公开(公告)号：WO2002081441A1

公开(公告)日：2002-10-17

申请号：PCT/US2002/008074

申请日：2002-03-18

Applicant: ABBOTT LABORATORIES

Inventor： WITTENBERGER, Steven, J. ,  BHAGAVATULA, Lakshmi ,  DEGOEY, David, A. ,  DEMATTEI, John ,  HILL, David, R. ,  MCLAUGHLIN, Maureen, A. ,  GUPTA, Ashok, K. ,  MANNA, Sukumar ,  NICHOLS, Paul, J. ,  RAMIYA, Premchandran, H. ,  TIAN, Zhenping ,  RASMUSSEN, Michael, W.

IPC: C07D207/16

CPC classification number: C07D207/26 ,  C07D207/12 ,  C07D207/16

Abstract: A process for the preparation of neuraminidase inhibitors having structural formula (28) or therapeutically acceptable salts thereof, in which R1 is alkyl, cycloalkyl, cycloalkylalkyl, or arylalkyl; R2 is alkyl, cycloalkyl, cycloalkylalkyl, or arylalkyl; R4 is alkyl, cycloalkyalkyl, or aryl-(C2-C4-alkyl); R10 is methyl, ethyl, iso-propyl, or vinyl; and R12 is hydrogen or alkyl and intermediates useful for the process are disclosed.

Abstract translation: 制备具有结构式（28）或其治疗上可接受的盐的神经氨酸酶抑制剂的方法，其中R 1是烷基，环烷基，环烷基烷基或芳基烷基; R2是烷基，环烷基，环烷基烷基或芳基烷基; R4是烷基，环烷基或芳基 - （C 2 -C 4 - 烷基）; 甲基，乙基，异丙基或乙烯基; 并且R 12是氢或烷基，并且公开了可用于该方法的中间体。

公开(公告)号：EP1129076A1

公开(公告)日：2001-09-05

申请号：EP99961631.1

申请日：1999-11-09

Applicant: ABBOTT LABORATORIES

Inventor： HAVIV, Fortuna ,  DWIGHT, Wesley, J. ,  CRAWFORD, Bradley, W. ,  SWENSON, Rolf, E. ,  BRUNCKO, Milan ,  KAMINSKI, Michele, A. ,  FREY, Lisa, M. ,  DEMATTEI, John ,  GREER, Jonathan

IPC: C07D217/04 ,  C07D217/14 ,  C07D217/16 ,  A61K31/472 ,  A61P5/00 ,  C07D217/20 ,  C07D217/26 ,  C07D223/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/10 ,  C07D491/04 ,  C07D401/08

CPC classification number: C07D401/04 ,  C07D217/04 ,  C07D217/14 ,  C07D217/16 ,  C07D217/18 ,  C07D217/20 ,  C07D217/22 ,  C07D223/16 ,  C07D401/06 ,  C07D401/12 ,  C07D491/04

Abstract: Tetrahydroisoquinoline derivatives of formula (I): or a pharmaceutically acceptable salt, ester, or prodrug thereof, having activity as an LHRH antagonist, as well as pharmaceutical compositions containing the same, and methods for their use and preparation.