AR048484A1 - Derivados de diacilhidrazina, su uso como inhibidor de raf quinasa y composiciones farmaceuticas que los contienen - Google Patents
Derivados de diacilhidrazina, su uso como inhibidor de raf quinasa y composiciones farmaceuticas que los contienenInfo
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- AR048484A1 AR048484A1 ARP040104607A ARP040104607A AR048484A1 AR 048484 A1 AR048484 A1 AR 048484A1 AR P040104607 A ARP040104607 A AR P040104607A AR P040104607 A ARP040104607 A AR P040104607A AR 048484 A1 AR048484 A1 AR 048484A1
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Abstract
Reivindicacion 1: Derivados de diacilhidrazina de la formula: A-D-B en donde D es un resto de diacilhidrazina bivalente o uno de sus derivados; A es un resto insustituido o sustituido de hasta 40 átomos se C de la formula -L-(M-L')a, en donde L es una estructura cíclica de 5, 6 o 7 miembros seleccionada, con preferencia, del grupo integrado por arilo, heteroarilo, arileno y heteroarileno, unida directamente con D, L' comprende un resto cíclico opcionalmente sustituido que tiene al menos 5 miembros seleccionado, con preferencia, del grupo integrado por arilo, heteroarilo, aralquilo, cicloalquilo y heterociclilo, M es un enlace o un grupo puente que tiene al menos un átomo, a es un numero entero de 1-4; y cada estructura cíclica de L y L' contiene 0-4 miembros del grupo integrado por N, O y S, donde L' está sustituido, con preferencia, por al menos un sustituyente del grupo integrado por -SObRx, -C(O)Rx y -C(NRy)Rz; B es un resto de arilo o heteroarilo hasta tricíclico sustituido o insustituido de hasta 30 átomos de C, que comprende al menos una estructura cíclica de 5, 6 o 7 miembros, unida directamente con D que contiene 0-4 miembros del grupo integrado por N, O y S, donde dicha estructura cíclica directamente unida a D está seleccionada, con preferencia, del grupo integrado por arilo, heteroarilo y heterociclilo, Ry es H o un resto carbonado de hasta 24 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente halosustituido, hasta perhalo, Rz es H o un resto carbonado de hasta 30 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con halogeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halogeno; Rx es Rz o NRaRb, donde Ra y Rb son a) de forma independiente, H, un resto carbonado de hasta 30 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con halogeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halogeno, u -OSi(Rf)3, donde Rf es H o un resto carbonado de hasta 24 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con halogeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halogeno; o b) Ra y Rb forman juntos una estructura heterocíclica de 5-7 miembros de 1-3 heteroátomos seleccionados de N, S y O, o una estructura heterocíclica sustituida de 5-7 miembros de 1-3 heteroátomos seleccionados de N, S y O sustituida con halogeno, hidroxi o sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos de N, S y O y que están opcionalmente sustituidos con halogeno; o c) uno de Ra o Rb es -C(O)-, un grupo alquileno divalente C1-5 o un grupo alquileno divalente C1-5 sustituido unido con el resto L para formar una estructura cíclica con al menos 5 miembros, en donde los sustituyentes del grupo alquileno divalente C1-5 sustituido están seleccionados del grupo integrado por halogeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halogeno; en donde B está sustituido, L está sustituido o L' está adicionalmente sustituido, los sustituyentes están seleccionados del grupo integrado por halogeno, hasta perhalo, y Wg, en donde g es 0-3; en donde cada W está seleccionado, de forma independiente, del grupo integrado por -CN, -CO2R, C(O)NR5R5, -C(O)-R5, -NO2, -OR5, -SR5, -NR5R5, NR5C(O)OR5, -NR5C(O)R5, -Q-Ar, y restos carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con uno o varios sustituyentes seleccionados, de forma independiente, del grupo integrado por -CN, -CO2R, C(O)NR5R5, -C(O)-R5, - NO2, -OR5, -SR5, -NR5R5, NR5C(O)OR5, -NR5C(O)R5, y halogeno hasta perhalo; con cada R5 seleccionado, de forma independiente, de H o un resto carbonado de hasta 24 átomos de C, que opcionalmente contiene heteroátomos seleccionados de N, S y O y que opcionalmente está sustituido con halogeno, en donde Q es -O-, -S-, N(R5)-, -(CH2)b, -C(O)-, -CH(OH)-, -(CH2)b-, -(CH2)bS-, -(CH2)bN(R5)-, -O-(CH2)b-CHHal-, -CHal2-, S-(CH2)- y N(R5)(CH2)b-, donde b = 1-3 y Hal es halogeno; y Ar es una estructura aromática de 5 o 6 miembros que contiene 0-2 miembros seleccionados del grupo integrado por N, O y S, que está opcionalmente sustituida con halogeno, hasta perhalo y opcionalmente sustituida con Zd1, donde d1 es 0 a 3 y cada Z está seleccionado, de forma independiente, del grupo integrado por -CN, -CO2R5, C(O)NR5R5, -C(O)-R5, -NO2, -OR5, -SR5, SO2R5, -SO3H, NR5R5, NR5C(O)OR5, -NR5C(O)R5, y un resto carbonado de hasta 24 átomos de C, que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo integrado por -CN, -CO2R5, -C(O)NR5R5, -C(O)-R5, -NO2, -OR5, -SR5, -SO2R5, -SO3H, -NR5R5, -NR5C(O)OR5, -NR5C(O)R5, y sus derivados, sales y solvatos farmacéuticamente aceptables
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EP03028268 | 2003-12-10 |
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AR048484A1 true AR048484A1 (es) | 2006-05-03 |
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ARP040104607A AR048484A1 (es) | 2003-12-10 | 2004-12-10 | Derivados de diacilhidrazina, su uso como inhibidor de raf quinasa y composiciones farmaceuticas que los contienen |
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US (1) | US20070093529A1 (es) |
EP (1) | EP1692110A1 (es) |
JP (1) | JP2007515412A (es) |
AR (1) | AR048484A1 (es) |
AU (1) | AU2004299174A1 (es) |
CA (1) | CA2548571A1 (es) |
WO (1) | WO2005058832A1 (es) |
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US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
ATE556713T1 (de) | 1999-01-13 | 2012-05-15 | Bayer Healthcare Llc | Omega-carboxyarylsubstituierte-diphenyl- harnstoffe als p38-kinasehemmer |
AU2003209116A1 (en) | 2002-02-11 | 2003-09-04 | Bayer Pharmaceuticals Corporation | Aryl ureas with angiogenesis inhibiting activity |
WO2003068229A1 (en) | 2002-02-11 | 2003-08-21 | Bayer Pharmaceuticals Corporation | Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors |
US7557129B2 (en) | 2003-02-28 | 2009-07-07 | Bayer Healthcare Llc | Cyanopyridine derivatives useful in the treatment of cancer and other disorders |
PT1636585E (pt) | 2003-05-20 | 2008-03-27 | Bayer Pharmaceuticals Corp | Diarilureias com actividade inibidora de cinase |
JP4777887B2 (ja) | 2003-07-23 | 2011-09-21 | バイエル、ファーマシューテイカルズ、コーポレイション | 病気および状態の処置および防止のためのフロロ置換オメガカルボキシアリールジフェニル尿素 |
WO2008153801A1 (en) | 2007-05-29 | 2008-12-18 | Intrexon Corporation | Chiral diachylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex |
CN103087054B (zh) * | 2013-02-27 | 2015-12-23 | 山东大学 | 4-吡啶苯基醚类化合物及其制备方法与应用 |
CA2940272C (en) * | 2014-02-28 | 2022-03-29 | Tohoku University | Amide derivative |
CN107001329B (zh) * | 2014-09-12 | 2020-09-01 | 诺华股份有限公司 | 作为激酶抑制剂的化合物和组合物 |
WO2016044390A1 (en) * | 2014-09-17 | 2016-03-24 | Intrexon Corporation | Boron-containing diacylhydrazine compounds |
CN112778156B (zh) * | 2019-11-08 | 2023-03-14 | 中国科学院上海药物研究所 | 双酰肼结构类化合物、其制备方法及其应用 |
TWI794742B (zh) | 2020-02-18 | 2023-03-01 | 美商基利科學股份有限公司 | 抗病毒化合物 |
EP4323362A1 (en) | 2021-04-16 | 2024-02-21 | Gilead Sciences, Inc. | Methods of preparing carbanucleosides using amides |
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JPS61222790A (ja) * | 1984-12-10 | 1986-10-03 | Canon Inc | 記録媒体 |
JPS61156119A (ja) * | 1984-12-28 | 1986-07-15 | Canon Inc | 記録媒体 |
US5354762A (en) * | 1986-07-14 | 1994-10-11 | Rohm And Haas Company | Six-membered heterocyclic derivatives of N'-substituted N,N'-diacylhydrazines |
EP0253468B1 (en) * | 1986-07-14 | 1991-11-06 | Rohm And Haas Company | Six-membered heterocyclic derivatives of n'substituted-n,n'-diacylhydrazines |
JPH06107648A (ja) * | 1992-09-29 | 1994-04-19 | Ricoh Co Ltd | 新規なオキサジアゾール化合物 |
WO1993024468A1 (en) * | 1992-06-02 | 1993-12-09 | Ciba-Geigy Ag | Pyrimidinyl- and triazinyl- salicyl- and picolylamides and the use, as herbicides, and preparation thereof |
JP3341090B2 (ja) * | 1992-07-27 | 2002-11-05 | 株式会社リコー | オキサジアゾール誘導体ならびにその製造法 |
JPH06199853A (ja) * | 1992-11-27 | 1994-07-19 | Ricoh Co Ltd | チアジアゾール誘導体及びその製造方法 |
JPH06184125A (ja) * | 1992-12-24 | 1994-07-05 | Idemitsu Kosan Co Ltd | 1,3,4−ジアゾール誘導体 |
EP0704436B1 (en) * | 1994-03-16 | 1998-09-16 | Sumitomo Electric Industries, Ltd. | Triazole derivative and organic electroluminescent element produced therefrom |
EP1140840B1 (en) * | 1999-01-13 | 2006-03-22 | Bayer Pharmaceuticals Corp. | -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
JP2001018533A (ja) * | 1999-07-09 | 2001-01-23 | Ricoh Co Ltd | 感熱記録材料 |
JP2001105741A (ja) * | 1999-10-08 | 2001-04-17 | Oki Electric Ind Co Ltd | 熱可逆性記録材料および熱可逆性記録媒体 |
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WO2003037864A1 (fr) * | 2001-10-29 | 2003-05-08 | Japan Tobacco Inc. | Compose indolique, et utilisation a des fins therapeutiques |
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MXPA04010379A (es) * | 2002-04-23 | 2005-02-17 | Squibb Bristol Myers Co | Compuestos de pirrolo-triazina anilina utiles como inhibidores de cinasa. |
ATE402700T1 (de) * | 2002-08-27 | 2008-08-15 | Merck Patent Gmbh | Glycinamid-derivate als raf-kinase-hemmer |
CN1705645A (zh) * | 2002-10-24 | 2005-12-07 | 默克专利有限公司 | 作为raf-激酶抑制剂的亚甲基脲衍生物 |
CN1764645A (zh) * | 2003-03-24 | 2006-04-26 | 默克专利有限公司 | 作为raf-激酶抑制剂的草酰胺衍生物 |
-
2004
- 2004-11-11 EP EP04820392A patent/EP1692110A1/en not_active Withdrawn
- 2004-11-11 US US10/582,496 patent/US20070093529A1/en not_active Abandoned
- 2004-11-11 WO PCT/EP2004/012764 patent/WO2005058832A1/en active Application Filing
- 2004-11-11 CA CA002548571A patent/CA2548571A1/en not_active Abandoned
- 2004-11-11 AU AU2004299174A patent/AU2004299174A1/en not_active Abandoned
- 2004-11-11 JP JP2006543396A patent/JP2007515412A/ja active Pending
- 2004-12-10 AR ARP040104607A patent/AR048484A1/es unknown
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EP1692110A1 (en) | 2006-08-23 |
AU2004299174A1 (en) | 2005-06-30 |
WO2005058832A1 (en) | 2005-06-30 |
US20070093529A1 (en) | 2007-04-26 |
CA2548571A1 (en) | 2005-06-30 |
JP2007515412A (ja) | 2007-06-14 |
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