ES2320204T3 - Pirimidinas inhibidoras de cdk, su preparacion y su utilizacion como medicamentos. - Google Patents

Pirimidinas inhibidoras de cdk, su preparacion y su utilizacion como medicamentos. Download PDF

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Publication number
ES2320204T3
ES2320204T3 ES02738100T ES02738100T ES2320204T3 ES 2320204 T3 ES2320204 T3 ES 2320204T3 ES 02738100 T ES02738100 T ES 02738100T ES 02738100 T ES02738100 T ES 02738100T ES 2320204 T3 ES2320204 T3 ES 2320204T3
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Spain
Prior art keywords
alkyl
group
cycloalkyl
phenyl
hydroxy
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Expired - Lifetime
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ES02738100T
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Inventor
Thomas Brumby
Rolf Jautelat
Olaf Prien
Martina Schafer
Gerhard Siemeister
Ulrich Lucking
Christoph Huwe
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Bayer Pharma AG
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Bayer Schering Pharma AG
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Priority claimed from DE10127581A external-priority patent/DE10127581A1/de
Priority claimed from DE10212098A external-priority patent/DE10212098A1/de
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Publication of ES2320204T3 publication Critical patent/ES2320204T3/es
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    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3

Abstract

Compuestos de la fórmula general I** ver fórmula** en la que R1 significa halógeno R2 representa -CH(CH3)-(CH2)n-R 5 , -CH-(CH2OH)2, -(CH2)nR 7 , -CH(C3H7)-(CH2)n-R 5 , -CH(C2H5)-(CH2)n- R 5 , -CH 2-CN, -CH(CH 3)COCH 3, -CH(CH 3)-C(OH)(CH 3) 2, -CH(CH(OH)CH 3)OCH 3, -CH(C 2H 5)CO-R 5 , alquinilo de C 2-C 4, -(CH 2) n-COR 5 , -(CH 2) n-CO-alquilo de C 1-C 6, -(CH 2) n-C(OH)(CH 3)-fenilo (Ph), -CH (CH3)-C(CH3)-R 5 , -CH(CH3)-C(CH3)(C2H5)-R 5 , -CH(OCH3)-CH2-R 5 , -CH2-CH(OH)-R 5 , -CH(OCH3)- CHR 5 -CH3, -CH(CH3)-CH(OH)-CH2-CH=CH2, -CH(C2H5)-CH(OH)-(CH2)n-CH3, -CH(CH3)-CH(OH)- (CH2)n-CH3, -CH(CH3)-CH(OH)-CH(CH3)2, (CH2OAC)2, -(CH2)n-R 6 , -(CH2)n-(CF2)n-CF3, -CH(CH2)n- R 5 ) 2, -CH(CH 3)-CO-NH 2, -CH(CH 2OH)-fenilo,- CH(CH 2OH)-CH(OH)-(CH 2) nR 5 , -CH(CH 2OH)CH(OH)fenilo, -CH(CH 2OH)-C 2H 4-R 5 , -(CH 2) n-C*C-C(CH 3)=CH-COR 5 , -CH(Ph)-(CH 2) n-R 5 -(CH 2) n-COR 5 , -(CH2)nPO3(R 5 )2, -(CH2)n-COR 5 , -CH((CH2)nOR 5 )CO-R 5 , -(CH2)nCONHCH((CH2)nR 5 )2, -(CH2)nNH- COR 5 , -CH(CH2)nR 5 -(CH2)n-cicloalquilo de C3-C10, -(CH2)n-cicloalquilo de C3-C10, cicloalquilo de C3- C10, alquilo de C1-C6 eventualmente sustituido una vez o múltiples veces, de igual o diferente manera, con hidroxi, alquilo de C 1-C 6 o con el grupo -COONH(CH 2) nCH 3 o -NR 3 R 4 , cicloalquilo de C 3-C 10, -(CH 2) n-O- (CH 2)n-R 5 , -(CH 2) n-NR 3 R 4 , -CH(C 3H 7)-(CH 2) n-OC(O)-(CH 2) n-CH 3, -(CH 2) n-R 5 , -C(CH 3) 2-(CH 2) n-R 5 , -C (CH2)n(CH3)-(CH2)nR 5 , -C(CH2)n-(CH2)nR 5 , -CH(t-butil)-(CH2)n-R 5 , -CCH3(C3H7)-(CH2)nR 5 , -CH(C3H7)- (CH2)n-R 5 , -CH(C3H7)-COR 5 , -CH(C3H7)-(CH2)n-OC(O)-NH-Ph, -CH((CH2)n(C3H7))-(CH2)nR 5 , -CH (C3H7)-(CH2)n-OC(O)-NH-Ph(OR 5 )3, -NR 3 R 4 , -NH-(CH2)n-NR 3 R 4 , R 5 -(CH2)n-C*H-CH(R 5 )(CH2)n-R 5 , -(CH 2) n-CONH-(CH 2) n-CO-R 5 , -OC(O)NH-alquilo de C 1-C 6 o -(CH 2) n-CO-NH-(CH 2) n-CH-((CH 2) nR 5 ) 2, o representa un cicloalquilo de C 3-C 10, que está sustituido con el grupo** ver fórmula** o representa el grupo ** ver fórmula** X representa oxígeno o representa el grupo -NH- o -N(alquilo de C 1-C 3), o R 2 representa el grupo** ver fórmula** X y R 2 forman en común un grupo ** ver fórmula** A representa el grupo -SO 2R 7, SO 2-C 2H 4-OH, -SO 2CF 3 o -SO 2-NR 3 R 4 , B representa hidrógeno, hidroxi o alquilo de C1-C3 o A y B pueden formar en común un grupo ** ver fórmula** R 3 y R 4 representan, en cada caso independientemente uno de otro, hidrógeno, fenilo, benciloxi, alquilo de C1-C12, alcoxi de C1-C6, alqueniloxi de C2-C4, cicloalquilo de C3-C6, hidroxi, hidroxi-alquilo de C1-C6, dihidroxialquilo de C1-C6, heteroarilo, heterociclo-alquilo de C3-C10, heteroaril-alquilo de C1-C3, cicloalquil de C3- C 6-alquilo de C 1-C 3 eventualmente sustituido con ciano, o representan alquilo de C 1-C 6 eventualmente sustituido una vez o múltiples veces, de igual o diferente manera con fenilo, piridilo, feniloxi, cicloalquilo de C3-C6, alquilo de C1-C6 o con alcoxi de C1-C6, pudiendo el propio fenilo estar sustituido una vez o múltiples veces, de igual o diferente manera, con halógeno, trifluorometilo, alquilo de C1-C6, alcoxi de C1- C6 o con el grupo -SO2NR 3 R 4 , o representan el grupo -(CH 2) nNR 3 R 4 , -CNHNH 2 o -NR 3 R 4 o representan** ver fórmula** que eventualmente pueden estar sustituidos con alquilo de C 1-C 6, R 5 representa hidroxi, fenilo, alquilo de C1-C6, cicloalquilo C3-C6, benzoxi, alquiltio de C1-C6 o alcoxi de C1- C6, R 6 representa el grupo ** ver fórmula** R 7 representa halógeno, hidroxi, fenilo, alquilo de C1-C6, -(CH2)nOH, -NR 3 R 4 o el grupo R 8 , R 9 y R 10 representan hidrógeno, hidroxi, alquilo de C1-C6 o el grupo -(CH2)n-COOH, y n representa 0-6 así como sus diastereoisómeros, enantiómeros y sales.
ES02738100T 2001-05-29 2002-05-23 Pirimidinas inhibidoras de cdk, su preparacion y su utilizacion como medicamentos. Expired - Lifetime ES2320204T3 (es)

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