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1. 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).

2. 发明授权

US4942227A Bifunctional molecules having a DNA intercalator or DNA groove binder linked to ethylene diamine tetraacetic acid, their preparation and use to cleave DNA 失效
公开(公告)号：US4942227A
公开(公告)日：1990-07-17
申请号：US6442
申请日：1987-01-23
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： C07D221/12 , C07D207/34
摘要： 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(II)) 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 on opposite strands 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).

3. 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.

4. 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。

5. 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。

6. 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.

7. 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。

8. 发明授权

US06958240B1 Inhibition of major groove DNA binding proteins by modified polyamides 有权
标题翻译：通过改性聚酰胺抑制大槽DNA结合蛋白
公开(公告)号：US06958240B1
公开(公告)日：2005-10-25
申请号：US09374704
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： A61K38/00 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/785 , A61K38/04 , A61K41/00 , A61K47/48 , A61K49/00 , A61P43/00 , C07D207/34 , C07D233/90 , C07D403/12 , C07D403/14 , C07H21/04 , C07K5/078 , C07K7/02 , C07K7/04 , C08G69/00 , C08G69/08 , C12N15/09 , C12Q1/68 , A61K7/06 , A61K7/11 , C07H5/04 , C12N5/00
CPC分类号： C07K7/02 , A61K38/00 , A61K47/595 , A61K47/645 , C07D207/34 , C07D233/90 , C07D403/14 , C07K5/06139 , C07K5/06182 , C07K7/04 , C08G69/00 , C12Q1/6839
摘要： This invention provides improved polyamides comprising a positive patch for contacting the phosphate backbone or major groove of a DNA molecule. As such, the improved polyamides are capable of inhibiting the function or binding of a DNA-binding protein to a DNA molecule. The improved polyamide provides for more efficient function of the polyamide.
摘要翻译：本发明提供改进的聚酰胺，其包含用于接触DNA分子的磷酸酯主链或主要沟槽的阳性贴剂。因此，改进的聚酰胺能够抑制DNA结合蛋白与DNA分子的功能或结合。改进的聚酰胺提供了聚酰胺更有效的功能。

9. 发明授权

US06506906B1 Preparation and use of bifunctional molecules having DNA sequence binding specificity 有权
标题翻译：具有DNA序列结合特异性的双功能分子的制备和使用
公开(公告)号：US06506906B1
公开(公告)日：2003-01-14
申请号：US09414611
申请日：1999-10-08
申请人： Peter B. Dervan
发明人： Peter B. Dervan
IPC分类号： C07D23100
CPC分类号： C07D403/14 , A61K38/00 , A61K47/595 , C07D207/34 , C07D233/90 , C07K5/06139 , C07K5/06182 , C07K7/02 , C07K7/04 , C08G69/00 , C12Q1/6839
摘要： Small molecule polyamides that specifically bind with subnanomolar affinity to any predetermined sequence in the human genome with potential use in molecular biology and human medicine are described. Further, the designed compounds which target the minor groove of B-form double helical DNA offer a general approach for the control of gene-expression. Simple rules are disclosed which provide for rational control of the DNA-binding sequence specificity of synthetic polyamides containing N-methylpyrrole and N-methylimidazole amino acids. A series of molecular templates for polyamide design are disclosed which provide for small molecules which recognize predetermined DNA sequences with affinities and specificities comparable to sequence-specific DNA-binding proteins such as transcription factors. These design rule are applied to provide a polyamide for specific targeting of a predetermined 7 base pair sequence from a conserved HIV gene promoter at subnanomolar concentration. The pyrrole-imidazole polyamides described herein represent the only class of designed small molecules to date that can bind any predetermined sequence of double helical DNA.
摘要翻译：描述了在分子生物学和人类医学中具有潜在应用特异性结合人类基因组中任何预定序列的亚纳摩尔亲和力的小分子聚酰胺。此外，靶向B型双螺旋DNA的小沟的设计化合物提供了用于控制基因表达的一般方法。公开了简单的规则，其提供了合成含有N-甲基吡咯和N-甲基咪唑氨基酸的合成聚酰胺的DNA结合序列特异性的合理控制。公开了一系列用于聚酰胺设计的分子模板，其提供识别与序列特异性DNA结合蛋白如转录因子相当的亲和力和特异性的预定DNA序列的小分子。这些设计规则适用于提供聚酰胺，用于以亚纳摩尔浓度从保守的HIV基因启动子特异性靶向预定的7个碱基对序列。本文所述的吡咯 - 咪唑聚酰胺代表迄今唯一可以结合任何预定顺序的双螺旋DNA的设计小分子。

10. 发明授权

US06472537B1 Polyamides for binding in the minor groove of double stranded DNA 有权
标题翻译：用于在双链DNA的小沟中结合的聚酰胺
公开(公告)号：US06472537B1
公开(公告)日：2002-10-29
申请号：US09372473
申请日：1999-08-11
申请人： Eldon E. Baird , Peter B. Dervan
发明人： Eldon E. Baird , Peter B. Dervan
IPC分类号： C07D23102
CPC分类号： C07D403/14 , A61F2/82 , A61K38/00 , A61K47/595 , A61K47/645 , C07D207/34 , C07D233/90 , C07H21/00 , C07K5/06139 , C07K5/06182 , C07K7/02 , C07K7/04 , C08G69/00 , C12Q1/6839
摘要： The invention encompasses improved polyamides for binding to specific nucleotide sequences in the minor groove of double stranded DNA. The 3-hydroxy-N-methylpyrrole/N-methylpyrrole carboxamide pair specifically recognizes the T·A base pair, while the N-methylpyrrole/3-hydroxy-N-methylpyrrole pair recognizes A·T nucleotide pairs. Similarly, an N-methylimidizole/N-methylpyrrole carboxamide pair specifically recognizes the G·C nucleotide pair, and the N-methylpyrrole/N-methylimidizole carboxamide pair recognizes the C·G nucleotide pair.
摘要翻译：本发明包括用于结合双链DNA的小槽中的特定核苷酸序列的改进的聚酰胺。 3-羟基-N-甲基吡咯/ N-甲基吡咯甲酰胺对特异性识别T.A碱基对，而N-甲基吡咯/ 3-羟基-N-甲基吡咯对识别A.T核苷酸对。类似地，N-甲基亚氨基咪唑/ N-甲基吡咯甲酰胺对特异性识别G.C核苷酸对，并且N-甲基吡咯/ N-甲基亚胺唑羧酰胺对识别C.G核苷酸对。

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