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1. 发明申请

WO1997043298A1 NOVEL NUCLEOSIDE ANALOGS WITH POLYCYCLIC AROMATIC GROUPS ATTACHED, METHODS OF SYNTHESIS AND USES THEREFOR 审中-公开
标题翻译：具有多环芳族基团的新型核苷酸类似物，合成方法及其用途
公开(公告)号：WO1997043298A1
公开(公告)日：1997-11-20
申请号：PCT/US1997008307
申请日：1997-05-15
申请人： RESEARCH CORPORATION TECHNOLOGIES, INC.
发明人： RESEARCH CORPORATION TECHNOLOGIES, INC. , KOOL, Eric, T.
IPC分类号： C07H19/00
CPC分类号： C07H21/00 , C07H7/04 , C07H15/20
摘要： The present invention provides fluorescent nucleosides carrying polycyclic aromatic hydrocarbons such as anthracene, phenanthrene, pyrene, stilbene, tetracene or pentacene. The subject nucleosides may be synthesized using a C-glycosidic bond formation method employing organocadium or organozinc derivatives of the aromatic compounds and coupling with a 1- alpha -chlororibose or deoxyribose synthon. The alpha -anomers of the coupling reaction may be epimerized to the beta -anomers by acid-catalyzed equilibration. The fluorescent nucleosides act as a DNA or RNA base analogs and can be incorporated into nucleic acids. Resultant fluorescently tagged nucleic acids are useful as probes for target nucleic acids in tissues, solutions or immobilized on membranes.
摘要翻译：本发明提供携带多环芳烃的荧光核苷，例如蒽，菲，芘，芪，并四苯或并五苯。可以使用使用有机体或芳族化合物的有机锌衍生物的C-糖苷键形成方法并与1-α-半胱氨酸或脱氧核糖合成酶偶联来合成目标核苷。偶联反应的α-异构体可以通过酸催化的平衡而差向异构化为β-异构体。荧光核苷作为DNA或RNA碱基类似物，可以并入核酸。得到的荧光标记核酸可用作组织，溶液中的靶核酸的探针或固定在膜上。

2. 发明申请

WO1996030384A1 SINGLE-STRANDED CIRCULAR OLIGONUCLEOTIDES 审中-公开
标题翻译：单条圆形半球形
公开(公告)号：WO1996030384A1
公开(公告)日：1996-10-03
申请号：PCT/US1996003757
申请日：1996-03-21
申请人： RESEARCH CORPORATION TECHNOLOGIES, INC.
发明人： RESEARCH CORPORATION TECHNOLOGIES, INC. , KOOL, Eric, T.
IPC分类号： C07H21/00
CPC分类号： A61K31/7088 , A61K31/70 , A61K38/00 , C07H21/00 , C12N15/113 , C12N15/1131 , C12N15/1135 , C12N2310/152 , C12N2310/3183 , C12N2310/321 , C12N2310/53 , C12Q1/6813 , C12Q1/6839 , C12Q1/6886 , C12Q1/703 , C12Q2600/154 , C12N2310/3521
摘要： The present invention provides single-stranded circular oligonucleotides each with at least one parallel binding (P) domain and/or at least one corresponding anti-parallel binding (AP) domain separated from each other by loop domains. When more than one P or AP domain is included in a circular oligonucleotide of the present invention, the additional P or AP domains can constitute loop domains for a pair of corresponding P and AP domains, and vice versa. The present invention further provides single-stranded circular oligonucleotides with at least one Hoogsten anti-parallel (HAP) domain. Each P, AP and HAP domain has sufficient complementarity to bind to one strand of a defined nucleic acid target wherein the P domain binds in a parallel manner to the target and the HAP or AP domain binds in an anti-parallel manner to the target. Moreover, the present single-stranded circular oligonucleotides can bind to both single-stranded and double-stranded target nucleic acids. The present invention also provides methods of making and using these oligonucleotides as well as kits and pharmaceutical compositions containing these oligonucleotides.
摘要翻译：本发明提供单链的环状寡核苷酸，每一个具有至少一个平行结合（P）结构域和/或至少一个相应的反并行结合（AP）结构域，其通过环结构域彼此分离。当本发明的环状寡核苷酸中包含多于一个的P或AP结构域时，附加的P或AP结构域可以构成一对相应的P和AP结构域的环结构域，反之亦然。本发明还提供具有至少一个Hoogsten反平行（HAP）结构域的单链环状寡核苷酸。每个P，AP和HAP结构域具有足够的互补性以结合定义的核酸靶的一条链，其中P结构域以平行的方式与靶结合，并且HAP或AP结构域以反平行方式结合靶。此外，本发明的单链环状寡核苷酸可以结合单链和双链靶核酸。本发明还提供制备和使用这些寡核苷酸的方法以及含有这些寡核苷酸的试剂盒和药物组合物。

3. 发明申请

WO2001044220A3 FLUORESCENT NUCLEOSIDE ANALOGS AND COMBINATORIAL FLUOROPHORE ARRAYS COMPRISING SAME 审中-公开
公开(公告)号：WO2001044220A3
公开(公告)日：2001-06-21
申请号：PCT/US2000/033681
申请日：2000-12-13
申请人： RESEARCH CORPORATION TECHNOLOGIES, INC.
发明人： KOOL, Eric, T.
IPC分类号： C07D307/04
摘要： The present invention provides fluorescent nucleoside analogs which comprise a fluorescent cyclic compound joined to a carbon of a sugar molecule such as pentose, hexose, ribose or deoxyribose or analogs thereof in either an α or β configuration. The subject compounds are useful as probes in the study of the structure and dynamics of nucleid acids and their complexes with proteins. In addition, the subject compounds are useful in any technique which uses labeled oligonucleotides for detection. Non-fluorescent spacer molecules in which a cyclohexane, cyclohexene, decalin, or benzene is joined to a carbon of a sugar moiety such as pentose, hexose, ribose or deoxyribose are also provided. Also provided are the 5' dimethoxytrityl-3'-O-phosphoramidite derivatives, suitable for incorporation into oligonucleotides by automated synthesizers. Combinatorial fluorophore array (CFA) libraries comprising oligomers of the subjects nucleoside analogs attached to one or more solid supports are also provided as are methods of selecting fluorophores from the CFA libraries. The present invention also provides oligonucleotide analogs comprising one or more of the subject nucleoside analogs in place of the DNA or RNA base.

4. 发明申请

WO1996029097A1 STEM-LOOP AND CIRCULAR OLIGONUCLEOTIDES 审中-公开
标题翻译： STEM-LOOP和CIRCULAR OLIGONUCLEOTIDES
公开(公告)号：WO1996029097A1
公开(公告)日：1996-09-26
申请号：PCT/US1995003602
申请日：1995-03-21
申请人： RESEARCH CORPORATION TECHNOLOGIES, INC.
发明人： RESEARCH CORPORATION TECHNOLOGIES, INC. , KOOL, Eric, T.
IPC分类号： A61K48/00
CPC分类号： C12N15/113 , C07H21/00 , C12N2310/111 , C12N2310/152 , C12N2310/53 , C12Q1/6813 , C12Q1/6839 , C12Q1/686
摘要： The present invention provides stem-loop and circular oligonucleotides each with at least one Watson-Crick binding (WC) domain and at least one corresponding Hoogsteen binding (H) domain separated from each other by linker domains. Each WC domain has sufficient complementarity to bind to one strand of a defined nucleic acid target by Watson-Crick base pairing in an anti-parallel orientation. Each corresponding H domain is capable of binding to the WC domain by Hoogsteen base pairing in an anti-parallel manner. The present invention also provides methods of making and using these oligonucleotides as well as kits and pharmaceutical compositions containing these oligonucleotides.
摘要翻译：本发明提供了茎环和环状寡核苷酸，每个具有至少一个Watson-Crick结合（WC）结构域和至少一个相应的Hoogsteen结合（H）结构域，其通过接头结构域彼此分离。每个WC结构域具有足够的互补性，以反平行取向通过Watson-Crick碱基配对结合所定义的核酸靶的一条链。每个相应的H结构域能够以反平行方式通过Hoogsteen碱基配对结合到WC结构域。本发明还提供制备和使用这些寡核苷酸的方法以及含有这些寡核苷酸的试剂盒和药物组合物。

5. 发明申请

WO1992017484A1 SINGLE-STRANDED CIRCULAR OLIGONUCLEOTIDES 审中-公开
标题翻译：单条圆形半球形
公开(公告)号：WO1992017484A1
公开(公告)日：1992-10-15
申请号：PCT/US1992002480
申请日：1992-03-26
申请人： RESEARCH CORPORATION TECHNOLOGIES, INC.
发明人： RESEARCH CORPORATION TECHNOLOGIES, INC. , KOOL, Eric, T.
IPC分类号： C07H0
CPC分类号： A61K31/70 , A61K38/00 , C07H21/00 , C12N15/113 , C12N15/1135 , C12N2310/152 , C12N2310/3183 , C12N2310/321 , C12N2310/53 , C12Q1/6813 , C12Q1/6839 , C12Q1/6886 , C12Q1/703 , C12N2310/3521
摘要： The present invention provides single-stranded circular oligonucleotides each with a parallel binding (P) domain and an anti-parallel binding (AP) domain separated from each other by loop domains. Each P and AP domain has sufficient complementarity to bind to one strand of a defined nucleic acid target wherein the P domain binds in a parallel manner to the target and the AP domain binds in an anti-parallel manner to the target. Moreover, the present single-stranded circular oligonucleotides can bind to both single-stranded and double-stranded target nucleic acids. The present invention also provides methods of using these oligonucleotides as well as pharmaceutical compositions containing these oligonucleotides.
摘要翻译：本发明提供了单链的环状寡核苷酸，每一个具有平行结合（P）结构域和通过环结构域彼此分离的反平行结合（AP）结构域。每个P和AP结构域具有足够的互补性，以结合定义的核酸靶的一条链，其中P结构域以平行的方式与靶结合，并且AP结构域以反平行方式与靶结合。此外，本发明的单链环状寡核苷酸可以结合单链和双链靶核酸。本发明还提供了使用这些寡核苷酸的方法以及含有这些寡核苷酸的药物组合物。

6. 发明公开

EP0579771A1 SINGLE-STRANDED CIRCULAR OLIGONUCLEOTIDES 失效
标题翻译：单链环状寡核苷酸。
公开(公告)号：EP0579771A1
公开(公告)日：1994-01-26
申请号：EP92912127.0
申请日：1992-03-26
申请人： RESEARCH CORPORATION TECHNOLOGIES, INC.
发明人： KOOL, Eric, T.
IPC分类号： A61K48 , C07H21 , C12N15 , C12Q1 , A61K38
CPC分类号： A61K31/70 , A61K38/00 , C07H21/00 , C12N15/113 , C12N15/1135 , C12N2310/152 , C12N2310/3183 , C12N2310/321 , C12N2310/53 , C12Q1/6813 , C12Q1/6839 , C12Q1/6886 , C12Q1/703 , C12N2310/3521
摘要： Cette invention concerne des oligonucléotides circulaires à brin unique comprenant chacun un domaine (P) de liaison parallèle et un domaine (AP) de liaison antiparallèle séparés l'un de l'autre par des domaines à boucle. Chaque domaine P et AP présente une complémentarité suffisante pour se fixer sur un brin d'une cible définie d'acide nucléique dans laquelle le domaine P se fixe d'une manière parallèle sur la cible, et le domaine AP se fixe d'une manière antiparallèle sur la cible. En outre, les oligonucléotides circulaires à brin unique de cette invention peuvent se lier à des acides nucléiques cibles à brin unique et à des acides nucléiques à brins doubles. Cette invention concerne également des procédés d'utilisation de ces oligonucléotides ainsi que des compositions pharmaceutiques contenant ces derniers.

7. 发明公开

EP0927188A1 NOVEL NUCLEOSIDE ANALOGS WITH POLYCYCLIC AROMATIC GROUPS ATTACHED, METHODS OF SYNTHESIS AND USES THEREFOR 失效
标题翻译： NEW核苷ANALOG多环芳族基团作为取代基具有METHOD FOR PRODUCING及其应用
公开(公告)号：EP0927188A1
公开(公告)日：1999-07-07
申请号：EP97925598.0
申请日：1997-05-15
申请人： Research Corporation Technologies, Inc
发明人： KOOL, Eric, T.
IPC分类号： C12N15 , C07D307 , C07H7 , C07H15 , C07H21 , C12Q1
CPC分类号： C07H21/00 , C07H7/04 , C07H15/20
摘要： The present invention provides fluorescent nucleosides carrying polycyclic aromatic hydrocarbons such as anthracene, phenanthrene, pyrene, stilbene, tetracene or pentacene. The subject nucleosides may be synthesized using a C-glycosidic bond formation method employing organocadium or organozinc derivatives of the aromatic compounds and coupling with a 1-α-chlororibose or deoxyribose synthon. The α-anomers of the coupling reaction may be epimerized to the β-anomers by acid-catalyzed equilibration. The fluorescent nucleosides act as a DNA or RNA base analogs and can be incorporated into nucleic acids. Resultant fluorescently tagged nucleic acids are useful as probes for target nucleic acids in tissues, solutions or immobilized on membranes.

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