PE20060493A1 - Compuestos derivados de bifenil (di o tri) carboxamidas como inhibidores de serina/treonina quinasa p38 - Google Patents

Compuestos derivados de bifenil (di o tri) carboxamidas como inhibidores de serina/treonina quinasa p38

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Publication number
PE20060493A1
PE20060493A1 PE2005001166A PE2005001166A PE20060493A1 PE 20060493 A1 PE20060493 A1 PE 20060493A1 PE 2005001166 A PE2005001166 A PE 2005001166A PE 2005001166 A PE2005001166 A PE 2005001166A PE 20060493 A1 PE20060493 A1 PE 20060493A1
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PE
Peru
Prior art keywords
methyl
alkyl
cycloalkyl
serine
inhibitors
Prior art date
Application number
PE2005001166A
Other languages
English (en)
Inventor
Jeffrey Charles Boehm
James Francis Callahan
Hongxing Yang
Zehong Wang
Original Assignee
Smithkline Beecham Corp
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Filing date
Publication date
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20060493A1 publication Critical patent/PE20060493A1/es

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    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
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Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) EN DONDE R1 ES H, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON HALOGENO, CICLOALQUILO(C3-C7), ALCOXI(C1-C6), ENTRE OTROS; R2 ES H, ALQUILO(C1-C6) O -(CH2)P-CICLOALQUILO(C3-C7) OPCIONALMENTE SUSTITUIDO CON UNO O MAS GRUPOS ALQUILO(C1-C6) EN DONDE P ES 0 A 2; R3 ES HALOGENO O METILO; R4 ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C7), ENTRE OTROS; R8 ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C7), OPCIONALMENTE SUSTITUIDO; Y E X SE SELECCIONA INDEPENDIENTEMENTE ENTRE H, METILO Y HALOGENO; Z ES -(CH2)SCOOR16 O -(CH2)SCONR16R17, DONDE S ES 0 A 4, R16 Y R17 JUNTO CON NITROGENO FORMAN UN ANILLO DE 5 A 6 MIEMBROS OPCIONALMENTE SUSTITUIDO. SON COMPUESTOS PREFERIDOS: ACIDO 5'-[(CICLOPROPILAMINO)CARBONIL]-4-{[(2,2-DIMETILPROPIL)AMINO]-CARBONIL}-3'-FLUORO-2'-METIL-2-BIFENILCARBOXILICO, N2-[(1S)-1-CICLOHEXILETIL]-N3'-CICLOPROPIL-N4-(2,2-DIMETILPROPIL)-5'-FLUORO-6'-METIL-2,3',4-BIFENILTRICARBOXAMIDA, N3-CICLOPROPIL-N4'-(2,2-DIMETILPROPIL)-5-FLUORO-2'-[(4-HIDROXI-1-PIPERIDINIL)CARBONIL]-6-METIL-3,4'-BIFENILDICARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA SERINA/TREONINA QUINASA P38 SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES COMO ARTRITIS REUMATOIDE, ATEROSCLEROSIS
PE2005001166A 2004-10-05 2005-10-03 Compuestos derivados de bifenil (di o tri) carboxamidas como inhibidores de serina/treonina quinasa p38 PE20060493A1 (es)

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US61606504P 2004-10-05 2004-10-05
US71972905P 2005-09-22 2005-09-22

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EP (1) EP1805132A4 (es)
JP (1) JP2008515898A (es)
AR (1) AR055271A1 (es)
PE (1) PE20060493A1 (es)
TW (1) TW200628153A (es)
WO (1) WO2006110173A2 (es)

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EP2080750B1 (en) 2006-11-02 2020-07-29 Mitsubishi Gas Chemical Company, Inc. Radiation-sensitive composition
JP5446118B2 (ja) * 2007-04-23 2014-03-19 三菱瓦斯化学株式会社 感放射線性組成物
EP1992344A1 (en) 2007-05-18 2008-11-19 Institut Curie P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation
RU2456266C1 (ru) * 2011-04-06 2012-07-20 Максим Эдуардович Запольский Производные 4,4'-бифениламидов, обладающие фармакологической активностью, и лекарственные средства на их основе
WO2016029216A2 (en) * 2014-08-22 2016-02-25 Biocryst Pharmaceuticals, Inc. Method for producing amidine derivatives
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