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    COMPUESTOS A BASE DE ERITROMICINA 6-0 SUSTITUIDA Y TECNICA DE PRODUCCION.
    64.
    发明专利
    COMPUESTOS A BASE DE ERITROMICINA 6-0 SUSTITUIDA Y TECNICA DE PRODUCCION. 未知

    公开(公告)号：ES2252784T3

    公开(公告)日：2006-05-16

    申请号：ES97924605

    申请日：1997-05-06

    Applicant: ABBOTT LAB

    Inventor： OR YAT SUN ,  CLARK RICHARD F ,  MA ZHENKUN ,  GRIESGRABER GEORGE ,  LI LEPING ,  CHU DANIEL T

    IPC: C07H17/08 ,  A61K31/70

    Abstract: Un compuesto que tiene la fórmula o una sal farmacéuticamente aceptable del mismo, en la que X es =O, Ra es hidroxi; Rb es hidrógeno; Rc es hidrógeno y Rd es hidroxi; Re es metoxi; Rf es hidrógeno; y R se selecciona entre el grupo compuesto por (2) alquilo C2-C10 sustituido con uno o más sustituyentes seleccionados entre el grupo compuesto por (a) halógeno, (b) hidroxi, (c) alcoxi C1-C3, (d) alcoxi C1-C3-alcoxi C1-C3, (e) oxo, (f) -N3, (g) -CHO, (h) O-SO2-(alquilo C1-C6 sustituido), (i) -NR15R16 en la que R15 y R16 se seleccionan entre el grupo compuesto por (i) hidrógeno, (ii) alquilo C1-C12, (iii) alquilo C1-C12 sustituido, (iv) alquenilo C1-C12, (v) alquenilo C1-C12 sustituido, (vi) alquinilo C1-C12, (vii) alquinilo C1-C12 sustituido, (viii) arilo, (ix) cicloalquilo C3-C8, (x) cicloalquilo C3-C8 sustituido, (xi) arilo sustituido, (xii) heterocicloalquilo, (xiii) heterocicloalquilo sustituido, (xiv) alquilo C1-C12 sustituido con arilo, (xv) alquilo C1-C12 sustituido con arilo sustituido,(xvi) alquilo C1-C12 sustituido con heterocicloalquilo, (xvii) alquilo C1-C12 sustituido con sustituido heterocicloalquilo, (xviii) alquilo C1-C12 sustituido con cicloalquilo C3-C8, (xix) alquilo C1-C12 sustituido con cicloalquilo C3-C8 sustituido, (xx) heteroarilo, (xxi) sustituido heteroarilo, (xxii) alquilo C1-C12 sustituido con heteroarilo, y (xxiii) alquilo C1-C12 sustituido con heteroarilo sustituido, o R15 y R16 tomados junto con el átomo al que están unidos forman morfolinilo; (3) alquenilo C4-C10; y (4) alquinilo C3-C10.

    69.
    发明专利
    未知

    公开(公告)号：DK1291352T3

    公开(公告)日：2005-09-19

    申请号：DK02024559

    申请日：1997-09-02

    Applicant: ABBOTT LAB

    Inventor： OR YAT SUN ,  MA ZHENKUN ,  CLARK RICHARD F ,  CHU DANIEL T ,  PLATTNER JACOB J

    IPC: A61K31/70 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

    Abstract: 6-Substituted ketolides of e.g. formula (II) or (III), and their salts, esters and prodrugs are new: Y + Z = X; X = OH, =NOR1 or =NOC(R5)(R6)OR1; or one of Y and Z = H; and the other = H, OH, protected OH or NR7R8; R1 = 1-12C alkyl (optionally substituted), 3-12C cycloalkyl or SiR2R3R4; R2-R4 = 1-12C alkyl or aryl; R5, R6 = H or 1-12C alkyl (optionally substituted), or R5 + R6 = 3-12C cycloalkyl; R7, R8 = H or 1-6C alkyl; or NR7R8 = 3-7 membered ring which, when the ring is 5-7 membered may optionally contain O, NH, N(1-6C alkyl), N(aryl), N(aryl-1-6C alkyl), N (substituted aryl-1-6C alkyl), N(heteroaryl), N(heteroaryl-1-6C alkyl), N(substituted heteroaryl-1-6C alkyl), S or S(O)n; n = 1 or 2; Ra = H or OH; Rc = H or hydroxy protecting group; R9 = 1-6C alkyl (optionally substituted), 3-7C cycloalkyl or optionally substituted aryl or heteroaryl; M = CONH, NHCO, NH, N=, NMe, NHCOO, NHCONH, OCONHY, OCOO, O, S(O)n, COO, OCO or CO; R = methyl (substituted by CN, F, CO2R10, S(O)nR10, NHCOR10, NHCONR11R12, aryl, substituted aryl, heteroaryl or substituted heteroaryl); 2-10C alkyl (optionally substituted), 3C alkenyl (substituted by halo, CHO, CO2R10, COR9, CONR11R12, CN, optionally substituted aryl or heteroaryl, 3-7C cycloalkyl or 1-12C alkyl substituted by heteroaryl); 4-10C alkenyl (optionally substituted), or 3-10C alkynyl optionally substituted); R10 = 1-3C alkyl (optionally aryl substituted), or heteroaryl substituted 1-3C alkyl; R11, R12 = H or 1-3C alkyl (optionally substituted); A, B, D, E = H, 1-6C alkyl (optionally substituted by optionally substituted), 3-7C cycloalkyl, optionally substituted aryl or heteroaryl, heterocycloalkyl or 1-6C alkyl substituted by MR9; provided that \- 2 of A, B, D and E = H; or any one pair of substituents, consisting of AB, AD, AE, BD, BE or DE taken with the atoms to which they are attached, form a 3- to 7-membered ring optionally containing O, NH, N(1-6C alkyl), N(aryl-1-6C alkyl), N(substituted aryl-1-6C alkyl), N(heteroaryl-1-6C alkyl), N(substituted heteroaryl-1-6C alkyl), S, S(O)n, CONH, CONR12, NHCO, NR12CO or C(=NH)NH.

    70.
    发明专利
    未知

    公开(公告)号：DE69733723D1

    公开(公告)日：2005-08-18

    申请号：DE69733723

    申请日：1997-09-02

    Applicant: ABBOTT LAB

    Inventor： OR YAT SUN ,  MA ZHENKUN ,  CLARK RICHARD F ,  CHU DANIEL T ,  PLATTNER JACOB J

    IPC: A61K31/70 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

    Abstract: 6-Substituted ketolides of e.g. formula (II) or (III), and their salts, esters and prodrugs are new: Y + Z = X; X = OH, =NOR1 or =NOC(R5)(R6)OR1; or one of Y and Z = H; and the other = H, OH, protected OH or NR7R8; R1 = 1-12C alkyl (optionally substituted), 3-12C cycloalkyl or SiR2R3R4; R2-R4 = 1-12C alkyl or aryl; R5, R6 = H or 1-12C alkyl (optionally substituted), or R5 + R6 = 3-12C cycloalkyl; R7, R8 = H or 1-6C alkyl; or NR7R8 = 3-7 membered ring which, when the ring is 5-7 membered may optionally contain O, NH, N(1-6C alkyl), N(aryl), N(aryl-1-6C alkyl), N (substituted aryl-1-6C alkyl), N(heteroaryl), N(heteroaryl-1-6C alkyl), N(substituted heteroaryl-1-6C alkyl), S or S(O)n; n = 1 or 2; Ra = H or OH; Rc = H or hydroxy protecting group; R9 = 1-6C alkyl (optionally substituted), 3-7C cycloalkyl or optionally substituted aryl or heteroaryl; M = CONH, NHCO, NH, N=, NMe, NHCOO, NHCONH, OCONHY, OCOO, O, S(O)n, COO, OCO or CO; R = methyl (substituted by CN, F, CO2R10, S(O)nR10, NHCOR10, NHCONR11R12, aryl, substituted aryl, heteroaryl or substituted heteroaryl); 2-10C alkyl (optionally substituted), 3C alkenyl (substituted by halo, CHO, CO2R10, COR9, CONR11R12, CN, optionally substituted aryl or heteroaryl, 3-7C cycloalkyl or 1-12C alkyl substituted by heteroaryl); 4-10C alkenyl (optionally substituted), or 3-10C alkynyl optionally substituted); R10 = 1-3C alkyl (optionally aryl substituted), or heteroaryl substituted 1-3C alkyl; R11, R12 = H or 1-3C alkyl (optionally substituted); A, B, D, E = H, 1-6C alkyl (optionally substituted by optionally substituted), 3-7C cycloalkyl, optionally substituted aryl or heteroaryl, heterocycloalkyl or 1-6C alkyl substituted by MR9; provided that \- 2 of A, B, D and E = H; or any one pair of substituents, consisting of AB, AD, AE, BD, BE or DE taken with the atoms to which they are attached, form a 3- to 7-membered ring optionally containing O, NH, N(1-6C alkyl), N(aryl-1-6C alkyl), N(substituted aryl-1-6C alkyl), N(heteroaryl-1-6C alkyl), N(substituted heteroaryl-1-6C alkyl), S, S(O)n, CONH, CONR12, NHCO, NR12CO or C(=NH)NH.

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