公开(公告)号：WO1997042205A1

公开(公告)日：1997-11-13

申请号：PCT/US1997007051

申请日：1997-04-25

Applicant: ABBOTT LABORATORIES

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

IPC: C07H17/08

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.

Abstract translation: 具有选自：（a）（I），（b）（II），（c）（III））和（c）（III）的组中的具有抗菌活性的新型3-缩水甘油-2,3-脱水红霉素化合物及其药学上可接受的盐和酯 （d）（IV），包含治疗有效量的本发明式（I） - （IV）化合物与药学上可接受的载体组合的药物组合物，以及通过给予 哺乳动物含有治疗有效量的本发明式（I） - （IV）化合物的药物组合物。

公开(公告)号：WO1993016702A1

公开(公告)日：1993-09-02

申请号：PCT/US1993001766

申请日：1993-02-26

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  CHU, Daniel, T. ,  PLATTNER, Jacob, J. ,  HALLAS, Robert

IPC: A61K31/54

CPC classification number: C07D498/06 ,  C07D455/00 ,  C07D498/16 ,  C07D513/06 ,  Y02P20/55

Abstract: Quinobenzoxazine, quinobenzothiazines, and pyrido-acridine derivatives of formula (I) as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R is hydrogen or acarboxy-protecting group, R and R are substituents, A is oxygen, sulfur, or carbon, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.

Abstract translation: 公开了式（I）的喹苯并恶嗪，喹苯并噻嗪和吡啶并吖啶衍生物及其药学上可接受的盐，酯，酰胺和前药，其中R 1是氢或酰氧基保护基，R 2和R 3是取代基，A是氧，硫或碳，Z是卤素或含氮基团，X是氢，卤素或烷基，W是氢，烷基，氨基或卤素。 这些化合物具有有效的抗肿瘤活性。

公开(公告)号：WO1998009978A1

公开(公告)日：1998-03-12

申请号：PCT/US1997015506

申请日：1997-09-02

Applicant: ABBOTT LABORATORIES

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

IPC: C07H17/08

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.

Abstract translation: 具有式（II），（III），（IV），（IV-A）或（V）的抗微生物化合物及其药学上可接受的盐，酯或前药; 包含这些化合物的药物组合物; 通过施用这些化合物治疗细菌感染的方法; 以及制备肥料的过程。

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：WO1995010519A1

公开(公告)日：1995-04-20

申请号：PCT/US1994011166

申请日：1994-09-30

Applicant: ABBOTT LABORATORIES

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

IPC: C07D455/02

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

Abstract: Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; 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 loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract translation: 具有式（I）的抗菌配方及其药学上可接受的盐，酯和酰胺，其优选实例包括其中R 1为3至8个碳原子的环烷基或取代的苯基的那些芳族基团; R 2选自（a）卤素，（b）低级烷基，（c）低级烯基，（d）3至8个碳的环烷基，（e）4至8个碳的环烯基，（f ）低级烷氧基，（g）芳氧基，（h）芳基（低级烷基）氧基，（i）芳基（低级烷基），（j）环烷基（低级烷基），（k）氨基，（1）（低级烷基）氨基，（m） （低级烷基）氨基，（n）羟基取代的（低级烷基）氨基，（o）苯基，（p）取代的苯基，（q）双环含氮杂环，（r）含氮芳族杂环，和 具有式（Ia）的杂环，其中x在0和3之间; 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; R 6为低级烷基，以及含有这些化合物的药物组合物及其在治疗细菌感染中的用途。

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.

公开(公告)号：EP0723545A1

公开(公告)日：1996-07-31

申请号：EP94929998.0

申请日：1994-09-30

Applicant: ABBOTT LABORATORIES

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

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

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

Abstract: Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R2is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; 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 loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

公开(公告)号：EP0527889A1

公开(公告)日：1993-02-24

申请号：EP91909628.0

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

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

Abstract: Nouveaux composés de la formule (I) ainsi que leurs sels, esters et amides pharmaceutiquement acceptables, dans laquelle R1 est choisi entre (a) alkyle inférieur, (b) alcényle inférieur, (c) halo(alkyle inférieur), (d) alcoxy inférieur, (e) cycloalkyle contenant 3 à 8 atomes de carbone, (f) phényle, (g) halo, (h) cyano, (i) nitro, (j) bicycloalkyle, (k) alkynyle inférieur, (l) alcoxycarbonyle, (m) un hétérocycle aromatique contenant de l'azote et (n) un groupe de la formule -NR7R8; R2 est choisi dans le groupe composé d'halogène, alcoxy inférieur, aryloxycarbocyclique ou aryle(alkyle inférieur) oxycarbocyclique, alkyle inférieur, alcényle inférieur, cycloalkyle contenant 3 à 8 atomes de carbone, cycloalcényle contenant 4 à 8 atomes de carbone, aryle(alkyle inférieur) carbocyclique, cycloalkyle(alkyle inférieur), phényle, amino, (alkyle inférieur)amino, aryle(alkyle inférieur) amino carbocyclique, (alkyle inférieur)amino à substitution hydroxy, un hétérocycle aromatique contenant de l'azote, un hétérocycle contenant de l'azote bicyclique et un hétérocycle contenant de l'azote de la formule (II), dans laquelle x est compris entre 0 et 3; R9 est choisi entre (a)-(CH2)m-, où m représente 1, 2 ou 3, et (b)-(CH2)nR10(CH2)p-, où R10 est choisi entre S, O et N, n représente 1 ou 0 et p représente 1 ou 2; et Y représente un substituant différent de l'hydrogène choisi indépendamment parmi alkyle inférieur, halo(alkyle inférieur), alcoxy inférieur, alkyle inférieur à substitution hydroxy, hydroxy, amino(alkyle inférieur), halogène et un groupe ayant la formule -NR11R12; R3 représente hydrogène, halogène ou alcoxy inférieur; R4 est choisi dans le groupe composé d'hydrogène, alkyle inférieur, un cation pharmaceutiquement acceptable ainsi qu'un groupe d'esters de pro-médicaments; R5 est choisi dans le groupe composé d'hydrogène, halogène, hydroxy, alkyle inférieur, halo(aryle inférieur), alcoxy inférieur ainsi qu'un groupe ayant la formule -NR13R14; et A représente N ou CR6, où R6 est choisi parmi hydrogène, halogène, alkyle

公开(公告)号：EP1027362B1

公开(公告)日：2005-06-29

申请号：EP98956338.2

申请日：1998-10-29

Applicant: Abbott Laboratories

Inventor： PHAN, LY, Tam ,  OR, Yat, Sun ,  CHU, Daniel, T. ,  PLATTNER, Jacob, J. ,  CHEN, Yan ,  CLARK, Richard, F.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08 ,  Y02P20/55

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：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。