公开(公告)号：EP0871628A1

公开(公告)日：1998-10-21

申请号：EP96919103.0

申请日：1996-06-05

Applicant: Abbott Laboratories

Inventor： CHU, Daniel, T. ,  LI, Qun ,  COOPER, Curt, S. ,  FUNG, Anthony, K., L. ,  LEE, Cheuk, M. ,  PLATTNER, Jacob, J. ,  MA, Zhenkun ,  WANG, Wei-Bo

IPC: A61K31 ,  A61P31 ,  C07D213 ,  C07D455 ,  C07D471 ,  C07D491 ,  C07D495 ,  C07D519 ,  C07K5 ,  A61K38

CPC classification number: C07D471/04 ,  A61K38/00 ,  C07D213/61 ,  C07D213/68 ,  C07D455/02 ,  C07K5/06026

Abstract: Antibacterial compounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein A is =CR6-; R1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R2 is selected from the group consisting of (a), (b), (c) and (d); R3 is halogen; R4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R5 is hydrogen, loweralkyl, halo(loweralkyl), or -NR?13R14; and R6¿ is halogen, loeralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract translation: 具有式（I）的抗菌化合物及其药学上可接受的盐，酯和酰胺，其选择的优选实例包括其中A为= CR 6 - 的那些化合物; R 1是三至八个碳原子的环烷基或取代的苯基; R2选自（a），（b），（c）和（d）; R3是卤素; R4是氢，低级烷基，药学上可接受的阳离子或前药酯基团; R5是氢，低级烷基，卤代（低级烷基）或-NR8R14; （低级烷基），羟基取代的低级烷基，低级烷氧基（低级烷基），低级烷氧基或氨基（低级烷基），以及含有这些化合物的药物组合物以及它们在治疗细菌中的用途 感染。

公开(公告)号：EP1007530B1

公开(公告)日：2005-11-16

申请号：EP97924605.5

申请日：1997-05-06

Applicant: ABBOTT LABORATORIES

Inventor： OR, Yat, Sun ,  CLARK, Richard, F. ,  MA, Zhenkun ,  GRIESGRABER, George ,  LI, Leping ,  CHU, Daniel, T.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08 ,  Y02P20/55

Abstract: Antimicrobial compounds having formula (II), (III), (IV), (V), (VI), (VII), (VIII) and (IX); as well as the pharmaceutically acceptable salts, esters and 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 compounds.

公开(公告)号：EP1025114B1

公开(公告)日：2004-02-25

申请号：EP98946087.8

申请日：1998-09-16

Applicant: Abbott Laboratories

Inventor： OR, Yat, Sun ,  MA, Zhenkun ,  CHU, Daniel, T.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: Novel 3'-N-modified 6-O-substituted erythromycin ketolide compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I), (II), (III), (IV) or (V), 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：EP1015467B1

公开(公告)日：2004-01-07

申请号：EP98944680.2

申请日：1998-09-01

Applicant: Abbott Laboratories

Inventor： OR, Yat, Sun ,  CLARK, Richard, F. ,  CHU, Daniel, T. ,  PLATTNER, Jacob, J.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I), (II), or (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：EP0922050B1

公开(公告)日：2003-07-30

申请号：EP97921411.1

申请日：1997-04-25

Applicant: ABBOTT LABORATORIES

Inventor： ELLIOTT, Richard, L. ,  OR, Yat, Sun ,  CHU, Daniel, T. ,  GRIESGRABER, George, W. ,  PLATTNER, Jacob, J. ,  PIREH, Daisy

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08 ,  Y02P20/55

Abstract: Novel 3-descladinose-2,3-anhydroerythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity selected from the group consisting of: (a) (I), (b) (II), (c) (III), and (d) (IV), pharmaceutical compositions comprising a therapeutically effective amount of a compound of formulas (I)-(IV) 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 formulas (I)-(IV) of the invention.

公开(公告)号：EP1027360A2

公开(公告)日：2000-08-16

申请号：EP98941119.4

申请日：1998-09-01

Applicant: Abbott Laboratories

Inventor： OR, Yat, Sun ,  LI, Leping ,  RUPP, Michael, J. ,  CHU, Daniel, T.

IPC: C07H17/00

CPC classification number: C07H17/08

Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula selected from the group consisting of (I), (II), (III), (IV) and (V), compositions comprising a therapeutically eff ective 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 formulas (I)-(V).

公开(公告)号：EP0527889B1

公开(公告)日：2000-08-02

申请号：EP91909628.9

申请日：1991-05-01

Applicant: ABBOTT LABORATORIES

Inventor： CHU, Daniel, T. ,  LEE, Cheuk, M. ,  LI, Qun ,  COOPER, Curt, S. ,  PLATTNER, Jacob, J.

IPC: C07D471/04 ,  C07D455/02 ,  C07D491/16 ,  C07D495/16 ,  C07D471/16 ,  C07D519/00 ,  A61K31/435 ,  A61K31/505 ,  A61K31/495 ,  A61K31/54 ,  A61K31/535

CPC classification number: C07D471/04 ,  A61K38/00 ,  C07D213/68 ,  C07D455/02 ,  C07K5/06026

Abstract: Novel compounds are disclosed having formula (I) as well as pharmaceutically acceptable salts, esters and amides thereof, wherein R1 is selected from (a) loweralkyl, (b) loweralkenyl, (c) halo(loweralkyl), (d) loweralkoxy, (e) cycloalkyl of from 3 to 8 carbons, (f) phenyl, (g) halo, (h) cyano, (i) nitro, (j) bicycloalkyl, (k) loweralkynyl, (l) alkoxycarbonyl, (m) nitrogen-containing aromatic heterocycle and (n) a group of the formula -NR7R8; R2 is selected from the group consisting of halogen, loweralkoxy, carbocyclic aryloxy or carbocyclic aryl(loweralkyl)oxy, loweralkyl, loweralkenyl, cycloalkyl of from 3 to 8 carbons, cycloalkenyl of from 4 to 8 carbons, carbocyclic aryl(loweralkyl), cycloalkyl(loweralkyl), phenyl, amino, (loweralkyl)amino, carbocyclic aryl(loweralkyl)amino, hydroxy-substituted (loweralkyl)amino, nitrogen-containing aromatic heterocycle, bicyclic nitrogen-containing heterocycle and nitrogen-containing heterocycle having formula (II), wherein x is 0 to 3; R9 is selected from (a)-(CH¿2?)m-, wherein m is 1, 2 or 3, and (b) -(CH2)nR?10(CH¿2)p-, wherein R10 is selected from S, O and N, n is 1 or 2, and p is 1 or 2; and Y is a non-hydrogen substituent independently selected from loweralkyl, halo(loweralkyl), loweralkoxy, hydroxy-substituted loweralkyl, hydroxy, amino(loweralkyl), halogen and a group having the formula -NR?11R12; R3¿ is hydrogen, halogen or loweralkoxy; R4 is selected from the group consisting of hydrogen, loweralkyl, a pharmaceutically acceptable cation and a prodrug ester group; R5 is selected from the group consisting of hydrogen, halogen, hydroxy, loweralkyl, halo(loweralkyl), loweralkoxy and a group having the formula -NR13R14; and A is N or CR6, wherein R6 is selected from hydrogen, halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy and amino(loweralkyl) or, alternatively, R?1 and R6¿, taken together with the atoms to which they are attached, form a 6-membered saturated ring which may contain an oxygen or a sulfur atom and which may be substituted with loweralkyl; with the proviso that when R5 is hydrogen and A is CH then either (a) R?1 is NR7R8¿, or (b) R2 is a group having formula (III), wherein x is 1-3 and R9 and Y are as defined above.

公开(公告)号：EP1015467A1

公开(公告)日：2000-07-05

申请号：EP98944680.2

申请日：1998-09-01

Applicant: Abbott Laboratories

Inventor： OR, Yat, Sun ,  CLARK, Richard, F. ,  CHU, Daniel, T. ,  PLATTNER, Jacob, J.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I), (II), or (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：EP0922050A1

公开(公告)日：1999-06-16

申请号：EP97921411.0

申请日：1997-04-25

Applicant: ABBOTT LABORATORIES

Inventor： ELLIOTT, Richard, L. ,  OR, Yat, Sun ,  CHU, Daniel, T. ,  GRIESGRABER, George, W. ,  PLATTNER, Jacob, J. ,  PIREH, Daisy

IPC: A61K31 ,  C07H17

CPC classification number: C07H17/08 ,  Y02P20/55

Abstract: Novel 3-descladinose-2,3-anhydroerythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity selected from the group consisting of: (a) (I), (b) (II), (c) (III), and (d) (IV), pharmaceutical compositions comprising a therapeutically effective amount of a compound of formulas (I)-(IV) 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 formulas (I)-(IV) of the invention.

公开(公告)号：EP0929563B1

公开(公告)日：2005-06-01

申请号：EP97939765.0

申请日：1997-09-02

Applicant: Abbott Laboratories

Inventor： OR, Yat, Sun ,  MA, Zhenkun ,  CLARK, Richard, F. ,  CHU, Daniel, T. ,  PLATTNER, Jacob, J.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08 ,  Y02P20/55

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.