公开(公告)号：EP0345627A2

公开(公告)日：1989-12-13

申请号：EP89109890.7

申请日：1989-06-01

Applicant: ABBOTT LABORATORIES

Inventor： Pariza, Richard J. ,  Maring, Clarence J. ,  Lartey, Paul A. ,  Klein, Larry L.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: Semisynthetic antibiotics with improved therapeutic properties are disclosed. In particular, 9-R-azacyclic derivatives of erythromycin, its derivatives, and their salts and esters show superior antimicrobial activity compared to other macrolide compounds.

Abstract translation: 公开了具有改善的治疗性能的半合成抗生素。 特别地，与其他大环内酯类化合物相比，红霉素，其衍生物及其盐和酯的9-R-氮杂环十二烷基衍生物显示出优异的抗菌活性。

公开(公告)号：EP1315698A1

公开(公告)日：2003-06-04

申请号：EP99917414.7

申请日：1999-04-12

Applicant: ABBOTT LABORATORIES

Inventor： Maring, Clarence J. ,  Gu, Yu-Gui ,  Chen, Hui-Ju ,  Chen, Yuanwei ,  Degoey, David A. ,  Flosi, William J. ,  Giranda, Vincent L. ,  Grampovnik, David J. ,  Kati, Warren M. ,  Kempf, Dale J. ,  Klein, Larry L. ,  Krueger, Allan C. ,  Lin, Zhen ,  Madigan, Darold L. ,  McDaniel, Keith F. ,  Muchmore, Steven W. ,  Sham, Hing L. ,  Stewart, Kent D. ,  Stoll, Vincent S. ,  Sun, Minghua ,  Wang, Gary T. ,  Wang, Sheldon ,  Xu, Yibo ,  Yeung, Ming C. ,  Zhao, Chen ,  Kennedy, April

IPC: C07D207/16

CPC classification number: C07D207/327 ,  C07D207/16 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/06 ,  C07D413/04 ,  C07D417/04 ,  C07D417/06 ,  C07F9/5722

Abstract: Disclosed are compounds of formula (I) which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.

公开(公告)号：EP0424802A2

公开(公告)日：1991-05-02

申请号：EP90119985.1

申请日：1990-10-18

Applicant: ABBOTT LABORATORIES

Inventor： Chu, Daniel T. ,  Plattner, Jacob J. ,  Klein, Larry L. ,  Shen, Linus L.

IPC: C07C333/06 ,  C07D513/04 ,  C07D519/00 ,  A61K31/435

CPC classification number: C07D513/04 ,  C07C333/06 ,  C07C2601/02 ,  C07D513/14

Abstract: Isothiazolo-quinoline derivatives of the formula I which may exist as tautomers (formula II) are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.
wherein R is selected from (a) lower alkyl, (b) haloalkyl, (c) lowercycloalkyl, (d) alkylamino, (e) an aromatic heterocyclic group and (f) a phenyl group; W, X and Z are independently selected from hydrogen, halogen and lower alkyl; and Y is selected from a (a) phenyl group, (b) -NR₂R₃, (c) a bicyclic N-containing heterocyclic group, and (d) -OR₁₀, wherein R₁₀ is hydrogen, lower alkyl or a phenyl group;
or any two of W, X, Y and Z taken together form a fused, substituted or unsubstituted, aromatic group or heterocyclic group.

Abstract translation: 描述了可以以互变异构体（式II）存在的式I的异噻唑并喹啉衍生物，其对各种肿瘤细胞系是细胞毒性的，并且可用于治疗肿瘤性疾病。 其中R选自（a）低级烷基，（b）卤代烷基，（c）低级环烷基，（d）烷基氨基，（e）芳族杂环基和（f）苯基; W，X和Z独立地选自氢，卤素和低级烷基; 并且Y选自（a）苯基，（b）-NR2R3，（c）双环含氮杂环基和（d）-OR10，其中R10是氢，低级烷基或苯基; 或W，X，Y和Z中的任意两个一起形成稠合，取代或未取代的芳族基团或杂环基。

公开(公告)号：EP2336138A2

公开(公告)日：2011-06-22

申请号：EP10184668.1

申请日：2005-06-29

Applicant: ABBOTT LABORATORIES

Inventor： Degoey, DAvid A ,  Flosi, William J ,  Grampovnik, David J. ,  Klein, Larry L. ,  Kempf, Dale J. ,  Wang, Xiu C.

IPC: C07F9/09 ,  A61K31/661 ,  A61P35/00

CPC classification number: A61K45/06 ,  A61K31/661 ,  A61K2300/00

Abstract: A compound of the formula I, II or III is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions of inhibiting HIV protease activity and treating HIV infection are also disclosed.

Abstract translation: 公开了式I，II或III的化合物作为HIV蛋白酶抑制剂的前药。 还公开了抑制HIV蛋白酶活性和治疗HIV感染的方法和组合物。

公开(公告)号：EP0424802A3

公开(公告)日：1992-05-06

申请号：EP90119985.1

申请日：1990-10-18

Applicant: ABBOTT LABORATORIES

Inventor： Chu, Daniel T. ,  Plattner, Jacob J. ,  Klein, Larry L. ,  Shen, Linus L.

IPC: C07C333/06 ,  C07D513/04 ,  C07D519/00 ,  A61K31/435

CPC classification number: C07D513/04 ,  C07C333/06 ,  C07C2601/02 ,  C07D513/14

Abstract: Isothiazolo-quinoline derivatives of the formula I which may exist as tautomers (formula II) are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.
wherein R is selected from (a) lower alkyl, (b) haloalkyl, (c) lowercycloalkyl, (d) alkylamino, (e) an aromatic heterocyclic group and (f) a phenyl group; W, X and Z are independently selected from hydrogen, halogen and lower alkyl; and Y is selected from a (a) phenyl group, (b) -NR₂R₃, (c) a bicyclic N-containing heterocyclic group, and (d) -OR₁₀, wherein R₁₀ is hydrogen, lower alkyl or a phenyl group;
or any two of W, X, Y and Z taken together form a fused, substituted or unsubstituted, aromatic group or heterocyclic group.

Abstract translation: 描述了可以互变异构体形式存在的式I异噻唑并喹啉衍生物（式II），其对各种肿瘤细胞系具有细胞毒性，并可用于治疗肿瘤疾病。 （a）低级烷基，（b）卤代烷基，（c）低级环烷基，（d）烷基氨基，（e）芳族杂环基和（f）苯基; W，X和Z独立地选自氢，卤素和低级烷基; （a）苯基，（b）-NR 2 R 3，（c）双环含N杂环基和（d）-OR 10，其中R 10是氢，低级烷基或苯基; 或者W，X，Y和Z中的任意两个一起形成稠合的取代或未取代的芳族基团或杂环基团。

公开(公告)号：EP0424802B1

公开(公告)日：1995-12-20

申请号：EP90119985.1

申请日：1990-10-18

Applicant: ABBOTT LABORATORIES

Inventor： Chu, Daniel T. ,  Plattner, Jacob J. ,  Klein, Larry L. ,  Shen, Linus L.

IPC: C07C333/06 ,  C07D513/04 ,  C07D519/00 ,  A61K31/435

CPC classification number: C07D513/04 ,  C07C333/06 ,  C07C2601/02 ,  C07D513/14

公开(公告)号：EP0345627A3

公开(公告)日：1991-09-11

申请号：EP89109890.7

申请日：1989-06-01

Applicant: ABBOTT LABORATORIES

Inventor： Pariza, Richard J. ,  Maring, Clarence J. ,  Lartey, Paul A. ,  Klein, Larry L.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: Semisynthetic antibiotics with improved therapeutic properties are disclosed. In particular, 9-R-azacyclic derivatives of erythromycin, its derivatives, and their salts and esters show superior antimicrobial activity compared to other macrolide compounds.

公开(公告)号：EP2336138A3

公开(公告)日：2011-11-16

申请号：EP10184668.1

申请日：2005-06-29

Applicant: ABBOTT LABORATORIES

Inventor： Degoey, DAvid A ,  Flosi, William J ,  Grampovnik, David J. ,  Klein, Larry L. ,  Kempf, Dale J. ,  Wang, Xiu C.

IPC: C07F9/09 ,  A61K31/661 ,  A61P35/00

CPC classification number: A61K45/06 ,  A61K31/661 ,  A61K2300/00

Abstract: A compound of the formula I, II or III is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions of inhibiting HIV protease activity and treating HIV infection are also disclosed.

公开(公告)号：EP0345627B1

公开(公告)日：1997-04-16

申请号：EP89109890.7

申请日：1989-06-01

Applicant: ABBOTT LABORATORIES

Inventor： Pariza, Richard J. ,  Maring, Clarence J. ,  Lartey, Paul A. ,  Klein, Larry L.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08