PE20070811A1 - Analogos de arilpropionamida, arilacrilamida, arilpropinamida, o arilmetilurea como inhibidores del factor xia - Google Patents

Analogos de arilpropionamida, arilacrilamida, arilpropinamida, o arilmetilurea como inhibidores del factor xia

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Publication number
PE20070811A1
PE20070811A1 PE2006001610A PE2006001610A PE20070811A1 PE 20070811 A1 PE20070811 A1 PE 20070811A1 PE 2006001610 A PE2006001610 A PE 2006001610A PE 2006001610 A PE2006001610 A PE 2006001610A PE 20070811 A1 PE20070811 A1 PE 20070811A1
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Prior art keywords
phenyl
chloro
tromboembolic
indazol
propionamide
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PE2006001610A
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English (en)
Inventor
Donald J Pinto
Joanne M Smallheer
James R Corte
Zilun Hu
Cavallaro L Cullen
Paul Gilligan
Mimi L Quan
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Bristol Myers Squibb Co
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Publication of PE20070811A1 publication Critical patent/PE20070811A1/es

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Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE A ES UN CARBOCICLO(C3-C10) O UN HETEROCICLO DE 5 A 12 MIEMBROS SUSTITUIDOS CON 0-1 R1 O 0-3 R2, DONDE R1 ES F, Cl, Br, CF3, ENTRE OTROS; R2 ES =O, F, Cl, CN, NO2, ENTRE OTROS; L1 ES -CH2CH2-, -CH=CH-, OCH2, ENTRE OTROS; M ES UN COMPUESTO DE FORMULA (a), (b), ENTRE OTROS, DONDE R3 ES (CH2)r-CARBOCICLO(C3-C10) O (CH2)r-HETEROCICLO DE 5 A 12 MIEMBROS SUSTITUIDOS CON 0-3 R3a O 0-1 R3d, EN DONDE R3a ES =O, F, I, NO2, ENTRE OTROS; R3d ES H, F, CN, NO2, ENTRE OTROS; r ES DE 0 A 4; R4 ES H, F, Cl, Br, CF3, ENTRE OTROS; R11 ES HALOALQUILO(C1-C4), -C(O)Ra, -CH2C(O)Ra, ENTRE OTROS, DONDE Ra ES H, CF3, ALQUILO(C1-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-{(S)-1-[4-(3-AMINO-1H-INDAZOL-6-IL)-5-CLORO-1H-IMIDAZOL-2-IL]-2-FENIL-ETIL}-3-(2,4-DIFLUORO-FENIL)-PROPIONAMIDA, N-{(S)-1-[4-(3-AMINO-1H-INDAZOL-6-IL)-5-CLORO-1H-IMIDAZOL-2-IL]-2-FENIL-ETIL}-3-(2-METOXI-FENIL)-PROPIONAMIDA, N-{(S)-1-[4-(3-AMINO-1H-INDAZOL-6-IL)-5-CLORO-1H-IMIDAZOL-2-IL]-2-FENIL-ETIL}-3-(2-CLORO-FENIL)-PROPIONAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES SELECTIVOS DE ENZIMAS DE SERINA PROTEASA DE LA CASCADA DE COAGULACION TAL COMO TROMBINA, FACTOR XIa, FACTOR Xa, ENTRE OTROS, SIENDO UTILES PARA EL TRATAMIENTO DE TRANSTORNOS TROMBOEMBOLICOS TAL COMO ANGINA INESTABLE, ATEROESCLEROSIS, TROMBOSIS VENOSA, TROMBOFLEBITIS
PE2006001610A 2005-12-14 2006-12-14 Analogos de arilpropionamida, arilacrilamida, arilpropinamida, o arilmetilurea como inhibidores del factor xia PE20070811A1 (es)

Applications Claiming Priority (3)

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US75013005P 2005-12-14 2005-12-14
US82116306P 2006-08-02 2006-08-02
US86521106P 2006-11-10 2006-11-10

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PE20070811A1 true PE20070811A1 (es) 2007-08-13

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US (4) US7626039B2 (es)
EP (1) EP1981854B1 (es)
JP (1) JP5225098B2 (es)
KR (1) KR20080087817A (es)
AR (1) AR058379A1 (es)
AT (1) ATE511502T1 (es)
AU (1) AU2006325754B2 (es)
BR (1) BRPI0620010A2 (es)
CA (1) CA2633252A1 (es)
EA (1) EA014245B1 (es)
IL (1) IL192033A0 (es)
NO (1) NO20082444L (es)
NZ (1) NZ568595A (es)
PE (1) PE20070811A1 (es)
TW (1) TW200730477A (es)
WO (1) WO2007070826A1 (es)

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