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1. 发明授权

EP0705279B1 TOPOLOGICALLY SEGREGATED, ENCODED SOLID PHASE LIBRARIES 失效
标题翻译：拓扑别的编码固相文库
公开(公告)号：EP0705279B1
公开(公告)日：2003-02-19
申请号：EP94919294.2
申请日：1994-05-27
申请人： SELECTIDE CORPORATION
发明人： LEBL, Michal , LAM, Kit S. , SALMON, Sydney E. , KRCHNAK, Victor , SEPETOV, Nikolai , KOCIS, Peter
IPC分类号： C07K17/00 , C12Q1/68 , C12P21/00
CPC分类号： C07K1/047 , B01J2219/00572 , B01J2219/00596 , C40B70/00
摘要： The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports. In particular, the invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. Each of the solid phase synthesis support beads contains a single type of synthetic test compound. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.

2. 发明公开

EP0705279A1 TOPOLOGICALLY SEGREGATED, ENCODED SOLID PHASE LIBRARIES 失效
标题翻译：拓扑别的编码固相文库
公开(公告)号：EP0705279A1
公开(公告)日：1996-04-10
申请号：EP94919294.0
申请日：1994-05-27
申请人： SELECTIDE CORPORATION
发明人： LEBL, Michal , LAM, Kit S. , SALMON, Sydney E. , KRCHNAK, Victor , SEPETOV, Nikolai , KOCIS, Peter
IPC分类号： G01N33 , C07B61 , C07K1 , C07K17 , C40B70
CPC分类号： C07K1/047 , B01J2219/00572 , B01J2219/00596 , C40B70/00
摘要： The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports. In particular, the invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. Each of the solid phase synthesis support beads contains a single type of synthetic test compound. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.

3. 发明公开

EP1310510A3 Topologically segregated, encoded solid phase libraries 失效
标题翻译：拓扑不同编码固相文库
公开(公告)号：EP1310510A3
公开(公告)日：2004-04-21
申请号：EP03003577.8
申请日：1994-05-27
申请人： SELECTIDE CORPORATION
发明人： Lebl, Michal , Lam Kit S. , Salmon, Sudney E. , Krchnak, Victor , Sepetov, Nikolai , Kocis, Peter
IPC分类号： C07K1/04 , C07B61/00
CPC分类号： C07K1/047 , B01J2219/00572 , B01J2219/00596 , C40B70/00
摘要： The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.

4. 发明公开

EP0797776A1 COMBINATORIAL LIBRARIES HAVING A PREDETERMINED FREQUENCY OF EACH SPECIES OF TEST COMPOUND 失效
标题翻译：以预定的频率测试连接的任何种组合库
公开(公告)号：EP0797776A1
公开(公告)日：1997-10-01
申请号：EP95942579.0
申请日：1995-12-07
申请人： SELECTIDE CORPORATION
发明人： LEBL, Michal
IPC分类号： B01J19 , C07B61 , C07K1 , C40B30 , G01N33 , C40B40 , C40B60 , C40B70
CPC分类号： C40B30/04 , B01J19/0046 , B01J2219/00315 , B01J2219/00515 , B01J2219/00527 , B01J2219/00545 , B01J2219/00554 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00621 , B01J2219/00626 , B01J2219/00637 , B01J2219/00644 , B01J2219/00657 , B01J2219/00659 , B01J2219/00725 , C07B2200/11 , C07K1/047 , C40B40/10 , C40B60/14 , C40B70/00 , G01N33/54353 , G01N33/6845
摘要： A technique is disclosed for generating nonrandom combinatorial libraries on solid phase supports in which each of a set of predetermined species of test compounds is present on a predetermined number of solid phase supports, preferably on only one, and each solid phase support has only a single species of test compound. Each of the predetermined species of test compounds is prepared with absolute certainty because the technique does not employ any random division of the solid phase supports. Rather, the method is based on the stepwise division of a continuous solid phase support matrix prior to each synthetic step in which more than one type of subunit is added. Non-limiting examples of matrices of the solid phase supports include polypropylene membranes, polytetrafluoropropylene membranes and cotton thread. The combinatorial libraries made by the technique are also disclosed.

5. 发明授权

EP0797776B1 COMBINATORIAL LIBRARIES HAVING A PREDETERMINED FREQUENCY OF EACH SPECIES OF TEST COMPOUND 失效
标题翻译：以预定的频率测试连接的任何种组合库
公开(公告)号：EP0797776B1
公开(公告)日：2002-06-12
申请号：EP95942579.4
申请日：1995-12-07
申请人： SELECTIDE CORPORATION
发明人： LEBL, Michal
IPC分类号： C07K1/04 , G01N33/543
CPC分类号： C40B30/04 , B01J19/0046 , B01J2219/00315 , B01J2219/00515 , B01J2219/00527 , B01J2219/00545 , B01J2219/00554 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00621 , B01J2219/00626 , B01J2219/00637 , B01J2219/00644 , B01J2219/00657 , B01J2219/00659 , B01J2219/00725 , C07B2200/11 , C07K1/047 , C40B40/10 , C40B60/14 , C40B70/00 , G01N33/54353 , G01N33/6845
摘要： A technique is disclosed for generating nonrandom combinatorial libraries on solid phase supports in which each of a set of predetermined species of test compounds is present on a predetermined number of solid phase supports, preferably on only one, and each solid phase support has only a single species of test compound. Each of the predetermined species of test compounds is prepared with absolute certainty because the technique does not employ any random division of the solid phase supports. Rather, the method is based on the stepwise division of a continuous solid phase support matrix prior to each synthetic step in which more than one type of subunit is added. Non-limiting examples of matrices of the solid phase supports include polypropylene membranes, polytetrafluoropropylene membranes and cotton thread. The combinatorial libraries made by the technique are also disclosed.

6. 发明授权

EP0804281B1 APPARATUS AND METHOD FOR MULTIPLE SYNTHESIS OF ORGANIC COMPOUNDS ON POLYMER SUPPORT 失效
标题翻译： DEVICE AND METHOD FOR有机化合物的多条生产上的载体聚合物
公开(公告)号：EP0804281B1
公开(公告)日：2002-06-05
申请号：EP96906212.4
申请日：1996-01-19
申请人： SELECTIDE CORPORATION
发明人： KRCHNAK, Viktor , LEBL, Michal , SELIGMANN, Bruce
IPC分类号： C07K1/04 , G05B13/00 , B01J19/00 , B25J9/16
CPC分类号： B25J9/1679 , B01J19/0046 , B01J2219/00288 , B01J2219/0029 , B01J2219/00308 , B01J2219/00351 , B01J2219/00353 , B01J2219/00416 , B01J2219/00418 , B01J2219/00423 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00691 , B01J2219/00695 , B01J2219/0072 , B01J2219/00725 , C07K1/045 , C07K1/047 , C40B40/10 , C40B60/14 , G05B2219/40101 , G05B2219/45092 , Y10S706/906
摘要： A solid phase synthesis system is provided by employing a fully automated robot (20) that operates with a novel timing protocol executed by a computer (25) for handling multiple synthetic tasks efficiently. The fully automated robot (20) moves along a track (35) and is equipped with a gripper arm (30) which can pick up, position, and operate syringes (40, 60) which can contain solid supports and amino acid reactants. The novel timing protocol is realized by performing steps in the synthesis cycles for different compounds, such as peptides, concurrently rather than on a sequential basis.

7. 发明公开

EP1085943A1 THREE-DIMENSIONAL ARRAY OF SUPPORTS FOR SOLID-PHASE PARALLEL SYNTHESIS AND METHOD OF USE 有权
标题翻译：固相和电路并联合成方法采用三维立体基板MATRIX
公开(公告)号：EP1085943A1
公开(公告)日：2001-03-28
申请号：EP99923278.8
申请日：1999-05-20
申请人： SELECTIDE CORPORATION
发明人： STEIN, David, T. , BAUM, Stephen, A.
IPC分类号： B01L3/00 , B01L11/00 , B01L9/00 , G01N33/53 , G01N33/543
CPC分类号： B82Y30/00 , B01J19/0046 , B01J2219/00286 , B01J2219/0031 , B01J2219/00317 , B01J2219/00319 , B01J2219/00322 , B01J2219/00461 , B01J2219/00468 , B01J2219/00475 , B01J2219/00497 , B01J2219/005 , B01J2219/00502 , B01J2219/00522 , B01J2219/00527 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00668 , B01J2219/00675 , B01J2219/00689 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , B01L2300/0819 , B01L2300/0829 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , G01N33/543
摘要： A three-dimensional (3D) array of solid-phase supports is adapted to provide parallel synthesis of a library of molecules with 3D diversity. Individual locations in the 3D array may be assigned to selected molecules in the library such that molecules may be synthesized at and retrieved from such locations. Also, the supports include aperture walls in stacked plates; the supports may be suspended within stacked plate apertures; the 3D array includes discrete supports arranged in columns in one or more wells; the supports include tube inner walls or may be suspended in tubes, the tubes being secured in stacked, two-dimensional (2D) frameworks; or the supports include beads contained in porous enclosures having non-porous side walls and being secured in stacked, 2D frameworks. A support transfer device enables transfer of solid-phase supports used in a 3D array. Such apparatus includes: a rack of rods sized to be inserted through supports and a mechanism to prevent supports from coming off the rack; tubes connected to a vacuum manifold to suction supports one Z plane at a time; or a transfer block having recesses to receive one or more supports and at least one gate withholding supports from passing through the gate when in a closed position. A method of 3D synthesis includes: a) functionalizing solid-phase supports; b) placing supports in a 3D array; and c) performing parallel synthesis with 3D diversity. At least one unique R1 group member may be assigned to each Z plane.

8. 发明公开

EP0751779A1 SELECTIVELY CLEAVABLE LINKERS BASED ON IMINODIACETIC ACID ESTER BONDS 失效
标题翻译：选择性FISSILE连接对IMMINODIESSIGSÄURE埃斯特·邦兹BASED
公开(公告)号：EP0751779A1
公开(公告)日：1997-01-08
申请号：EP94920294.0
申请日：1994-06-21
申请人： SELECTIDE CORPORATION
发明人： LEBL, Michal , KRCHNAK, Viktor , KOCIS, Petr , LAM, Kit S.
IPC分类号： A61K38 , C07K5 , C07K1
CPC分类号： C07K1/042
摘要： The present invention is directed to linkers based on ester bond linkages, especially iminodiacetic acid ester bond linkages, for use in solid phase peptide synthesis. In particular, the invention is directed to cleavable linkers that can release peptide from the solid phase support under relatively mild conditions by formation of a diketopiperazine or other cyclic structure, such that the cyclic structure remains on the solid phase support, and, in a second cleavage, under more stringent conditions of high pH. The invention is further directed to solid phase supports prepared with multiple cleavable linkers, including a linker that is cleaved by formation of a cyclic product. One such second linker is an ester of hydroxymethylbenzoic acid, or esters formed by carboxy groups of aspartic or glutamic acid.

9. 发明公开

EP1310510A2 Topologically segregated, encoded solid phase libraries 失效
标题翻译： Topologisch getrennte，kodierende Festphasen-Bibliotheken
公开(公告)号：EP1310510A2
公开(公告)日：2003-05-14
申请号：EP03003577.8
申请日：1994-05-27
申请人： SELECTIDE CORPORATION
发明人： Lebl, Michal , Lam Kit S. , Salmon, Sudney E. , Krchnak, Victor , Sepetov, Nikolai , Kocis, Peter
IPC分类号： C07K1/04 , C07B61/00
CPC分类号： C07K1/047 , B01J2219/00572 , B01J2219/00596 , C40B70/00
摘要： The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.
摘要翻译：本发明涉及连接到分离相合成载体上的合成试验化合物文库，其中还包含编码合成试验化合物结构的编码分子。分子可以是聚合物或多个非聚合物分子。合成试验化合物可以具有带有键合的主链结构，例如酰胺，脲，氨基甲酸酯（即氨基甲酸酯），酯，氨基，硫化物，二硫化物或碳 - 碳，如烷烃和烯烃，或其任何组合。提供了适用于不同连接化学物质的亚基的实例。合成试验化合物也可以是分子支架，例如双环碳水化合物，类固醇，糖，杂环结构，多芳族结构或能够作为脚手架的其它结构的单环衍生物。提供合适的分子支架的实例。本发明还涉及合成这些文库的方法以及这些文库在合成测试化合物文库中鉴定和表征目的分子的用途。

10. 发明授权

EP0751779B1 SELECTIVELY CLEAVABLE LINKERS BASED ON IMINODIACETIC ACID ESTER BONDS 失效
标题翻译：选择性FISSILE连接对亚氨基二乙酸埃斯特·邦兹BASED
公开(公告)号：EP0751779B1
公开(公告)日：2001-12-19
申请号：EP94920294.9
申请日：1994-06-21
申请人： SELECTIDE CORPORATION
发明人： LEBL, Michal , KRCHNAK, Viktor , KOCIS, Petr , LAM, Kit S.
IPC分类号： A61K38/00
CPC分类号： C07K1/042
摘要： The present invention is directed to linkers based on ester bond linkages, especially iminodiacetic acid ester bond linkages, for use in solid phase peptide synthesis. In particular, the invention is directed to cleavable linkers that can release peptide from the solid phase support under relatively mild conditions by formation of a diketopiperazine or other cyclic structure, such that the cyclic structure remains on the solid phase support, and, in a second cleavage, under more stringent conditions of high pH. The invention is further directed to solid phase supports prepared with multiple cleavable linkers, including a linker that is cleaved by formation of a cyclic product. One such second linker is an ester of hydroxymethylbenzoic acid, or esters formed by carboxy groups of aspartic or glutamic acid.

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