公开(公告)号：WO1998030574A1

公开(公告)日：1998-07-16

申请号：PCT/US1997005871

申请日：1997-04-07

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  OR, Yat, Sun ,  PHAN, Ly, Tam ,  CHU, Daniel, T. ,  SPINA, Kenneth, P. ,  HALLAS, Robert ,  ELLIOTT, Richard, L. ,  TUFANO, Michael

IPC: C07H17/00

CPC classification number: C07H17/08 ,  C07H17/00

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

Abstract translation: 化合物或其药学上可接受的盐和酯，其具有下式：（I）; （II）; （III）; 或（IV）; 其特征在于具有抗菌活性的A，B，D和E，R 1，R 2和Z，含有所述化合物的药物组合物，用这些组合物治疗细菌感染，以及制备化合物的方法 。

公开(公告)号：WO1992010191A1

公开(公告)日：1992-06-25

申请号：PCT/US1991009419

申请日：1991-12-12

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  CHU, Daniel, T. ,  COOPER, Curt, S.

IPC: A61K31/47

CPC classification number: C07D401/04 ,  C07D471/04 ,  C07D491/10

Abstract: Novel antibacterial compounds are disclosed having formula (I) as well as pharmaceutically acceptable salts, esters, amide and prodrugs thereof, wherein R1 is selected from the group consisting of (a) lower alkyl, (b) halo(lower alkyl), (c) lower alkyl(alkynyl), (d) lower cycloalkyl, (e) lower alkylamino, (f) nitrogen-containing aromatic heterocycle, (g) bicyclic alkyl and (h) phenyl; R2 is selected from the group consisting of hydrogen, lower alkyl, a pharmaceutically acceptable cation, and a prodrug ester group; R?3 and R4¿ are independently selected from the group consisting of hydrogen, halogen, amino, and lower alkyl; R5 is either a nitrogen-containing heterocycle or a nitrogen-containing spiro-bicyclic-heterocycle; and A is N or C-R6, wherein R6 is selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy, or R?1 and R6¿ taken together with the atoms to which they are attached form a 6-membered ring which may contain an oxygen or sulfur atom and which may be substituted with lower alkyl; as well as pharmaceutical compositions comprising such novel compounds and the therapeutic use thereof.

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：WO1997042206A1

公开(公告)日：1997-11-13

申请号：PCT/US1997007702

申请日：1997-05-06

Applicant: ABBOTT LABORATORIES

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

IPC: C07H17/08

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.

Abstract translation: 具有式（II），（III），（IV），（V），（VI），（VII），（VIII）和（IX）的抗微生物化合物; 以及其药学上可接受的盐，酯和前药; 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; 和化合物的制备方法。

公开(公告)号：WO1997017357A1

公开(公告)日：1997-05-15

申请号：PCT/US1996017892

申请日：1996-11-06

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  OR, Yat, Sun ,  CHU, Daniel, T. ,  ELLIOTT, Richard, L. ,  PIREH, Daisy

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: A compound selected from groups (I), (II), and (III), wherein A, B, V, W, X and R are specifically defined; pharmaceutical compositions thereof; a method of treating or preventing bacterial infections by administering therapeutically effective pharmaceutical compositions thereof; and a process for the preparation thereof.

Abstract translation: 选自基团（I），（II）和（III）的化合物，其中A，B，V，W，X和R 8是具体定义的; 其药物组合物; 通过施用其治疗有效的药物组合物来治疗或预防细菌感染的方法; 及其制备方法。

公开(公告)号：WO1996037495A1

公开(公告)日：1996-11-28

申请号：PCT/US1996006813

申请日：1996-05-13

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  CHU, Daniel, T. ,  LI, Qun ,  RAYE, Kathleen

IPC: C07D491/16

CPC classification number: C07D491/16

Abstract: Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine compounds having formula (I), wherein A is sulfur or oxygen; R is selected from the group consisting of hydroxy, protected-hydroxy, C1-C6-alkoxy, halo, amino, C1-C6-alkylamino, hydroxy-C1-C6-alkylamino, bicyclic nitrogen-containing heterocycle, nitrogen-containing aromatic heterocycle, and nitrogen-containing heterocycle; R is selected from the group consisting of hydrogen, halo, C1-C6-alkyl, or halo-C1-C6-alkyl; R is selected from the group consisting of hydrogen, C1-C6-alkyl or C5-C7-cycloalkyl; and R and R are independently selected from the group consisting of hydrogen, C1-C6-alkyl or C1-C6-alkoxyl, having utility as intermediates or having antibacterial or antineoplastic activity.

Abstract translation: 苯并[5.6]吡喃并[2,3,4-ij]喹嗪和具有式（I）的苯并[5,6]噻喃并[2,3,4-ij]喹嗪化合物，其中A是硫或氧; R 1选自羟基，被保护的羟基，C 1 -C 6 - 烷氧基，卤素，氨基，C 1 -C 6烷基氨基，羟基-C 1 -C 6 - 烷基氨基，双环含氮杂环，含氮 芳族杂环和含氮杂环; R 2选自氢，卤素，C 1 -C 6 - 烷基或卤代-C 1 -C 6 - 烷基; R 3选自氢，C 1 -C 6 - 烷基或C 5 -C 7 - 环烷基; R 4和R 5独立地选自氢，C 1 -C 6烷基或C 1 -C 6烷氧基，其可用作中间体或具有抗细菌或抗肿瘤活性。

公开(公告)号：WO1997017356A1

公开(公告)日：1997-05-15

申请号：PCT/US1996016585

申请日：1996-10-17

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  OR, Yat, Sun ,  PHAN, Ly, Tam ,  CHU, Daniel, T. ,  SPINA, Kenneth, P. ,  HALLAS, Robert ,  ELLIOTT, Richard, L.

IPC: C07H17/08

CPC classification number: 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.

Abstract translation: 式（I）的化合物或其药学上可接受的盐和酯; （II）; （III）或（IV）其中A，B，D和E，R 1，R 2和Z具体定义为具有抗菌活性，含有所述化合物的药物组合物，用这些组合物治疗抗菌感染，以及 制备化合物的方法。

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：WO1994006766A1

公开(公告)日：1994-03-31

申请号：PCT/US1993007894

申请日：1993-08-19

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  CHU, Daniel, T. ,  LI, Qun

IPC: C07D207/24

CPC classification number: C07C255/25 ,  C07C229/12 ,  C07D207/12 ,  C07D207/14 ,  C07D207/24

Abstract: Chiral compounds having formulae (III), (IV), (V), (VI), (VII) and (VIII), useful in the synthesis of quinolone intermediates.

Abstract translation: 具有式（III），（IV），（V），（VI），（VII）和（VIII）的手性化合物可用于合成喹诺酮中间体。