公开(公告)号：WO2010030359A2

公开(公告)日：2010-03-18

申请号：PCT/US2009/005082

申请日：2009-09-10

Applicant: ENANTA PHARJMACEUTICALS, INC. ,  ABBOTT LABORATORIES ,  KU, Yiyin ,  MCDANIEL, Keith, F. ,  CHEN, Hui-ju ,  SHANLEY, Jason, P. ,  KEMPF, Dale, J. ,  GRAMPOVNIK, David, J. ,  SUN, Ying ,  LIU, Dong ,  GAI, Yonghua ,  OR, Yat, Sun ,  WAGAW, Sable, H. ,  ENGSTROM, Ken ,  GRIEME, Tim ,  SHEIKH, Ahmad ,  MEI, Jianzhang

Inventor： KU, Yiyin ,  MCDANIEL, Keith, F. ,  CHEN, Hui-ju ,  SHANLEY, Jason, P. ,  KEMPF, Dale, J. ,  GRAMPOVNIK, David, J. ,  SUN, Ying ,  LIU, Dong ,  GAI, Yonghua ,  OR, Yat, Sun ,  WAGAW, Sable, H. ,  ENGSTROM, Ken ,  GRIEME, Tim ,  SHEIKH, Ahmad ,  MEI, Jianzhang

IPC: A61K38/12

CPC classification number: C07K1/113 ,  C07D487/04

Abstract: The present invention relates to novel macrocyclic compounds and methods of use thereof. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

Abstract translation: 本发明涉及新的大环化合物及其使用方法。 本发明还涉及药物组合物，其包含本发明化合物或其药学上可接受的盐，酯或前药以及药学上可接受的载体或赋形剂。

公开(公告)号：WO2003002548A1

公开(公告)日：2003-01-09

申请号：PCT/US2002/019115

申请日：2002-06-11

Applicant: ABBOTT LABORATORIES

Inventor： KU, Yi-Yin ,  GRIEME, Tim ,  MORTON, Howard, E. ,  KING, Steven, A.

IPC: C07D311/80

CPC classification number: C07D491/04 ,  C07D215/14

Abstract: The present invention relates to the preparation of chiral glucocorticoid receptor agents via biaryl atropisomers.

Abstract translation: 本发明涉及通过联芳基阻转异构体制备手性糖皮质激素受体剂。

公开(公告)号：EP1272500A2

公开(公告)日：2003-01-08

申请号：EP00942860.8

申请日：2000-06-15

Applicant: Abbott Laboratories

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: C07H17/08 ,  A61K31/70 ,  A61P31/04

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.

公开(公告)号：EP2340029A2

公开(公告)日：2011-07-06

申请号：EP09813360.6

申请日：2009-09-10

Applicant: Enanta Pharmaceuticals, Inc. ,  Abbott Laboratories

Inventor： KU, Yiyin ,  MCDANIEL, Keith, F. ,  CHEN, Hui-ju ,  SHANLEY, Jason, P. ,  KEMPF, Dale, J. ,  GRAMPOVNIK, David, J. ,  SUN, Ying ,  LIU, Dong ,  GAI, Yonghua ,  OR, Yat, Sun ,  WAGAW, Sable, H. ,  ENGSTROM, Ken ,  GRIEME, Tim ,  SHEIKH, Ahmad ,  MEI, Jianzhang

IPC: A61K38/00 ,  A61K38/12

CPC classification number: C07K1/113 ,  C07D487/04

Abstract: The present invention relates to novel macrocyclic compounds and methods of use thereof. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

公开(公告)号：EP1272500B1

公开(公告)日：2005-05-04

申请号：EP00942860.8

申请日：2000-06-15

Applicant: Abbott Laboratories

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: C07H17/08 ,  A61K31/70 ,  A61P31/04

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.