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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.
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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
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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.
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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.
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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.
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公开(公告)号:BG63547B1
公开(公告)日:2002-04-30
申请号:BG10329299
申请日:1999-03-26
Applicant: ABBOTT LAB
Inventor: OR YAT S , MA ZHENKUN , CLARK RICHARD F , CHU DANIEL T , PLATTNER JACOB J
IPC: A61K31/70 , A61K31/7048 , A61P31/04 , C07H17/00 , C07H17/08
Abstract: The invention relates to compounds of antibacterial effect with formulae wherein the substituents have the meanings listed in the description, and to their pharmaceutically acceptable salts, esters or prodrugs. The invention also relates to pharmaceutical compounds containing them, to methods for treatment of bacterial infections by administering the compounds, as well as to methods for their preparation. 34 claims
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公开(公告)号:DE69132435T2
公开(公告)日:2001-05-10
申请号:DE69132435
申请日:1991-11-04
Applicant: ABBOTT LAB
Inventor: KEMPF DALE J , CODACOVI LYNN M , NORBECK DANIEL W , PLATTNER JACOB J , SHAM HING L , WITTENBERGER STEVEN J , ZHAO CHEN
IPC: A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/444 , A61K38/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C53/134 , C07C211/00 , C07C215/18 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/80 , C07C219/18 , C07C233/40 , C07C237/10 , C07C237/22 , C07C269/04 , C07C271/02 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/24 , C07D20060101 , C07D213/00 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/36 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D213/79 , C07D215/20 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D237/10 , C07D239/26 , C07D241/12 , C07D261/08 , C07D261/12 , C07D263/20 , C07D263/32 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/02 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/34 , C07D307/42 , C07D307/66 , C07D333/16 , C07D333/36 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D521/00 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/08 , C07K14/81 , A61K38/55 , C07D211/16 , C07D295/20
Abstract: An intermediate of the formula: and an intermediate of the formula: or an acid addition salt thereof.M
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公开(公告)号:DK0486948T3
公开(公告)日:2001-02-05
申请号:DK91119464
申请日:1991-11-04
Applicant: ABBOTT LAB
Inventor: PLATTNER JACOB J , SHAM HING L , KEMPF DALE J , CODACOVI LYNN M , NORBECK DANIEL W , WITTENBERGER STEVEN J , ZHAO CHEN
IPC: A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/444 , A61K38/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C53/134 , C07C211/00 , C07C215/18 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/80 , C07C219/18 , C07C233/40 , C07C237/10 , C07C237/22 , C07C269/04 , C07C271/02 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/24 , C07D20060101 , C07D213/00 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/36 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D213/79 , C07D215/20 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D237/10 , C07D239/26 , C07D241/12 , C07D261/08 , C07D261/12 , C07D263/20 , C07D263/32 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/02 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/34 , C07D307/42 , C07D307/66 , C07D333/16 , C07D333/36 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D521/00 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/08 , C07K14/81 , A61K37/64 , A61K38/55 , C07D211/16 , C07D295/20
Abstract: An intermediate of the formula: and an intermediate of the formula: or an acid addition salt thereof.M
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公开(公告)号:DE69132435D1
公开(公告)日:2000-11-09
申请号:DE69132435
申请日:1991-11-04
Applicant: ABBOTT LAB
Inventor: KEMPF DALE J , CODACOVI LYNN M , NORBECK DANIEL W , PLATTNER JACOB J , SHAM HING L , WITTENBERGER STEVEN J , ZHAO CHEN
IPC: A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/444 , A61K38/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C53/134 , C07C211/00 , C07C215/18 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/80 , C07C219/18 , C07C233/40 , C07C237/10 , C07C237/22 , C07C269/04 , C07C271/02 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/24 , C07D20060101 , C07D213/00 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/36 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D213/79 , C07D215/20 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D237/10 , C07D239/26 , C07D241/12 , C07D261/08 , C07D261/12 , C07D263/20 , C07D263/32 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/02 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/34 , C07D307/42 , C07D307/66 , C07D333/16 , C07D333/36 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D521/00 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/08 , C07K14/81 , A61K38/55 , C07D211/16 , C07D295/20
Abstract: An intermediate of the formula: and an intermediate of the formula: or an acid addition salt thereof.M
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公开(公告)号:TR200000620T2
公开(公告)日:2000-09-21
申请号:TR200000620
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.
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