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1. 发明申请

WO0138268A9 APPARATUS AND METHOD FOR SYNTHESIZING COMBINATORIAL LIBRARIES 审中-公开
标题翻译：用于合成组合图书馆的装置和方法
公开(公告)号：WO0138268A9
公开(公告)日：2002-05-23
申请号：PCT/US0032104
申请日：2000-11-22
申请人： SELECTIDE CORP
发明人： PATEK MARCEL , PAVEL SAFAR , SMRCINA MARTIN , WEGRZYNIAK ERIC , STROP PETER , FLYNN GARY A , BAUM STEPHEN A
IPC分类号： C07B61/00 , B01J19/00 , C40B40/06 , C40B40/10 , C40B50/00 , C40B50/14 , C40B60/00 , C40B60/14 , C40B70/00 , G01N33/543
CPC分类号： B82Y30/00 , B01J19/0046 , B01J2219/00286 , B01J2219/0031 , B01J2219/00313 , B01J2219/00315 , B01J2219/00317 , B01J2219/00319 , B01J2219/00322 , B01J2219/00328 , B01J2219/00459 , B01J2219/00461 , B01J2219/00468 , B01J2219/00472 , B01J2219/00475 , B01J2219/00497 , B01J2219/005 , B01J2219/00502 , B01J2219/00522 , B01J2219/00527 , B01J2219/00565 , B01J2219/00585 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00659 , B01J2219/00664 , B01J2219/00668 , B01J2219/00675 , B01J2219/00689 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , B01L2300/0819 , B01L2300/0829 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , C40B70/00 , G01N33/543 , Y10T436/24 , Y10T436/25 , Y10T436/255
摘要： An apparatus and method for synthesizing a combinatorial library comprising a plurality of chemical compounds such that the chemical composition of each compound is easily tracked. The library compounds are synthesized on solid-phase supports, which are spatially arranged in frames during synthesis according to a predetermined protocol, such that each solid-phase support passes through a series of unique spatial 2D or 3D addresses by which the chemical composition of each compound may be determined at any point during synthesis. Solid-phase supports include hollow tubular-lanterns and gears.
摘要翻译：一种用于合成包含多种化学化合物的组合文库的装置和方法，使得易于追踪每种化合物的化学组成。文库化合物在固相载体上合成，根据预定的方案在合成过程中在空间上排列成帧，使得每个固相载体通过一系列独特的空间2D或3D地址，通过这些独特的空间2D或3D地址，化合物可以在合成过程中的任何时间点确定。固相支架包括中空管状灯笼和齿轮。

2. 发明专利

JP2003327597A Selectively cleavable linker based on iminodiacetic acid ester 有权
标题翻译：基于氨基酸酯酶的选择性可清除的连接酶
公开(公告)号：JP2003327597A
公开(公告)日：2003-11-19
申请号：JP2003159838
申请日：2003-06-04
申请人： Selectide Corp , セレクタイドコーポレーション
发明人： LEBL MICHAL , KRCHNAK VIKTOR , KOCIS PETR , LAM KIT S
IPC分类号： A61K38/00 , C07K5/00 , C07K1/04
CPC分类号： C07K1/042
摘要： PROBLEM TO BE SOLVED: To provide a cleavable linker forming a peptide having a substantially unchanged structure, especially a peptide having unbonded diketopiperazine part. SOLUTION: The linker based on an ester bond linkage, especially an iminodiacetic acid ester bond linkage for use in solid phase peptide synthesis is provided. In particular, the cleavable linker can release a peptide from the solid phase support under relatively mild conditions by formation of a diketopiperazine or other cyclic structure remaining on the solid phase support, and, in a second cleavage, under more stringent conditions of high pH. The solid phase supports are prepared with multiple cleavage 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. COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：提供形成具有基本上不变的结构的肽的可切割连接物，特别是具有未结合的二酮哌嗪部分的肽。解决方案：提供了基于酯键连接的接头，特别是用于固相肽合成的亚氨基二乙酸酯键键。特别地，可切割接头可以在相对温和的条件下通过形成二酮哌嗪或保留在固相载体上的其它环状结构，以及在更高严格条件下的高pH下在第二次裂解中从固相支持物释放肽。固相载体用多个裂解连接子制备，包括通过形成环状产物而切割的连接体。一个这样的第二接头是羟甲基苯甲酸的酯，或由天冬氨酸或谷氨酸的羧基形成的酯。版权所有（C）2004，JPO

3. 发明公开

EP0705279A4 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：EP0705279A4
公开(公告)日：1999-03-24
申请号：EP94919294
申请日：1994-05-27
申请人： SELECTIDE CORP
发明人： LEBL MICHAL , LAM KIT S , SALMON SYDNEY E , KRCHNAK VICTOR , SEPETOV NIKOLAI , KOCIS PETER
IPC分类号： G01N33/53 , C07B61/00 , C07K1/04 , C07K17/00 , C40B70/00 , G01N33/543 , G01N33/566 , C12P21/00 , C12Q1/68
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.

4. 发明公开

EP0804281A4 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：EP0804281A4
公开(公告)日：1998-09-02
申请号：EP96906212
申请日：1996-01-19
申请人： SELECTIDE CORP
发明人： KRCHNAK VIKTOR , LEBL MICHAL , SELIGMANN BRUCE
IPC分类号： B01J19/00 , B25J9/16 , C07K1/04 , C40B40/10 , C40B60/14 , B01J8/02 , C07K1/06 , C07K1/08 , C07K1/10 , C08F283/00 , C08G69/10 , G05B13/00 , G05B19/402
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.

5. 发明公开

EP0797776A4 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：EP0797776A4
公开(公告)日：1998-07-01
申请号：EP95942579
申请日：1995-12-07
申请人： SELECTIDE CORP
发明人： LEBL MICHAL
IPC分类号： B01J19/00 , C07B61/00 , C07K1/04 , C40B30/04 , C40B40/10 , C40B60/14 , C40B70/00 , G01N33/543 , G01N33/68
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. 发明公开

EP1085943A4 THREE-DIMENSIONAL ARRAY OF SUPPORTS FOR SOLID-PHASE PARALLEL SYNTHESIS AND METHOD OF USE 有权
标题翻译：三维立体基板MATRIX固相平行合成和应用过程
公开(公告)号：EP1085943A4
公开(公告)日：2006-08-02
申请号：EP99923278
申请日：1999-05-20
申请人： SELECTIDE CORP
发明人： STEIN DAVID T , BAUM STEPHEN A
IPC分类号： B01J19/00 , B01L3/00 , B01L9/00 , B01L99/00 , C07B61/00 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/00 , C40B60/14 , 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.

7. 发明公开

EP0751779A4 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：EP0751779A4
公开(公告)日：1998-12-09
申请号：EP94920294
申请日：1994-06-21
申请人： SELECTIDE CORP
发明人： LEBL MICHAL , KRCHNAK VIKTOR , KOCIS PETR , LAM KIT S
IPC分类号： A61K38/00 , C07K5/00 , C07K1/04
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.

8. 发明专利

DE69432147T2 未知
公开(公告)号：DE69432147T2
公开(公告)日：2003-11-27
申请号：DE69432147
申请日：1994-05-27
申请人： SELECTIDE CORP
发明人： LEBL MICHAL , LAM KIT S , SALMON SYDNEY E , KRCHNAK VICTOR , SEPETOV NIKOLAI , KOCIS PETER
IPC分类号： G01N33/53 , C07B61/00 , C07K1/04 , C07K17/00 , C40B70/00 , G01N33/543 , G01N33/566 , C12P21/00 , C12Q1/68

9. 发明专利

PT705279E 未知
公开(公告)号：PT705279E
公开(公告)日：2003-07-31
申请号：PT94919294
申请日：1994-05-27
申请人： SELECTIDE CORP
发明人： LEBL MICHAL , LAM KIT S , SALMON SYDNEY E , KRCHNAK VICTOR , SEPETOV NIKOLAI , KOCIS PETER
IPC分类号： G01N33/53 , C07B61/00 , C07K1/04 , C07K17/00 , C40B70/00 , G01N33/543 , G01N33/566 , C12P21/00 , C12Q1/68

10. 发明专利

IL116837A Automated system and method for multiple synthesis of organic compounds on polymer support 未知
公开(公告)号：IL116837A
公开(公告)日：2000-02-29
申请号：IL11683796
申请日：1996-01-19
申请人： SELECTIDE CORP
IPC分类号： B01J19/00 , B25J9/16 , C07K1/04 , C40B40/10 , C40B60/14 , B01J8/02

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