Abstract:
Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula selected from the group consisting of (I), (II), (III), (IV) and (V), compositions comprising a therapeutically eff ective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically effective amount of a compound of formulas (I)-(V).
Abstract:
Un compuesto seleccionado del grupo formado por un compuesto de **fórmula** o una sal, solvato, éster o profármaco del mismo farmacéuticamente aceptable, donde o bien: (a) Y y Z tomados juntos definen un grupo X, y X se selecciona del grupo formado por (1) =O, (2) =N-OH, (3) =N-O-R1 donde R1 se selecciona del grupo formado por (a) alquilo C1-C12 no sustituido, (b) alquilo C1-C12 sustituido con arilo, (c) alquilo C1-C12 sustituido con arilo sustituido, (d) alquilo C1-C12 sustituido con heteroarilo, (e) alquilo C1-C12 sustituido con heteroarilo sustituido, (f) cicloalquilo C3-C12, y (g) -Si-(R2)(R3)(R4) donde R2, R3 y R4 se seleccionan cada uno independientemente entre alquilo C1- C12 y arilo; o cualquier par de sustituyentes, que consta de AB, AD, AE, BD, BE o DE, se toma junto con el átomo o átomos a los que están anclados para formar un anillo de 3 a 7 miembros que contiene opcionalmente una heterofunción seleccionada del grupo formado por -O-, -NH-, -N(alquilo C1-C6-)-, -N(arilalquilo C1-C6-)-, -N(arilalquilo C1-C6 sustituido-)-, -N(heteroarilalquilo C1-C6-)-, -N(heteroarilaquilo C1-C6 sustituido-)-, -S- o -S(O)n-, donde n es 1 o 2, -C(O)-NH, -C(O)-NR12-, donde R12 se selecciona del grupo formado hidrógeno, alquilo C1-C3, alquilo C1-C3 sustituido con arilo, arilo sustituido, heteroarilo, o heteroarilo sustituido, -NH-C(O)-, y -NR12-C(O)-.
Abstract:
The instant invention provides novel macrolide compounds and compositions useful in treating bacterial infections. Also provided are processes for preparing same. These macrolides are substituted on the 6-O-position with X'-Y'-Z', wherein X' is selected from the group consisting of C1-C10 alkyl, C3-C10 alkenyl, and C3-C10 alkynyl; Y' and Z' are independently selected from the group consisting of: (c) optionally substituted aryl, and (d) optionally substituted heteroaryl, with the proviso that both Y' and Z' are not both phenyl, and with the further proviso that Y' is not isoxazole when Z' is thiophenyl.
Abstract:
Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula selected from the group consisting of (I), (II), (III), (IV) and (V), compositions comprising a therapeutically eff ective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically effective amount of a compound of formulas (I)-(V).
Abstract:
يتعلقهذاالاختراعبمركباتإريثروميسينمتعددةالحلقةجديدةوأملاحهاواستراتهاالمقبولةصيدلياالتيلهافعاليةمضادةللبكتيرياولهاصيغةتختارمنالفئةالتيتتكونمنوبتراكيبتشتملعلىمقدارفعالعلاجيامنمركبالاختراعفيتوليفةمعحاملمقبولصيدليا،بالاضافةإلىطريقةلمعالجةالاصاباتالبكتيريةباعطاءثدييتركيباصيدليايحتويعلىمقدارفعالعلاجيامنمركببالصيغمن (١) إلى (5).
Abstract:
Antibacterial compounds with improved pharmacokinetic profiles having formul a (I), and salts, prodrugs, and salts of prodrugs thereof, processes for makin g the compounds and intermediates used in the processes, compositions containi ng the compounds, and methods for prophylaxis and treatment of bacterial infections using the compounds are disclosed.
Abstract:
The instant invention provides novel macrolide compounds and compositions useful in treating bacterial infections. Also provided are processes for preparing same. These macrolides are substituted on the 6-O-position with X'-Y'-Z', wherein X' is selected from the group consisting of C1-C10 alkyl, C3-C10 alkenyl, and C3-C10 alkynyl; Y' and Z' are independently selected from the group consisting of: (c) optionally substituted aryl, and (d) optionally substituted heteroaryl, with the proviso that both Y' and Z' are not both phenyl, and with the further proviso that Y' is not isoxazole when Z' is thiophenyl.
Abstract:
The instant invention provides novel macrolide compounds and compositions useful in treating bacterial infections. Also provided are processes for preparing same. These macrolides are substituted on the 6-O-position with X'-Y'-Z', wherein X' is selected from the group consisting of C1-C10 alkyl, C3-C10 alkenyl, and C3-C10 alkynyl; Y' and Z' are independently selected from the group consisting of: (c) optionally substituted aryl, and (d) optionally substituted heteroaryl, with the proviso that both Y' and Z' are not both phenyl, and with the further proviso that Y' is not isoxazole when Z' is thiophenyl. 14 claims