公开(公告)号：DK1291350T3

公开(公告)日：2005-09-26

申请号：DK02024557

申请日：1997-09-02

Applicant: ABBOTT LAB

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

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.

公开(公告)号：AT299508T

公开(公告)日：2005-07-15

申请号：AT02024558

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.

公开(公告)号：DE69733422D1

公开(公告)日：2005-07-07

申请号：DE69733422

申请日：1997-09-02

Applicant: ABBOTT LAB

Inventor： OR SUN ,  MA ZHENKUN ,  CLARK F ,  CHU T ,  PLATTNER 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.

公开(公告)号：AT296831T

公开(公告)日：2005-06-15

申请号：AT97939765

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.

公开(公告)号：AT296307T

公开(公告)日：2005-06-15

申请号：AT02024557

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.

公开(公告)号：DE60010442T2

公开(公告)日：2005-05-12

申请号：DE60010442

申请日：2000-03-08

Applicant: ABBOTT LAB

Inventor： OR SUN ,  CLARK F ,  MA ZHENKUN ,  RUPP J

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

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.

公开(公告)号：ES2222189T3

公开(公告)日：2005-02-01

申请号：ES00913805

申请日：2000-03-08

Applicant: ABBOTT LAB

Inventor： OR YAT SUN ,  CLARK RICHARD F ,  MA ZHENKUN ,  RUPP MICHAEL J

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

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)-.

公开(公告)号：ES2208334T3

公开(公告)日：2004-06-16

申请号：ES00936424

申请日：2000-05-31

Applicant: ABBOTT LAB

Inventor： PHAN LY T ,  OR YAT SUN ,  MA ZHENKUN ,  CHEN YAN

IPC: A61K31/7056 ,  A61P31/04 ,  C07H17/08 ,  A61K31/7048

公开(公告)号：DE60010442D1

公开(公告)日：2004-06-09

申请号：DE60010442

申请日：2000-03-08

Applicant: ABBOTT LAB

Inventor： OR SUN ,  CLARK F ,  MA ZHENKUN ,  RUPP J

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

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.

公开(公告)号：AT266036T

公开(公告)日：2004-05-15

申请号：AT00913805

申请日：2000-03-08

Applicant: ABBOTT LAB

Inventor： OR YAT SUN ,  CLARK RICHARD F ,  MA ZHENKUN ,  RUPP MICHAEL J

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

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.