公开(公告)号：ES2242812T3

公开(公告)日：2005-11-16

申请号：ES02024559

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 (v) o una sal farmacéuticamente aceptable del mismo, donde Rb se selecciona del grupo formado por hidroxi, -O-C(O)-NH2 y -O-C(O)-imidazolilo; Rp 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) -CO2R10, donde R10 es alquilo C1-C3 o alquilo C1-C3 sustituido con arilo o alquilo C1-C3 sustituido con heteroarilo, (d) S(O)nR10 donde n es 0, 1 o 2 y R10 se define como antes, (e) NHC(O)R10 donde R10 se define como antes, (g) arilo, (h) arilo sustituido, (i) heteroarilo, y (j) 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, NHC(O)NR11R12 donde R11 y R12 se seleccionan independientemente entre hidrógeno, alquilo C1-Calquilo C1-C3 sustituido con arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, (e) oxo, (f) -N3, (g) -CHO, (h) O-SO2-(alquilo C1-C6 sustituido), (i) -NR 13 R 14.

公开(公告)号：DK1291353T3

公开(公告)日：2005-10-03

申请号：DK02024560

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：PT1291352E

公开(公告)日：2005-09-30

申请号：PT02024559

申请日：1997-09-02

Applicant: ABBOTT LAB

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

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

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：PT1027362E

公开(公告)日：2005-08-31

申请号：PT98956338

申请日：1998-10-29

Applicant: ABBOTT LAB

Inventor： OR YAT SUN ,  CHU DANIEL T ,  CLARK RICHARD F ,  PLATTNER JACOB J ,  PHAN LY TAM ,  YAN CHEN

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

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：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：ES2218604T3

公开(公告)日：2004-11-16

申请号：ES96936579

申请日：1996-10-17

Applicant: ABBOTT LAB

Inventor： OR YAT SUN ,  PHAN LY TAM ,  CHU DANIEL T ,  SPINA KENNETH P ,  HALLAS ROBERT ,  ELLIOTT RICHARD L

IPC: C07H17/00 ,  A61K31/00 ,  A61K31/70 ,  A61K31/7042 ,  A61P31/00 ,  A61P31/04 ,  C07H17/08

Abstract: Compounds, or pharmaceutically acceptable salts and esters thereof, of formulae (I); (II); (III) or (IV) wherein A, B, D and E, R , R and Z are specifically defined, having antibacterial activity, pharmaceutical compositions containing said compounds, treatment of antibacterial infections with such compositions, and processes for the preparation of the compounds.

公开(公告)号：AT259823T

公开(公告)日：2004-03-15

申请号：AT96936579

申请日：1996-10-17

Applicant: ABBOTT LAB

Inventor： OR YAT SUN ,  PHAN LY TAM ,  CHU DANIEL T ,  SPINA KENNETH P ,  HALLAS ROBERT ,  ELLIOTT RICHARD L

IPC: C07H17/00 ,  A61K31/00 ,  A61K31/70 ,  A61K31/7042 ,  A61P31/00 ,  A61P31/04 ,  C07H17/08

Abstract: Compounds, or pharmaceutically acceptable salts and esters thereof, of formulae (I); (II); (III) or (IV) wherein A, B, D and E, R , R and Z are specifically defined, having antibacterial activity, pharmaceutical compositions containing said compounds, treatment of antibacterial infections with such compositions, and processes for the preparation of the compounds.