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1. 发明授权

US09630950B2 Inhibitors for steroid response elements and RNA polymerase II and related methods 有权
公开(公告)号：US09630950B2
公开(公告)日：2017-04-25
申请号：US14027073
申请日：2013-09-13
申请人： Peter B. Dervan , Nicholas G. Nickols , Claire S. Jacobs , Michelle E. Farkas , Daniel A. Harki
发明人： Peter B. Dervan , Nicholas G. Nickols , Claire S. Jacobs , Michelle E. Farkas , Daniel A. Harki
IPC分类号： C07D403/14 , A61K31/785
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/785
摘要： The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The present invention also relates to polyamides capable of modulating the activity of RNA polymerase II and p53. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation and to RNA polymerase II and p53 activity.

2. 发明授权

US07935530B2 Polyamides with tail structures capable of binding DNA 有权
标题翻译：具有能够结合DNA的尾部结构的聚酰胺
公开(公告)号：US07935530B2
公开(公告)日：2011-05-03
申请号：US11998446
申请日：2007-11-28
申请人： Peter B. Dervan , Claire S. Jacobs , Nicholas G. Nickols , Daniel A. Harki
发明人： Peter B. Dervan , Claire S. Jacobs , Nicholas G. Nickols , Daniel A. Harki
IPC分类号： C12N15/00 , A61K38/04
CPC分类号： C08L77/00 , C12N15/63
摘要： The present invention relates to polyamides with a tail comprising a linker and an end-group. A preferred end-group is isophthalic acid and derivatives thereof. Polyamides of the invention are capable of entering the nucleus of cells. Polyamides of the invention are capable of selectively binding DNA. The invention also relates to methods of using the polyamides in therapy and research.
摘要翻译：本发明涉及具有包含接头和端基的尾部的聚酰胺。优选的端基是间苯二甲酸及其衍生物。本发明的聚酰胺能够进入细胞核。本发明的聚酰胺能够选择性地结合DNA。本发明还涉及在治疗和研究中使用聚酰胺的方法。

3. 发明申请

US20080269138A1 Polyamides with tail structures 有权
标题翻译：具有尾部结构的聚酰胺
公开(公告)号：US20080269138A1
公开(公告)日：2008-10-30
申请号：US11998446
申请日：2007-11-28
申请人： Peter B. Dervan , Claire S. Jacobs , Nicholas G. Nickols , Daniel A. Harki
发明人： Peter B. Dervan , Claire S. Jacobs , Nicholas G. Nickols , Daniel A. Harki
IPC分类号： C07K7/06 , A61K38/08 , C12N15/00
CPC分类号： C08L77/00 , C12N15/63
摘要： The present invention relates to polyamides with a tail comprising a linker and an end-group. A preferred end-group is isophthalic acid and derivatives thereof. Polyamides of the invention are capable of entering the nucleus of cells. Polyamides of the invention are capable of selectively binding DNA. The invention also relates to methods of using the polyamides in therapy and research.
摘要翻译：本发明涉及具有包含接头和端基的尾部的聚酰胺。优选的端基是间苯二甲酸及其衍生物。本发明的聚酰胺能够进入细胞核。本发明的聚酰胺能够选择性地结合DNA。本发明还涉及在治疗和研究中使用聚酰胺的方法。

4. 发明申请

US20140194483A1 INHIBITORS FOR STEROID RESPONSE ELEMENTS AND RNA POLYMERASE II AND RELATED METHODS 有权
标题翻译： STEROID反应元件和RNA聚合酶II的抑制剂及相关方法
公开(公告)号：US20140194483A1
公开(公告)日：2014-07-10
申请号：US14027073
申请日：2013-09-13
申请人： Peter B. Dervan , Nicholas G. Nickols , Fei Yang
发明人： Peter B. Dervan , Nicholas G. Nickols , Fei Yang
IPC分类号： C07D403/14
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/785
摘要： The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The present invention also relates to polyamides capable of modulating the activity of RNA polymerase II and p53. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation and to RNA polymerase II and p53 activity.
摘要翻译：本发明涉及能够抑制细胞中ARE-，GRE-和ERE介导的基因调节的聚酰胺。本发明还涉及能够调节RNA聚合酶II和p53的活性的聚酰胺。本发明还涉及治疗与ARE-，GRE-和ERE介导的基因调节有关的疾病和RNA聚合酶II和p53活性的方法。

5. 发明申请

US20170260169A1 INHIBITORS FOR STEROID RESPONSE ELEMENTS AND RNA POLYMERASE II AND RELATED METHODS 审中-公开
公开(公告)号：US20170260169A1
公开(公告)日：2017-09-14
申请号：US15493048
申请日：2017-04-20
申请人： Peter B. Dervan , Nicholas G. Nickols
发明人： Peter B. Dervan , Nicholas G. Nickols
IPC分类号： C07D403/14 , A61K31/4178
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/785
摘要： The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The present invention also relates to polyamides capable of modulating the activity of RNA polymerase II and p53. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation and to RNA polymerase II and p53 activity.

6. 发明申请

US20090042965A1 Inhibitors for steroid response elements and related methods 有权
标题翻译：类固醇反应元素抑制剂及相关方法
公开(公告)号：US20090042965A1
公开(公告)日：2009-02-12
申请号：US12148943
申请日：2008-04-22
申请人： Peter B. Dervan , Nicholas G. Nickols
发明人： Peter B. Dervan , Nicholas G. Nickols
IPC分类号： A61K31/4178 , C07D403/14 , A61P35/00
CPC分类号： A61K31/785 , A61K31/40 , A61K31/4025 , A61K31/4164 , C07D207/50 , C07D233/54 , C07D233/88 , C07D403/14
摘要： The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.
摘要翻译：本发明涉及能够抑制细胞中ARE-，GRE-和ERE介导的基因调节的聚酰胺。本发明还涉及治疗与ARE，GRE和ERE介导的基因调控有关的疾病的方法。

7. 发明授权

US08835480B2 Inhibitors for steroid response elements and related methods 有权
标题翻译：类固醇反应元素抑制剂及相关方法
公开(公告)号：US08835480B2
公开(公告)日：2014-09-16
申请号：US12148943
申请日：2008-04-22
申请人： Peter B. Dervan , Nicholas G. Nickols
发明人： Peter B. Dervan , Nicholas G. Nickols
IPC分类号： A61K31/4164 , C07D233/54 , A61K31/40 , C07D207/50 , A61K31/785 , C07D403/14 , C07D233/88 , A61K31/4025
CPC分类号： A61K31/785 , A61K31/40 , A61K31/4025 , A61K31/4164 , C07D207/50 , C07D233/54 , C07D233/88 , C07D403/14
摘要： The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.
摘要翻译：本发明涉及能够抑制细胞中ARE-，GRE-和ERE介导的基因调节的聚酰胺。本发明还涉及治疗与ARE，GRE和ERE介导的基因调控有关的疾病的方法。

8. 发明授权

US07049061B1 Stereochemical control of the DNA binding affinity, sequence specificity, and orientation-preference of chiral hairpin polyamides in the minor groove 有权
标题翻译：立体化学控制手性发夹聚酰胺在小槽中的DNA结合亲和力，序列特异性和取向偏好
公开(公告)号：US07049061B1
公开(公告)日：2006-05-23
申请号：US09374702
申请日：1999-08-12
申请人： Eldon E. Baird , Peter B. Dervan
发明人： Eldon E. Baird , Peter B. Dervan
IPC分类号： C12Q1/68 , A01N43/04 , A61K38/00 , C07K1/00
CPC分类号： C07D403/14 , A61K38/00 , A61K47/595 , A61K47/645 , C07D207/34 , C07D233/90 , C07K5/06139 , C07K5/06182 , C07K7/02 , C07K7/04 , C08G69/00 , C12Q1/6839
摘要： This invention provides improved polyamides comprising a hairpin loop derived from γ-aminobutyric acid which bind to the minor groove of a promoter regions of a DNA sequence. Binding of the polyamide to the DNA sequence of the promoter region inhibits expression of the requisite gene. The improvement relates to the use of R-2,4-diaminobutyric acid and derivatives of the 2-amino group to form the hairpin loop. The improved asymmetric hairpin provides for tighter binding of the polyamides to the minor groove of DNA and additionally provides an amine function for derivatizing polyamides by, for example, forming amide linkages. Such derivatives may serve to attach detectable labels to the polyamide.
摘要翻译：本发明提供了改进的聚酰胺，其包含衍生自γ-氨基丁酸的发夹环，其结合DNA序列的启动子区的小沟。聚酰胺与启动子区DNA序列的结合抑制必需基因的表达。该改进涉及使用R-2,4-二氨基丁酸和2-氨基的衍生物形成发夹环。改进的不对称发夹提供聚酰胺更紧密地结合到DNA的小沟槽，另外提供胺功能，用于通过例如形成酰胺键来衍生聚酰胺。这样的衍生物可用于将可检测标记附着到聚酰胺上。

9. 发明授权

US06673940B1 Compositions and methods relating to cyclic compounds that undergo nucleotide base pair-specific interactions with double-stranded nucleic acids 有权
标题翻译：与与双链核酸进行核苷酸碱基对特异性相互作用的环状化合物相关的组合物和方法
公开(公告)号：US06673940B1
公开(公告)日：2004-01-06
申请号：US09479279
申请日：2000-01-06
申请人： Peter B. Dervan , Eldon E. Baird
发明人： Peter B. Dervan , Eldon E. Baird
IPC分类号： C07D23102
CPC分类号： C07H19/00 , C07D487/22 , C07H21/02
摘要： The design, synthesis, and use of cyclic compounds, including cyclic polyamides, is described. Such compounds comprise at least two polymer portions, one of which comprises at least three molecular units, and the other comprises at least four molecular units. At least one molecular unit of such a compound is a hydrogen bond donor or acceptor. The polymer portions are covalently linked to form a cycle. These compounds are capable of targeting specific nucleotide sequences in double-stranded nucleic acids, particularly double-stranded DNA. Accordingly, such compounds can be used to modulate, e.g., increase or decrease, the expression of one or more genes in vitro or in vivo.
摘要翻译：描述了包括环状聚酰胺在内的环状化合物的设计，合成和使用。这样的化合物包含至少两个聚合物部分，其中之一包含至少三个分子单元，另一个包含至少四个分子单元。这种化合物的至少一个分子单元是氢键供体或受体。聚合物部分共价连接形成一个循环。这些化合物能够靶向双链核酸，特别是双链DNA中的特异性核苷酸序列。因此，这些化合物可以用于在体外或体内调节，例如增加或减少一种或多种基因的表达。

10. 发明授权

US4665184A Bifunctional molecules having a DNA intercalator or DNA groove binder linked to ethylene diamine tetraacetic acid 失效
公开(公告)号：US4665184A
公开(公告)日：1987-05-12
申请号：US860604
申请日：1986-05-07
申请人： Peter B. Dervan , Robert P. Hertzberg
发明人： Peter B. Dervan , Robert P. Hertzberg
IPC分类号： C07D207/34 , C07D221/12
CPC分类号： C07D207/34 , C07D221/12
摘要： Novel bifunctional molecules having a DNA intercalator or DNA groove binder linked to ethylene diamine tetraacetic acid such as compounds having the formula: ##STR1## wherein R is methyl or ethyl. Also, the method of cleaving DNA by contact with one of the above-identified molecules in the presence of ferrous ion and oxygen.The process of preparing said molecules by the reaction of P-carboxy methidium halide, p-carboxy ethidium halide, or other DNA intercalator or DNA groove binder with 1-3-diaminopropane followed by condensation with ethylenediamine tetraacetic acid.Distamycin-EDTA.Fe(II)(DE.FE(II)) contains EDTA attached to the amino terminus of the groove binder tripeptide (tris-N-methylpyrrolecarboxamide). DE.Fe(II) cleaves DNA contiguous to a five base pair A+T rich sequence. This is a novel and unique molecule and superior in sequence specificity to the naturally occurring antitumor compound used in man, bleomycin which cleaves DNA at a two base pair recognition site. EDTA-distamycin-Fe(II)(ED.Fe(III)) contains EDTA attached to the carboxy terminus of the groove binder tripeptide, tris-N-methylpyrrolecarboxamide. ED.Fe(II) cleaves DNA contiguous to a five base pair A+T rich sequence. Penta-N-methylpyrrolecarboxamide-EDTA.Fe(II)(P5E.Fe(II)) cleaves DNA on opposite strand at the six base pair recognition level in a catalytic reaction. This is the first designed synthetic molecule that approximates the double strand sequence specific cleavage of DNA(4-6 bp recognition level) by the natural substance restriction enzymes, tools which make possible recombinant DNA manipulations. P5E.Fe(II) cuts DNA at sequences not available by the naturally occurring restriction enzymes.The dimers, bis(EDTA-distamycin.Fe(II) and EDTA-bisdistamycin.Fe(II) which double strand cleave DNA at the eight base pair recognition level (A+T rich).

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