AR040250A1 - Compuestos de amidas de acido 3-amino-tieno(2,3-b)-piridino-2-carboxilico sustituido y procedimientos para prepararlos y sus usos - Google Patents

Compuestos de amidas de acido 3-amino-tieno(2,3-b)-piridino-2-carboxilico sustituido y procedimientos para prepararlos y sus usos

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Publication number
AR040250A1
AR040250A1 ARP030102022A ARP030102022A AR040250A1 AR 040250 A1 AR040250 A1 AR 040250A1 AR P030102022 A ARP030102022 A AR P030102022A AR P030102022 A ARP030102022 A AR P030102022A AR 040250 A1 AR040250 A1 AR 040250A1
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Argentina
Prior art keywords
phenylamino
alkyl
optionally substituted
phenyl
optionally
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Suspension/Interruption
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ARP030102022A
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English (en)
Inventor
Charles L Cywin
Zhidong Chen
Jonathan Emeigh
Roman Wolfgang Fleck
Ming Hong Hao
Eugene Richard Hickey
Will Weimin Liu
Daniel R Marshall
Tina Marie Morwick
Peter Allen Nemoto
Ronald J Sorcek
Sanxing Sun
Jiang-Ping Wu
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Boehringer Ingelheim Pharma GmbH Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Original Assignee
Boehringer Ingelheim Pharma GmbH Co KG
Boehringer Ingelheim Pharmaceuticals Inc
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Application filed by Boehringer Ingelheim Pharma GmbH Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of AR040250A1 publication Critical patent/AR040250A1/es
Suspension/Interruption legal-status Critical Current

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    • C08G63/00—Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
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Abstract

Compuestos que son útiles como inhibidores de la actividad de quinasa del complejo de IkB quinasa (IKK). Por lo tanto, los compuestos son útiles en el tratamiento de enfermedades mediadas por IKK que incluyen enfermedades inmunes, enfermedades inflamatorias y cáncer. Se describen también composiciones farmacéuticas que comprenden estos compuestos y procedimientos para preparar estos compuestos. Reivindicación 1: Un compuesto de fórmula (1), en la cual, R1 es: (a) fenilo o heteroarilo seleccionado entre furanilo, tienilo, piridilo, pirrolilo, imidazolilo y benzofuranilo, opcionalmente sustituidos con uno o dos R3; (b) heterociclilo seleccionado entre 1-piperidinilo, 1-piperazinilo, 1-pirrolidinilo y 4-morfolinilo, opcionalmente sustituidos con uno o dos grupos seleccionados entre alquilo C1-6, -CO2-alquilo(C1-5), fenilo, bencilo, -OH, y C(O)heteroarilo, en los que el grupo heteroarilo se selecciona entre furanilo, tienilo, piridilo y pirrolilo; (c) R6(CH2)mO-; (d) R6OCH2-; (e) R6(CH2)mNH-; (f) R6(CH2)p(CH=CH)m-; (g) alquilo C1-6, opcional, parcial o completamente halogenado y opcionalmente sustituido con uno a dos R9; (h) alcoxi C1-8, opcional, parcial o completamente halogenado y opcionalmente sustituido con uno a dos R9; (i) alquilo (C1-8)-S(O)n; opcional, parcial o completamente halogenado y opcionalmente sustituido con uno a dos R9; (j) -N(R4)(R5); o (k) -C(O)NHR´, en donde R´ es R6, piridilo o -CH3; R2 es (a) alquilo C1-6, opcional, parcial o completamente halogenado y opcionalmente sustituido con uno o dos R10; (b) alcoxi C1-6, opcional, parcial o completamente halogenado y opcionalmente sustituido con uno a dos R10; (c) alquilamino C1-6, opcional, parcial o completamente halogenado y opcionalmente sustituido con uno a dos R10, (d) alquiltio C1-6, opcional, parcial o completamente halogenado y opcionalmente sustituido con uno a dos R10; (e) heterociclil-(CH2)m- en donde dicho heterociclo se selecciona entre piperidinilo, piperazinilo, morfolinilo, azepanilo, pirrolidinilo, 1,4-diazacicloheptanilo, azepanilo, 2,5-diazabiciclo[2.2.1]heptanilo, oxazepanilo y tiomorfolino y está opcionalmente sustituido con uno o tres R7; (f) heterociclil-CH2O- en donde el heterociclilo se selecciona entre 1-piperidinilo, 1-piperazinilo, 4-morfolinilo y 1-pirrolidinilo, opcionalmente sustituido con alquilo C1-6; (g) fenilo, opcionalmente sustituido con uno o tres R3; (h) -N(R4)(R5); (i) heteroarilo seleccionado entre furanilo, tienilo, imidazolilo, piridilo y pirrolilo, o (j) -H; R3 se escoge entre alquilo C1-6, alcoxi C1-6, hidroxi-alquilo C1-6, halógeno, CN, -CO2H, -CO2-alquilo(C1-6), -S(O)n-alquilo(C1-6), -NO2, -OH, -CF3, -N(R4)(R5), -NHC(O)NH-alquilo (C1-6), -C(O)N(R4)(R5) y fenilo opcionalmente sustituido con halógeno, alquilo C1-6, -CN o alcoxi C1-6; R4 y R5 se seleccionan independientemente entre H, alquilo C1-6, -C(O)-alquilo(C1-6), -SO2-alquilo(C1-6), fenilo, piridilo, bencilo, piperidinilo, feniletilo y (CH3)3COC(O)-; R6 es un grupo fenilo opcionalmente sustituido con uno o dos grupos seleccionados entre halógeno, alquilo C1-6, -CN, -CO2-alquilo(C1-6), -C(O)NR4R5, -SO2NH2, -NO2, -OH, -NH2, CF3 y alcoxi C1-6 o R6 es cicloalquilo C3-6, -CH2OH, naftalen-2-ilo, naftalen-1-ilo o 2-tienilo; R7 se selecciona entre -OH, -CN, oxo, -CO2alquilo(C1-6), -CO2H, -C(O)N(R4)(R5), -N(R4)(R5), -CH2N(R4)(R5), -CH2OH, alquilo C1-6, CO2bencilo, hidroxialquilo C1-6, -C(O)-alquil(C1-6)N(R4)(R5), -NHCO2alquilo(C1-6), -NHC(O)N(R4)(R5), -S(O)nalquilo(C1-6), (CH3)3COC(O)-, fenilo, piridilo, H2NCH(R8)C(O)-, HO(CH2)mCH2CH(NH2)C(O)-, HOCH(R6)CH2NH- R6CH2CH(OH)CH2NH-, R6OCH2CH(OH)CH2NH- y -C(O)heterociclilo, en donde dicho heterociclilo se selecciona de piperidinilo, piperazinilo, morfolinilo y pirrolidinilo, o R7 es 2-hidroxietilamino, metilcarbamidoilo, hidroxiimino, hidrazinocarbonilo, sulfamoilo, metanosulfonilamino, metilsulfonilhidrazino, 2-hudroxipropilamino, 2,3-dihidroxipropilamino, 2-hidroxi-1-metiletilamino, carbamoilmetilamino, N´-fenilhidrazinocarbonilo o tolueno-4-sulfonilamino; R8 se selecciona entre alquilo C1-6, -(CH2)1-4NH2, fenilo o bencilo; R9 se selecciona entre oxo, -OH, NR4R5, -CO2H y alcoxi C1-6; R10 se selecciona entre oxo, -OH, -N(R4)(R5), alcoxi C1-6, -C(O)-alquilo(C1-6), -C(O)N(R4)(R5), R6 y heteroarilo seleccionado entre furanilo, tienilo, imidazolilo, piridilo, indolilo y pirrolilo; m es 0 o 1; n es 0, 1, o 2; y p es 0, 1, 2 o 3; y sus sales, ésteres, tautómeros, isómeros individuales y mezclas de isómeros farmacéuticamente aceptables; con la condición de que si R1 es fenilo o heteroarilo, alquilo C1-6, -CF3, -C(O)NR4R5 o heterociclilo, entonces R2 no es alquilo C1-6, fenilo, heteroarilo, -CF3 o H.
ARP030102022A 2002-06-06 2003-06-06 Compuestos de amidas de acido 3-amino-tieno(2,3-b)-piridino-2-carboxilico sustituido y procedimientos para prepararlos y sus usos Suspension/Interruption AR040250A1 (es)

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US38631202P 2002-06-06 2002-06-06
US45786703P 2003-03-26 2003-03-26

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AR040250A1 true AR040250A1 (es) 2005-03-23

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KR (1) KR20050005548A (es)
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AR (1) AR040250A1 (es)
AT (1) ATE415966T1 (es)
AU (1) AU2003237330A1 (es)
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