公开(公告)号：DE69733422T2

公开(公告)日：2006-05-04

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: 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：DE69830739T2

公开(公告)日：2006-04-20

申请号：DE69830739

申请日：1998-10-29

Applicant: ABBOTT LAB

Inventor： PHAN TAM ,  OR SUN ,  CHU T ,  PLATTNER J ,  CHEN YAN ,  CLARK F

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

Abstract: Novel 2-halo-6-O-substituted ketolide derivatives and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I) or (II), compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, 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, and processes for their preparation.

公开(公告)号：DE69830739D1

公开(公告)日：2005-08-04

申请号：DE69830739

申请日：1998-10-29

Applicant: ABBOTT LAB

Inventor： PHAN TAM ,  OR SUN ,  CHU T ,  PLATTNER J ,  CHEN YAN ,  CLARK F

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

Abstract: Novel 2-halo-6-O-substituted ketolide derivatives and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I) or (II), compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, 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, and processes for their preparation.

公开(公告)号：DE69821009T2

公开(公告)日：2004-11-18

申请号：DE69821009

申请日：1998-09-01

Applicant: ABBOTT LAB

Inventor： OR SUN ,  CLARK F ,  CHU T ,  PLATTNER 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：DE69821009D1

公开(公告)日：2004-02-12

申请号：DE69821009

申请日：1998-09-01

Applicant: ABBOTT LAB

Inventor： OR SUN ,  CLARK F ,  CHU T ,  PLATTNER 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：DE69734678T2

公开(公告)日：2006-08-17

申请号：DE69734678

申请日：1997-05-06

Applicant: ABBOTT LAB

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

IPC: C07H17/08 ,  A61K31/70

公开(公告)号：DE69734678D1

公开(公告)日：2005-12-22

申请号：DE69734678

申请日：1997-05-06

Applicant: ABBOTT LAB

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

IPC: C07H17/08 ,  A61K31/70

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：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：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.