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Cephalosporins as antibacterial agents
专利权人:
PFIZER INC.
发明人:
申请号:
ARP120101502
公开号:
AR086204A1
申请日:
2012.04.27
申请国别(地区):
AR
年份:
2013
代理人:
摘要:
This provides cephalosporins Derivatives of the formula (1), its use for the treatment of infections in Mammals, Pharmaceutical composition containing the compounds and Methods for the preparation of these compounds.Claim 1: a compound of the formula (1) or a pharmaceutically acceptable Salt thereof, wherein: R1 is nr4r5 so2r6 -, -, - C (= o) nr4r4 SR4, - S, - (c = o) - o (R4, R4 (c = S), SC (= or or4), SC (= o) - nhr4, SP (= o) (OR 2 or4); r1 is alkyl substituted C1 - 8 - SR4, S - (c = o) - o (R4, R4 (c = S), SC (= o) - (= or4, SC (o) NH R4, SP (= o) (or4) 2 - (c = o) - nr4r5, so2r6; or - C1 R1 is alkyl or substituted with - 8 - SR4, S - (c = o) RS - (c = o) - (R4 = or4 or SC), SC (= o) - nhr4, SP (= o) (or4) 2 - (c = o) - nr4r5, or so2r6; R2 and R3 are independently - H, - CN, - Oh, Halo, NO2 -, alkyl - or - C1 - 10, 10 - N - alkyl C1, (R4); 2 or R1 and R3 together with the carbons to which together form an aryl or heteroaryl; R4 is H or alkyl of C1 - 10; R5 is so2r4 -, - C (= o) alkyl C1 - 10; R6 is H, alkyl or C1 - 6, in each nr4r4 Presence;C1 is optionally substituted alkyl - 10 to - Oh, - CN, - NO2, Halo, alkyl - or - C1 - 6, - SH, - S - S c1-4 alkyl, - (c = o) c1-4 alkyl or alkyl of C1 (c = o) - 4; and N is 1, 2, or 3.La presente proporciona derivados de cefalosporinas de la fórmula (1), su uso para el tratamiento de infecciones en mamíferos, composición farmacéutica que contiene estos compuestos y métodos para la preparación de estos compuestos.Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: R1 es -NR4R5, -SO2R6, -C(=O)NR4R4, -SR4, -S(C=O)R4, -S(C=S)R4, -SC(=O)OR4, SC(=O)NHR4, -SP(=O)(OR4)2; o R1 es -alquilo C1-8 sustituido con -SR4, -S(C=O)R4, -S(C=S)R4, -SC(=O)OR4, -SC(=O)NHR4, -SP(=O)(OR4)2, -C(=O)NR4R5, -SO2R6; o R1 es -O-alquilo C1-8 sustituido con -SR4, -S(C=O)R4, -S(C=S)R4, -SC(=O)OR4, -SC(=O)NHR4, -SP(=O)(OR4)2, -C(=O)NR4R5, o -SO2R6; R2 y R3 son de manera independiente -H, -OH, -CN, halo, -
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