公开(公告)号：CA2263972C

公开(公告)日：2008-01-29

申请号：CA2263972

申请日：1997-09-02

Applicant: ABBOTT LAB

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

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

Abstract: Antimicrobial compounds having formula (II), (III), (IV), (IV-A) or (V) as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compunds.

公开(公告)号：HRP20060278A2

公开(公告)日：2007-10-31

申请号：HRP20060278

申请日：2006-08-11

Applicant: ABBOTT LAB

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

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

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：HRP20060276A2

公开(公告)日：2007-10-31

申请号：HRP20060276

申请日：2006-08-11

Applicant: ABBOTT LAB

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

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

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：HRP970473B1

公开(公告)日：2007-02-28

申请号：HRP970473

申请日：1997-09-03

Applicant: ABBOTT LAB

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

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

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：DE69733369T2

公开(公告)日：2006-01-26

申请号：DE69733369

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：ES2244716T3

公开(公告)日：2005-12-16

申请号：ES02024558

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: La presente invención proporciona una clase novedosa de derivados de eritromicina 6-O-sustituidos que poseen una estabilidad a los ácidos incrementada en relación con la eritromicina A y la 6-O-metileritromicina A y una actividad aumentada hacia las bacterias gram negativas y las bacterias gram positivas resistentes a los macrólidos.

公开(公告)号：ES2242811T3

公开(公告)日：2005-11-16

申请号：ES02024557

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: Un compuesto con la siguiente fórmula (IV-A) o una sal farmacéuticamente aceptable del mismo, donde R p es hidrógeno o un grupo protector de hidroxi; R se selecciona del grupo formado por (1) metilo sustituido con un radical seleccionado del grupo formado por (a) CN, (b) F, (c) S(O)nR 10 donde n es 0, 1 o 2 y donde R 10 es alquilo C1-C3 o alquilo C1-C3 sustituido con arilo o alquilo C1-C3 sustituido con heteroarilo, (d) NHC(O)R 10 donde R 10 se define como antes, (e) NHC(O)NR 11 R 12 donde R 11 y R 12 se seleccionan independientemente entre hidrógeno, alquilo C1-C3, alquilo C1-C3 sustituido con arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, (f) arilo, (g) arilo sustituido, (h) heteroarilo, e (i) heteroarilo sustituido, (2) alquilo C2-C10 sustituido con uno o más sustituyentes seleccionado del grupo formado por (a) halógeno, (b) hidroxi, (c) alcoxi C1-C3, (d) alcoxi C1-C3-alcoxi C1-C3, 5 10 (e) oxo, (f) -N3, (g) -CHO, (h) O-SO2-(alquilo C1-C6 sustituido), (i) -NR 13 R 14 .

公开(公告)号：PT1291353E

公开(公告)日：2005-10-31

申请号：PT02024560

申请日：1997-09-02

Applicant: ABBOTT LAB

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

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

公开(公告)号：PT1015467E

公开(公告)日：2004-05-31

申请号：PT98944680

申请日：1998-09-01

Applicant: ABBOTT LAB

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

IPC: A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula (I) (II), (III), compositions comprising a therapeutically effective 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 the invention.

公开(公告)号：DK1015467T3

公开(公告)日：2004-05-03

申请号：DK98944680

申请日：1998-09-01

Applicant: ABBOTT LAB

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

IPC: A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula (I) (II), (III), compositions comprising a therapeutically effective 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 the invention.