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公开(公告)号:HU0101959A2
公开(公告)日:2001-09-28
申请号:HU0101959
申请日:1999-03-05
Applicant: ABBOTT LAB
Inventor: ABAD-ZAPATERO CELERINO , GREER JONATHAN , NIENABER VICKI L , NORBECK DANIEL W
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公开(公告)号:NO20004860A
公开(公告)日:2000-11-24
申请号:NO20004860
申请日:2000-09-27
Applicant: ABBOTT LAB
Inventor: SAUER DARYL R , HAVIV FORTUNA , RANDOLPH JOHN , MORT NICHOLAS A , DALTON CHRISTOPHER ROBIN , BRUNCKO MILAN , KAMINSKI MICHELE A , CRAWFORD BRADLEY W , FREY LISA MARIE , GREER JONATHAN
IPC: A61K31/7042 , A61K31/7048 , A61K31/7056 , A61P5/24 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07H17/08
CPC classification number: C07H17/08
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公开(公告)号:CA2351187A1
公开(公告)日:2000-05-25
申请号:CA2351187
申请日:1999-11-09
Applicant: ABBOTT LAB
Inventor: CRAWFORD BRADLEY W , HAVIV FORTUNA , SWENSON ROLF E , BRUNCKO MILAN , KAMINSKI MICHELE A , DWIGHT WESLEY J , FREY LISA M , DEMATTEI JOHN , GREER JONATHAN
IPC: C07D217/06 , A61K31/472 , A61K31/4725 , A61K31/4741 , A61K31/55 , A61P5/00 , A61P13/08 , A61P15/00 , A61P35/00 , C07D217/04 , C07D217/14 , C07D217/16 , C07D217/18 , C07D217/20 , C07D217/22 , C07D217/26 , C07D223/16 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/12 , C07D491/04 , C07D491/056 , C07D221/00 , C07D317/00 , C07D319/00 , C07D401/10
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.
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公开(公告)号:CA2321968A1
公开(公告)日:1999-09-10
申请号:CA2321968
申请日:1999-03-05
Applicant: ABBOTT LAB
Inventor: NORBECK DANIEL W , ABAD-ZAPATERO CELERINO , GREER JONATHAN , NIENABER VICKI L
Abstract: X-ray crystallography can be used to screen compounds that are not known ligands of a target biomolecule for their ability to bind the target biomolecule. The method includes obtaining a crystal of a target biomolecule; exposing the target biomolecule crytal to one or more test samples; and obtaining an X-ray crystal diffraction pattern to determine whether a ligand/receptor complex is formed. The target is exposed to the test samples by either co-crystallizing a biomolecule in the presence of one or more test samples or soaking the biomolecule crystal in a solution of one or more test samples. In another embodiment, structural information from ligand/receptor complexes are used to design ligands that bind tighter, that bind more specifically, that have better biological activity or that have better safety profile. A further embodiment of the invention comprises identifying or designing biologically-active moieties by the instant process. In a further embodiment, a biomolecule crystal having an easily accessible active site is formed by co-crystallizing the biomolecule with a degradable ligand and degrading the ligand.
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公开(公告)号:CA2136078A1
公开(公告)日:1994-06-23
申请号:CA2136078
申请日:1993-11-30
Applicant: ABBOTT LAB
Inventor: GREER JONATHAN , HAVIV FORTUNA , FITZPATRICK TIMOTHY D , SWENSON ROLF E , NICHOLS CHARLES J , MORT NICHOLAS A
Abstract: 2136078 9413313 PCTABS00032 The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A1-D2-E3-G4-J5-L6-M7-Q8-R9-T10. The compounds of the percent invention are characterized by having an .OMEGA.-amino-functionalized side chain on the D-aminoacyl residue at position 6. The .OMEGA.-amino group of this side chain is further derivatized by the attachment of an extending group which likewise has a terminal amino group which is capped by an acyl group.
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公开(公告)号:NO903454A
公开(公告)日:1991-02-08
申请号:NO903454
申请日:1990-08-06
Applicant: ABBOTT LAB
Inventor: HAVIV FORTUNA , GREER JONATHAN , PALABRICA CHRISTOPHER A , FITZPATRICK TIMOTHY D
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公开(公告)号:AU767991B2
公开(公告)日:2003-11-27
申请号:AU2987899
申请日:1999-03-05
Applicant: ABBOTT LAB
Inventor: NIENABER VICKI L , GREER JONATHAN , ABAD-ZAPATERO CELERINO , NORBECK DANIEL W
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公开(公告)号:TR200101127T2
公开(公告)日:2002-06-21
申请号:TR200101127
申请日:1999-03-05
Applicant: ABBOTT LAB
Inventor: NIENABER VICKI L , GREER JONATHAN , ABAD-ZAPATERO CELERINO , NORBECK DANIEL W
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公开(公告)号:DE69330838T2
公开(公告)日:2002-04-25
申请号:DE69330838
申请日:1993-12-14
Applicant: ABBOTT LAB
Inventor: HAVIV FORTUNA , GREER JONATHAN , SWENSON ROLF E , SAUER DARYL R
Abstract: A class of potent LHRH decapeptide antagonists possess N-alkylated aminoacyl residues where the side-chain portion of the residue is a 4-(substimtedamino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or OMEGA -(substitutedamino)alkyl group, and additionally the aminoacyl residues at position 5 are N-alkylated on the nitrogen atom of the peptide backbone.
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公开(公告)号:TR200101200T2
公开(公告)日:2002-02-21
申请号:TR200101200
申请日:1999-03-05
Applicant: ABBOTT LAB
Inventor: NIENABER VICKI L , GREER JONATHAN , ABAD-ZAPATERO CELERINO , NORBECK DANIEL W
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