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公开(公告)号：WO1999045389A2
公开(公告)日：1999-09-10
申请号：PCT/US1999004518
申请日：1999-03-01
Applicant: ABBOTT LABORATORIES
Inventor： ABBOTT LABORATORIES , NIENABER, Vicki, L. , GREER, Jonathan , ABAD-ZAPATERO, Celerino , NORBECK, Daniel, W.
IPC: G01N33/50
CPC classification number: G01N33/6845 , C07K2299/00 , C30B7/00 , G01N23/20 , G01N33/68 , G01N33/6803 , G01N33/6842 , G01N2333/9723 , G01N2500/00
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 crystal 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.
Abstract translation: 可以使用X射线晶体学来筛选目标生物分子的未知配体的化合物，以获得其结合目标生物分子的能力。 该方法包括获得目标生物分子的晶体; 将目标生物分子晶体暴露于一个或多个测试样品; 并获得X射线晶体衍射图，以确定是否形成配体/受体复合物。 通过在一个或多个测试样品的存在下共生结晶生物分子或将生物分子晶体浸泡在一个或多个测试样品的溶液中，将靶标暴露于测试样品。 在另一个实施方案中，来自配体/受体复合物的结构信息用于设计更紧密结合的配体，其更具体地结合，具有更好的生物活性或具有更好的安全性。 本发明的另一个实施方案包括通过本方法识别或设计生物活性部分。 在另一个实施方案中，通过使生物分子与可降解配体共结晶并使配体降解而形成具有易于接近的活性位点的生物分子晶体。
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2.发明申请LHRH ANTAGONISTS HAVING MODIFIED AMINOACYL RESIDUES AT POSTIONS 5 AND 6 审中-公开在第5和第6位具有改性氨基酸残基的LHRH拮抗剂
公开(公告)号：WO1994014841A1
公开(公告)日：1994-07-07
申请号：PCT/US1993012196
申请日：1993-12-14
Applicant: ABBOTT LABORATORIES
Inventor： ABBOTT LABORATORIES , HAVIV, Fortuna , GREER, Jonathan , SWENSON, Rolf, E. , SAUER, Daryl, R.
IPC: C07K07/00
Abstract: A class of potent LHRH decapeptide antagonists possess N-alkylated aminoacyl residues where the side-chain portion of the residue is a 4-(substituted-amino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or OMEGA -(substituted-amino)alkyl group, and additionally the aminoacyl residues at position 5 are N-alkylated on the nitrogen atom of the peptide backbone.
Abstract translation: 一类有效的LHRH十肽拮抗剂具有N-烷基化氨酰基残基，其中残基的侧链部分是4-（取代的 - 氨基）苯丙氨酰基，4-（取代的 - 氨基）环己基丙氨酰或OMEGA - （取代的 - 氨基） 烷基，另外第5位的氨酰基残基在肽骨架的氮原子上进行N-烷基化。
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3.发明公开TETRAHYDROISOQUINOLINE DERIVATIVES AS LHRH ANTAGONISTS 审中-公开TETRAHYDROISOCHINOLINE衍生物在ALS LHRH受体拮抗剂
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.
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4.发明授权LHRH ANTAGONISTS HAVING MODIFIED AMINOACYL RESIDUES AT POSTIONS 5 AND 6 失效LHRH拮抗剂WITH改性氨TO THE 5和6位
公开(公告)号：EP0683792B1
公开(公告)日：2001-09-26
申请号：EP94905391.2
申请日：1993-12-14
Applicant: ABBOTT LABORATORIES
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-(substituted-amino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or OMEGA -(substituted-amino)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：EP1210589B1
公开(公告)日：2012-09-19
申请号：EP00957348.6
申请日：2000-08-09
Applicant: ABBOTT LABORATORIES
Inventor： OLSON, Jeffrey, A. , JONES, Ronald, B. , NIENABER, Vicki, L. , MUCHMORE, Steven, W. , PAN, Jeffrey, Y. , GREER, Jonathan
CPC classification number: G01N23/20 , Y10T436/25
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Patent Agency Ranking
公开(公告)号：EP1210589A2
公开(公告)日：2002-06-05
申请号：EP00957348.6
申请日：2000-08-09
Applicant: ABBOTT LABORATORIES
Inventor： OLSON, Jeffrey, A. , JONES, Ronald, B. , NIENABER, Vicki, L. , MUCHMORE, Steven, W. , PAN, Jeffrey, Y. , GREER, Jonathan
CPC classification number: G01N23/20 , Y10T436/25
Abstract: Method and apparatus for mounting a sample comprising a crystal for X-ray crystallographic analysis, a method for aligning a sample comprising a crystal for X-ray crystallographic analysis, which sample is mounted on a positioning device, and a method for determining the structure of a sample containing a crystal by means of X-ray crystallography.
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公开(公告)号：EP1068531B1
公开(公告)日：2007-10-10
申请号：EP99911174.3
申请日：1999-03-05
Applicant: ABBOTT LABORATORIES
Inventor： NIENABER, Vicki, L. , GREER, Jonathan , ABAD-ZAPATERO, Celerino , NORBECK, Daniel, W.
CPC classification number: G01N33/6845 , C07K2299/00 , C30B7/00 , G01N23/20 , G01N33/68 , G01N33/6803 , G01N33/6842 , G01N2333/9723 , G01N2500/00
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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8.发明公开LHRH ANTAGONISTS HAVING MODIFIED AMINOACYL RESIDUES AT POSTIONS 5 AND 6 失效与LHRH antagoniste修改后的实体TO THE 5位和第6
公开(公告)号：EP0683792A1
公开(公告)日：1995-11-29
申请号：EP94905391.0
申请日：1993-12-14
Applicant: ABBOTT LABORATORIES
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-(substituted-amino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or Φ-(substituted-amino)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：EP1068531A2
公开(公告)日：2001-01-17
申请号：EP99911174.3
申请日：1999-03-05
Applicant: Abbott Laboratories
Inventor： NIENABER, Vicki, L. , GREER, Jonathan , ABAD-ZAPATERO, Celerino , NORBECK, Daniel, W.
CPC classification number: G01N33/6845 , C07K2299/00 , C30B7/00 , G01N23/20 , G01N33/68 , G01N33/6803 , G01N33/6842 , G01N2333/9723 , G01N2500/00
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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10.发明公开6-POSITION MODIFIED DECAPEPTIDE LHRH ANTAGONISTS 失效LHRH ANTAGONISTISCHE DECAPEPTIDE IN POSITTION 6 MODIFIZIERT。
公开(公告)号：EP0673254A1
公开(公告)日：1995-09-27
申请号：EP94903367.0
申请日：1993-11-30
Applicant: ABBOTT LABORATORIES
Inventor： GREER, Jonathan , HAVIV, Fortuna , FITZPATRICK, Timothy D. , SWENSON, Rolf E. , NICHOLS, Charles J. , MORT, Nicholas A.
Abstract: The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A?1-D2-E3-G4-J5-L6-M7-Q8-R9-T10¿. The compounds of the percent invention are characterized by having an Φ-amino-functionalized side chain on the D-aminoacyl residue at position 6. The Φ-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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