AR035851A1 - 3-cianoquinolinas, 3-ciano-1,6-naftiridinas y 3-ciano-1,7-naftiridinas como inhibidoras de proteina quinasas - Google Patents

3-cianoquinolinas, 3-ciano-1,6-naftiridinas y 3-ciano-1,7-naftiridinas como inhibidoras de proteina quinasas

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AR035851A1
AR035851A1 ARP010101423A ARP010101423A AR035851A1 AR 035851 A1 AR035851 A1 AR 035851A1 AR P010101423 A ARP010101423 A AR P010101423A AR P010101423 A ARP010101423 A AR P010101423A AR 035851 A1 AR035851 A1 AR 035851A1
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Argentina
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nhr5
r6oc
nhc
conh2
optionally substituted
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ARP010101423A
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Wyeth Corp
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Abstract

Estos compuestos resultan útiles como agentes antineoplásicos y en el tratamiento de la osteoporosis y la enfermedad poliquística renal. Reivindicación 1: Un compuesto de la Fórmula (1), en la cual X es -NH-, -NR5- -O- ó -S(O)m-; n es un entero de valor 0 ó 1; m es un entero de valor 0 a 2; q es un entero de valor 0 a 1; p es un entero de valor 2 a 5; s es un entero de valor 0 a 5; r es un entero de valor 0 a 5; J es halógeno; A es -(C(R9)2)r-, -C(O)-, -C(O)(C(R9)2)r-, -(C(R9)2)rRC(O)-, cicloalquilo o está ausente; T y Z son, cada uno independientemente, carbono o N, siempre que T y Z no sean simultáneamente N; R1 se selecciona entre: un anillo cicloalquilo C3-10 sustituido opcionalmente con uno o más grupos alquilo de 1 a 6 átomos seleccionados independientemente; arilo C6-12 sustituido opcionalmente con 1 a 4 sustituyentes que pueden ser iguales o diferentes, seleccionados independientemente entre los grupos -H, -J, -NO2, -NH2, -OH, -SH, -CN, -N3, -COOH, -CONH2, -NHC(O)NH2, -C(O)H, -CF3, -OCF3, -R5, -OR5, -NHR5, -Q, -S(O)mR5, -NHSO2R5, -R6OH, -R6OR5, -R6NH2, -R6NHR5, -R6Q, -R6SH, -R6S(O)mR5, -NHR7OH, -NHR7OR5, -N(R5)R7OH, -N(R5)R7OR5, -NHR7NH2, -NHR7NHR5, -NHR7Q, -N(R5)R7NH2, -N(R5)R7NR5, -N(R5)R7Q, -OR7OH, -OR7OR5, -OR7NH2, -OR7NHR5, -OR7Q, -OC(O)R5, -NHC(O)R5, -NHC(O)NHR5, -OR6C(O)R5, -NHR6C(O)R5, -C(O)R5, -C(O)NHR5, -C(O)Q, -R6C(O)H, -R6C(O)R5, -R6C(O)OH, -R6C(O)OR5, -R6C(O)NH2, -R6C(O)NHR5, -R6C(O)Q, -R6OC(O)R5, -R6OC(O)NH2, -R6OC(O)NHR5, -R6OC(O)Q e YR8 en el cual Y se selecciona independientemente entre -C(O)-, -C(O)O-, -OC(O)-, -C(O)NH-, -NHC(O)-, -NHSO2-, -SO2NH-, -C(OH)H-, -O(C(R9)2)q-, -S(O)m(C(R9)2)q-, -NH-(C(R9)2)q-, -NR10(C(R9)2)q-, -(C(R9)2)q-, -(C(R9)2)rO-, -(C(R9)2)q-S(O)m, -(C(R9)2)qNH-, -(C(R9)2)qNR10-, -CsC-, cis y trans -C=C- y cicloalquilo C3-10; un anillo heteroarilo de 5 ó 6 miembros que contenga de 1 a 4 heteroátomos o en particular 1 ó 2 heteroátomos que pueden ser iguales o diferentes, seleccionados entre N, O y S, en el cual el anillo heteroarilo puede estar opcionalmente sustituido con 1 a 4 sustituyentes que pueden ser iguales o diferentes seleccionados entre los grupos -H, -J, -NO2, -NH2, -OH, -SH, -CN, -N3, -COOH, -CONH2, -NHC(O)NH2, -C(O)H, -CF3, -OCF3, -R5, -OR5, -NHR5, -Q, -S(O)mR5, -NHSO2R5, -R6OH, -R6OR5, -R6NH2, -R6NHR5, -R6Q, -R6SH, -R6S(O)mR5, -NHR7OH, -NHR7OR5, -N(R5)R7OH, -N(R5)R7OR5, -NHR7NH2, -NHR7NHR5, -NHR7Q, -N(R5)R7NH2, -N(R5)R7NR5, -N(R5)R7Q, -OR7OH, -OR7OR5, -OR7NH2, -OR7NHR5, -OR7Q, -OC(O)R5, -NHC(O)R5, -NHC(O)NHR5, -OR6C(O)R5, -NHR6C(O)R5, -C(O)R5, -C(O)NHR5, -C(O)Q, -R6C(O)H, -R6C(O)R5, -R6C(O)OH, -R6C(O)OR5, -R6C(O)NH2, -R6C(O)NHR5, -R6C(O)Q, -R6OC(O)R5, -R6OC(O)NH2, -R6OC(O)NHR5, -R6OC(O)Q y YR8 en el cual Y se selecciona independientemente entre -C(O)-, -C(O)O-, -OC(O)-, -C(O)NH-, -NHC(O)-, -NHSO2-, -SO2NH-, -C(OH)H-, -O(C(R9)2)q-, -S(O)m(C(R9)2)q-, -NH-(C(R9)2)q-, -NR10(C(R9)2)q-, -(C(R9)2)q- -(C(R9)2)rO-, -(C(R9)2)q-S(O)m, -(C(R9)2)qNR10-, -CsC-, cis y trans -C=C- y cicloalquilo C3-10; un sistema de anillos heteroarilo bicíclico que posea entre 8 y 20 átomos que contenga de 1 a 4 heteroátomos, que pueden ser iguales o diferentes, seleccionados entre N, O y s, en el cual el sistema de anillos heteroarilo bicíclico puede estar opcionalmente sustituido con 1 a 4 sustituyentes que pueden ser iguales o diferentes seleccionados entre los grupos -H, -J, -NO2, -NH2, -OH, -SH, -CN, -N3, -COOH, -CONH2, -NHC(O)NH2, -C(O)H, -CF3, -OCF3, -R5, -OR5, -NHR5, -Q, -S(O)mR5, -NHSO2R5, -R6OH, -R6OR5, -R6NH2, -R6NHR5, -R6Q, -R6SH, -R6S(O)mR5, -NHR7OH, -NHR7OR5, -N(R5)R7OH, -N(R5)R7OR5, -NHR7NH2, -NHR7NHR5, -NHR7Q, -N(R5)R7NH2, -N(R5)R7NHR5, -N(R5)R7Q, -OR7OH, -OR7OR5, -OR7NH2, -OR7NHR5, -OR7Q, -OC(O)R5, -NHC(O)R5, -NHC(O)NHR5, -OR6C(O)R5, -NHR6C(O)R5, -C(O)R5, -C(O)NHR5, -C(O)Q, -R6C(O)H, -R6C(O)R5, -R6C(O)OH, -R6C(O)OR5, -R6C(O)NH2, -R6C(O)NHR5, -R6C(O)Q, -R6OC(O)R5, -R6OC(O)NH2, -R6OC(O)NHR5, -R6OC(O)Q y YR8 en el cual Y se selecciona independientemente entre -C(O)-, -C(O)O-, -OC(O)-, -C(O)NH-, -NHC(O)-, -NHSO2-, -SO2NH-, -C(OH)H-, -O(C(R9)2)q-, -S(O)m(C(R9)2)q-, -NH-(C(R9)2)q-, -NR10(C(R9)2)q-, -(C(R9)2)q- -(C(R9)2)rO-, -(C(R9)2)q-S(O)m, -(C(R9)2)qNR10-, -CsC-, cis y trans -C=C- y cicloalquilo C3-10; y un grupo de fórmula (2), en donde E es -NH-, -NR5-, -O-, -S(O)m-, -C(O)-, -CH2-, -CHR5- ó -CR5R5-; Q es -NR5R5 y además siempre que cada R5 se seleccione independientemente entre alquilo y alquenilo, R5R5 pude tomarse opcionalmente en forma conjunta con el átomo de nitrógeno al cual están unidos formando un anillo heterociclo de entre 3 y 8 átomos, conteniendo opcionalmente 1 ó 2 heteroátomos adicionales, que pueden ser iguales o diferentes, seleccionados entre N, O y S; R1a, R1b, R1c, R1d y R1e se seleccionan cada uno, independientemente entre -H, -J, -NO2, -NH2, -OH, -SH, -CN, -N3, -COOH, -CONH2, -NHC(O)NH2, -C(O)H, -CF3, -OCF3, -R5, -OR5, -NHR5, -Q, -S(O)mR5, -NHSO2R5, -R6OH, -R6OR5, -R6NH2, -R6NHR5, -R6Q, -R6SH, -R6S(O)mR5, -NHR7OH, -NHR7OR5, -N(R5)R7OH, -N(R5)R7OR5, -NHR7NH2, -NHR7NHR5, -NHR7Q, -N(R5)R7NH2, -N(R5)R7NR5, -N(R5)R7Q, -OR7OH, -OR7OR5, -OR7NH2, -OR7NHR5, -OR7Q, -OC(O)R5, -NHC(O)R5, -NHC(O)NHR5, -OR6C(O)R5, -NHR6C(O)R5, -C(O)R5, -C(O)NHR5, -C(O)Q, -R6C(O)H, -R6C(O)R5, -R6C(O)OH, -R6C(O)OR5, -R6C(O)NH2, -R6C(O)NHR5, -R6C(O)Q, -R6OC(O)R5, -R6OC(O)NH2, -R6OC(O)NHR5, arilo, -CH2-arilo, NH-arilo, -O-arilo, S(O)m-arilo, -OR11 y -R6OC(O)Q; R2a, R2b y R2c se seleccionan cada uno, independientemente entre -H, -arilo, -CH2-arilo, -NH-arilo, -O-arilo, -S(O)m-arilo, -J, -NO2, -OH, -SH, -CN, -N3, -COOH, -CONH2, -NHC(O)NH2, -C(O)H, -CF3, -OCF3, -R5, -OR5, -S(O)mR5, -NHSO2R5, -R11, -OR11, -R6OH, -R6OR5, -R6SH, -R6S(O)mR5, -OR7OH, -OR7OR5, -OC(O)R5, -NHC(O)R5, -NHC(O)NHR5, -OR6C(O)R5, -NHR6C(O)R5, -C(O)R5, -C(O)OR5, -C(O)NHR5, -C(O)Q, -R6C(O)H, -R6C(O)R5, -R6C(O)OH, -R6C(O)OR5, -R6C(O)NH2, -R6C(O)NHR5, -R6C(O)Q, -R6OC(O)R5, -R6OC(O)NH2, -R6OC(O)NHR5, -R6OC(O)Q, -G-(C(R9)2)p-R12, -(C(R9)2)q-R12, R18-CONH(CH2)r-, R18CsC-CONH(CH2)r-, N(R18)2C(O)O(CH2)r-, N(R18)2C(O)NH(CH2)r-, N(R18)2C(S)NH(CH2)r-, R18OC(O)NH(CH2)r-, C(R18)2=C(R18)CONH(CH2)r y -C(R18)2=C(R18)SO2NH(CH2)r-; G es -NH-, -NR10-, -O- ó -S(O)m-; R3 se selecciona entre: alquenilo C2-6, opcionalmente sustituido con uno o más entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; alquinilo C2-6, sustituido opcionalmente con un o más entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; arilo C6-12 sustituido opcionalmente con 1 a 4 sustituyentes que pueden ser iguales o diferentes, seleccionado entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; un anillo heteroarilo de 5 ó 6 átomos que contenga 1 a 4 heteroátomos o en particular 1 ó 2 heteroátomos que pueden ser iguales o diferentes, seleccionados entre N, O y S, en donde el anillo heteroarilo puede estar opcionalmente sustituido con 1 a 4 sustituyentes que pueden ser iguales o diferentes, seleccionados entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; un sistema de anillos heteroarilo bicíclico que posea entre 8 y 20 átomos que contenga de 1 a 4 heteroátomos, que pueden ser iguales o diferentes seleccionados entre N, O y S, en el cual el sistema de anillos heteroarilo bibíclico puede estar opcionalmente sustituido con 1 a 4 sustituyentes que pueden ser iguales o diferentes seleccionados entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; R4 se selecciona entre -(C(R9)2)rH, opcionalmente sustituido con uno o más de entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; alquenilo C2-6, opcionalmente sustituido con uno o más entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; alquinilo C2-6, sustituido opcionalmente con uno o más entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; arilo C6-12 sustituido opcionalmente con 1 a 4 sustituyentes que pueden ser iguales o diferentes, seleccionados entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R9)2)qNH2, -(C(R9)2)rH, -G(C(R9)2)pOR10, -G(C(R9)2)pR12 y -G(C(R9)2)pOH; un anillo heteroarilo de 5 ó 6 átomos que contenga 1 a 4 heteroátomos o en particular 1 ó 2 heteroátomos que pueden ser iguales o diferentes, seleccionados entre N, O y S, en donde el anillo heteroarilo puede estar opcionalmente sustituido con 1 a 4 sustituyentes que pueden ser iguales o diferentes, seleccionados entre -R10, -(C(R9)2)s-R12, -CHO, 1,3-dioxolano, -NO2, -CN, -CO2H, -CONH2, -CO2R10, -CONHR10, -COR10, -(C(R9)2)q-OH, -(C(R9)2)qOR10, -(C(R9)2)qNHR10, -(C(R9)2)qJ, -(C(R
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Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7067532B2 (en) * 2000-11-02 2006-06-27 Astrazeneca Substituted quinolines as antitumor agents
EP1409481B1 (en) 2001-07-16 2006-10-04 Astrazeneca AB Quinoline derivatives and their use as tyrosine kinase inhibitors
TWI275390B (en) * 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
US20040204458A1 (en) 2002-08-16 2004-10-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of Lck inhibitors for treatment of immunologic diseases
DE10237423A1 (de) * 2002-08-16 2004-02-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verwendung von LCK-Inhibitoren für die Behandlung von immunologischen Erkrankungen
CL2003002287A1 (es) * 2002-11-25 2005-01-14 Wyeth Corp COMPUESTOS DERIVADOS DE TIENO[3,2-b]-PIRIDINA-6-CARBONITRILOS Y TIENEO[2,3-b]-PIRIDINA-5-CARBONITRILOS, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION Y COMPUESTOS INTERMEDIARIOS, Y SU USO EN EL TRATAMIENTO DEL CANCER, APOPLEJIA, OSTEOPOROSIS
US7276519B2 (en) 2002-11-25 2007-10-02 Wyeth Thieno[3,2-b]pyridine-6-carbonitriles and thieno[2,3-b]pyridine-5-carbonitriles as protein kinase inhibitors
DE10318690B3 (de) * 2003-04-24 2004-11-11 Merck Patent Gmbh Verfahren zur Herstellung von Nicotinaldehyden
TW200510271A (en) * 2003-08-08 2005-03-16 Ube Industries Alkynyl substituded condensed heterocyclic compound, method for producing the same and organic electroluminescence element using the same
US7365203B2 (en) * 2003-09-15 2008-04-29 Wyeth Process for the synthesis of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile
AU2003291245A1 (en) * 2003-11-06 2004-06-06 Wyeth 4-anilino-3-quinolinecarbonitriles for the treatment of chronic myelogenous leukemia (cml)
WO2005118543A1 (ja) * 2004-06-03 2005-12-15 Ono Pharmaceutical Co., Ltd. キナーゼ阻害薬およびその用途
JP2008501696A (ja) 2004-06-04 2008-01-24 アンフォラ ディスカバリー コーポレーション Ａｔｐ利用酵素阻害活性を示すキノリンおよびイソキノリン系化合物、ならびにその組成物および使用
US7479561B2 (en) * 2004-08-16 2009-01-20 Wyeth 4-(2,4-dichloro-5-methoxyphenyl)amino-6-methoxy-7-{[5-substituted-amino)methyl]-3-furyl}-3-quinolinecarbonitriles as kinase inhibitors
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
CN1830964B (zh) * 2005-03-11 2011-06-15 中国科学院上海药物研究所 4-取代苯氨基-3-硝基喹啉类化合物及其制备方法和用途
JP2009526048A (ja) * 2006-02-08 2009-07-16 ワイス パラジウム媒介カップリング反応を介する７−アルケニル−３キノリンカルボニトリルの調製
TW200829555A (en) * 2006-11-10 2008-07-16 Astrazeneca Ab Chemical compounds
US20080293712A1 (en) * 2007-03-05 2008-11-27 Wyeth Benzo[C][2,7]Naphtyridine Derivatives, Methods of Making Thereof and Methods of Use Thereof
US7829574B2 (en) * 2008-05-09 2010-11-09 Hutchison Medipharma Enterprises Limited Substituted quinazoline compounds and their use in treating angiogenesis-related diseases
WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
NZ600857A (en) 2010-01-29 2014-06-27 Boehringer Ingelheim Int Substituted naphthyridines and their use as syk kinase inhibitors
CN102649778A (zh) * 2011-02-23 2012-08-29 苏州波锐生物医药科技有限公司 喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途
EA024845B1 (ru) * 2011-07-26 2016-10-31 Бёрингер Ингельхайм Интернациональ Гмбх Замещенные хинолины и их применение в качестве лекарственных средств
WO2014086284A1 (zh) * 2012-12-04 2014-06-12 上海医药集团股份有限公司 一类氘代3-氰基喹啉类化合物、其药用组合物、制备方法及其用途
CA2900652C (en) 2013-02-15 2021-05-04 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
WO2014130612A1 (en) 2013-02-20 2014-08-28 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
MX355330B (es) 2013-11-01 2018-04-16 Kala Pharmaceuticals Inc Formas cristalinas de compuestos terapeuticos y sus usos.
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
WO2015086523A1 (en) * 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused bicyclic heteroaromatic derivatives as modulators of tnf activity
CN104151216B (zh) * 2014-08-22 2016-08-17 山东铂源药业有限公司 一种拉帕替尼侧链的合成方法
JP6559785B2 (ja) 2014-12-15 2019-08-14 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン Ｅｇｆｒ及びｐｉ３ｋの小分子阻害剤
WO2017003995A1 (en) * 2015-06-29 2017-01-05 Merck Patent Gmbh TBK/IKKε INHIBITOR COMPOUNDS AND USES THEREOF
EP3509422A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
CN109688818A (zh) 2016-09-08 2019-04-26 卡拉制药公司 治疗化合物的晶型及其用途
EP3509423A4 (en) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
US20220229072A1 (en) 2019-06-04 2022-07-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
MX2023007550A (es) 2020-12-22 2023-11-14 Mekanistic Therapeutics Llc Compuestos de aminobencil heteroarilo sustituidos como inhibidores de receptor de factor de crecimiento epidermico (egfr) y/o fosfoinositol 3-cinasa (pi3k).

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU733551B2 (en) * 1996-09-25 2001-05-17 Astrazeneca Ab Qinoline derivatives inhibiting the effect of growth factors such as VEGF
UA73073C2 (uk) * 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
SK284846B6 (sk) * 1998-09-29 2005-12-01 Wyeth Holdings Corporation Deriváty substituovaného 3-kyanochinolínu, spôsob ich prípravy, ich použitie a farmaceutický prostriedok s ich obsahom
ES2457396T3 (es) * 1998-09-29 2014-04-25 Wyeth Holdings Llc 3-Cianoquinolinas sustituidas como inhibidores de las proteínas tirosina quinasas

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ES2291311T3 (es) 2008-03-01
TWI297007B (en) 2008-05-21
JP2003528857A (ja) 2003-09-30
CA2404662A1 (en) 2001-10-04
DE60130200T2 (de) 2008-03-13
EP1268431B1 (en) 2007-08-29
EP1268431A1 (en) 2003-01-02
DK1268431T3 (da) 2007-12-10
CN1419545A (zh) 2003-05-21
ATE371647T1 (de) 2007-09-15
BR0109650A (pt) 2003-04-22
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