libraries thereof |
DE10021468A1 (de) | 2000-05-04 | 2001-11-08 | Basf Ag | Verwendung von PARP-Inhibitoren in kosmetischen Zubereitungen |
US7728026B2 (en) | 2005-04-11 | 2010-06-01 | Abbott Laboratories, Inc. | 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors |
TWI375673B (en) | 2005-04-11 | 2012-11-01 | Abbott Lab | 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors |
CN101316834A (zh) | 2005-09-29 | 2008-12-03 | 艾博特公司 | 在2位取代有苯基的1h-苯并咪唑-4-甲酰胺是强效parp抑制剂 |
TW200736229A (en) | 2005-11-15 | 2007-10-01 | Abbott Lab | Substituted 1H-benzimidazole-4-carboxamides are potent PARP inhibitors |
ES2437132T3 (es) | 2006-01-17 | 2014-01-09 | Abbvie Bahamas Ltd. | Tratamiento combinado con inhibidores de PARP |
WO2007131016A2 (en) | 2006-05-02 | 2007-11-15 | Abbott Laboratories | Substituted 1h-benzimidazole-4-carboxamides are potent parp inhibitors |
US8067613B2 (en) | 2007-07-16 | 2011-11-29 | Abbott Laboratories | Benzimidazole poly(ADP ribose)polymerase inhibitors |
-
1999
- 1999-10-28 AT AT99955894T patent/ATE284392T1/de not_active IP Right Cessation
- 1999-10-28 BR BR9915013-1A patent/BR9915013A/pt not_active IP Right Cessation
- 1999-10-28 US US09/830,992 patent/US7781596B1/en not_active Expired - Fee Related
- 1999-10-28 PL PL99347500A patent/PL347500A1/xx not_active Application Discontinuation
- 1999-10-28 KR KR1020017005550A patent/KR20010100977A/ko not_active Application Discontinuation
- 1999-10-28 IL IL14291799A patent/IL142917A0/xx unknown
- 1999-10-28 AU AU12665/00A patent/AU765224B2/en not_active Ceased
- 1999-10-28 HU HU0200312A patent/HUP0200312A3/hu unknown
- 1999-10-28 CA CA002349227A patent/CA2349227C/en not_active Expired - Fee Related
- 1999-10-28 DE DE1999511249 patent/DE59911249D1/de not_active Expired - Lifetime
- 1999-10-28 CZ CZ20011546A patent/CZ20011546A3/cs unknown
- 1999-10-28 EP EP99955894A patent/EP1127052B1/de not_active Expired - Lifetime
- 1999-10-28 WO PCT/EP1999/008169 patent/WO2000026192A1/de not_active Application Discontinuation
- 1999-10-28 TR TR2001/01239T patent/TR200101239T2/xx unknown
- 1999-10-28 SK SK595-2001A patent/SK5952001A3/sk unknown
- 1999-10-28 ES ES03024899.1T patent/ES2449713T3/es not_active Expired - Lifetime
- 1999-10-28 CN CN99814796A patent/CN1331682A/zh active Pending
- 1999-10-28 EP EP03024899.1A patent/EP1391457B1/de not_active Expired - Lifetime
- 1999-10-28 JP JP2000579581A patent/JP2002528531A/ja active Pending
- 1999-10-28 ES ES99955894T patent/ES2234318T3/es not_active Expired - Lifetime
- 1999-10-28 PT PT99955894T patent/PT1127052E/pt unknown
- 1999-10-28 TR TR2002/00972T patent/TR200200972T2/xx unknown
- 1999-10-28 ID IDW00200101198A patent/ID28787A/id unknown
- 1999-11-02 AR ARP990105543A patent/AR024517A1/es not_active Application Discontinuation
- 1999-11-03 CO CO99069358A patent/CO5140126A1/es unknown
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2001
- 2001-05-02 NO NO20012158A patent/NO20012158L/no not_active Application Discontinuation
- 2001-05-16 BG BG105515A patent/BG105515A/xx unknown
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2002
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2005
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2006
- 2006-08-02 JP JP2006211209A patent/JP2007024902A/ja active Pending
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