公开(公告)号：WO0224648A3

公开(公告)日：2002-06-13

申请号：PCT/US0129408

申请日：2001-09-20

Applicant: ABBOTT LAB

Inventor： GUPTA ASHOK K ,  KING STEVEN A ,  LEE ELAINE C ,  MORTON HOWARD E ,  PLATA DANIEL J ,  PU YU-MING ,  SHARMA PADAM N

IPC: C07D209/08

CPC classification number: C07D209/08

Abstract: The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors, comprising the reaction of 1-formyl indoline with clorosulfonic acid and thionyl chloride, followed by reaction with an aromatic amine.

Abstract translation: 本发明公开了一种合成取代的吲哚细胞增殖抑制剂的方法，其包括1-甲酰基二氢吲哚与氯磺酸和亚硫酰氯的反应，然后与芳族胺反应。

公开(公告)号：WO9608455A3

公开(公告)日：1996-06-13

申请号：PCT/US9511522

申请日：1995-09-14

Applicant: ABBOTT LAB

Inventor： CHORGHADE MUKUND S ,  DOLPHIN DAVID H ,  HILL DAVID R ,  HINO FUMIO ,  LEE ELAINE C

IPC: G01N33/15 ,  B01J31/18 ,  C07B33/00 ,  C07D231/44 ,  C07D233/36 ,  C07D405/04 ,  C07D413/04 ,  C07D487/22

CPC classification number: B01J31/1815 ,  B01J2531/025 ,  B01J2531/16 ,  B01J2531/62 ,  B01J2531/72 ,  B01J2531/821 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  C07B33/00 ,  C07D231/44 ,  C07D233/36 ,  C07D405/04 ,  C07D413/04

Abstract: A method for the systematic and efficient synthetic preparation and identification of metabolites of a pharmaceutical product in order to study possible toxic and/or otherwise biologically-active metabolites of such pharmaceutical products as early and conveniently as possible in the very expensive drug development process, comprising adding samples of the pharmaceutical product to a series of combinations of a synthetic metalloporphyrin (SMP) with a synthetic metalloporphyrin-co-oxidizing reagent in the presence of a suitable solvent, under specified conditions, in a manner such that each sample of pharmaceutical product is reacted with a different combination of synthetic metalloporphyrin, SMP-co-oxidizing reagent and solvent, followed by separation and isolation of the resulting oxidative products, then confirmation of the identity of metabolites from the pre-identified oxidative products by appropriate animal model studies, and subjecting the actual metabolites prepared in larger quantities by the above method to toxicologic, pathologic, histopathologic, mechanistic or genotoxic testing in order to identify toxic and/or otherwise metabolically-active beneficial or detrimental individual metabolites.

公开(公告)号：WO0078773A3

公开(公告)日：2001-02-22

申请号：PCT/US0016579

申请日：2000-06-15

Applicant: ABBOTT LAB

Inventor： STONER ERIC J ,  PETERSON MATTHEW J ,  KU YI-YIN ,  CINK RUSSELL D ,  COOPER ARTHUR J ,  DESHPANDE MAHENDRA N ,  GRIEME TIM ,  HAIGHT ANTHONY R ,  HILL DAVID R ,  HSU MARGARET CHI-PING ,  KING STEVEN A ,  LEANNA MARVIN R ,  LEE ELAINE C ,  MCLAUGHLIN MAUREEN A ,  MORTON HOWARD E ,  NAPIER JAMES J ,  PLATA DANIEL J ,  RAJE PRASAD S ,  RASMUSSEN MICHAEL ,  RILEY DAVID ,  TIEN JIEN-HEH J ,  WITTENBERGER STEVEN J

IPC: A61P31/04 ,  C07B61/00 ,  C07H1/00 ,  C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4"-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

Abstract translation: 一方面，本发明涉及一种制备6-O-取代的红霉素衍生物的方法，包括在钯催化剂和膦存在下使2'-取代的和任选的4'-取代的9-肟红霉素衍生物与烷基化剂反应。 另一方面，本发明涉及使用钯催化的烷基化反应制备6-O-取代的红霉素酮内酯的方法。

公开(公告)号：AT294809T

公开(公告)日：2005-05-15

申请号：AT00942860

申请日：2000-06-15

Applicant: ABBOTT LAB

Inventor： STONER ERIC J ,  PETERSON MATTHEW J ,  KU YI-YIN ,  CINK RUSSELL D ,  COOPER ARTHUR J ,  DESHPANDE MAHENDRA N ,  GRIEME TIM ,  HAIGHT ANTHONY R ,  HILL DAVID R ,  HSU MARGARET CHI-PING ,  KING STEVEN A ,  LEANNA MARVIN R ,  LEE ELAINE C ,  MCLAUGHLIN MAUREEN A ,  MORTON HOWARD E ,  NAPIER JAMES J ,  PLATA DANIEL J ,  RAJE PRASAD S ,  RASMUSSEN MICHAEL ,  RILEY DAVID ,  TIEN JIEN-HEH J ,  WITTENBERGER STEVEN J

IPC: A61P31/04 ,  C07B61/00 ,  C07H1/00 ,  C07H17/08 ,  A61K31/70

Abstract: In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4''-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

公开(公告)号：DE69825785D1

公开(公告)日：2004-09-23

申请号：DE69825785

申请日：1998-11-17

Applicant: ABBOTT LAB

Inventor： KU YI-YIN ,  RILEY DAVID A ,  LEE ELAINE C ,  TIEN JIEN-HEH J

IPC: C07H17/08

Abstract: The claimed invention provides a novel method of preparing 6-O-methyl erythromycin A. The process comprises the steps of reducing the 9-keto group of erythromycin A to form a 9-hydroxy erythromycin A, protecting the 9-, 2'-, and/or 4''-hydroxyl groups of erythromycin A, selectively methylating the 6-position of the 9-hydroxy erythromycin A derivative, deprotecting the hydroxyl groups and oxidizing the 9-hydroxyl to afford 6-O-methyl erythromycin A.

公开(公告)号：CA2375364A1

公开(公告)日：2000-12-28

申请号：CA2375364

申请日：2000-06-15

Applicant: ABBOTT LAB

Inventor： MORTON HOWARD E ,  HAIGHT ANTHONY R ,  MCLAUGHLIN MAUREEN A ,  GRIEME TIM ,  RASMUSSEN MICHAEL ,  HSU MARGARET CHI-PING ,  KING STEVEN A ,  RILEY DAVID ,  WITTENBERGER STEVEN J ,  TIEN JIEN-HEH J ,  LEANNA MARVIN R ,  RAJE PRASAD S ,  HILL DAVID R ,  PLATA DANIEL J ,  DESHPANDE MAHENDRA N ,  COOPER ARTHUR J ,  KU YI-YIN ,  CINK RUSSELL D ,  LEE ELAINE C ,  PETERSON MATTHEW J ,  STONER ERIC J ,  NAPIER JAMES J

IPC: A61P31/04 ,  C07B61/00 ,  C07H1/00 ,  C07H17/08 ,  A61K31/70

Abstract: In one aspect, the invention relates to a process for preparing 6-O- substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4"-substituted 9-oxime erythromycin derivatives with an alkylatin g agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

公开(公告)号：CA2375364C

公开(公告)日：2008-11-25

申请号：CA2375364

申请日：2000-06-15

Applicant: ABBOTT LAB

Inventor： MCLAUGHLIN MAUREEN A ,  HAIGHT ANTHONY R ,  MORTON HOWARD E ,  PETERSON MATTHEW J ,  GRIEME TIM ,  RILEY DAVID ,  DESHPANDE MAHENDRA N ,  WITTENBERGER STEVEN J ,  NAPIER JAMES J ,  TIEN JIEN-HEH J ,  RAJE PRASAD S ,  PLATA DANIEL J ,  KU YI-YIN ,  CINK RUSSELL D ,  COOPER ARTHUR J ,  KING STEVEN A ,  RASMUSSEN MICHAEL ,  STONER ERIC J ,  HSU MARGARET CHI-PING ,  LEE ELAINE C ,  LEANNA MARVIN R ,  HILL DAVID R

IPC: C07H17/08 ,  A61K31/7048 ,  A61P31/04 ,  C07B61/00 ,  C07H1/00

Abstract: In one aspect, the invention relates to a process for preparing 6-O- substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4"-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates t o processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

公开(公告)号：PT1044209E

公开(公告)日：2004-11-30

申请号：PT98959481

申请日：1998-11-17

Applicant: ABBOTT LAB

Inventor： RILEY DAVID A ,  TIEN JIEN-HEH J ,  KU YI-YIN ,  LEE ELAINE C

IPC: C07H17/08

Abstract: The claimed invention provides a novel method of preparing 6-O-methyl erythromycin A. The process comprises the steps of reducing the 9-keto group of erythromycin A to form a 9-hydroxy erythromycin A, protecting the 9-, 2'-, and/or 4''-hydroxyl groups of erythromycin A, selectively methylating the 6-position of the 9-hydroxy erythromycin A derivative, deprotecting the hydroxyl groups and oxidizing the 9-hydroxyl to afford 6-O-methyl erythromycin A.

公开(公告)号：AU1526999A

公开(公告)日：1999-07-05

申请号：AU1526999

申请日：1998-11-17

Applicant: ABBOTT LAB

Inventor： RILEY DAVID A ,  KU YI-YIN ,  LEE ELAINE C ,  TIEN JIEN-HEH J

IPC: C07H17/08

Abstract: The claimed invention provides a novel method of preparing 6-O-methyl erythromycin A. The process comprises the steps of reducing the 9-keto group of erythromycin A to form a 9-hydroxy erythromycin A, protecting the 9-, 2'-, and/or 4''-hydroxyl groups of erythromycin A, selectively methylating the 6-position of the 9-hydroxy erythromycin A derivative, deprotecting the hydroxyl groups and oxidizing the 9-hydroxyl to afford 6-O-methyl erythromycin A.

公开(公告)号：CA2195873A1

公开(公告)日：1996-03-21

申请号：CA2195873

申请日：1995-09-14

Applicant: ABBOTT LAB

Inventor： CHORGHADE MUKUND ,  DOLPHIN DAVID H ,  HILL DAVID R ,  HINO FUMIO ,  LEE ELAINE C

IPC: G01N33/15 ,  B01J31/18 ,  C07B33/00 ,  C07D231/44 ,  C07D233/36 ,  C07D405/04 ,  C07D413/04 ,  C07D487/22

Abstract: A method for the systematic and efficient synthetic preparation and identification of metabolites of a pharmaceutical product in order to study possible toxic and/or otherwise biologically-active metabolites of such pharmaceutical products as early and conveniently as possible in the very expensive drug development process, comprising adding samples of the pharmaceutical product to a series of combinations of a synthetic metalloporphyrin (SMP) with a synthetic metalloporphyrin-co-oxidizing reagent in the presence of a suitable solvent, under specified conditions, in a manner such that each sample of pharmaceutical product is reacted with a different combination of synthetic metalloporphyrin, SMP-co-oxidizing reagent and solvent, followed by separation and isolation of the resulting oxidative products, then confirmation of the identity of metabolites from the preidentified oxidative products by appropriate animal model studies, and subjecting the actual metabolites prepared in larger quantities by the above method to toxicologic, pathologic, histopathologic, mechanistic or genotoxic testing in order to identify toxic and/or otherwise metabolically-active beneficial or detrimental individual metabolites.