公开(公告)号：WO1996039407A1

公开(公告)日：1996-12-12

申请号：PCT/US1996008991

申请日：1996-06-05

Applicant: ABBOTT LABORATORIES

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

IPC: C07D471/04

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 =CR -; R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a), (b), (c) and (d); R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R 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 = CR 6 - 的那些化合物; R 1是3至8个碳原子的环烷基或取代的苯基; R 2选自（a），（b），（c）和（d）; R 3是卤素; R 4是氢，低级烷基，药学上可接受的阳离子或前药酯基; R 5是氢，低级烷基，卤代（低级烷基）或-NR 13 R 14; 和R 6是卤素，低级烷基，卤代（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及其在治疗中的用途 的细菌感染。

公开(公告)号：EP0971919B1

公开(公告)日：2001-10-31

申请号：EP98904979.6

申请日：1998-02-06

Applicant: Abbott Laboratories

Inventor： WANG, Wei-Bo ,  KERDESKY, Francis, A., J. ,  HSIAO, Chi-Nung, W. ,  LI, Qun ,  CHU, Daniel, T.

IPC: C07D455/02

CPC classification number: C07D455/02

Abstract: A process for the preparation of a compound having formula (a) wherein R?1, R2, R3, R4, and R5¿ are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.

公开(公告)号：EP1276726A2

公开(公告)日：2003-01-22

申请号：EP01932712.1

申请日：2001-04-25

Applicant: Abbott Laboratories

Inventor： WANG, Wei-Bo ,  CURTIN, Michael, L. ,  FAKHOURY, Stephen, A. ,  GWALTNEY, Stephen, L., II ,  HASVOLD, Lisa A. ,  HUTCHINS, Charles, W. ,  LI, Qui ,  LIN, Nan-Horng ,  JENNINGS NELSON, Lissa, Taka ,  O'CONNOR, Stephen, J. ,  SHAM, Hing, L. ,  SULLIVAN, Gerald, M. ,  WANG, Gary, T. ,  WANG, Xilu

IPC: C07D233/54 ,  A61K31/33 ,  A61P43/00 ,  C07D401/10 ,  C07D249/08 ,  C07D231/12 ,  C07D333/16 ,  C07D409/10 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D213/57 ,  C07D213/74 ,  C07D277/24 ,  C07D213/38 ,  C07D401/14 ,  C07D409/12

CPC classification number: C07D213/30 ,  C07D213/36 ,  C07D231/12 ,  C07D233/64 ,  C07D249/04 ,  C07D249/08 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D333/16 ,  C07D333/24 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D409/10 ,  C07D413/12 ,  C07D417/06

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, inhibit farnesyltransferase. Methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.

公开(公告)号：EP0971919A1

公开(公告)日：2000-01-19

申请号：EP98904979.6

申请日：1998-02-06

Applicant: Abbott Laboratories

Inventor： WANG, Wei-Bo ,  KERDESKY, Francis, A., J. ,  HSIAO, Chi-Nung, W. ,  LI, Qun ,  CHU, Daniel, T.

IPC: C07D455/02

CPC classification number: C07D455/02

Abstract: A process for the preparation of a compound having formula (a) wherein R?1, R2, R3, R4, and R5¿ are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.

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。